Patent granted in India to PFIZER INC

As per patent office journal dated 30/07/2021 patent number 372466 has been granted to PFIZER INC. that is titled SUBSTITUTED DIHYDROISOQUINOLINONE COMPOUNDS.

The primary independent claim of this patent states a compound of formula, or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of F, C1-C4 alkyl, C1-C4 alkoxy, C(O)R5 , C3-C8 cycloalkyl, 3-12 membered heterocyclyl and 5-12 membered heteroaryl, where each said C1-C4 alkyl or C1-C4 alkoxy is optionally substituted by one or more R6 , and each said C3-C8 cycloalkyl, 3-12 membered heterocyclyl or 5-12 membered heteroaryl is optionally substituted by one or more R7 ; R2 is H, F or C1-C4 alkyl; L is a bond or a C1-C4 alkylene; R3 is selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, OH, CN, C(O)R8 , COOR9 , NR10R11, OR12 , C3-C8 cycloalkyl, 3-12 membered heterocyclyl and 5-12 membered heteroaryl, where each said C1-C4 alkyl or C1-C4 alkoxy is optionally substituted by one or more R6 , and each said C3-C8 cycloalkyl, 3-12 membered heterocyclyl or 5-12 membered heteroaryl is optionally substituted by one or more R7 ; R4 is H, halo or C1-C4 alkyl, where each said C1-C4 alkyl is optionally substituted by one or more R6 ; R5 is C1-C4 alkyl, where each said C1-C4 alkyl is optionally substituted by one or more R14; each R6 is independently OH, F, CN or C1-C4 alkoxy; each R7 is independently C1-C4 alkyl, OH, F, CN, C1-C4 alkoxy, =O, CHO, C(O)R13, SO2R13 or 3-6 membered heterocyclyl; R8 is C1-C4 alkyl, where each said C1-C4 alkyl is optionally substituted by one or more R14; R9 is H or C1-C4 alkyl, where each said C1-C4 alkyl is optionally substituted by one or more R14; R10 and R11 are independently H or C1-C4 alkyl, where each said C1-C4 alkyl is optionally substituted by one or more R14; R12 is selected from the group consisting of C3-C8 cycloalkyl, 3-12 membered heterocyclyl and 5- 12 membered heteroaryl, where each said C3-C8 cycloalkyl, 3-12 membered heterocyclyl or 5-12 membered heteroaryl is optionally substituted by one or more R7 ; each R13 is independently C1-C4 alkyl, where each said C1-C4 alkyl is optionally substituted by one or more R15; each R14 and R15 is independently OH, F, CN or C1-C4 alkoxy; and X and Z are independently C1-C4 alkyl, C1-C4 fluoroalkyl, C1-C4 alkoxy or C1-C4 fluoroalkoxy.

During the patent prosecution, the patent examiner objected to this patent under section 3(d) of the Indian Patents Act. The patent applicant responded to this objection by stating that Section 3(d) does not apply to all pharmaceutical and chemical inventions. The provision clarifies its application that for a “new form of known substances” there has to be a “known substance”. In the absence of a “known substance” there cannot be a “new form”. The section further clarifies that even “new forms of known substances” are patentable – if significant therapeutic efficacy is shown. Further, applicant stated that  Section 3(d) of the Indian Patents Act 1970 stipulates that: a) there has to be a known substance; b) the application has to be for a new form of that substance; c) that new form in order to be patentable has to demonstrate therapeutic efficacy d) therapeutic efficacy has to be established by means of filing comparative data. In the view of this, the present invention does not fall under the purview of Section 3(d).

 

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