Novel pyrazolone-derivatives and their use as pd4 inhibitors

Details Novel pyrazolone-derivatives and their use as pd4 inhibitors Novel pyrazolone-derivatives and their use as pd4 inhibitors

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/454 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2742922

The compounds of formula (1) wherein R1 represents a phenyl derivative of formulae (a), (b) or (c) R10 is 1-3C-alkyl and R11 is 1-3C-alkyl, or R10 and R11 together with the carbon atom, to which they are bonded, form a spiro-linked 3-, 4-, 5- or 6-membered hydrocarbon ring, A is C(O) or S(O)2, and R12 is phenyl, naphthalenyl, pyridinyl, quinolinyl, isoquinolinyl, quinoxalinyl, 1,6-naphthyridinyl, 1,8-naphthyridinyl, indolyl, phenyl substituted by R13, R14, R15 and R16, pyridinyl substituted by R17 and R18, naphthalenyl substituted by R19 and R20, quinolinyl substituted by R21 or indolyl substituted by R22, are novel effective inhibitors of the type 4 phosphodiesterase.

La présente invention porte sur les composés représentés par la formule (1) dans laquelle R1 est un dérivé phénylique représenté par les formules (a), (b) ou (c); R10 est alkyle C1-C3 et R11 est alkyle C1-C3, ou R10 et R11 conjointement avec l'atome de carbone auquel ils sont liés forment un noyau hydrocarboné de 3, 4, 5 ou 6 chaînons à liaison spiro, A est C(O) ou S(O)2 et R12 est phényle, naphtalényle, pyridinyle, quinolinyle, isoquinolinyle, quinoxalinyle, 1,6-naphtyridinyle, 1,8-naphtyridinyle, indolyle, phényle substitué par R13, R14, R15 et R16, pyridinyle substitué par R17 et R18, naphtalényle substitué par R19 et R20, quinolinyle substitué par R21 ou indolyle substitué par R22. Ces produits sont de nouveaux inhibiteurs efficaces de la phosphodiestérase de type 4.

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