Pyrazoloquinolinone derivatives as protein kinase c inhibitors

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/437 (2006.01)

Patent

CA 2392674

This invention provides a compound of the formula (I): (See formula I) or the pharmaceutically acceptable salts thereof wherein the dashed lines represent optional double bonds; C1, C2, C3 and C4 are carbon atom; R1 is C1-4 alkyl ; R2 is H, amino, etc.; R3 is H, halo-CH2-, C2-8 alkyl or Q1-, wherein said C2-8 alkyl is optionally substituted with up to 3 substituents selected from halo, C1-3 alkyl, R4(R5)N, etc.; R4 is H, C1-7 alkyl, etc.; R5 is H, C1-7alkyl, etc.; R6 and R7 are independently selected from H and C1-4 alkyl; R8 is aryl or heteroaryl; Q1 is a 4-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 4 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4 alkyl, etc.; Y5, Y6, Y7 and Y8 are hydrogen ; Y1, Y2, Y3 and Y4 are independently selected from hydrogen, halo, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 3 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4alkyl-, etc.; These compounds have protein kinase C inhibitory activity and thus are useful for the treatment of neuropathic pain, acute or chronic inflammatory pain, auditory deficiency (synaptic repair), or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

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