Thiazole derivatives as phosphodiesterase iv inhibitors

Details Thiazole derivatives as phosphodiesterase iv inhibitors Thiazole derivatives as phosphodiesterase iv inhibitors

C - Chemistry, Metallurgy

07

D

C07D 417/14 (2006.01) A61K 31/50 (2006.01) A61P 11/06 (2006.01) A61P 19/02 (2006.01) A61P 19/10 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2489902

Thiazole derivatives of the formula I (see formula I) in which R1 and R2 are each, independently of one another, H, OH, OR8, -SR8, -SOR8, -SO2R8 or Hal; R1 and R2 together are alternatively -OCH2O- or -OCH2CH2O-; R3 and R3' are each, independently of one another, H, A"R7, COA"R7, COOA'R7, CONH2, CONHA"R7, CON(A"R7)(A"'R7), CONR10Het, NH2, NHA"R7, N(A"R7)(A"'R7), NCOA"R7 or NCOOA"R7; V and W are oxygen or hydrogen substituents; B is an optionally substituted aromatic isocyclic or heterocyclic radical; X is N or CR3' ; R7 is H, COOH, COOA, CON H2, CONHA, CONAA', NH2, NHA, NAA', NCOA, NCOOA, OH or OA; R8 is A, cycloalkyl, alkylenecycloalkyl or alkenyl; Y is alkylene or alkenylene; in which one, two or three CH2 groups may be replaced and/or 1-7 H atoms may be replaced; A and A' are each, independently of one another, alkyl or alkenyl, in which one, two or three CH2 groups may be replaced and/or 1-7 H atoms may be replaced, or aryl or Het; A and A' together are alternatively an alkylene chain, in which one, two or three CH2 groups may be replaced; A" and A"' are each, independently of one another, absent, alkylene, alkenylene or cycloalkylene, in which one, two or three CH2 groups may be replaced and/or 1-7 H atoms may be replaced; A" and A"' together are alternatively an alkylene chain, in which one, two or three CH2 groups may be replaced; aryl is optionally substituted phenyl, naphthyl, fluorenyl or biphenyl; Het is an optionally substituted monocyclic or bicyclic saturated, unsaturated or aromatic heterocyclic ring having 1 or 2 N, O and/or S atoms; and Hal is F, Cl, Br or I act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.

L'invention concerne des dérivés thiazole de la formule (I) dans laquelle R?1¿, R?2¿, R?3¿, V, W, X et B ont les significations données dans le descriptif, servant d'inhibiteurs de phosphodiestérase IV. Lesdits dérivés thiazole peuvent servir au traitement de l'ostéoporose, de tumeurs, de la cachexie, de l'athérosclérose, de l'arthrite rhumatoïde, de la sclérose multiple, du diabète sucré, de processus inflammatoires, d'allergies, de l'asthme, de maladie auto-immunitaires, de maladies du myocarde et de SIDA.

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