Syngenta Participations Ag vs Controller Of Patents Designs
- Court
- Delhi High Court
* IN THE HIGH COURT OF DELHI AT NEW DELHI
% Judgment reserved on 09.03.2026
Judgment delivered on: 04.05.2026
+ C.A.(COMM.IPD-PAT) 49/2023
SYNGENTA PARTICIPATIONS AG .....Appellant
versus
CONTROLLER OF PATENTS DESIGNS .....Respondent
Advocates who appeared in this case:
For the Appellant: Mr. Pravin Anand, Advocate with Ms. Arpita,
Advocate.
For the Respondent: Ms. Manisha Agrawal Narain, CGSC with Mr.
Navneet Saharan, Mr. Nipun Jain, Advocates.
CORAM:
HON’BLE MR. JUSTICE TUSHAR RAO GEDELA
J U D G M E N T
TUSHAR RAO GEDELA, J.
1. Present appeal has been filed under Section 117A of the Patents Act,
1970 (hereinafter referred to as “ the Act ”) assailing the order dated 21.07.2023
passed by the respondent-Controller of Patents & Designs (hereinafter referred
to as “ learned Controller ”) refusing the Indian patent application titled
"POLYMORPHS OF 3-DIFLUOROMETHYL-1 -METHYL-1 H-PYRAZOLE-
4-CARBOXYLIC ACID (9-DICHLOROMETHYLENE -1,2,3,4-
TETRAHYDRO-1,4-METHANO -NAPHTHALEN-5-YL)-AMIDE " bearing no.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 1 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
201617031900 (hereinafter referred to as “ subject application ”), on the
ground of lack of inventive step under Section 2(1)(ja) and Section 3(d) of the
Act.
BRIEF FACTS:-
2. The subject application was filed on 19.09.2016 before the Indian
patent office, and the corresponding PCT application was filed on 24.02.2015
claiming priority from application GB 1403438.3 filed on 27.02.2014.
3. The subject application was published on 13.01.2017. The First
Examination Report (hereinafter referred to as “ FER ”) was issued on
26.07.2019, and the response thereto was submitted by the appellant on
08.04.2020.
4. Thereafter, the hearing notice was issued on 03.04.2023, scheduling the
hearing on 03.05.2023, which was attended by the appellant.
5. Thereafter, the appellant submitted the post hearing written submissions
on 29.05.2023 and the impugned order was passed on 21.07.2023. It is this
order which is challenged before this Court by way of the present appeal.
CONTENTIONS OF THE APPELLANT:-
6. Mr. Pravin Anand, learned counsel appearing for the appellant submits
that the impugned order of the respondent is erroneous on the ground that the
respondent has erred in rejecting thermal stability data provided in the
specification and the affidavit of Dr. John Hone. As per the learned counsel,
the respondent has erred in holding that the difference in thermal stability is an
inherent property of any monohydrate form as compared to its non-hydrate/
anhydrous form. In support of the above, learned counsel has submitted that
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 2 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
thermal stability is not an inherent property as polymorphic forms are
unpredictable in nature. Further, the learned counsel also submitted that the
respondent has failed to cite any reference to demonstrate that thermal
stability is an inherent property of monohydrate crystalline polymorph of the
compound of formula I. Reliance was placed on paragraph 34 of the
judgement in AGFA NV & Anr. vs. The Assistant Controller of Patents and
Designs & Anr., 2023:DHC:4030 .
7. Another ground raised by Mr. Anand, learned counsel is that the
respondent has erred in holding that the monohydrate crystalline polymorph of
compound of formula I lacks inventive step without considering the
comparative data in terms of “lowering phytotoxicity” furnished by the
appellant. He further submitted that the applicant has provided comparative
data, and the law on inventive step does not identify that only a particular kind
of data can qualify for such a determination.
8. A reliance was placed on the following judgements:
●
F-Hoffmann-la Roche Ltd. &Anr. vs Cipla Ltd ., 2015:DHC:9674-
DB
●
Agriboard International LLC vs Deputy Controller of Patents &
Designs, 2022:DHC:1206
9. In support of the above, learned counsel further submitted that the
applicant has conducted experiments to determine the thermal stability of the
hydrate and anhydrous form by using Differential Scanning Calorimetry
(DSC).
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 3 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
10. As per the learned counsel, the applicant prepared slurries of both
anhydrous polymorph form 1 as well as the monohydrate crystalline
polymorph of compound of formula I in different water/methanol mixtures
and at different temperatures. Reliance was placed on Example 3 and Table 3
of the complete specification (hereinafter referred to as “ CS ”) of the subject
application.
11. It was argued that the phase diagram shown in Table 3 indicates that
temperatures more than of 60°C would be required to dehydrate the hydrate of
compound (I) at normal ambient relative humidities, and this indicates that the
hydrate of IN`1900 would be the stable form of compound (I) in suspension
concentrate (hereinafter referred to as “ SC ”) formulations. In addition, would
also be more stable in other, non-aqueous, formulations after their dilution
with water in the spray tank.
12. While referring to the said Example 5 of the CS of the subject
application the learned counsel submitted that the two standard SC
formulations were separately prepared using the anhydrous Form 1 polymorph
and the hydrated polymorph. The SC of the anhydrous Form 1 was
contaminated with 5% of the hydrated form and was placed in a temperature
cycling oven varying from 0°C to 40°C over 12 hours. Thereafter, two weeks
later, the sample was inspected and the microscopy showed that the size of the
crystals had increased substantially. Some crystals were removed from the
formulation and dried and thereafter, the powder X-ray diffraction pattern was
collected and in the outcome, all of the anhydrous polymorph Form 1 were
fully converted to the hydrated form. The comparative powder X-ray
diffraction trace is shown in FIG. 7.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 4 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
13. Regarding the objection on the ground of Section 3(d) of the Act, the
learned counsel for the appellant submitted that the respondent has erred in
holding that the monohydrate crystalline polymorph of compound of formula I
falls under Section 3(d) of the Act in the absence of non-consideration of the
enhanced efficacy data in terms of “lowering phytotoxicity” over the
anhydrous form of cited art.
14. Learned counsel further submits that the thermal stability data qualifies
as enhanced efficacy data. The present invention pertains to the field of
agrochemicals and Section 3(d) of the Act does not define efficacy for
inventions in the field of agrochemicals unlike pharmaceuticals where the
efficacy is defined as being therapeutic efficacy. Reliance was placed on the
decision of the Supreme Court in Novartis vs. Union of India & Others:
(2013) 6 SCC, only to submit that the test of therapeutic efficacy under
Section 3(d) of the Act is limited only to medicines/pharmaceuticals
preparation and not agrochemicals.
15. He also cited the judgment in Novozymes vs. Assistant Controller of
Patent: (T) CMA (PT) No.33 of 2023 delivered by the High Court of Madras.
He submitted that thermal stability of the crystalline polymorph of the present
invention results in lowering of phytotoxicity. It was submitted that a specific
polymorph may have properties which make it more advantageous in a
particular use compared to another polymorph of the same compound and the
physical, chemical and biological properties can have a significant effect on
the development of production methods and formulations and the quality as
well as efficacy of plant treatment agents like fungicides.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 5 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
16. Thus, according to Mr. Anand, the impugned order needs to be set aside
and matter remanded for de novo consideration.
CONTENTIONS OF THE RESPONDENT:-
17. Per contra , Ms. Manisha Agrawal Narain, learned CGSC for the
respondent no.3, opposed the arguments addressed on behalf of the appellant.
18. She submitted that all the prior art documents D1 to D4 were
considered as the closest prior art and the cited D1 discloses the crystalline
form of the compound of present formula I (3- difluoromethyl-1 -methyl- 1 H-
pyrazole-4-carboxylic acid (9- dichloromethylene-1, 2, 3, 4-tetrahydro-1, 4-
methano- naphthalen-5-yl)- amide) and intermediates along with their
preparation process. The following compounds from the cited prior arts were
submitted by the learned CGSC:
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 6 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
19. She further submitted that D2 to D4 also disclose the same compound
of formula I as well as its process for preparation. As per the learned CGSC,
the compound of formula I prepared in the cited literature D1 to D4 generally
involved in the crystallisation and/or recrystallisation process in non-aqueous
medium that led to the formation of final crystalline product.
20. She submitted that the distinguishing feature of the present application
compared to the cited prior arts is the “monohydrate” form of compound of
formula I instead of “nonhydrate” form of compound of formula I. She further
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 7 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
submitted that it is acknowledged that none of the cited documents discloses
the “monohydrate” form of compound of formula I and therefore, the
technical problem underlying the subject application has to be seen as the
provision of further alternate “polymorph” form of compound of formula I
having an unexpected effect with regard to the cited prior arts D1 to D4.
21. Learned CGSC for the respondent no. 3 further submitted that the
present application does not contain any evidence for such surprising effect
over the cited documents D1 to D4 and in the absence of such credible
evidence of surprising effect over D1 to D4, the mandate of the inventive step
under Section 2(1)(ja) of the Act cannot be considered to be satisfied.
22. She submitted that the X-ray diffraction pattern in claim 1 provided by
the appellant is only characterisation data, and it cannot be considered as a
technical feature of the presently claimed compound.
23. The learned CGSC submitted that regarding claim no 3, it is found that
any agro-chemically active compound should only be applied in form
composition and therefore, as discussed in the preceding para, claim no.3 does
not meet the requirements of Section 2(1)(ja) of the Act.
24. Regarding the objection under Section 3(d) of the Act, it was submitted
that as the compound in its “nonhydrate/anhydrous” form is already known
from cited prior arts, the claimed crystalline “monohydrate polymorph” of the
subject application is considered as “new form of known substance which
does not result in the enhancement of known efficacy”. Therefore, the subject
matter as claimed in claim nos.1 and 2 is not allowable under Section 3(d) of
the Act.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 8 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
ANALYSIS AND CONCLUSION:-
25. The present invention is directed to a crystalline polymorph of
compound of formula I which is a monohydrate containing 4.3 ± 0.2% w/w
water. This polymorph has a dehydration/melting point of between 80 and
125°C. The polymorphs of the present invention can be used for the control of
plant pathogenic fungi on a number of plant species. The invention of IN'
1900 relates to a new solid form of I, 3-difluoromethyl-1-methyl-lH-pyrazole-
4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-l,4-methano-
naphthalen-5-yl)-amide which is compound of formula I. The structure of
formula I is as follows:
26. The claims refused vide impugned order are as follows:
“We claim:
1. A crystalline polymorph of the compound of formula I
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 9 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
which has a powder X-ray diffraction pattern comprising at least three
d values, measured in Å, selected from the group consisting of 10.45 ±
0.2, 7.45 ± 0.2, 6.71 ± 0.2, 6.31 ± 0.2, 5.99 ± 0.2, 5.42 ± 0.2, 5.23 ± 0.2,
4.78 ± 0.2, 4.60 ± 0.2, 4.53 ± 0.2, 4.33 ± 0.2, 4.14 ± 0.2, 3.97 ± 0.2,
3.86 ± 0.2, 3.73 ± 0.2, 3.62 ± 0.2, 3.49 ± 0.2, 3.37 ± 0.2, 3.30 ± 0.2,
3.23 ± 0.2, 3.19 ± 0.2, 3.14 ± 0.2, 3.06 ± 0.2 and 3.00 ± 0.2 and which
has no peak in the powder X-ray diffraction pattern at d = 16.58 ± 0.2
and d = 16.84 ± 0.2, wherein said polymorph is a monohydrate
containing 4.3 ± 0.2% w/w water.
2. The crystalline polymorph as claimed in claim 1, which has the
following lattice parameters: a=18.28(5), b=12.65(5), c=7.81(5), a =
2
90.00, β = 90.00, γ = 90.00 and volume = 1805.0(5) A .
3. An agricultural composition comprising a polymorph as claimed in
any one of claims 1 to 2 and at least one agriculturally acceptable
carrier or diluent.”
27. The CS of the subject application specifies the problem in prior art that
if the existing form of a compound is not stable in such an SC formulation,
polymorphic conversion might occur leading to unwanted crystal growth.
Such crystal growth is detrimental because it leads to, for example, thickening
and potentially solidification of the formulation which can lead to blockages
in application equipment, e.g. in spray nozzles in agricultural application
machinery. Using a stable polymorphic form would overcome these issues.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 10 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
28. Further, the CS of the subject application at page 124 specifies how the
issues present in the prior art can be overcome using the present invention. For
better understanding, the relevant para of the CS is reproduced hereunder:
“For example, a suspension concentrate (SC) formulation may be
preferred over an emulsion concentrate (EC) because the lack of solven 5
in the SC often means that the formulation is likely to be less phytotoxic
than an equivalent EC formulation - however, if the existing form of a
compound is not stable in such an SC formulations, polymorphic
conversion might occur leading to unwanted crystal growth. Such crystal
growth is detrimental because it leads to, for example, thickening and
potentially solidification of the formulation which can lead to blockages in
application 10 equipment, e.g. in spray nozzles in agricultural application
machinery. Using a stable polymorphic form would overcome these
issues.”
29. Further, the CS of the subject application at page 123 specifies that the
structure of different polymorphs of a compound has different arrangements of
atoms/molecules in their crystal structure and therefore, properties of any of
these crystal forms is challenging to predict. The relevant portion of the same
is extracted hereunder:
“……Different polymorphs of a compound have different arrangements of
atoms and or molecules in their crystal structure. When the compound is a
biologically active compound, such as a fungicide, the difference in crystal
structures can lead to different polymorphs having differing chemical,
physical and biological properties. Properties which may be affected
include crystal shape, density, 25 hardness, colour, chemical stability,
melting point, hydroscopicity, suspensibility, dissolution rate and
biological availability. As such, a specific polymorph may have properties
which make it more advantageous in a particular use relative to another
polymorph of the same compound: in particular, the physical, chemical
and biological properties listed above can have a significant effect on the
development of production methods and formulations and the 30 quality
and efficacy of plant treatment agents, such as fungicides. It is noted that
predicting whether the solid state of a compound may be present as more
than one polymorph is not possible and nor is it possible to predict the
properties of any of these crystal forms.”
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 11 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
30. The learned Controller has rejected the subject application on the
grounds of lack of inventive step under Section 2(1)(ja) and non-patentability
under Section 3(d) of the Act. In the aforesaid backdrop, the merits of the
present appeal need to be examined.
OBJECTION UNDER SECTION 2(1) (ja) OF THE ACT:-
31. This Court has heard the learned counsel for the parties and has perused
the record. This Court shall now proceed to analyse the submissions made and
the material on record.
32. Before this Court adverts to the merits of the present appeal, since the
issue relates to a polymorph it would be appropriate to refer to certain articles
which have been collated after deep research into the behaviour of a
polymorph. It is important to note that the impugned order notes that thermal
stability is an inherent property of polymorphs.
33. In the Article “Facts and Fictions about Polymorphism” (Chem Soc
Rev, 2015, 44, 8619-8635) written by Auror J. et al , the authors quote “in
spite of an impressive array of contributions across a broad spectrum of their
chemical and physical aspects, polymorphic systems are in a many ways still
enigmatic, echoing the 1937 observation by Buerger and Bloom ‘ with the
accumulation of data, there is developing the gradual realization of the
generality of polymorphic behavior, but to many chemists polymorphism is
still a strange and unusual phenomenon .’” It is noted in the Article that among
the many solid state forms of a drug substance, a form that is both
thermodynamically stable and meets the design requirements of the drug
product is generally progressed in pharmaceutical development. Therefore, the
importance of identifying the thermodynamically stable form in early drug
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 12 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
product development cannot be overstated. The authors in the concluding
paragraph have stated “ many fictions have entered in the literature about the
connection between the molecular nature of compounds and their propensity
for polymorphism. Although, we have shown that there may be some possible
trends, the truth remains that polymorphism is unpredictable on the basis of
molecular structure ”. For better understanding, the relevant paras from pages
6 and 18 of the document are reproduced hereunder:
“ In spite of an impressive array of contributions across a broad
spectrum of their chemical and physical aspects, poly-morphic systems
are in many ways still enigmatic, echoing the 1937 observation by
Buerger and Bloom "with the accumula-tion of data, there is developing
a gradual realization of the generality of polymorphic behavior, but to
many chemists polymorphism is still a strange and unusual
phenomenon."
“Many fictions have entered in the literature about the connection
between the molecular nature of compounds and their propensity for
polymorphism. Although we have shown that there may be some possible
trends, the truth remains that polymorphism is unpredictable on the
basis of molecular structure”.
[emphasis supplied]
34. John F. Bauer, in his Article “Polymorphism- A Critical Consideration
in Pharmaceutical Development, Manufacturing and Stability” (Journal of
Validation Technology 2008) has conducted an in depth study of various
features, forms and laboratory studies to determine polymorphism and based
his Article on the API “ritonavir” which was the active ingredient in the
Norvir Capsule. The Ritonavir case was a classic example where the API
Ritonavir was identified as the key component in various protease inhibitor
cocktails used for the successful treatment of HIV infections. This enhanced
the therapeutic effectiveness of many aids therapies. After a number of lots of
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 13 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
the Norvir capsules had been successfully manufactured, in the summer of
1998, a sudden change in the physical properties of Ritonavir brought
production to a halt. The crystal form of Ritonavir had unexpectedly changed.
The said change resulted in solubility change for the drug which in turn
resulted in a bioavailability change and affected the therapeutic effect of the
drug. This only shows that though the drug would remain the same entity and
have the same chemical properties of stability, reactivity etc., it may not
always act in the same way in the solid state. The Ritonavir problem was
caused by a change in the solubility of Ritonavir that caused the drug to
precipitate from the capsule formulation and reduced its bioavailability to less
than 5%. The reason attributed to this change is stated to be a phenomenon
called polymorphism. Various polymorphs are chemically identical but can
have different physical properties. The conclusion of the abovementioned
document is reproduced hereunder:
“CONCLUSIONS
Although the chemical and physiological properties of a pharmaceutical
compound determine the potential of the compound as a commercially
viable drug product, the solid state properties of the compound are
extremely important in determining whether it can be reproduc-ibly
manufactured. Laboratory studies are key to deter-mining the potential of
a compound to form multiple polymorphs, under what conditions the
polymorphs are formed, the physical properties of each polymorph, and
the stability of each polymorph. Awareness, knowl-edge, and
understanding of polymorphism is important throughout the product
lifecycle. Polymorphism may impact product development, clinical studies,
product manufacturing, product quality, and product stability. The large
majority of manufacturing problems encoun-tered in commercial scale
manufacturing are related to the physical properties of the APL and/or
excipients. These problems may be caused by polymorphic changes.
Change management and validation in API manufacturing and product
manufacturing should address the potential impact of formulation and
process changes on API polymorphism.”
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 14 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
35. In the Ritonavir case, the change in solid form had a great effect on
solubility which in turn drastically reduced the bioavailability.
36. The author has also stated that as to which polymorph of a crystalline
drug will form under certain conditions cannot be predicted. It would be
apposite to extract relevant portion of the said Article to emphasize the
aforesaid observation, which is as under:
“POLYMORPHISM
The ritonavir problem was caused by a change in the - solubility of
ritonavir that caused the drug to precipi--tate from the capsule
formulation, and reduced its bioavailability to less than 5%. The reason
for this change is a phenomenon known as polymorphism. As described
previously, solids can exist as crystal-line, amorphous, solvate (hydrate),
and desolvated - (dehydrated) forms. Complicating this situation is the
fact that crystalline solids (and solvates/hydrates
anddesolvated/dehydrated solvates/hydrates) can exist in L what are
known as polymorphs. Crystals exist with the molecules arranged in a
repeating pattern with an identifiable symmetry However, there can be
more than one possible repeating pattern for many drugs. This can be
demonstrated by visualizing a number of identical Lego pieces of a
specific shape. Each Lego piece represents a drug molecule. These
individual Lego pieces can be assembled in several different ways to form
different symmetrical patterns. Each of the different patterns contains the
same number and type of individual Lego pieces.
Each of these different patterns would represent a different polymorph of
the drug. These various polymorphs are chemically identical but can have
significantly different physical properties. Because the molecules are
arranged differently in the different polymorphs, it is possible to have
different portions or functional groups of the molecule exposed at the
surfaces of the crystal. These differences, especially when they involve
hydrogen bonding groups, can cause the crystal to interact differently with
solvents and therefore change the solubility of the drug. This was the case
with ritonavir. A much less soluble poly-morph having five times lower
solubility was formed. The significantly different solubility of the new rito-
navir polymorphmadeitimpossible to manufacture the original Norvir
formulations.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 15 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
Different crystal arrangements or crystal lattices are possible for any
particular compound. Under particular temperature, pressure, and
humidity conditions, the various polymorphs of a drug have different
energies, There is one polymorph that has the lowest energy and is
considered the most stable. All other forms are referred to as metastable,
although they may be quite stable under that particular combination of
temperature, pressure, and humidity. Theoretically any metastable form
will convert to the stable form under particular conditions. However, this
conver-sion will be extraordinarily slow unless mediated by a solvent. In
the case of ritonavir, the solvent system in the capsule mediated the crystal
form change. The stability referred to here is the ease with which one solid
form converts to another solid form, for example, conversion of
amorphous solid to crystalline form or one polymorph to another. Crystal
polymorphs can also differ in chemical stability because the groups
present on the surface of the molecule will be more or less labile or
reactive. The tendency of a compound to attract water from the
atmosphere (i.e. hygroscopicity) is also the result of surface groups.
LABORATORY STUDIES TO DETERMINE POLYMORPHISM
Which polymorph of a crystalline drug will form under certain
conditions cannot be predicted . However, labora-tory experiments can be
conducted that will determine the potential for formation of multiple
polymorphs. These studies are performed by crystallizing the drug from
multiple solvents of differing polarities, different solvent combinations, at
different temperatures, at differ-ent rates of cooling, and other
experimental conditions. These studies are conducted in solid state
laboratories using a laboratory robot system.
The crystal form that will be easiest to form is the one closest in
arrangement to the drug in solution under the same environmental
conditions. This transition requires the least energy, and the form
produced is called the kinetic form. There may also be other forms that are
not as closely related to the dissolved drug but can also form under the
specific environmental conditions. The form that has the strongest internal
attractions within the crystal is the most stable form under these
conditions and is referred to as the thermodynamic form Given enough
time and especially if solvent mediated, the thermody-namic form of the
crystal would be the final and-most stable polymorphic crystal form
produced. When dif-ferent temperatures are involved, more complexity
may be introduced. For example, the simplest situations are those in which
a single polymorph is always the most stable polymorph regardless of
temperature, these systems are called monotropic systems. However, there
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 16 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
may be situations in which a different polymorph is the most stable
polymorph at a higher temperature; these systems are called enantiotropic
systems.
When multiple polymorphs of a drug are formed it is necessary to
understand their conditions of for-mation and the physical properties
associated with each form, Polymorphic interconversions have been
reported in the solid state caused by mechanical stress and/or high
temperature. The stability of each form must be studied. The information
learned in these studies is used in the selection of the appro-priate form
for development. Thereafter, laboratory information is useful for
development of the active pharmaceutical ingredient (API) manufactur-ing
process. When multiple-polymorphic-forms-are possible, it is critical to
understand the conditions under which they can interconvert In many
cases the forms do not differ enough to affect the manu-facture, stability,
and/or efficacy of the compound. However, this information is only known
through appropriate laboratory investigations.
One other important benefit of understanding the various polymorphs and
methods of preparation of dif-ferent polymorphs is that polymorphs are
patentable. This knowledge may thus provide commercial benefit for the
organization.”
[emphasis supplied]
37. Further under the heading “Polymorphs in pharmaceutical product
manufacturing” , the author states as under:
“POLYMORPHS IN PHARMACEUTICAL PRODUCT
MANUFACTURING
There are many reported examples of changes in solid form due to
conditions typical of product manufacturing processes. Examples of
processing that may cause poly-morphic changes including grinding,
milling, heating, and compressing. Manufacturing conditions that include
a solvent (e.g., wet granulation, polymorphs in solution, polymorphs in
suspension) may also facilitate conversion to the thermodynamic
polymorph. An often-cited article entitled "Disappearing Polymorphs" (3)
describes mul-tiple cases where a crystal form was developed and even
patented and marketed when a new polymorph suddenly appeared, and the
first form could no longer be produced. The extreme example of ritonavir
(Norvir) exemplifies the criticality of solid-state investigations during the
development of a new drug entity and manufacturing process development.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 17 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
This has been an important area of concern and emphasis by FDA and
International Conference on Harmonisation (ICH) in recent years.
The Norvir polymorph example discussed previously suggests an
additional concern in the formulation of liquid solution
products.Conventional wisdom suggests that since the drug is in solution,
polymorphic forms should be of no concern. However, extraneous
materials can sometimes seed new thermodynamic crystal forms that may
precipitate from solution. When solution prod-ucts are formulated, the
drug concentrations should be well below the saturation concentrations of
any of the known drug product polymorphs.
Any changes to the API manufacturing process or to the product
manufacturing process should address the potential for polymorphic
changes to the API crystal. The original API development work is helpful
in addressing the impact of these changes. Experimental research and
development studies should indicate whether there is potential for the API
molecule to form multiple poly-morphs, and the ease of interconversion
between poly-morphic forms. This information will form the basis for
appropriate testing in process validation.”
38. In another Article “Rapid Conversion of API Hydrates to Anhydrous
Forms in Aqueous Media” (Journal of Pharmaceutical Sciences, Vol. 98, No.
11.11.2009, by Petrova et al .), the authors have, in the abstract stated as under:
“ABSTRACT: Three anhydrous polymorphs, a monohydrate and a
dihydrate of an active pharmaceutical ingredient, N-([(5S)-3-(4-(6-
[(1R,5S)-6-cyano-3-oxabicyclo[3.1.0]hex-6-yl)pyridin-3-yl)phenyl)-2-
oxo-1,3-oxazolidin-5-yl]methyl)acetamide (Compound 1), have been
crystallized and characterized. Slurry experiments and thermal data have
been used to determine their relative thermodynamic stability. The
hydrates of Compound 1 were found to be less stable than the most stable
anhydrous Form I and converted into Form I in water within 15 min. The
rate of conversion in a dry state was found to depend on the relative
humidity (RH) and was highest at the two RH extremes examined, 5%
and 97.5% RH. 2009 Wiley-Liss, Inc. and the American Pharmacists
Association J Pharm Sci 98-4111-4118, 2009.”
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 18 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
39. From the above, it appears that there are multiple factors to be
considered by an entity while manufacturing a drug for therapeutic purposes
involving API where the occurrence of polymorphism is not unknown. It also
appears that various polymorphs are chemically identical but may have
significantly different properties. Specially, when they involve hydrogen
bonding groups, the differences can cause the crystal to interact differently
with solvents and therefore change the solubility of the drug which was the
case with Ritonavir. Thus, under a particular temperature, pressure and
humidity conditions, various polymorphs of a drug may have different
energies.
40. Further, the learned Controller has not cited any source while relying on
the common general knowledge. In AGFA NV (supra) , this Court emphasised
that while relying on ‘common general knowledge’ as a ground for refusing a
patent application, it is essential to specify the source of the said knowledge.
The relevant paras of the decision is reproduced hereunder:
“34. From the above extract, for the Controller to rely on ‘common
general knowledge’ as a ground for refusing a patent application, it is
essential to specify the source of the said knowledge. It would be essential
that the said source of the ‘common general knowledge’ would have been
published before the priority date of the patent application. In addition,
the fact that a theory or principal or knowledge has become common
knowledge needs to be substantiated by some evidence. The said evidence
could be in the form of references to the ‘common general knowledge’
textbooks or research articles or standard documents.
*
37. In the present case, however, the Controller has failed to give any
source of the common knowledge that has been considered. Therefore, it
cannot be construed as to what precise element of ‘common general
knowledge’ has been considered along with the cited prior art to claim
that the combination of the teachings of the prior art and the ‘common
general knowledge’ led to a finding of lack of inventive step.”
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 19 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
41. Therefore, the statement of the learned Controller that thermal stability
is an inherent property of polymorphs cannot be accepted in view of the above
cited documents as well as failure of the learned Controller to cite any sources
to support such statement.
42. It is the case of the respondent that the prior art documents D1 to D4
were considered as the closest prior arts. D1 discloses the crystalline form of
the compound of present formula-I (3-difluoromethy1-1 –methyl- 1 H-
pyrazole-4/carboxylic acid (9-dichloromethylene-1, 2, 3, 4-tetrahydro-1, 4-
methano- nephthalen-5-yl)-amide) and intermediates alongwith their
preparation process. It was also contended that prior art D2 to D4 also disclose
the same compound of formula-1, and its process for preparation. It is further
stated that the compound of formula-1 prepared in cited literature D1 to D4
generally involved in the crystallization and/or recrystallization process in
non-aqueous medium (hexane, xylene/methycyclohexane etc.) which led to
the formation of final crystalline product.
43. The respondent acknowledged that the distinguishing feature of the
subject application in comparison to the cited prior arts is the “monohydrate”
form of compound of formula-1 instead of “non-hydrate” form of compound
of formula-1. The respondent also admitted that none of the cited prior art
documents disclose the monohydrate form of compound of formula-1 and
thereby accepted the novelty of the claimed invention of the subject
application. However, the respondent found lack of evidence for any
surprising effect over the cited prior arts D1 to D4. According to the
respondent, the evidence which ought to have been furnished by the appellant
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 20 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
could be in the form of a comparative data in terms of lowering phytotoxicity
between the monohydrate form of compound of formula-1 and the non-
hydrate form as disclosed in the prior art D1 to D4. Since the appellant did not
provide the comparative data, there was no credible evidence of a surprising
effect over prior art D1 to D4. It was on this basis that the respondent did not
find any inventive step under Section 2(1)(ja) of the Act.
44. As per the respondent, the x-ray diffraction pattern provided by the
appellant was only a characterization data which could not be considered as a
technical feature. Respondents claim that the diffraction pattern may provide
information about the compound structure, however, does not contribute to the
technical advancement.
45. The respondent also stated that the claimed composition does not
comprise any component that has its own technical feature and rather it
comprises only excipient and carrier which is commonly known to the person
skilled in the art.
46. It is important to note that the appellant conducted experiments to
determine thermal stability of the hydrate and anhydrous form using
Differential Scanning Calorimetry (DSC). The Example 3 and Table 3 of the
CS of subject application disclose the experiment where slurries of both
anhydrous polymorph form 1 and the monohydrate crystalline polymorph of
compound of formula I were prepared in different water/methanol mixtures
and at different temperatures. Table 3 from the CS of the subject application is
reproduced below which provides the results of the experiments:
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 21 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
47. Further, as per the CS of the subject application, a phase diagram as
shown below in FIG. 3 is plotted with the water activities from the
abovementioned Table 3:
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 22 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
48. The aforesaid phase diagram demonstrates that temperature in excess of
60 °C would be required to dehydrate the hydrate of compound of formula I at
normal ambient relative humidities which indicates that the hydrate of
formula-1 would be the stable form of compound I in suspension concentrate
formulations and would also be more stable in other, non-aqueous,
formulations upon their dilution with water in the spray tank. In case the
anhydrous form-1 is used under these conditions, it is likely to lead to
polymorphic conversion to the hydrate and resultant crystal growth which
would potentially result in blocked nozzles in spray equipment.
49. The CS of the subject application under Example 5 also compares the
stability of the formulations of polymorphs. Here, two standard SC
formulations were prepared separately using the anhydrous Form 1 polymorph
and the hydrated polymorph. The SC of the anhydrous Form 1 was
contaminated with 5% of the hydrated form and was placed in a temperature
cycling oven varying in the range 0°C to 40°C over a period of 12 hours.
Thereafter, the sample was inspected after two weeks and microscopy showed
that the size of the crystals had increased substantially. Some crystals were
removed from the formulation and dried. The powder X-ray diffraction pattern
was collected which showed that all of the anhydrous polymorph Form 1 were
completely converted into the hydrated form. The comparative powder X-ray
diffraction trace is shown in FIG. 7 and is reproduced below:
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 23 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
50. The appellant had demonstrated that the suspension concentrate of
crystalline polymorph of compound of formula-1 which is a monohydrate
containing 4.3 ± 0.2 % w/w water is more stable than the suspension
concentrate of the comparative anhydrous form. Since the suspension
concentrate used less chemicals, it was presumed that the suspension
concentrate would have a reduced phytotoxicity. In order to show the
distinction between the subject application and that of the prior documents D1
to D4, it appears necessary to extract hereunder the disclosures in such
documents:
“5.3.7. Documents D1 to D4 cited by the Respondent disclose the
following:
- D1 (WO 2011/131544A1) relates to a process for the preparation of 3-
difluoromethyl-lmethyl-I H-pyrazole-4-carboxylic acid (9-
dichloromethylene-l ,2,3,4-tetrahydro-1 ,4methano-naphthalen-5-yl)-
amide which is the compound of formula I. D1 at step f) of the examples at
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 24 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
lines 8-9 of page 327 of the appeal states that the product was extracted
and crystallized in mixture of xylene/methylcyclohexane. Therefore, the
compound of D1 is anhydrous and the monohydrate crystalline form of IN
`1900 is not disclosed in D1.
- D2 (WO 2011/131545A1) also relates to a process for the preparation of
3- difluoromethyl-l methyl-I H-pyrazole-4-carboxyIic acid (9-
dichloromethylenel ,2,3,4-tetrahydro-1 ,4methano-naphthalen-5-yl) amide
which is the compound of formula I. D2 at step g) of the examples at line
15 of page 357 of the appeal states that the product was extracted and
crystallized in mixture of xylene/methylcyclohexane. Therefore, the
compound of D2 is anhydrous and the monohydrate crystalline form of IN
`1900 is not disclosed in D2.
- D3 (WO 2011/131546A1) also relates to a process for the preparation of
3- difluoromethyl-l methyl-I H-pyrazole-4-carboxyIic acid (9-
dichloromethylenel ,2,3,4-tetrahydro-1 ,4methano-naphthalen-5-yl) amide
which is the compound of formula I. D3 at step d) of the examples at lines
24-25 of page 383 of the appeal states that the product was extracted and
crystallized in mixture of xylene/methylcyclohexane. Therefore, the
compound of D3 is anhydrous and the monohydrate crystalline form of IN
`1900 is not disclosed in D3.
- D4 (US 2012/136162A1) relates to a process for the preparation of
compound of formula I. D4 at example P6 [para 82] at page 399 of the
appeal states that the crude material was dissolved in mixture of xylene
and methylcyclohexane. Therefore, the compound of D4 is anhydrous and
the monohydrate crystalline form of IN `1900 is not disclosed in D4.”
51. As per the respondent, the statement in the affidavit of Dr. John Hone
states that the use of the compound of the present invention might be
advantageous, however, is not definite. It indicates that it might not be
advantageous or the crystal may not form in every case.
52. From the affidavit, the respondent submits that the expert does not give
a definitive opinion that there is a problem which is solved. The respondent
has also emphasised that Dr. John Hone does not opine that there is an
enhancement of efficacy. The relevant paragraph of the said affidavit is
extracted hereunder:
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 25 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
“Technical Solution provided by the Current ApplicationIt is important to
mention that the use of a specific polymorph allows the use of new
formulations compared with existing polymorphic/amorphous forms of a
compound. This might be advantageous for a number of reasons. For
example, a suspension concentrate (SC) formulation may be preferred
over an emulsion
Nonetheless, if the existing form of a compound is not stable in such an SC
formulation, polymorphic conversion might occur leading to unwanted
crystal growth. Such crystal growth is detrimental because it leads to, for
example, thickening and potentially solidification of the formulation which
can lead to blockages in application equipment, e.g. in spray nozzles in
agricultural application machinery. Using a stablepolymorphic form
would overcome these issues.”
53. After going through the said affidavit, this Court agrees with the
submissions of the respondent that a specific conclusion cannot be drawn.
Therefore, it appears appropriate to not take into consideration the opinion in
the affidavit at this stage.
54. From the above, it can be gathered that the respondent does not dispute
that the monohydrate crystalline polymorph of compound of formula-1 of the
subject patent application was not known; the specifications clearly provided
the thermal stability data to demonstrate that the monohydrate crystalline
polymorph of formula-1 is more stable than the anhydrous form-1 which
would indicate a technical advance over the cited documents D1 to D4. The
improved thermal stability can be presumed to be the technical effect that
ensures the compound can be delivered as a SC provided the same is present
as monohydrate crystalline polymorph of compound of formula-1 and not in
any other form. Since the formulation is in SC, the enhanced thermal stability
would be linked to the lowering of phytotoxicity. The learned Controller has
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 26 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
to provide reasoning as to how the provided data is not sufficient/relevant to
show the inventive step.
55. It is relevant to also consider at this stage whether thermal stability of a
polymorph would be a relevant consideration in order to determine efficacy.
As noted by this Court in the preceding paragraphs containing excerpts of
various Articles regarding polymorphism, it is clear that polymorphic forms
are unpredictable in nature. It is verily not possible to predict whether a
compound can be present in more than one polymorphic form nor is it
possible to predict the properties of any of the crystal forms. Prior to the
research and study conducted by the appellant, it could not be stated with
conviction that the monohydrate crystalline polymorph would be thermally
more stable than the anhydrous form. It can be safely presumed that
preparation of a polymorphic compound is highly unpredictable and would
require extensive research in order to achieve a desired polymorphic
compound. It is in this context that the learned Controller ought to have seen
that none of the prior arts disclose that a monohydrate crystalline polymorph
of compound of formula-1 of the subject patent invention could exist or that
the said polymorph would be more stable than its anhydrous form.
56. Thus, the conclusion of the objection regarding the lack of inventive
step under Section 2(1)(ja) of the Act was not satisfactorily explained, is
unmerited and untenable.
57. In the aforesaid circumstances, it appears apposite to examine the
enquiries which are to be conducted by the learned Controller for the
determination of obviousness. This Court in F-Hoffmann-la Roche Ltd. &
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 27 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
Anr. vs. Cipla Ltd . : 2015:DHC:9674-DB held the following enquiries
necessary to be conducted for determination of obviousness:
“Step No.1 To identify an ordinary person skilled in the art,
Step No.2 To identify the inventive concept embodied in the patent,
Step No.3 To impute to a normal skilled but unimaginative ordinary
person skilled in the art what was common general knowledge in the art at
the priority date. Step No.4 To identify the differences, if any, between the
matter cited and the alleged invention and ascertain whether the
differences are ordinary application of law or involve various different
steps requiring multiple, theoretical and practical applications,
Step No.5 To decide whether those differences, viewed in the knowledge of
alleged invention, constituted steps which would have been obvious to the
ordinary person skilled in the art and rule out a hindsight approach.”
58. Similarly, in so far as the determination of lack of inventive step is
concerned, this Court in Agriboard International LLC vs. Deputy Controller
of Patents and Designs: 2022 SCC Online Del 940 held as under:
“24. In the opinion of this Court, while rejecting an invention for lack of
inventive step, the Controller has to consider three elements-
• the invention disclosed in the prior art,
• the invention disclosed in the application under consideration,
and
• the manner in which subject invention would be obvious to a
person skilled in the art.
•
25. Without a discussion on these three elements, arriving at a bare
conclusion that the subject invention is lacking inventive step would not be
permissible, unless it is a case where the same is absolutely clear. Section
2(1)(ja) of the Act defines `inventive step' as under:
(ja) "inventive step" means a feature of an invention that involves
technical advance as compared to the existing knowledge or
having economic significance or both and that makes the invention
not obvious to a person skilled in the art.
26. Thus, the Controller has to analyse as to what the existing knowledge
is and how the person skilled in the art would move from the existing
knowledge to the subject invention, captured in the application under
consideration. Without such an analysis, the rejection of the patent
application under Section 2(1)(ja) of the Act would be contrary to the
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 28 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
provision itself. The remaining prior arts which are cited by the ld.
Counsel having not been considered in the impugned order, the Court
does not wish to render any opinion in this regard.”
59. Since the learned Controller has failed to cite the documents while
stating that the thermal stability is an inherent property of the polymorphs, it
can be concluded that the abovementioned steps are not followed.
60. Based on the above discussion and data provided by the appellant, it has
demonstrated that the crystalline polymorph of compound of formula I which
is a monohydrate containing 4.3 ± 0.2 % w/w water is more stable than SC of
the comparative anhydrous form. Further, as per the CS of the subject
application, such stable SC are less phytotoxic. Based on the documents
discussed above, it is pertinent that it was difficult to prepare a stable SC of
base compound of formula 1. Therefore, in view of the above, it appears that
the learned Controller could not have concluded with conviction that the
appellant has not been able to overcome the objection under Section 2(1)(ja)
of the Act.
OBJECTION UNDER SECTION 3(d) OF THE ACT
61. The other objection raised by the learned Controller is under Section 3
(d) of the Act. The counsel for the respondent submitted that under Section 3
(d) of the Act, polymorphs shall be considered to be the same substance,
unless they differ significantly in properties with regard to efficacy. For better
understanding Section 3(d) of the Act is reproduced as follows:
“(d) the mere discovery of a new form of a known substance which does
not result in the enhancement of the known efficacy of that substance or
the mere discovery of any new property or new use for a known substance
or of the mere use of a known process, machine or apparatus unless such
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 29 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
known process results in a new product or employs at least one new
reactant.
Explanation.—For the purposes of this clause, salts, esters, ethers,
polymorphs, metabolites, pure form, particle size, isomers, mixtures of
isomers, complexes, combinations and other derivatives of known
substance shall be considered to be the same substance, unless they differ
significantly in properties with regard to efficacy.”
[emphasis supplied]
62. The other argument under objection of Section 3(d) of the Act raised by
the Patent Office was in respect of lack of evidence regarding therapeutic
efficacy of the subject patent application. In other words, the enhancement of
thermodynamic stability of the monohydrate crystalline polymorph of
compound of formula-1 at temperatures around 50°C to 60°C which may
result in non-clogging of the spraying equipment, however, does not enhance
the therapeutic efficacy of the compound itself. The respondent had
vehemently objected that in pharmaceutical preparations or agro chemicals,
the efficacy has to be measured in terms of enhancement in the therapeutic
efficacy of the compound alone. Since admittedly, there is no enhancement in
the therapeutic efficacy of the compound itself, the enhancement in the
thermodynamic stability of the monohydrate crystalline polymorph of
compound of formula-1, by itself, cannot satisfy the objection under Section
3(d) of the Act. The respondent had relied upon the judgment of the Supreme
Court in Novartis AG ( supra ).
63. It is important to determine the applicability of the 2005 amendment of
the Section 3(d) of the Act. In Novartis AG ( supra ), the Supreme Court held
that the amended portion of Section 3(d) of the Act clearly sets up a second
tier of qualifying standards for chemical substances/pharmaceutical products
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 30 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
to leave the door open for genuine inventions and also to check evergreening.
The relevant para is reproduced hereunder:
“ 87. We are clearly of the view that the importance of the amendment
made in section 3(d), that is, the addition of the opening words in the
substantive provision and the insertion of explanation to the substantive
provision, cannot be under-estimated. It is seen above that, in course of
the Parliamentary debates, the amendment in section 3(d) was the only
provision cited by the Government to allay the fears of the Opposition
members concerning the abuses to which a product patent in medicines
may be vulnerable. We have, therefore, no doubt that the
amendment/addition made in section 3(d) is meant especially to deal with
chemical substances, and more particularly pharmaceutical products. The
amended portion of section 3(d) clearly sets up a second tier of
qualifying standards for chemical substances/pharmaceutical products
in order to leave the door open for true and genuine inventions but, at
the same time, to check any attempt at repetitive patenting or extension
of the patent term on spurious grounds.”
[emphasis supplied]
64. No doubt that what was engaging the attention of the Supreme Court in
Novartis AG (supra) was the significance of amendment in the year 2005 to
Section 3(d) of the Act. The Supreme Court had, in detail, considered the
amendment, the Parliamentary debates, the TRIPS agreement and the public
health interest involved while rendering its opinion in the said judgment. The
Supreme Court had also noted that 80% of the parliamentary debates revolve
around pharmaceutical preparations, medicines and drugs; and 20% were in
respect of agro chemicals. The Supreme Court also noted that the
apprehension of “Evergreening” of certain inventions though is made out, yet,
encouragement of incremental inventions ought to also to be taken into
consideration. It is to be noted that the Supreme Court was considering and
had rendered its judgment in the context of pharmaceuticals and medicines,
though it also referred to agro chemicals but more, in the humble opinion of
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 31 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
this Court, in the passing. The Supreme Court in para 157 of the judgment had
considered what “Efficacy” would mean. It would be beneficial to extract para
157 of the said judgement as hereunder:
“157. What is “efficacy”? Efficacy means “the ability to produce a
desired or intended result”. Hence, the test of efficacy in the context of
section 3(d) would be different, depending upon the result the product
under consideration is desired or intended to produce. In other words, the
test of efficacy would depend upon the function, utility or the purpose of
the product under consideration. Therefore, in the case of a medicine
that claims to cure a disease, the test of efficacy can only be “therapeutic
efficacy”. The question then arises, what would be the parameter of
therapeutic efficacy and what are the advantages and benefits that may be
taken into account for determining the enhancement of therapeutic
efficacy? With regard to the genesis of section 3(d), and more particularly
the circumstances in which section 3(d) was amended to make it even
more constrictive than before, we have no doubt that the “therapeutic
efficacy” of a medicine must be judged strictly and narrowly. Our
inference that the test of enhanced efficacy in case of chemical substances,
especially medicine, should receive a narrow and strict interpretation is
based not only on external factors but there are sufficient internal
evidence that leads to the same view. It may be noted that the text added to
section 3(d) by the 2005 amendment lays down the condition of
“enhancement of the known efficacy”. Further, the explanation requires
the derivative to “differ significantly in properties with regard to
efficacy”. What is evident, therefore, is that not all advantageous or
beneficial properties are relevant, but only such properties that directly
relate to efficacy, which in case of medicine, as seen above, is its
therapeutic efficacy.”
[emphasis supplied]
65. From a plain understanding of para 157, it appears that the Supreme
Court had considered enhancement in “therapeutic efficacy” as the test to pass
the objection in Section 3(d) of the Act. In other words, unless there is an
enhancement in therapeutic effect of the known substance, the patent
application would be barred under the provisions of Section 3(d) of the Act.
The sentence “ Therefore, in the case of a medicine that claims to cure a
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 32 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
disease, the test of efficacy can only be “therapeutic efficacy” indicates that
the efficacy would be therapeutic efficacy in case of the medicine. Therefore,
it can be stated that in other cases, the test of efficacy would be determined as
per their function, utility or the purpose of the product under consideration. It
would also be relevant to extract para 164 of the abovementioned judgement:
“164. In whatever way therapeutic efficacy may be interpreted, this much
is absolutely clear: that the physico-chemical properties of beta crystalline
form of Imatinib Mesylate, namely (i) more beneficial flow properties, (ii)
better thermodynamic stability, and (iii) lower hygroscopicity, may be
otherwise beneficial but these properties cannot even be taken into
account for the purpose of the test of section 3(d) of the Act, since these
properties have nothing to do with therapeutic efficacy. 188. This leaves
us to consider the issue of increased bioavailability. It is the case of the
appellant that the beta crystalline form of Imatinib Mesylate has 30 per
cent increased bioavailability as compared to Imatinib in free base form.
If the submission of Mr. Grover is to be accepted, then bioavailability also
falls outside the area of efficacy in case of a medicine. Leaving aside the
submission of Mr. Grover on the issue, however, the question is, can a
bald assertion in regard to increased bioavailability lead to an inference
of enhanced therapeutic efficacy? Prof. Basheer quoted from a
commentator1 on the issue of bioavailability as under:
“It is not the intent of a bio-availability study to demonstrate
effectiveness, but to determine the rate and extent of absorption. If
a drug product is not bioavailable, it cannot be regarded as
effective. However, a determination that a drug product is bio-
available is not in itself a determination of effectiveness.”
[emphasis supplied]
66. Clearly, the Supreme Court spelt out what would not amount to
enhancement of the therapeutic effect of a medicinal preparation or a drug. In
that, neither the more beneficial flow properties nor better thermodynamic
stability or lower hygroscopicity would fall within the meaning of “therapeutic
efficacy”. It is in that context that the respondent appears to have raised the
objection that the mere enhancement of the thermodynamic stability of the
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 33 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
monohydrate crystalline polymorph of the compound of formula 1 of the
subject patent application would not come within the definition of therapeutic
efficacy as defined by the Supreme Court in Novartis AG ( supra ).
67. In the present case, it is not disputed that the subject patent invention
claims primarily thermodynamic stability of a polymorph at temperatures
ranging upto 50°C – 60°C. It is also to be noted that the subject patent
application concerns an agrochemical. The respondent does not dispute that
the thermodynamic stability which is the subject matter of the patent
application is likely to prevent formation of crystals in the compound which
causes the formation of lumps which is used in the tank of the spraying
machine which in turn clogs the spray gun preventing spraying of agro
chemical on the plants. One cannot lose sight of the fact that the agricultural
sector in India, largely are in regions where temperatures ordinarily would be
above 35°C to 48°C–50°C. In which case, the monohydrate crystalline
polymorph of compound of formula-1 of the subject application would
enhance the efficacy of the compound to be sprayed on the plants without the
crystallization of the compound itself, which would prevent formation of clogs
in the spray gun itself. The mere fact that the fungicide could be made
available to be used in such regions with such high temperatures, in the
considered opinion of this Court, would be an enhancement in the efficacy
under Section 3(d) of the Act. In the opinion of this Court, in the context of
present agro chemical, enhancement of efficacy of a known substance,
particularly in view of the present polymorph, would also include the
thermodynamic stability at high temperatures. The Court is rendering this
opinion on the basis of excerpts of the Articles referred to above in the
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 34 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
preceding paragraphs, which are based on detailed research and opined that
polymorphs are unpredictable in nature. Therefore, stability of the polymorph
at high temperature such as claimed in the subject application, the said
thermodynamic stability preventing the crystal formation, by itself would be
an enhancement in efficacy.
68. The Madras High Court in Novozymes (supra) interpreted the ratio laid
down in Novartis AG (supra) to hold that the Supreme Court had tested the
definition of efficacy in the context of pharmaceutical products and therefore,
so far as efficacy in the context of biochemical substances/phytase variant is
concerned, which was the subject matter of the petition before the Madras
High Court, the learned Single Judge held that the expression “the
enhancement of known efficacy of that substance” does not limit such
enhancement to any particular type of efficacy. The learned Single Judge had
also held that an increase of thermostability would mean that the enzyme can
resist and survive exposure to higher temperature and as a consequence, it
enables pelletization without deactivation or denaturation of enzymatic
activity. Thus, the thermostability enables products, storage and sale in pellet
form would amount to an enhancement in efficacy. The Court, based on the
Novartis AG (supra), emphasized that the test of efficacy would be different
depending on the function, purpose or utility of the product. The relevant
paras are reproduced hereunder:
“20. From the data set out in Table 5 of the complete specification, it is
discernible that the thermostability of the reference phytases was much
lower than the thermostability of the variants. While Section 3(d) uses the
expression “the enhancement of the known efficacy of that substance”,
there is nothing in the text that limits such enhancement to any specific
type of efficacy. As discussed earlier, in Novartis SC, the Supreme Court
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 35 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
concluded that the test of efficacy would be different depending on the
function, purpose or utility of the product. The respondent contended
that phytase is an enzyme and that, therefore, the enhancement of
efficacy means no more than enhancement of the enzymatic activity of
the variant of phytase.
*
22. Without doubt, the primary function of phytase is to act as a catalyst
that aids digestion. That does not mean that enhanced hydrolysis of
phytate by the variants of phytase should be established as an essential
pre-requisite to pass through the filter of enhancement of the known
efficacy of phytase. An increase in thermostability admittedly means the
enzyme can Dresist and survive exposure to higher temperature. As a
consequence, it enables pelletization without de-activation or
denaturation of enzymatic activity. The application of molecular
techniques to prospect thermostable phytases appears to be critical for the
animal feed and fuel industries and reference may be made, in such
regard, to the article by Ushashree Mrudula Vasudevan, Amit K.Jaiswal,
Shyam Krishna, Ashok Pandey, “Thermostable phytase in feed and fuel
industries”in Bioresource Technology, Volume 278, 2019, pages 400-407.
Since increased thermostability precludes denaturation and enables
production, storage and sale in pellet form, it enhances the known
efficacy of the enzyme in aiding digestion especially when used in
animal feed. In my view, there is nothing in the text or context of Section
3(d) which supports the interpretation that enhancement of known
efficacy of the substance should be restricted to engineering or
prospecting variants of phytase with inherently greater enzymatic activity
over the reference phytase.”
[emphasis supplied]
69. It is important to note that the Court also held that there is nothing in the
text/context of Section 3(d) of the Act which supports the interpretation that
enhancement of known efficacy of the substance should be restricted to
engineering/prospecting variants of phytase with inherently enhanced
enzymatic activity as compared to the reference phytase.
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 36 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
70. Similarly, in the present case, the monohydrate crystalline polymorph of
the compound of form-1, which is the subject matter of subject patent
application ensures that the compound “Benzovindiflupyr” remains stable
even at temperatures between 50°C–60°C and does not form crystals which
would result in the formation of lumps clogging the spraying machine and is
available for being sprayed on the plants even in high temperature zones. The
mere fact that the fungicide named above is made available to be used and
sprayed at regions where the temperature would ordinarily go beyond 40°C
without crystallisation would clearly be an enhancement in the efficacy of the
compound. Therefore, as per this Court, there is a reasonable enhancement of
efficacy under the claimed invention of the subject application and satisfies
the requirement of enhancement of the efficacy under Section 3(d) of the Act.
It is in this context that the non-enhancement of therapeutic efficacy in the
claimed invention of the subject application would not be a bar under Section
3(d) of the Act.
CONCLUSION:-
71. Therefore, without going into the merits of the issues arising out of
prior art documents D1 to D4, and other cited documents, in the opinion of
this Court, the omission of the submitted data by the Patent Office without any
sufficient reasoning and reliance on the existing knowledge without citing the
relevant source, vitiates the impugned order.
72. Accordingly, in view of the above discussion, the impugned order
dated 21.07.2023 passed by the learned Controller is set aside, and the matter
is remanded back to the Patent Office for fresh consideration. The learned
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 37 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09
Controller shall afford a fresh opportunity of hearing to the appellant before
deciding the subject application.
73. The learned Controller shall decide the matter on the merits in
accordance with the law, uninfluenced by any observations in respect of the
objection raised under Section 2(1)(ja) of the Act. However, as far as the
objection under Section 3(d) of the Act is concerned, this Court has made a
clear opinion. The learned Controller shall reconsider and decide the matter
accordingly within a period of six months from the date of this decision.
74. A copy of the Order also be brought to the notice of the learned
Controller General of Patents, Designs and Trademarks for the necessary
administrative action.
75. The appeal is disposed of in the aforesaid terms.
TUSHAR RAO GEDELA
(JUDGE)
MAY 04, 2026
yrj/rl
Signature Not Verified
C.A.(COMM.IPD-PAT) 49/2023 Page 38 of 38
Digitally Signed
By:YASHRAJ
Signing Date:04.05.2026
17:48:09