The Patent (Amended) Act And The Patent Rules , 2003 as amended b y The Patent (amended ) Rules

In the matter of t h e p r o v i s i o n s under The Section 25(1) of The Patents (Amendment) Act 2 0 0 5 a n d T h e Patents Rules (Amendment) 2006 And In the matter of Patent application no.3176/KOLNP/2007dtd.29/08/2007 filed by M/ s Mitsubishi Pharma Corporation And

In the matter of Pre grant by way of representation u/s 25(1) of the Act by M/s Lupin Ltd Hearing Held on 23/09/2015 at 11.30a.m before Dr. S. Chattopadhyay, Astt. Controller, Patents & Designs Present: 1.

Dr. S.Ganguly and others ,agent for opposition

2.

Dr.S. Banerjee & Dr.I Banerjee , Agent for applicant

DECISION

A representation u/s.25(1) of the Patent Act, 1970, against the Patent application3176/KOLNP/2007 dtd. 29/08/2007 has been filed by M/s S.Majumdar & Co.,Kolkata on behalf of M/s Lupin Ltd , Mumbai on 03/02/2012 on the following grounds:a)

The invention so far as claimed in any claim of the complete specification has been published before the priority date of the claimi) in any specification filed in pursuance of an application for a patent made in India on or after the 1st day of January ,1912; or ii) in India or elsewhere, in any other document: Provided that the ground specified in sub-clause (ii) shall not be available where such publication does not constitute an anticipation of the invention by virtue of sub-section (2) or sub-section (3) of section 29;

b) The invention so far as claimed in any claim of the complete specification was publicly known or publicly used in India before the priority date of that claim, c) The invention so far as claimed in any claim of the complete specification is obvious and clearly does not involve any inventive step, having regard to the matter published before the priority date of the claim (i) in any specification filed in pursuance of an application for a patent made in India on or after the 1st day of January, 1912; or in India or elsewhere, in any other document; or having regard to what was used in India before the priority date of the applicant’s claim, d) That the subject of any claim of the complete specification is not an invention within the meaning of this Act, or is not patentable under this Act; e) That the complete specification does not sufficiently and clearly describe the invention or the method by which it is to be performed. f) The applicant has failed to disclose to the Controller the information required by Sec.8 or has furnished the information, which in any material particular was false to his knowledge. After completion of the procedure prescribed u/s 25(1) to read with Rule 55 under prevailing Rules a hearing has been scheduled on 23/09/2015 at 11.30a.m to dispose the above mentioned pre grant representation u/s 25(1) against the subject application3176/KOLNP/2009 dtd. 29/08/2007.

The hearing has taken place as scheduled and oral submission followed by written response of the opponent along with applicant have been taken on record and annexed as A and B respectively along with subject decision.

It has been clarified during the hearing by undersigned on query of opponent of the proceedings that the arguments and counter arguments shall be done on the basis of initially filed claims . The present application deals with salt of compound referred as compound 1 in the specification which is 3-{(2S, 4S)-4-[4-(3-methyl1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine and is generally referred as Teneligliptin and useful as a DPP-IV inhibitor and in order to solve the problems with compounds 1 i.e 3 hydrochoride salt of prior art compound with regard to superior properties in terms of stability, solubility, hygroscopicity¸ bioavailability the crystal structure of compound 1 with mono, di, tri-basic acids in the subject application have been prepared. First of all in their submission the opponent pointed out several issues as furnished in the complete specification and with this introduction the opponent argued on the basis of following grounds of opposition 1.Anticipation 2.Obviousness / lack of inventive step 3Not an invention/ Not patentable 4.Insufficiency 5.Prior Public knowledge Upon consideration of the grounds of opposition raised by opponent vis a vis the arguments placed by the agent of the applicant under the provision of section 25(1) of the Act and prevailing Rules followed by written note of arguments I shall turn my eyes to the grounds of opposition submitted by opponent for pregnant opposition and subsequent submission thereby from the applicant and discuss some of the pertinent grounds in my consideration. At first I would like to discuss the ground raised by opponent regarding obviousness /lack of inventive step as alleged by opponent and it is found after scrutiny that D1 which is the US counterpart of the acknowledged prior art WO02002014271 has taught the compounds of teneligliptin and their salts including HCl, HBr salts and in the example 222 there is a definite mention of 3HCl salt and teaching regarding polymorphic crystals and solvates/ hydrates have been described in the said example of prior art. Further , I found that the method of formation of e 2.5 HBr salt of teneligliptin involves the regular method preparing the salt which is also pointed out by the opponent during the hearing. There is no mention in the specification the therapeutic efficacy of the claimed 2.5 HBr salt of teleligliptin through data indicating the solubility and hygroscopicity of the said compound are furnished. With these teaching of prior art and above discussion I am in the opinion that the allegation recited above by the opponent has not been addressed by the applicant in appropriate manner and even for sake of argument if the annexure B is considered (though it has been conveyed at the beginning of the hearing that the submission should be strictly on initial filing ) still it is found again to be devoid of any comparative experimental data on therapeutic efficacy of the claimed salt over the prior art compounds. In order to overcome the undesirable properties of the prior art salts with regard to stability, hygroscopicity the present application emerges but the same does not provide any comparative data to show any technical advancement of such salt and solvates. Further I would like to discuss that D2 has also definite mention of teneligliptin 3HCl and 2HCl salt of teneligliptin and polymorph is also mentioned therein and D3 being a general document states that hygroscopicity increases with polarity of salt , so it can be concluded that HCl salts being more polar is more hygroscopic and increasing stability reduces hygroscopicity. Hence , it is obvious conclusion that HBr salt is less hygroscopic and more stable with regard to HCl salt. Further , it is well known in the art that a particular crystalline form of a compound possesses a particular physical property like stability which does not address the inventive step issue and hence , I opine that there is no contribution of the applicant to impose the said property to the claimed substance rather than it is inherent physical property for the same and applicant has gone through experimentation to assess the same only . Hence a person ordinarily skilled in the art can prepare the various salts that are disclosed in prior art to overcome the stability problem and he may arrive to the claimed compound in a routine manner. Therefore, with the teaching of two cited prior art and subsequent discussion and submission by the opponent and applicant thereby motivates undersigned to conclude that inventive step issue as alleged by the opponent is not at all addressed in appropriate manner by the applicant for the impugned application.. In the light of above discussion it can be summarized that inventive step of the subject application is not at all substantiated with enhanced therapeutic efficacy of the claimed compounds and described the physical parameter of the compounds which are inherent property of the same and it eventually unable to address the therapeutic solution of the addressed problem as stated in the specification and method of preparation of the claimed 2.5HBr is nothing but a routine method , so I am finally in opinion that skilled person may achieve with these teaching of prior art to the subject application in a routine manner. Hence, I conclude regarding inventive step issue over prior art the applicant was unable to succeed to prove upon its points to establish the same and eventually failed to prove upon the allegations as raised by opponent for obviousness/inventive step ground.

Next I would like to discuss the grounds not an invention in the light of section 3(d) of the Act which stipulates an incremental invention based on already existing substance having established medicinal activity which shall be deemed to be treated as a same substance .The application in question does not take pain to show the efficacy particularly therapeutic efficacy of the alleged compound . There is no acceptable experimental data which has been provided with regard to already known prior art compound except for solubility and hygroscopicity of the claimed compound. Further, I found that the applicant has prepared 2.5 HCl, 2.5HBr salts of teniligliptin and their solvate /hydrates which have defined XRD peak value indicating crystal forms. But there is no support in the specification that regarding efficacy except data for solubility and hygroscopicity of claimed teniligliptin salt and it did not focuses on stability issue also appropriately. Though it has been stated during hearing and subsequent written note of arguments that salt of the present invention has low toxicity and hence the salt is safe and can be used as oral administration but the same claim lacks in support with experimental data. It is pertinent to mention that stability per se can not be considered as patentable subject matter until and unless it has substantial efficacy more precisely therapeutic efficacy and that also needs to be substantiated by the comparative clinical data. I am in the opinion that solubility and hygroscopicity per se which are physical properties of the claimed compound should not be the criteria for establishing the present section and capable to overcome section 3(d) for the impugned application over the prior art and I consider the subject claim of the impugned application eventually leads to a mere discovery, not an invention. Even if the annexure B is considered for the sake of argument it is found further that the document is also devoid of any data regarding therapeutic efficacy and provides data for physical parameter like stability and formation of crystals which in my consideration does not enable the application to overcome the grounds of opposition as raised by opponent against section 3(d) of the Act which is alleged as not an invention by opponent.

In the present context I am skipping the discussion related to rest allegation raised by opponent as the said discussion does not have meaningful and significant contribution to the same over the above mentioned paragraphs. So in view of the facts and circumstances of the application as above against the pre grant opposition u/s 25(1) of the Act I hereby accept the representation filed by opponent under section 25(1) to read with rule 55(1) and refuse the patent application no. 3176/KOLNP/2007dtd. 29/08/2007 u/s 25(1) to read with Rule 55(6) under prevailing Rules under the provision of Patent Act, 1970 (as amended).

Dtd. 08/12/2015 Enclosed : Annexure A and B

(Dr. S. Chattopadhyay)) ASST. CONTROLLER OF PATENTS AND DESIGNS