Patent ID: 6673829
Filing Date: 2004-01-06
Classification: A61K,C07D

Abstract:
A compound of the general formula (I): whereinR1 represents hydrogen, C1-8-alkyl, C3-8-alkenyl or C3-8-alkynyl, â€ƒwhich may optionally be substituted with one or more halogen atoms, cyclobutyl, C3-7-cycloalkenyl, C4-8-bicycloalkyl, C3-7-cycloalkyl-C1-3-alkyl or C3-7-cycloalkenyl-C1-3-alkyl, â€ƒwhich may optionally be substituted at any position with one or more halogen atoms, R2 represents C1-6-alkyl, f is 0, 1 or 2, X represents â€”(CH2)mâ€”(Z)nâ€”(CHZ)oâ€”, m and o independently are 0, 1, 2, 3 or 4, n is 0 or 1, Z is â€”Oâ€”, â€”NHâ€”, â€”N(CH3)â€”, â€”C(&boxH;O)â€”, â€”CH(OH)â€”, â€”CH(Oâ€”C1-6-alkyl)-, â€”C(&boxH;Nâ€”OH)â€”, â€”Sâ€”, â€”S(&boxH;O)â€”, â€”S&boxH;O)2â€”, â€”CH&boxH;CHâ€” or â€”C&boxH;Câ€”, Y is (a) aryl or heteroaryl, which may optionally be substituted with one or more substituents selected from halogen, nitro, cyano, hydroxy, C1-6-alkanoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkyl, C1-6-alkoxy, C3-8-cycloalkyl, trifluoromethyl, trifluoromethoxy, â€”NR3R4 and â€”O(C&boxH;O)NR3R4, or wherein two substituents in adjacent positions form a radical â€”Oâ€”(CH2)1-3â€”Oâ€”, â€ƒwherein R3 and R4 independently are hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C1-6-alkanoyl or aryl, or R3 and R4 together with the nitrogen atom to which they are attached form a 4 to 7 membered, saturated or unsaturated azetidinyl, pyrrolidinyl, piperidyl or azepanyl ring, â€ƒwherein said heteroaryl is selected from the group consisting of furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, tetrazolyl, thiadiazinyl, indolyl, isoindolyl, benzofuryl, benzothienyl, indazolyl, benzimidazolyl, benzothiazolyl, benzoisothiazolyl, benzoxazolyl, benzisoxazolyl, purinyl, quinazolinyl, quinolizinyl, quinolinyl, isoquinolinyl, quinoxalinyl, napththyridinyl, pteridinyl, carbazolyl, azepinyl, diazepinyl, acridinyl and partially hydrogenated derivatives thereof aryl, aryloxy, aryl-C1-6-alkyl and aryl-C1-6-alkoxy, wherein the ring moieties optionally may be substituted with one or more substituents selected from halogen, nitro, cyano, hydroxy, C1-6-alkanoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkyl, C1-6-alkoxy, C3-8-cycloalkyl, trifluoromethyl, trifluoromethoxy, â€”NR5R6 and â€”O(C&boxH;O)NR5R6, or wherein two substituents in adjacent positions form a radical â€”Oâ€”(CH2)1-3â€”Oâ€”, â€ƒwherein R5 and R6 independently are hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C1-6-alkanoyl or aryl, or R5 and R6 together with the nitrogen atom to which they are attached form a 4 to 7 membered, saturated or unsaturated azetidinyl, pyrrolidinyl, piperidyl or azepanyl ring, (b) C3-8-cycloalkyl or C5-8-cycloalkenyl, which may optionally be substituted with one or more substituents selected from C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, cyano, trifluoromethyl, trifluoromethoxy and halogen, aryl and aryloxy, wherein the ring moieties optionally may be substituted with one or more substituents selected from halogen, nitro, cyano, hydroxy, C1-6-alkanoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkyl, C1-6-alkoxy, C3-8-cycloalkyl, trifluoromethyl, trifluoromethoxy, â€”NR7R8 and â€”O(C&boxH;O)NR7R8, or wherein two substituents in adjacent positions form a radical â€”Oâ€”(CH2)1-3â€”Oâ€”, â€ƒwherein R7 and R8 independently are hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C1-6-alkanoyl or aryl, or R7 and R8 together with the nitrogen atom to which they are attached form a 4 to 7 membered, saturated or unsaturated azetidinyl, pyrrolidinyl, piperidyl or azepanyl ring, as well as any diastereomer or enantiomer or tautomeric form thereof including mixtures of these or a pharmaceutically acceptable salt thereof,with the proviso that,when m, n, and o are 0, R1 must not be ethyl, or methyl,and with the proviso that the compound must not be