首页> 外国专利> DERIVATIVES tetrahydrocarbazole, their preparation, pharmaceutical compositions, medicines and SET based on them, methods of treatment and / or prophylaxis of physiological and / or pathological diseases mediated coupled receptors G-protein or of a physiological and / or pathological diseases that IT IS POSSIBLE TO INFLUENCE THE MODULATION OF THESE RECEPTORS THROUGH THE ABOVE DERIVATIVES

DERIVATIVES tetrahydrocarbazole, their preparation, pharmaceutical compositions, medicines and SET based on them, methods of treatment and / or prophylaxis of physiological and / or pathological diseases mediated coupled receptors G-protein or of a physiological and / or pathological diseases that IT IS POSSIBLE TO INFLUENCE THE MODULATION OF THESE RECEPTORS THROUGH THE ABOVE DERIVATIVES

机译:衍生四氢咔唑,其制剂,药物组合物,药物和基于它们的SET,治疗和/或预防生理和/或病理疾病介导的偶联受体G蛋白或可能的生理和/或病理疾病的方法通过上面的导数影响这些接收器的调制

摘要

1. Derivatives of tetrahydrocarbazole covered by the general structural formula (I)! ! (A) V, W are independently selected from the group consisting of = O, = S, = S + -O-, geminally bound H2; ! R1, R1 * - when present - together independently form = O, = S or = S + -O- or independently both represent hydrogen; ! R2, R3 are independently selected from the group consisting of! (i) hydrogen, alkyl, (C9-C30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, -F, -Cl, -Br, -I, - CN, -CF3, -N3 , -NH2, -NHX1, -NX2X3, -NO2, -OH, = O, -OCF3, -SH, -O-SO3H, -OR (O) (OH) 2, -CHO, -COOH, -C (O ) NH2, -SO3H, -P (O) (OH) 2, -C (O) -X4, -C (O) O-X5, -C (O) NH-X6, -C (O) NX7X8, - O-X9, -O (-X10-O) a-H (a = 1, 2, 3, 4, 5), -O (-X11-O) b-X12 (b = 1, 2, 3, 4 , 5), -OC (O) -X13, -OC (O) -O-X14, -OC (O) -NHX15, -OC (O) -NX16X17, -OP (O) (OX18) (OX19), -OSi (X20) (X21) (X22), -OS (O2) -X23, -NHC (O) -NH2, -NHC (O) -X24, -NX25C (O) -X26, -NH-C (O ) -O-X27, -NH-C (O) -NH-X28, -NH-C (O) -NX29X30, -NX31-C (O) -O-X32, -NX33-C (O) -NH- X34, -NX35-C (O) -NX36X37, -NHS (O2) -X38, -NX39S (O2) -X40, -S-X41, -S (O) -X42, -S (O2) -X43, - S (O2) NH-X44, -S (O2) NX45X46, -S (O2) O-X47, -P (O) (OX48) (OX49), -Si (X50) (X51) (X52), -C (NH) -NH2, -C (NX53) -N H2, -C (NH) -NHX54, -C (NH) -NX55X56, -C (NX57) -NHX58, -C (NX59) - NX60X61, -NH-C (O) -NH-O-X62, -NH -C (O) -NX63-O-X64, -NX65-C (O) -NX66-O-X67, -N (-C (O) -NH-O-X68) 2, -N (-C (O ) -NX69-O-X70) 2, -N (-C (O) -NH-O-X71) (- C (O) -NX72-O-X73), -C (S) -X74, -C ( S) -O-X75, -C (S) -NH-X76, -C (S) -NX77X78, -C (O) -NH-O-X79, -C (O) -NX80-O-X81, - C (S) -NH-O-X82, -C (S) -NX83-O-X84, -C (O) -NH-NH-X85, -C (O) -NH-NX86X87, -C (O) -NX88-NX89X90, -C (S) -NH-NH-X91, -C (S) -NH-NX92X93, -C (S) -NX94-NX95X96, -C (O) -C (O) -O- X97, -C (O) -C (O) -NH2, -C (O) -C (O) -NHX98, -C (O) -C (O) -NX99X100, -C (S) -C (O ) -O-X101, -C (O) -C (S) -O-X102, -C (S) -C (S) -O-X103, -C (S) -C (O) -NH2, - C (S) -C (O) -NHX104, -C (S) -C (O) -NX105X106, -C (S) -C (S) -NH2, -C (S) -C (S) -NHX107 , -C (S) -C (S) -NX108X109, -C (O) -C (S) -NH2, -C (O) -C (S) -NHX110, -C (O) -C (S) -NX111X112,! in which X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28, X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40, X41, X42, X43, X44, X45, X46, X47, X48, X49, X50, X51, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64, X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77, X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90, X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102, X103, X104, X105, X106, X107, X108, X109, X110, X111, X112 independent
机译:1.通式(I)涵盖的四氢咔唑衍生物! ! (A)V,W独立地选自= O,= S,= S + -O-,双键结合的H 2; ! R 1,R 1 *-当存在时-一起独立地形成= O,= S或= S + -O-或独立地都代表氢; ! R2,R3独立地选自: (i)氢,烷基,(C 9 -C 30)烷基,环烷基,环烷基烷基,杂环基,杂环基烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,-F,-Cl,-Br,-I,-CN,-CF 3,-N 3 ,-NH2,-NHX1,-NX2X3,-NO2,-OH,= O,-OCF3,-SH,-O-SO3H,-OR(O)(OH)2,-CHO,-COOH,-C(O )NH2,-SO3H,-P(O)(OH)2,-C(O)-X4,-C(O)O-X5,-C(O)NH-X6,-C(O)NX7X8,- O-X9,-O(-X10-O)aH(a = 1,2,3,4,5),-O(-X11-O)b-X12(b = 1,2,3,4,5 ),-OC(O)-X13,-OC(O)-O-X14,-OC(O)-NHX15,-OC(O)-NX16X17,-OP(O)(OX18)(OX19),-OSi (X20)(X21)(X22),-OS(O2)-X23,-NHC(O)-NH2,-NHC(O)-X24,-NX25C(O)-X26,-NH-C(O)- O-X27,-NH-C(O)-NH-X28,-NH-C(O)-NX29X30,-NX31-C(O)-O-X32,-NX33-C(O)-NH- X34, -NX35-C(O)-NX36X37,-NHS(O2)-X38,-NX39S(O2)-X40,-S-X41,-S(O)-X42,-S(O2)-X43,-S( O2)NH-X44,-S(O2)NX45X46,-S(O2)O-X47,-P(O)(OX48)(OX49),-Si(X50)(X51)(X52),-C(NH )-NH2,-C(NX53)-NH2,-C(NH)-NHX54,-C(NH)-NX55X56,-C(NX57)-NHX58,-C(NX59)-NX60X6 1,-NH-C(O)-NH-O-X62,-NH -C(O)-NX63-O-X64,-NX65-C(O)-NX66-O-X67,-N(-C( O)-NH-O-X68)2,-N(-C(O)-NX69-O-X70)2,-N(-C(O)-NH-O-X71)(-C(O)- NX72-O-X73),-C(S)-X74,-C(S)-O-X75,-C(S)-NH-X76,-C(S)-NX77X78,-C(O)-NH -O-X79,-C(O)-NX80-O-X81,-C(S)-NH-O-X82,-C(S)-NX83-O-X84,-C(O)-NH-NH -X85,-C(O)-NH-NX86X87,-C(O)-NX88-NX89X90,-C(S)-NH-NH-X91,-C(S)-NH-NX92X93,-C(S) -NX94-NX95X96,-C(O)-C(O)-O- X97,-C(O)-C(O)-NH2,-C(O)-C(O)-NHX98,-C(O )-C(O)-NX99X100,-C(S)-C(O)-O-X101,-C(O)-C(S)-O-X102,-C(S)-C(S)- O-X103,-C(S)-C(O)-NH2,-C(S)-C(O)-NHX104,-C(S)-C(O)-NX105X106,-C(S)-C (S)-NH2,-C(S)-C(S)-NHX107,-C(S)-C(S)-NX108X109,-C(O)-C(S)-NH2,-C(O) -C(S)-NHX110,-C(O)-C(S)-NX111X112 ,!其中X1,X2,X3,X4,X5,X6,X7,X8,X9,X10,X11,X12,X13,X14,X15,X16,X17,X18,X19,X20,X21,X22,X23,X24, X25,X26,X27,X28,X29,X30,X31,X32,X33,X34,X35,X36,X37,X38,X39,X40,X41,X42,X43,X44,X45,X46,X47,X48,X49, X50,X51,X52,X53,X54,X55,X56,X57,X58,X59,X60,X61,X62,X63,X64,X65,X66,X67,X68,X69,X70,X71,X72,X73,X74, X75,X76,X77,X78,X79,X80,X81,X82,X83,X84,X85,X86,X87,X88,X89,X90,X91,X92,X93,X94,X95,X96,X97,X98,X99, X100,X101,X102,X103,X104,X105,X106,X107,X108,X109,X110,X111,X112独立

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