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NEW CHEMICAL ENTITIES – ASPECTS OF DRAFTING AND PROSECUTION
IN INDIA
Khurana & Khurana, Advocates & IP Attorneys Noida(New Delhi) | Mumbai | Pune | Bangalore
An ISO 9001:2015 Certified FirmE-13, UPSIDC, Site-IV, Kasna Road, Greater Noida, National Capital Region Delhi - 201308, India
CHALLENGES WITH MARKUSH CLAIMS• The Markush claims are drafted to obtain a wide scope of
protection encompassing a large number of compounds whose properties might not have been tested, but only theoretically inferred from the equivalence with other compounds within the claim
• Quite often the Markush claims generate confusions regarding the novelty, non-obviousness and industrial applicability of a group of compounds covered within the said Markush formula
• Also, the Markush claims may invoke the questions of sufficiency and plurality of distinct group of inventions surrounding such claims
• Claim 1 and therefore its dependent claims lack novelty/inventive step in view of documents:
D1: US4996335 D2: BE889563 D3: Pharmaceutical Research (1999), 16(6), 961-967
(abstract). Documents D1-D3 disclose compounds which are included in the general formulas as defined by the claims of the application. Therefore, these claims cannot be regarded as novel or inventive.
With these arguments and assertions accepted, the patent wasgranted on the grounds that the structural formula of thecompounds could not be anticipated by the markush formulaof the compounds disclosed in cited prior art documents andhence the subject matter covered by the instant application isnovel and involves inventive step.
Conclusion1. From the analysis of prosecution history of IN, EP and US patents, following
references were found to be cited by the Examiner –
• It could be concluded that references cited by the examiner during prosecution of Indian Patent application matches closely to those cited during prosecution of EP application in comparison to US patent application.
Conclusion2. From the analysis of allowed independent claims, it can be concluded
that the scope of the first independent claim of EP patent (EP2004667) is significantly broad when compared to their Indian (IN272676) and US (US8785425) counterparts. Following major differences could be observed-
In EP2004667 and IN272676, R1 could be hydrogen or methyl or methylene. However, in US8785425, R1 was restricted to be selected only from hydrogen or methyl.
In EP2004667, R5 could be any group selected from (C1-C10)-alkyl, (C3-C13)-cycloalkyl, -O- (C1-C10)-alkyl, aryl or heterocyclic ring and others. However, in US8785425 and IN272676, R5 was restricted to be selected from (C1-C4)-alkyl, (C3-C6)-cycloalkyl, -O- (C1-C4)-alkyl, and a phenyl ring or heterocyclic ring and others.
• In the amended claims, the variable R in formula I was restricted to represent substituted or unsubstituted alkyl, substituted or unsubstituted aryl or substituted or
unsubstituted heteroaryl.
• But D1-D4 disclosed such compounds with a hydrogen or Amido group at the corresponding position.
• Applicant further stated that although D5 disclosed pyrazole and the use thereof as cannabinoid receptor modulators, but none of those compounds disclosed a bridged ring system condensed with the pyrazoles.
With these arguments and assertions accepted, the patent wasgranted on the grounds that the structural formula of thecompounds could not be anticipated by the formulaof the compounds disclosed in cited prior art documents andhence the subject matter covered by the instant application isnovel and involves inventive step.
IN255055 US7923465 EP1902034NAGAI et al., Chem. Pharm. Bull.
(1979), 27(8), 1764-1770- NAGAI et al., Chem. Pharm. Bull.
(1979), 27(8), 1764-1770
EGG et al., Monatshefte Fur Chemie (1969), 100, 1256-1259
Egg et al., 1969, CAS: 71: 101768 EGG et al., Monatshefte Fur Chemie (1969), 100, 1256-1259
Database Crossfire Beilstein, Frankfurt Am Main, DE; 1982,
XP002402588
- Database Crossfire Beilstein, Frankfurt Am Main, DE; 1982,
XP002402588
WALLACH et al., Justus Liebigs Ann. Chem. (1903), 329, 109-133
- WALLACH et al., Justus Liebigs Ann. Chem. (1903), 329, 109-133
- Watson et al., 1995, CAS: 124:104533
WO0158869
- Nagai et al., 1980, CAS: 92:181074 WO0132629
- - WO0132663
- - WO2006/030124
Conclusion
Conclusion2. From the analysis of allowed independent claims, it can be concluded that the
scope of the first independent claim of EP patent (EP1902034) is significantly broad when compared to its Indian (IN255055) and US (US7923465) counterparts. Following major differences could be observed-
In EP1902034, U and V are independently C or N and W, X and Y are independently C, N, O, S or –C(O)-. However, in IN255055, U and V are restricted to C and W, X and Y are restricted to C and N. Further, in US7923465, the inner ring atoms are clearly specified as C and N.
In IN255055 and EP1902034 R1 and R2 may be joined together to form an optionally substituted 3 to 7 membered saturated or unsaturated cyclic ring. However, in US7923465 R1 and R2 may be joined together to form an optionally substituted piperidinyl ring.
In EP1902034, each occurrence of B is independently O, S or NR3. However, B is restricted only to O in US7923465 and IN255055.
Further, it could be concluded that references cited by the examiner during prosecution of Indian Patent application matches closely to those cited during prosecution of EP application in comparison to US patent application.
Objections Raised by ExaminerThe application lacks novelty because the subject matter of claims 1-3,5,6,8-11,13-16,18-25,27-29 is not new in view of the cited documents:
D1: WO2005/075463D2: WO00/3681 A2D3: FR-A-2661676D4: Database Chemcats Chemical Abstracts service, Colombus, Ohio, US; (2005-07-03),XP002414754D5: WO 03/080578 A (MERCK SHARP AND DOHME [GB]; BROWN REBECCA ELIZABETH[GB]; DOUGHTY VICTOR) (2003-10-02) cited in the application
• Necessary amendments were made by the applicant. The applicant renumbered claim 39 as claim 1 and amended it to specify that R1 and R2 together form a cyclobutane or fully saturated pyran as well as substituents R7 and R8 are replaced by isoquinoline moiety.
• In support of the assertion made, the applicant further stated that D1 although discloses the benzopyran derivatives containing thioureido side chain, it fails to suggest or motivate PHOSITA to prepare benzopyran derivatives containing urea substituted with isoquinoline moiety.
• He further stated that D2 discloses benzopyran derivatives with an amide substitution at 6th position whereas the instant application did not cover derivatives with such substitution.
• He asserted that D3 and D4 did not suggest or motivate PHOSITA to prepare benzopyran derivatives of urea having bicyclic ring such as isoquinoline moiety as another substituent.
• He concluded his remarks for novelty and inventive step with D5 not citing any example of benzopyran derivatives even though substituted urea derivatives are disclosed.
With these arguments and assertions accepted, the patent wasgranted on the grounds that the structural formula of thecompounds could not be anticipated by the formulaof the compounds disclosed in cited prior art documents andhence the subject matter covered by the instant application isnovel and involves inventive step.
Database Chemcats Chemical Abstracts service, Colombus, Ohio,
US; (2005-07-03),XP002414754
- Database Chemcats Chemical Abstracts Service, Columbus, Ohio,
US; (2005-07-03), XP002414754
WO 03/080578 A (MERCK SHARP AND DOHME [GB]; BROWN REBECCA ELIZABETH[GB]; DOUGHTY VICTOR) (2003-10-02) cited in the application
Wolff et al., Burger's Medicinal Chemistry and Drug Discovery (1994), Wiley-Interscience, Fifth Edition, vol. I: Principles and Practice, pp. 975-977
WO030/80578
- D2: Vippagunta et al., Advanced Drug Delivery Reviews (2001), 48, pp. 3
and 18
Database Chemcats Chemical Abstracts Service, Columbus, Ohio,
US; (2006-01-24), XP002414755
Conclusion2. From the analysis of allowed independent claims, it can be concluded
that the scope of the first independent claim of EP patent (EP1931681) is significantly broad when compared to its Indian (IN249412) and US (US7842703) counterparts. Following major differences could be observed-
While different Substituted Benzofused Derivatives falling under the ambit of following Markush structure (Formula I) were allowed in EP (EP1931681) and IN (IN249412) patents, only a specific Substituted Benzofused Derivative- 1-(3,4-dihydro-spiro-[2H-1-benzopyran-2,1’-cyclobutane]-4-yl)-3-(isoquinolin-5-yl)urea and its pharmaceutically acceptable salts were allowed in their US counterpart (US7842703).
Further, it could be concluded that references cited by the examiner during prosecution of Indian Patent application matches closely to those cited during prosecution of EP application in comparison to US patent application.
Section 8Information and Undertaking Regarding Foreign Applications –
8(1) Where an applicant for a patent under this Act is prosecuting either alone or jointly with any other person an application for a patent in any country outside India in respect of the same or substantially the same invention, or where to his knowledge such an application is being prosecuted by some person through whom he claims or by some person deriving title from him, he shall file along with his application or subsequently within the prescribed period as the Controller may allow— (a) a statement setting out detailed particulars of such application; and
(b) an undertaking that, up to the date of grant of patent in India, he would keep the Controller informed in writing, from time to time, of detailed particulars as required under clause (a) in respect of every other application relating to the same or substantially the same invention, if any, filed in any country outside India subsequently to the filing of the statement referred to in the aforesaid clause, within the prescribed time.
8(2) At any time after an application for patent is filed in India and till the grant of a patent or refusal to grant of a patent made thereon, the Controller may also require the applicant to furnish details, as may be prescribed, relating to the processing of the application in a country outside India, and in that event the applicant shall furnish to the Controller information available to him within such period as may be prescribed.
Case Study - 4• IN212695 Assigned to Allergan Inc.
Application Date 20-10-2003; Grant Date 14-12-2007)
• Claim 1: A composition comprising a blend of a timolol component present in an amount effective to reduce ocular hypertension when applied to a hypertensive eye, and a hypotensive lipid component, different from the timolol component, present in an amount effective to reduce ocular hypertension when applied to a hypertensive eye,. said composition when applied to an eye being effective to treat ocular hypertension, the hypotensive lipid component being selected from the group consisting of cyclopentane E-ethyl heptenamide-5-cis-2- (3α-hydroxy-S-phenyl-l-trans-pentenyl)- 3,5-dihydroxy,[1α.2β,3α,5α], pharmaceutically acceptable salts thereof and mixtures thereof.
Ajanta Pharma Vs. Allergan IncAjanta filed revocation petitions on the bases of obviousness and Breach of section (8) of IPA:– The counsel submitted that Form 3 Dt. 20.01.2004 furnished by the
respondent in IPO indicated that Korea, New Zealand, Canada, China and Japan were pending applications. However, the application numbers of the same were not disclosed.
– No information on the prosecution of EPO and US counterpart applications was furnished. According to the counsel, corresponding US application No. 10/153,043 which was being prosecuted by the respondent and response to the office actions in US were filed before the response to FER in India.
– EPO issued its own Examination report February 11, 2005 in respect of the corresponding application (Page 388 - 385; Exhibit EA3 to the MP).
The IPAB found that invention is obvious and section 8 violation has been proved. Based on the observations revocation application was allowed and the grant of Patent No.212695 was set aside.