Delhi High Court
Chugai Seiyaku Kabushiki Kaisha vs Controller Of Patents And Design on 6 April, 2022
Author: Prathiba M. Singh
Bench: Prathiba M. Singh
Signature Not Verified
Digitally Signed
By:DEVANSHU JOSHI
Signing Date:14.04.2022
08:26:01
$~1
* IN THE HIGH COURT OF DELHI AT NEW DELHI
Date of Decision: 6th April, 2022
+ C.A.(COMM.IPD-PAT) 4/2021
CHUGAI SEIYAKU KABUSHIKI KAISHA ..... Appellant
Through: Mr. Jayant Kumar, Advocate.
versus
CONTROLLER OF PATENTS AND DESIGN ..... Respondent
Through: Mr. Harish V. Shankar, CGSC with
Ms. S. Bushra Kazim and Mr. Srish
Kumar Mishra, Advocates.
(M:9810788606)
CORAM:
JUSTICE PRATHIBA M. SINGH
Prathiba M. Singh, J. (Oral)
1. This hearing has been done through hybrid mode.
2. The present appeal has been filed challenging the order dated 23rd February, 2021 passed by the Assistant Controller of Patents and Designs, New Delhi (hereinafter, "Controller"). By the impugned order, the patent application No.201617023236 dated 6th July, 2016 filed by the Appellant/Applicant - Chugai Seiyaku Kabushiki Kaisha (hereinafter the 'Appellant') has been rejected by the Controller.
3. The said patent application relates to an invention titled 'Solid Preparation Containing Tofogliflozin and Process for Producing Same' (hereinafter "subject patent"). The case of the Appellant is that the subject invention provides a novel production method of solid preparations of the compound, the International Nonproprietary Name (INN) or generic name of which is Tofogliflozin (chemical name: 1,1-Anhydro-1-C-[5-(4- ethylphenyl)methyl-2-(hydroxymethyl)phenyl]-β-D-glucopyranose). The C.A.(COMM.IPD-PAT) 4/2021 Page 1 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 compound Tofogliflozin is used in the treatment of diabetes mellitus. The compound Tofogliflozin is represented by the following chemical formula:
4. The subject invention specifically provides a method for preparation of a tablet comprising Tofogliflozin from the powder mixture by direct compression. The Appellant submits that its invention provides a tablet comprising Tofoglifozin with improved disintegration and dissolution properties as compared to the conventional production methods and is hence entitled to grant of a patent.
5. The National Phase Application was based on the PCT Application No. PCT/JP2014/084561 dated 26th December, 2014 in India in the name of 'Chugai Seiyaku Kabushiki Kaisha' and claimed priority from Japanese Application No.JP 273060/2013 dated 27th December, 2013. The application was published on 31st August, 2016 and request for examination was filed by the Appellant on 1st December, 2017. The First Examination Report (hereinafter "FER") was issued by the Patent Office on 8th March, 2019. The following objections were taken under the FER:
(a) Claims 1 to 15 were hit by Section 2(1)(j) of the Patents Act, C.A.(COMM.IPD-PAT) 4/2021 Page 2 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 1970 (hereinafter "Act") for lack of novelty and inventive step as also industrial applicability.
(b) Claims were also non-patentable under Section 3 of the Act.
(c) Claims were hit by Section 10(5) and 10(4)(c) of the Act for lack of clarity and conciseness as also definitiveness.
6. The summary of the FER dated 8th March, 2019 is extracted below:
7. In the FER, the Patent office cited the following three documents of the Appellant itself, as the prior arts in respect of the Claims 1-15:
"1. WO 2006/080421 A1 (Chugai Pharmaceutical Co., Ltd) published on 3rd August, 2006.
2. WO 2012/115249 A1 (Chugai Pharmaceutical Co., Ltd) published on 30th August, 2012.
3. WO 2009/154276 A1 (Chugai Pharmaceutical Co., Ltd) published on 13th December, 2009."
8. In response to the FER, the Appellant filed a Reply dated 6th C.A.(COMM.IPD-PAT) 4/2021 Page 3 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 September, 2019 amending the Claims as set out below:
"At the outset, we humbly bring to the Ld. Controller's notice that claims of present invention have been suitably amended as indicated below. The presently amended Claims 1 to 5 and 7 to 9 basically relate to Claims 1 to 8 of the corresponding US Patent No. 10,398,653 B2.
− Claim 1 is amended by introducing the limitations of current Claims 5, 7, 10 and 11 and a limitation that the tofogliflozin is present in a form of monohydrate crystal.
− Claims 5, 7, 9 to 11, and 15 are cancelled − Claims 6, 8, and 12 to 15 are renumbered as amended Claim 5 to 9.
− Minor revisions are made on current Claims 6 and 8 (amended Claims 5 and 6)."
9. In respect of the objection relating to lack of inventive step, it was argued in the Reply that none of the cited prior art documents i.e., D1 to D3, include any description or suggestion regarding the step of obtaining a tablet from the powder mixture by using the direct compression technique as recited in Claim 1. It was, thus, argued that the amended claims would be novel and inventive.
10. Insofar as the objection relating to non-patentability is concerned, the Appellant claimed that the method for which the patent was sought was not hit by Section 3(d) or 3(e) of the Act. The objections relating to lack of clarity and conciseness as also definitiveness, under Section 10 of the Act, were also addressed by the Appellant in the reply.
11. Thereafter, a hearing was given to the Appellant on 22nd January, 2020 and vide the impugned order dated 23rd February, 2021, the Appellant's patent application was rejected by the Controller. The broad C.A.(COMM.IPD-PAT) 4/2021 Page 4 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 grounds for rejection under the impugned order are set out below:
"(1) Noveltv and inventive steps:
The present invention is "A method for producing a pharmaceutical composition which is a tablet comprising tofogliflozin as an active ingredient, wherein the tofogliflozin is present in a form of monohydrate crystal "tofogliflozin is a pre- existing drug in prior art. Inventor has used its monohydrate crystal form to prepare compositions. In which tofogliflozin is an active ingredient, Which is already used in prior art as cited documents no D1 (WO 2006/080421 A1), D2 (WO 2012/115249 A1) and D3 (WO 2009/154276 A1). Therefore, this is a new use of a known drug.
There is no inventive step and no technical advancement in the invention. This invention is not a new product or process. Therefore, on combining the technical teachings of D1-D3 and mere common technical knowledge a person skilled in the art can arrive at the amended set of claims and hence lacks an inventive step." Section 3 (d) :
It is observed that the present invention is a new use of new form of a known drug tofogliflozin. Inventor has used a monohydrate crystal form of a known drug to prepare method of compositions. A monohydrate crystal form of tofogliflozin Which is a form of original drug. Therefore, this is an invention to make a product by process and its new use, No enhance efficacy has been found in this invention, Claims 1 to 8 falls within the scope of section 3(d) of the Patent (Amendment) Act, 2005 as the claimed "a method for producing a pharmaceutical composition" are mere new forms of known substance having no significant difference with regard to efficacy over the parent//base compound.
Thus, amended Claims 1-8 do fall within the scope C.A.(COMM.IPD-PAT) 4/2021 Page 5 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 of Section 3 (d) of the Patent Act 1970 as amended in 2005."
12. In view of the above grounds, the Controller concluded that the subject patent was lacking inventive step and also attracted Section 3(d) of the Act. Therefore, the patent application of the Appellant was rejected. The operative portion of the impugned order reads as under:
"Conclusion On considering all the submissions, documents and facts the invention made therein along with the amended set of claims, it is observed that the claims of Present invention on the subject matter the patent application does not involve inventive step under section 2(1)(j) and fall under section 3(d) of the Patents 1970 as (Amended) Act, 2005. Therefore, in view of the outstanding objections as above, this application no.20L617023236 is hereby refused under section 15 of the Patents Act."
13. Mr. Jayant Kumar, ld. Counsel appearing for the Appellant/Applicant has made the following submissions:
i. That the objection under Section 3(d) of the Act has been wrongly applied by the Controller while rejecting the Appellant's patent application. He submits that Section 3(d) of the Act would not be attracted in the present case as the claims relate to a method patent and the Appellant seeks a patent only for the process of manufacturing of a monohydrate crystal form of Tofogliflozin, which would be sold in the tablet form. ii. That, insofar as the objection relating to lack of inventive step is concerned, the Controller has wrongly held that this is a C.A.(COMM.IPD-PAT) 4/2021 Page 6 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 case of new use of known drug. Instead, the Appellant's case is not that of new use of a known drug, but for a method for producing a more stable tablet form of the original drug Tofogliflozin. Thus, even on account of lack of inventive step, the objection has been wrongly raised by the Controller. iii. That, after the amendment of the claims upon the receipt of the FER, the subject patent was liable to be granted since the pharmaceutical preparation itself was not sought to be patented, but merely the process was sought to be patented.
14. On the other hand, Mr. Harish Vaidyanathan Shankar, ld. CGSC appearing for the Controller, submits that the present case is squarely covered by the judgment of the Supreme Court in Novartis AG v. Union of India and Ors. [(2013) 6 SCC 1]. The drug Tofogliflozin is already a pharmaceutical preparation covered under the patents previously granted in favour of the Appellant. The seeking of the present patent is nothing but an attempt to evergreen the earlier patent. The mere method for preparation of a tablet form of Tofogliflozin by direct compression method would not be patentable as the same would not constitute enhancement in therapeutic efficacy of the drug.
15. Heard ld. Counsels for the parties.
16. It is not in dispute that the Appellant has applied for various patents in respect of Tofogliflozin. The said three patents have been cited in the FER as prior art documents D1, D2 and D3. All three patents relate to the same pharmaceutical preparation i.e., Tofogliflozin. A perusal of the said patents clearly show that the compound Tofogliflozin is clearly covered and tablet forms are also covered. Relevant extracts from the said patents are set out C.A.(COMM.IPD-PAT) 4/2021 Page 7 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 below:
1. WO 2006/080421 A1 (Chugai Pharmaceutical Co., Ltd) published on 3rd August, 2006:
"Specification Spiroquetal derivative and its use as a therapeutic agent for diabetes Technical field [0001] The present invention relates to pharmaceutically useful spiroketal derivatives. prodruggs thereof. and pharmacologically acceptable salts thereof. The present invention particularly relates to diabetes such as insulin- dependent diabetes mellitus [type 1 diabetes]. non-insulin dependent diabetes mellitus [type 2 diabetes mellitus]. diabetic complications. and obesity by inhibiting Na + -glucose cotransporter 2 [SGLT2]. Regarding spiroketal derivatives and prodrugs thereof and salts thereof. which are useful as prophylactic or therapeutic agents for diseases caused by hyperglycemia such as diabetes.
XXXX "Problems to be solved by the invention [0006] An object of the present invention is to provide a spiroketal derivative which is preferred as a pharmaceutical product and has properties. An object of the present invention is, in particular, to provide a spiroketal derivative having a hypoglycemic effect and further having favorable properties as a pharmaceutical product such as long-lasting drug efficacy, metabolic stability or C.A.(COMM.IPD-PAT) 4/2021 Page 8 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 safety. Furthermore, an object of the present invention is to prevent diseases caused by diabetes such as insulin-dependent diabetes mellitus [type 1 diabetes] and non-insulin- dependent diabetes mellitus [type 2 diabetes mellitus], diabetic complications, and hyperglycemia such as obesity. To provide a pharmaceutical composition used for treatment Means to solve problems [0007] As a result of diligent studies by the present invention in order to achieve the above object, the present invention was completed with the finding that the spiroketal derivative represented by the formula (1) has excellent SGLT2 inhibitory activity. It was.
That is, according to one aspect of the invention, the compound represented by formula (1):
[0009] [Chemicalization 1] XXXX [0101] The medicament of the present invention can be orally or locally administered systemically C.A.(COMM.IPD-PAT) 4/2021 Page 9 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 or locally or parenterally such as intrarectally, subcutaneously, intramuscularly, intravenously, or transdermally.
[0102] In order to use the compound of the present invention as a medicine, the optimum compound is selected as needed, regardless of the form of the solid composition, the liquid composition, and the other composition. The medicament of the present invention can be produced by blending a pharmaceutically acceptable carrier with the compound of the present invention. Specifically, a common formulation technology is added by adding a common excipient, a bulking agent, a binder, a disintegrant, a coating agent, a sugar coating agent, a pH adjuster, a solubilizer, or an aqueous or non-aqueous solvent. It can be prepared into tablets, pills, capsules, granules, powders, powders, liquids, emulsions, suspensions, injections, etc. Excipients and bulking agents include, for commonly used ingredients. I can give it."
2. WO 2012/115249 A1 (Chugai Pharmaceutical Co., Ltd) published on 30th August, 2012:
"Specification Invention title : Crystals of spiroketal derivatives Technical field [0001] The present invention relates to a novel crystal form of 1,1-anhydro-1-C-[5- (4- ethylphenyl) methyl-2- (hydroxylmethyl) phenyl1]
-B-D-glucopyranose, which is a spiroketal derivative, ..C.A.(COMM.IPD-PAT) 4/2021 Page 10 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01
Background technology [0002] Spiroquetal derivatives having a specific structure are known to be useful for the prevention or treatment of diabetes (Patent Documents 1 and 2). For example, in WO 2006/080421 (Patent Document 1), the formula (1):
[0003] The compound represented by [Chemical formula 1] : 1, 1-anhydro-1-C- [5- (4-ethylphenyl) methyl-2- (hydroxylmethyl) phenyl] -β-D-glucopyranose has been disclosed,. It is described that this compound has excellent SGLT2 inhibitory activity.
[0004] Further, WO 2009/154276 (Patent Document 2) discloses a monohydrate crystal, a sodium acetate co-crystal and a potassium acetate co-crystal of the compound represented by the formula (1), and the monohydrate crystal is disclosed. (Hereinafter referred to as type I crystal) is 3.5 , 6.9 , 10.4 , 13.8 , 16.0 , 17.2 , 0 0 0 0 0 0 18.2 , in the powder X-ray diffraction pattern. It 0 is described that it is characterized by having peaks at diffraction angles (2θ) near 4 , 20.8 , 0 0 21.4 , and 24.4 , . Further, in the document, 0 0 sodium acetate co-crystals are found in powder X-
ray diffraction patterns at 4.9 , 8.7 , 9.3 , 11.9 , 0 0 0 0 C.A.(COMM.IPD-PAT) 4/2021 Page 11 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 12.9 , 14.7 , 16. It has peaks at diffraction angles 0 0 (2θ) pattern, near 0 , 17.1 , 17.7 , 19.6 , 21.6 , 0 0 0 0 0 and 22.0 , and potassium acetate co-crysals are 0 powder X-rays. In the diffraction pattern, 5.0 , 0 10.0 , 10.4 , 12.4 , 14.5 , 15.1 , 19.0 , 20.1 , 0 0 0 0 0 0 0 21.4 , and it is described that it has a peak at a 0 diffraction angle (2θ) near 25.2 . 0 Outline of the invention Problems to be solved by the invention [0006] As described above, the compound represented by the formula (1) has an excellent effect as a pharmaceutical product. A specific monohydrate crystal (type I crystal) of the compound and a co-crystal with acetate are known, but no other crystal form has been reported.
[0007] An object of the present invention is 1, 1- anhydro-1-C- [5- (4-ethylphenyl) methyl-2- (hydroxylmethyl) phenyl] -β-D-glucopyranose used as an active ingredient of a pharmaceutical product. Is to provide a novel crystalline form of.
XXXX Effect of the Invention [0015] The crystal of the compound of the formula (1) provided by the present invention exists stably at room temperature and has properties suitable as a raw material for pharmaceutical products. Further, since it is easy to handle at the time of preparation, it is excellent as a raw material for safely and stably producing a drug containing the compound of the formula C.A.(COMM.IPD-PAT) 4/2021 Page 12 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 (1) as an active ingredient. The pharmaceutical composition containing the crystals is excellent is storage stability.
XXX "[0041] In addition, the pharmaceutical composition of the present invention contains, as an additional active ingredient, a therapeutic agent for diabetes having a different mechanism of action other than the SGLT2 inhibitor, a therapeutic agent for diabetic complications, a therapeutic agent for hyperlipidemia, a therapeutic agent for hypertension, and the like. It may be used, or it can be used in combination with those drugs.
[0042] The pharmaceutical composition of the present invention can be orally or locally administered systemically or locally or parenterally, such as intrarectally, subcutaneously, intramuscularly, intravenously, or transdermally, and contains a pharmaceutically acceptable carrier. Can be manufactured. Specifically, a commonly used excipient, bulking agent, binder, disintegrant, coating agent, sugar coating agent, pH adjuster, solubililzer, or aqueous or non-aqueous solvent is added, and the conventional formulation technique is used. It can be prepared into tablets, pills, capsules, granules, powders, powders, liquids, emulsions suspensions, injections, and the like. Examples of excipients and bulking agents include lactose, magnesium stearate, starch, talc, gelatin, agar, pectin, gum arabic, and other commonly used substances. The dose of the compound of the above formula (I) varies depending on the disease, symptom, body weight, C.A.(COMM.IPD-PAT) 4/2021 Page 13 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 age, sex, administration route, etc. but is preferably 0. It is 1 to 1000 mg / kg body weight / day, more preferably 0.1 to to 200 mg / kg body weight / day, and this can be administered once a day or in several divided doses."
3. WO 2009/154276 A1 (Chugai Pharmaceutical Co., Ltd) published on 13th December, 2009:
Specification Title of the invention: Crystals of spiroketal derivatives and methods for producing them.
Technical field [0001] The above-A Method for Producing A Spike Derivative. A Synthetic Intermediate Uselful for Production A Spike Derivative, and A Crystalline Substance of the Spike Derivative of the Spike Derivative Background Technology [0002] Spiroquetal Derivatives Having Specific Structure-Known to Be Uselful for the Preparation or Treatment of Diabetes (Patent et al. 1 to 4). For for Example, in WO 2006/080421 A1 (Patent Document 1, The Formula (A):
[0003] C.A.(COMM.IPD-PAT) 4/2021 Page 14 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 The compounds show in, and its use as therapeutic agent for diabetes.
XXXX [0100] According, to Yt Another Aspect of the Introduction, Formula (XI):
[0101] Crystals of the compounds of the compounds of are provided. In-one Aspect of the Introduction. The Crystal is A Monoclonal Rate. Here et al. The Monohydrate is Not Particle Limited As It is A Crystal That ably Retains Abouts I Equivalent of Water in An Environment (Temperature, Relative Humidity, etc.) In What What is the Drug is Normally Stock and Used. In one Aspect of the Abowave Aspect. The Crystal is provided As A Sodium Acetate Co-Crystal or a Potassium Acetate Co-Crystal. Moreover, According to Still C.A.(COMM.IPD-PAT) 4/2021 Page 15 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 Another Aspect of the Chloront Invention, Monohydrate Crystals of a Compound of High Purity Forms (XI).
[0102] The above Monohydrate Crystal of the Sensitomeric Crystal of the Colloidal X-Ray Diffusion Pattern in the Vicinal of 3.5 , 6.9 , 0 0 10.4 , and 13.8 , Special, 3.5 , 6.9 , 13 Near, 0 0 0 0 8.8 , 16.0 , 17.2 , and 18.2 . More Special 3.5 , 0 0 0 0 0 6.9 , 10.4 , 13.8 , 16.0 , 17.2 , 18.4 .0 0 0 0 0 0
20.8 , 21.4 , and 24.4 , characterization By 0 0 0 Having Penetration Angles (2θ). The Osodium Acetate Co-Crystal of the Colloidal X-Ray Diffusion Pattern in the Vicinal of 4.9 , 14.7 , 0 0 16.0 , 17.1 , and 19.6 . More Special 4.9 , 8.7 , 0 0 0 0 0 9.3 , 11.9 , 12.9 , 14.7 , 16.0 , 17.1 , 17.7 , 19.6 0 0 0 0 0 0 0 0 , 21.6 It is characterized by having a peak at a 0 diffusion angle (2θ) near and 22.0 . The 0 0 Sensitometric of 5.0 , 15.1 , 19.0 , 20.1 , and 0 0 0 0 25.2 . More 0 Special 5.0 Difficile Angles 0 Around 1, 10.0 , 10.4 , 12.4 , 14.5 , 15.1 , 19.0 0 0 0 0 0 0 , 20.1 , 21.4 , and 25.2 It characterization A 0 0 0 Peak At (2 theta). Here et al. The Powder X-Ray Diffusion Pattern can be measured by a Usual method. Further, the value of the diffusion angle of the powder X-ray diffraction on peak of the crystal of the sensitometric conditions and the state of the sample For For example. An Error of Abouts + 0.2 is exposed."
Thus, in all the above three patent documents, the compound and all forms of the compound Tofogliflozin are covered. Specifically, the various forms in which the said medicine can be administered are mentioned and covered.
17. The next question before this Court is whether in the light of the above prior art, the subject invention is entitled for grant of a patent in view C.A.(COMM.IPD-PAT) 4/2021 Page 16 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 of Section 3(d) of the Act.
18. Section 3(d) of the Act reads as under:
"3. What are not inventions.--The following are not inventions within the meaning of this Act,-- xxx xxx xxx
(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 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;
xxx xxx xxx"
19. As per the FER, the Document 1 cited therein covers Tofogliflozin and teaches that a solid composition such as Tofogliflozin tablet can be obtained using ordinary preparation techniques. It also indicates that the various examples and teachings in Document 1 clearly show that a tablet of Tofogliflozin can be obtained on the basis of the teachings in the said document. Document 2 seeks to disclose Type-II Tofogliflozin crystals, which can thereafter be made into an oral preparation, such as a tablet via ordinary preparation techniques. Document 3 discloses monohydrate crystals of Tofogliflozin. The relevant portion of the FER, raising the above objections, is set out below:
C.A.(COMM.IPD-PAT) 4/2021 Page 17 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01"Document 1 mentions tofogliflozin, and teaches that a solid composition such as a tablet can be obtained using ordinary preparation techniques. The document also indicates that an ordinary excipient, disintegrating agent, or the like may be added during this process, and lists lactose, magnesium stearate, and the like as examples of ordinary additives (claims, paragraph [0102], example 1).
Document 2 discloses type-II tofogliflozin crystals, and indicates that these crystals can be made into an oral preparation such as a tablet via ordinary preparation techniques. The document also indicates that an ordinary excipient, disintegrating agent, or the like may be added during this process, and lists lactose, magnesium stearate, and the like as examples of ordinary additives (claims, paragraph [0042]).
A comparison of the invention as in claim 1 of the present application and the inventions disclosed in documents 1 and 2 reveals that the two differ in that the former is a method for producing a tofogliflozin tablet in which tofogliflozin and an additive are mixed and a tablet is obtained via a direct mixing/compression process, whereas the production process is not specified in the latter.
Inasmuch as the tablets of documents 1 and 2 can be formed via ordinary preparation techniques, as discussed above, a person skilled in the art could easily conceive, in view of the matters disclosed therein, of forming these tablets using a direct mixing-compression method, which was a method in wide use. In addition, it is not found to require any particular creativity to add additives such as the lactose or magnesium stearate disclosed in documents 1 and 2, another ordinary C.A.(COMM.IPD-PAT) 4/2021 Page 18 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 disintegrating agent, and the like, and to select optimal amounts for the same, or to use known crystals such as the monohydrate crystals or sodium acetate cocrystals disclosed in document 3 (claims, paragraphs [0101], [0102]) as the tofogliflozin."
20. The FER also goes on to state that the disintegration and elution properties of directly mixed and compressed Tofogliflozin tablet with a superior elution and disintegration property would not entitle the Appellant for a patent as it would involve the same components apart from the use of disintegrating agents and lubricants used in the presence of calcium silicate. The patents clearly show that the subject patent is lacking in inventive step. The extract of the FER in this regard read as under:
"Next, to consider the effects of the invention according to the present application, the disintegration and elution properties of a directly mixed and compressed tofogliflozin tablet and a tofogliflozin tablet obtained via a wet granulation method are investigated in the examples, and the test results indicate that that direct mixing compression yields a tofogliflozin tablet of superior elution and disintegration properties (paragraph [0016]).
However, while the properties of drug preparations, such as disintegration and elution properties, are generally greatly affected by the amount of active ingredient and the types and amounts of additives, the only formulation actually confirmed to exhibit better disintegration properties than a tablet obtained by a wet granulation method is a formulation containing C.A.(COMM.IPD-PAT) 4/2021 Page 19 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 tofogliflozin, lactose, crystalline cellulose, low- substituted hydroxypropyl cellulose, and magnesium stearate (hereafter, "formulation 1"), the only formulation confirmed to exhibit integration properties similar to this formulation is a formulation containing tofogliflozin, lactose hydrate, crystalline cellulose, croscarmellose sodium, hydrogenated oil, and magnesium stearate (hereafter, "formulation 2"), and the only formulation given as an example of a formulation yielding elution properties similar to those of formulation 2 is a formulation containing tofogliflozin, lactose hydrate, crystalline cellulose, croscarmellose sodium, calcium silicate, magnesium stearate, talc, and hydrogenated oil. These three formulations contain the same components apart from the type of disintegrating agents and lubricants used in the presence of calcium silicate. A comparison of these formulations, which largely contain the same ingredients, shows that degradation in poststorage elution properties was observed in example 1, which is an instance of formulation 1 containing 40% tofogliflozin, and a preparation according to formulation 3, which contains calcium silicate, despite both of these being prepared via a direct mixing-compression method. In view of these facts, the disintegration and elution properties of a tofogliflozin tablet must be considered as being affected by the type of additive and the amount of tofogliflozin. Therefore, it cannot be found that all formulations containing any additive and an unspecified amount of tofogliflozin will yield improved disintegration and elution properties simply by virtue of being prepared via direct mixing-compression.
(iii) The invention as in claim 15 of the present application does not involve an inventive step in C.A.(COMM.IPD-PAT) 4/2021 Page 20 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 the light of documents D1-D3."
21. A perusal of the Claims of the subject patent would show that the Appellant seeks a process/method patent for producing a pharmaceutical preparation, which is a tablet comprising Tofogliflozin. The features of the said process/method patent are captured as under:
"1. A method for producing a pharmaceutical composition which is a tablet comprising tofogliflozin as an active ingredient, wherein the tofogliflozin is present in a form of monohydrate crystal, wherein the method comprises: mixing an additive and tofogliflozin to prepare a powder mixture, and obtaining a tablet from the powder mixture by direct compression, wherein the additive comprises at least one filler, and at least one lubricant, wherein the composition is substantially free from calcium silicate, wherein a weight ratio of the active ingredient tofogliflozin monohydrate ranges from 2.5 to 40 wt% with respect to the total weight of the composition, and wherein a weight ratio of the lubricant ranges from less than 4.0 wt% of the total weight of the composition.
2. The method as claimed in Claim 1, wherein the filler is selected from the group consisting of corn starch, potato starch, wheat starch, rice starch, partial alpha starch, alpha starch, lactose hydrate, fructose, glucose, mannitol, anhydrous dibasic calcium phosphate, crystalline cellulose, and precipitate calcium carbonate.
3. The method as claimed in Claim 1 or 2, wherein the additive further comprises at least one disintegrant.
4. The method as claimed in Claim 3, wherein the C.A.(COMM.IPD-PAT) 4/2021 Page 21 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 disintegrant is selected from the group consisting of sodium starch glycolate, carboxymethyl cellulose, carboxymethylcellulose calcium, carboxymethyl starch sodium, croscarmellose sodium, crospovidone, low substituted hydroxypropylcellulose, and hydroxypropyl starch.
5. The method as claimed in any one of Claims 1 to 4, wherein the lubricant is selected from the group consisting of magnesium stearate, calcium stearate, talc, sucrose fatty acid ester, sodium stearyl fumarate, and hydrogenated oil.
6. The method as claimed in any one of Claims 1 to 5, wherein the tofogliflozin monohydrate comprises a crystal form I, a crystal form II, or a mixture thereof.
7. The method as claimed in any one of Claims 3 to 6, wherein a weight ratio of the filler ranges from 20 to 80 wt% of the total weight of the composition and a weight ratio of the disintegrant ranges from 1.0 to 4.0 wt% of the total weight of the composition.
8. The method as claimed in any one of Claims 1 to 7, wherein the additive comprises lactose hydrate, crystalline cellulose, croscarmellose sodium, and hydrogenated oil and/or magnesium stearate.
9. A pharmaceutical composition which is a tablet produced by the method as claimed in any one of Claims 1 to 8."
22. A perusal of the Claims, as extracted above, shows that the various elements of the same active ingredient namely Tofogliflozin is present in a monohydrate crystal. The same are already known in the prior art documents being D1, D2 and D3. The mere process of preparing the tablet comprising C.A.(COMM.IPD-PAT) 4/2021 Page 22 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 Tofogliflozin by using a specific API ratio and lubricant ratio cannot result in a separate patent being granted for the method/process, inasmuch as the use of various ratios and proportions of the API, various excipients, lubricants and different forms of crystals are all generally known in the field. D1 being the genus patent, which covers Tofogliflozin, also covers various forms of Tofogliflozin, including the tablet form. The impugned order has clearly come to the conclusion that the prior art documents show various pharmaceutical compositions consisting of Tofogliflozin, including the tablet form.
23. This Court is of the opinion that a process/method patent, if granted in respect of Tofogliflozin tablets, would in effect be no different than the already granted patent in respect of Tofogliflozin. The various methods, processes etc. for the preparation of Tofogliflozin tablets cannot, unless proved to the contrary, result in a new patent for the same pharmaceutical preparation. This would be clearly hit by Section 3(d) of the Act, inasmuch as the tablet form of Tofogliflozin to be patented, through a method patent, cannot be a patentable invention. No significant enhancement of the known efficacy of Tofogliflozin has been explained in the subject patent with comparative data, inasmuch as the original patent being D1, also contemplates the preparation of the tablets of Tofogliflozin.
24. Moreover, the Appellant has sought to justify the method patent on the ground that comparative data has been set out in the examples, which have been given in patent specification. In the opinion of this Court, the monohydrate crystal form and the tablet form of Tofogliflozin was also known in the prior art documents. A perusal of comparative data that has been set out in the examples in the patent specifications shows that, the C.A.(COMM.IPD-PAT) 4/2021 Page 23 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 Appellant seeks to distinguish the subject patent from Tofogliflozin hydrate tablets produced by wet granulation method. The case sought to be made out on behalf of the Appellant is based upon two factors- time taken for disintegration and tablet hardness. It was contended that the disintegration was quicker than in the case of tablets produced by wet granulation method, though the tablet hardness was the same.
25. The comparative data, which has been placed on record, is in effect projected as enhanced therapeutic efficacy. However, in the opinion of this Court, the comparative data in this case does not qualify as significant enhancement of therapeutic efficacy, in terms of Novartis (supra). There is no data to show as to what would be the effect of early or shorter duration of disintegration, what would be the extent of the said shorter duration of disintegration as also what would be the effect of the same on the treatment of a patient.
26. In Novartis (supra), the Supreme Court clearly held as under:
"It may be seen that the word "efficacy" is used both in the text added to the substantive provision as also in the Explanation added to the provision.
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 C.A.(COMM.IPD-PAT) 4/2021 Page 24 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 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 is 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.
158. While dealing with the Explanation it must also be kept in mind that each of the different forms mentioned in the Explanation have some properties inherent to that form e.g. solubility to a salt and hygroscopicity to a polymorph. These forms, unless they differ significantly in property with regard to efficacy, are expressly excluded from the definition of " invention ". Hence, the mere C.A.(COMM.IPD-PAT) 4/2021 Page 25 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 change of form with properties inherent to that form would not qualify as "enhancement of efficacy" of a known substance. In other words, the Explanation is meant to indicate what is not to be considered as therapeutic efficacy.
XXX
164. In whatever way therapeutic efficacy may be interpreted, this much is absolutely clear:
that the physico-chemical properties of the 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.
165. 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% 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 commentator on the issue of bioavailability as under:
"It is not the intent of a bioavailability study to demonstrate effectiveness, but to determine the rate and extent of absorption. If a drug product is not C.A.(COMM.IPD-PAT) 4/2021 Page 26 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 bioavailable, it cannot be regarded as effective. However a determination that a drug product is bioavailable is not in itself a determination of effectiveness."
(emphasis supplied)
166. Thus, even if Mr Grover's submission is not taken into consideration on the question of bioavailability, the position that emerges is that just increased bioavailability alone may not necessarily lead to an enhancement of therapeutic efficacy. Whether or not an increase in bioavailability leads to an enhancement of therapeutic efficacy in any given case must be specifically claimed and established by research data. In this case, there is absolutely nothing on this score apart from the adroit submissions of the counsel. No material has been offered to indicate that the beta crystalline form of Imatinib Mesylate will produce an enhanced or superior efficacy (therapeutic) on molecular basis than what could be achieved with Imatinib free base in vivo animal model.
167. Thus, in whichever way Section 3(d) may be viewed, whether as setting up the standards of "patentability" or as an extension of the definition of " invention", it must be held that on the basis of the materials brought before this Court, the subject product, that is, the beta crystalline form of Imatinib Mesylate, fails the test of Section 3(d), too, of the Act.
168. We have held that the subject product, the beta crystalline form of Imatinib Mesylate, does not qualify the test of Section 3(d) of the Act but that is not to say that Section 3(d) bars C.A.(COMM.IPD-PAT) 4/2021 Page 27 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 patent protection for all incremental inventions of chemical and pharmaceutical substances. It will be a grave mistake to read this judgment to mean that Section 3(d) was amended with the intent to undo the fundamental change brought in the patent regime by deletion of Section 5 from the parent Act. That is not said in this judgment.
169. Section 2(1)(j) defines "invention" to mean, "a new product or ... ", but the new product in chemicals and especially pharmaceuticals may not necessarily mean something altogether new or completely unfamiliar or strange or not existing before. It may mean something "different from a recent previous" or "one regarded as better than what went before" or "in addition to another or others of the same kind". However, in case of chemicals and especially pharmaceuticals if the product for which patent protection is claimed is a new form of a known substance with known efficacy, then the subject product must pass, in addition to clauses (j) and (ja) of Section 2(1), the test of enhanced efficacy as provided in Section 3(d) read with its Explanation."
27. By applying the test contained in Novartis (supra) as also after perusing the data set out in the patent specifications, the claims originally sought as also the amended claims, this Court is of the opinion that the present patent application is nothing but an attempt to increase the term of the earlier patent for Tofogliflozin, which would not be permissible without a significant enhancement in therapeutic efficacy.
28. Accordingly, the Patent Application No.201617023236 dated 6th July, C.A.(COMM.IPD-PAT) 4/2021 Page 28 of 29 Signature Not Verified Digitally Signed By:DEVANSHU JOSHI Signing Date:14.04.2022 08:26:01 2016 filed by the Appellant in respect of the subject patent is liable is to be rejected. The impugned order dated 23rd February, 2021 does not warrant any interference.
29. The present appeal is dismissed. All pending applications are also disposed of.
PRATHIBA M. SINGH JUDGE APRIL 6, 2022/dk/ad (corrected and released on 13th April, 2022) C.A.(COMM.IPD-PAT) 4/2021 Page 29 of 29