SUBSTITUIERTE 3-PHENYL-5-ALKOXI-1,3,4-OXDIAZOL-2-ONE UND IHRE VERWENDUNG ZUR HEMMUNG DER HORMONSENSITIVEN LIPASE
    4.
    发明授权
    SUBSTITUIERTE 3-PHENYL-5-ALKOXI-1,3,4-OXDIAZOL-2-ONE UND IHRE VERWENDUNG ZUR HEMMUNG DER HORMONSENSITIVEN LIPASE 有权
    取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮和它们用于抑制激素敏感性脂肪酶

    公开(公告)号:EP1263745B1

    公开(公告)日:2004-05-19

    申请号:EP01905805.6

    申请日:2001-02-20

    摘要: The invention relates to substituted 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-ones of formula (I), wherein R1 means substituted C¿1?-C6-alkyl and C3-C9-cycloalkyl, R?2, R3, R4 and R5¿ mean hydrogen, halogen, nitro, C¿1?-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O-C3-C8-cycloalkyl or 2-oxo-pyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR?6-A-R-7¿, on the condition that R?2, R3, R4 and R5¿ do not mean simultaneously mean hydrogen and at least one of the radicals R?2, R3, R4 or R5¿ represents the radical 2-oxo-pyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with R6 = hydrogen, C¿1?-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A = a simple bond, COn, SOn or CONH, n = 1 or 2, R?7¿ = hydrogen, substituted C¿1?-C18-alkyl,C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, diphenyl, diphenyl-C1-C4-alkyl, indanyl or the group Het-(CH2)r-, with r = 0, 1,2 or 3 and Het = a saturated and unsaturated 5-7 membered heterocycle which can be benzoanellated and substituted. The invention also relates to a method for producing the same. The inventive compounds have an inhibitory effect on hormone-sensitive lipase, HSL.

    SUBSTITUIERTE 3-PHENYL-5-ALKOXI-1,3,4-OXDIAZOL-2-ONE UND IHRE VERWENDUNG ALS LIPASE-HEMMER
    9.
    发明授权
    SUBSTITUIERTE 3-PHENYL-5-ALKOXI-1,3,4-OXDIAZOL-2-ONE UND IHRE VERWENDUNG ALS LIPASE-HEMMER 有权
    取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮及其作为脂肪酶抑制剂

    公开(公告)号:EP1214302B1

    公开(公告)日:2003-10-29

    申请号:EP00962346.3

    申请日:2000-08-22

    CPC分类号: C07D271/113

    摘要: The invention relates to substituted 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-ones of formula (1) and their physiologically compatible salts and optical isomers, R1 meaning C¿1?-C6-alkyl, C3-C9-cycloalkyl, both of which can be optionally substituted, and R?2 and R3¿ meaning, independently of each other, hydrogen, C¿6?-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloximethyl, O-benzyl, O-C6-C10-aryl, O-C3-C8-cycloalkyl, O-C1-C6-alkyl, SO2-NH-C1-C6-alkyl, SO2-NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2-NH-C3-C8-cycloalkyl, SO2-N(C1-C6-alkyl)2 or COX, X representing O-C1-C6-alkyl, NH-C1-C6-alkyl, NH-C3-C8-cycloalkyl or N(C1-C6-alkyl)2; on the condition that the substituents R?2 and R3¿ can be partially optionally substituted and that they do not mean hydrogen at the same time. The invention also relates to a method for producing the inventive 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-ones. The compounds present an inhibiting effect on the hormone-sensitive lipase HSL.

    SUBSTITUIERTE 3-PHENYL-5-ALKOXI-1,3,4-OXDIAZOL-2-ONE UND IHRE VERWENDUNG ZUR HEMMUNG DER HORMONSENSITIVEN LIPASE
    10.
    发明公开
    SUBSTITUIERTE 3-PHENYL-5-ALKOXI-1,3,4-OXDIAZOL-2-ONE UND IHRE VERWENDUNG ZUR HEMMUNG DER HORMONSENSITIVEN LIPASE 有权
    取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮和它们用于抑制激素敏感性脂肪酶

    公开(公告)号:EP1263745A1

    公开(公告)日:2002-12-11

    申请号:EP01905805.6

    申请日:2001-02-20

    摘要: The invention relates to substituted 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-ones of formula (I), wherein R1 means substituted C¿1?-C6-alkyl and C3-C9-cycloalkyl, R?2, R3, R4 and R5¿ mean hydrogen, halogen, nitro, C¿1?-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O-C3-C8-cycloalkyl or 2-oxo-pyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR?6-A-R-7¿, on the condition that R?2, R3, R4 and R5¿ do not mean simultaneously mean hydrogen and at least one of the radicals R?2, R3, R4 or R5¿ represents the radical 2-oxo-pyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with R6 = hydrogen, C¿1?-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A = a simple bond, COn, SOn or CONH, n = 1 or 2, R?7¿ = hydrogen, substituted C¿1?-C18-alkyl,C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, diphenyl, diphenyl-C1-C4-alkyl, indanyl or the group Het-(CH2)r-, with r = 0, 1,2 or 3 and Het = a saturated and unsaturated 5-7 membered heterocycle which can be benzoanellated and substituted. The invention also relates to a method for producing the same. The inventive compounds have an inhibitory effect on hormone-sensitive lipase, HSL.