Indian Patent Office Refuses Janssen’s Secondary Patent Application For The Fumarate Salt Form Of Bedaquiline
FACTS
The applicant Janssen, a part of pharmaceutical company Johnson & Johnson (J&J) had filed an application for patent titled as "FUMARATE SALT OF (ALPHAS, BETA R) -6 - BROMO -ALPHA -[2- (DIMETHYLAMINO) -ETHYL] -2- METHOXY- ALPHA- 1- NAPHTHALENYL- BETA- PHENYL- 3-QUINOLINEETHANOL". This was a patent application for a salt of Bedaquiline which is a drug for treatment drug resistant Tuberculosis bearing Application No. 1220/MUMNP/2009.
Subsequently, the First Examination Report (FER) was issued on March 2012 pertaining to 22 claims by the Applicant and FER stated that the cited claims lacked inventive steps and was not an invention within the meaning under Section 2(1)(j). Janssen in response to the FER modified its claims in January 2013. For the following claims, two pre-grant opposition were filed by "Network of Maharashtra people living with HIV" and "Nandita Venkatesan and Phumeza Tisile" under Rule 55(4) of the Patents Rules.
ISSUES
Does the claimed invention satisfy the criteria laid down under the Indian Patents Act, so as to be granted patent?
ANALYSIS
Both opponent 1 and opponent 2 has filed representations under Section 25(1)(b), (c), (e), (f) and (b) and 25 (l)(b), (e), (f), (g) and (h) respectively. The Assistant Controller analyzed the patent application on the following grounds of opposition, namely:
• NOVELTY under Section 25(1)(b) and 25(d)
The opponents had claimed that the claimed invention is not patentable as the complete specification has been published before the priority claim (Section 25(1)(b)) and the complete specification was publicly known or used in India prior to the claim (Section 25(l)(d)). The Assistant Controller analyzed WO 2004/011436 which was relied on by both the oppositions to establish their ground of opposition. The cited document was about a possibility of various salts, in general, it refers for instance to both acid addition salts of a free base and base addition forms of an acid and a fumaric acid is available generally in organic acids.
The Assistant Controller on analysis of the document came to a conclusion that the WO 2004/011436 though makes general analysis towards formation of the claimed invention but the document does not disclose each and every particular feature of the claimed composition (i.e. the specific fumarate salt of (alpha S, beta R)- 6-bromo-a-[2- (dimcthylamino)ethyl]-2 methoxy-a-1-napthalenyl- -phenyl-3- quinolineethanol); with polyethylene glycol sorbitan fatty acid ester (TWEEN 20) as a wetting agent and pharmaceutically acceptable carriers in specific amounts as disclosed in claim 1. Hence the Assistant Controller came to a conclusion that the invention was novel, and the grounds raised by the opposition are non-sustainable.
• PRIOR CLAIMING under Section 25(1)(c)
To establish the same, the opponents relied on the Patent Application No. 220/DELNP/2005 (PCT/EP03/050322) filed on 20.1.2005 which was granted a patent on 23.11.2009 with Patent No. IN236811. But, the Assistant Controller on perusal of the application came to the conclusion that the application is not related to the prior claiming of the composition particularly fumarate salt of (alpha S, beta R)- 6-bromo-a-f2- (dimethylamino)ethylJ-2-methoxy-a-1-napthalenyl- -phenyl-3- quinolineethanol); with polyethylene glycol sorbitan fatty acid ester (TWEEN 20 ) as a wetting agent and pharmaceutically acceptable carriers and, hence, the said ground of opposition was deemed to be untenable by the Assistant Controller.
• OPPOSITION under Section 25(1)(e), Section 25(1)(f), i.e., Section 3(d) and Section 3(e)
Both the opponents claimed that:
(i) that the invention as claimed in any of the claims of the complete
specification is obvious and clearly does not involve any inventive step having regard to the matter published as mentioned in clause (b) or having regard to what was used in India before the priority date of the applicant's claim (under Section 25 (l)(e));
(ii) that the subject of any claim of the complete specification is not an invention within the meaning of this Act, or not patentable under this Act (under Section 25(1)(f) i.e. Section 3(d) and 3(e) of the Act.
The opponents cited various documents to establish their grounds of opposition, specifically to establish that there was no inventive steps involved in the claimed invention. The Assistant Controller noted the various documents cited, particularly, WO 2004/011436 titled "Quinoline derivatives and their use as mycobacterial inhibitors", WO 2006067048 (D2) titled, "Quinoline derivatives for the treatment of latent tuberculosis", WO 2006024667 (D3) titled "Fumarate of 4-((4-((4-(2-cyanoethenyl)-2,6- dimethylphenyl) amino)- 2-pyrimidinyl) amino) benzonitrile", Exhibit B titled Preparation of Water-soluble compounds through salt formation.
The Assistant Controller noted that D1 discloses the base compound along with the suggestion that fumarate salt of Bedaquiline may be feasible in another embodiment, Exhibit B discloses about the salt form of the base compound in the pharmaceutical field in general and the advantage of the salt form over the base compound in terms of the bioavailability; D3
elaborates especially about the use of TWEEN 20 (a polyethylene glycol sorbitan fatty acid ester) as wetting agent in pharmaceutical compositions in the range of 0.01 to 5.0%. The Assistant Controller held that the applicant was not able to produce any data in the complete specification to show that combination of fumarate salt of Bedaquiline along with Tween 20 would show surprising effect over the known the composition of Bedaquiline on the treatment of a patient, and the applicant merely combined the teachings and suggestion given in the various cited documents. Therefore, the Assistant Controller held that there was not inventive step involved in the claimed invention, and hence it is non-patentable under Section 3(d) of the Patents Act.
The Assistant Controller also noted that the complete specification has failed to disclose an improved therapeutic efficacy over the prior arts. The applicant has also in the affidavit disclosed increase in bio-availability by changes made in use of 0.01 to 5% of wetting agent, which could not lead to an improved efficacy, this can be practiced by changing in the dosages to make increase in bio-availability. The subject matter is mere admixture resulting only in the aggregation of the properties of the components. Therefore, it is non-patentable under Section 3(e) of the Patents Act.
• INSUFFICIENCY under Section 25(l)(g)
The Assistant Controller based on the complete specification came to the conclusion that the disclosure meets the statutory requirements as mandated under Section 10(4) of the Patents Act and that the person skilled in the art would be sufficiently enabled to work on the claimed invention without undue experimentation by simply relying on the disclosure made in the complete specification. Therefore, the Assistant Controller held that the opposition on this ground is not patentable.
• FAILED TO DISCLOSE INFORMATION UNDER SECTION 8; under Section 25(1)(h)
The Assistant controller noted that the applicant's agent submitted updated Form-3 to the Patent Office with current status of corresponding applications along with petition under rule 137 for condoning the irregularity of the procedure envisaged by Section 8 which was, subsequently, taken on record. As such, the Assistant Controller came to the conclusion that the said ground of opposition was untenable.
DECISION
The Assistant Controller after taking into consideration the opposition raised and analyzing the same came to the conclusion that the claimed invention does not meet the requirements of Section 2(l)(ja) and Sections 3(d) & 3(e) of the Patents Act and such held the claimed invention to be non-patentable.
CONCLUSION
The rejection of Janssen's patent application by the Indian patent office denotes the two aspect of patent grant in India. The first aspect is the importance of the provision of pre grant opposition with respect to opposition. The provision was for a long time considered of losing importance owing to the fact that most of the opposition raised are frivolous in recent times, but, the opposition raise in the present case were of extreme relevance. The second aspect is the importance of inclusion of inventive step in making of an invention such that the addition is not mere addition to already existing thing. These two aspects prevent separate patents for regular changes in the same drug so as to prevent ever greening of patents. The rejection of patent to Janssen has also granted to an opportunity to generic medicine manufacturer, who can now produce generic medicine of the drug which was till date costly, thereby, aiding in providing essential medicine at an affordable price in a country which made a target of being Tuberculosis free by 2025.
Disclaimer: This article was first published in the S&A Law Offices - 'Intellectual Property (IP-Tech)' newsletter in July 2024.