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New 1,2,3,4-tetrahydro-carbazole derivatives are G-protein coupled receptor ligands and gonadotropin releasing hormone inhibitors used e.g. for treating infertility or tumors or as contraceptives
New 1,2,3,4-tetrahydro-carbazole derivatives are G-protein coupled receptor ligands and gonadotropin releasing hormone inhibitors used e.g. for treating infertility or tumors or as contraceptives
3-Substituted 1,2,3,4-tetrahydrocarbazole derivatives (I) are new. 3-Substituted 1,2,3,4-tetrahydrocarbazole derivatives of formula (I) are new. R1 = H, 2-6C alkenyl or 1-6C alkyl and is optionally substituted (os) by COOR11 or aryl or heteroaryl (both os by 1-3 NO2, Me, CF3, OMe, OCF3 or halo); R11 = H, 1-12C alkyl, 1-12C aralkyl (sic), aryl, heteroaryl or COMe, and is os by CONH2, COMe, COOMe, SO2Me or aryl; R2-R5 = H, halo, COOH, CONH2, CF3, OCF3, NO2, CN, 1-6C alkyl, 2-6C alkenyl, 1-6C alkoxy, 1-12C aralkyl (sic), aryl or heteroaryl; R6 = CONR8R9, COOR8, CH2NR7R8, CH2R8, CH2OR8 or 2-12C alkenyl (os by R8 and R9); R8, R9 = H, 1-12C alkyl, 1-12C aralkyl (sic), aryl or heteroaryl, and is os by at least one OH, NH2, CONHR10, COOR10, NHC(=NH)NH2 or halo, or R8 + R9 = a group completing a ring, optionally containing heteroatoms; R10 = H, 1-12C alkyl, 1-12C aralkyl (sic), aryl or heteroaryl, and is os by CON(R11)2; R7 = H, 1-12C alkyl, 2-12C alkenyl, 1-12C aralkyl (sic), aryl, heteroaryl, NR12R13, NHCOR14, NHCONHR14 or NHSO2R14, and is os by at least one OH, NH2, CONH2, COOH or halo; R12, R13 = H, 2-6C alkenyl or 1-6C alkyl, and is os by aryl or heteroaryl (both os by 1-3 NO2, Me, CF3, OMe, OCF3 or halo); R14 = H, 1-12C alkyl, 2-12C alkenyl, 1-12C aralkyl (sic), aryl or heteroaryl, and is os by at least one NO2, Me, OR11, CF3, OCF3, OH, N(R11)2, OCOR11, COOH, CONH2, NHCONHR11, NHCOOR11 or halo, and Ra-Rf = H, halo, COOH, CONH2, CF3, OCF3, NO2, CN, 1-6C alkyl, 1-6C alkoxy, aryl or heteroaryl. The following compounds (I') are excluded: 3-amino-1,2,3,4-tetrahydrocarbazole-3-carboxylic acid, 3-amino-6-methoxy-1,2,3,4-tetrahydro-carbazole-3-carboxylic acid, 3-amino-6-benzyloxy-1,2,3,4-tetrahydro-carbazole-3-carboxylic acid, 3-acetamido-1,2,3,4-tetrahydrocarbazole-3-carboxylic acid, methyl 3-acetamido-1,2,3,4-tetrahydrocarbazole-3-carboxylate, (-)-menthyl 3-acetamido-1,2,3,4-tetrahydrocarbazole-3-carboxylate and 3-tert. butoxycarbonylamino-1,2,3,4-tetrahydrocarbazole-3-carboxylic acid. An Independent claim is included for the use of (I), including (I'), in the production of pharmaceutical compositions for inhibiting gonadotropin releasing hormone inhibitor and in male fertility control or in female contraception.
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机译：3-取代的1,2,3,4-四氢咔唑衍生物（I）是新的。式（I）的3-取代的1,2,3,4-四氢咔唑衍生物是新的。 R 1 ＝ H，2-6C烯基或1-6C烷基，并且任选地被（OR）被COOR 11或芳基或杂芳基（两个都被1-3个NO 2，Me，CF 3，OMe，OCF 3或卤素取代） ）; R 11 ＝ H，1-12C烷基，1-12C芳烷基（sic），芳基，杂芳基或COMe，并且由CONH 2，COMe，COOMe，SO 2 Me或芳基为os; R 2 -R 5 ＝ H，卤素，COOH，CONH 2，CF 3，OCF 3，NO 2，CN，1-6C烷基，2-6C烯基，1-6C烷氧基，1-12C芳烷基（sic），芳基或杂芳基; R 6 ＝ CONR 8 R 9，COOR 8，CH 2 NR 7 R 8，CH 2 R 8，CH 2OR 8或2-12C烯基（R 8的os和R 9）; R 8，R 9 ＝ H，1-12C烷基，1-12C芳烷基（sic），芳基或杂芳基，并且是由至少一种OH，NH 2，CONHR 10，COOR 10所取代。 NHC（＝ NH）NH 2或卤素，或R 8 + R 9 ＝完成环的基团，任选地包含杂原子; R 10 ＝ H，1-12C烷基，1-12C芳烷基（sic），芳基或杂芳基，并且通过CON（R 11）2为os。 R 7 ＝ H，1-12C烷基，2-12C烯基，1-12C芳烷基（sic），芳基，杂芳基，NR 12 R 13，NHCOR 14，NHCONHR 14或NHSO 2 R < 14>，并且是至少一种OH，NH 2，CONH 2，COOH或卤素的os; R 12，R 13 ＝ H，2-6C链烯基或1-6C烷基，并且是通过芳基或杂芳基形成的os（都是通过1-3个NO 2，Me，CF 3，OMe，OCF 3或卤素形成的）。 R 14 ＝ H，1-12C烷基，2-12C烯基，1-12C芳烷基（sic），芳基或杂芳基，并且为至少一种NO 2，Me，OR 11，CF 3，OCF 3，OH的os。 ，N（R 11）2，OCOR 11，COOH，CONH 2，NHCONHR 11，NHCOOR 11或卤素，且Ra-Rf = H，卤素，COOH，CONH 2，CF 3，OCF 3，NO 2， CN，1-6C烷基，1-6C烷氧基，芳基或杂芳基。排除以下化合物（I'）：3-氨基-1,2,3,4-四氢咔唑-3-羧酸，3-氨基-6-甲氧基-1,2,3,4-四氢咔唑-3 -羧酸，3-氨基-6-苄氧基-1,2,3,4-四氢咔唑-3-羧酸，3-乙酰氨基-1,2,3,4-四氢咔唑-3-羧酸，甲基3 -乙酰氨基-1,2,3,4-四氢咔唑-3-羧酸酯，（-）-薄荷基3-乙酰氨基-1,2,3,4-四氢咔唑-3-羧酸酯和3-叔胺。丁氧基羰基氨基-1，2，3，4-四氢咔唑-3-羧酸。包括（I），包括（I'）在内的独立权利要求在生产用于抑制促性腺激素释放激素抑制剂的药物组合物中以及在男性生育控制或女性避孕中的用途。
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