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公开(公告)号：US5741800A
公开(公告)日：1998-04-21
申请号：US564155
申请日：1995-12-21
申请人： David George Webber , Gerald Bernard Tometzki , Michael Henry Hockley , Roger Bernard Titman , Roy Victor Davies , Paul Anthony Bradley
发明人： David George Webber , Gerald Bernard Tometzki , Michael Henry Hockley , Roger Bernard Titman , Roy Victor Davies , Paul Anthony Bradley
IPC分类号： C07D401/06 , C07D521/00 , A61K31/445 , C07D403/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D401/06
摘要： A compound of the formula (I), ##STR1## as defined in the specification, having immunomodulatory activity, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compound, and processes to make and to use the compound are described.
摘要翻译： 描述了具有免疫调节活性的说明书中定义的式（I）化合物，其药学上可接受的盐，包含该化合物的药物组合物，以及制备和使用该化合物的方法。
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2.发明授权Heteroarylsulfonamide derivatives and pharmaceutical compositions containing them 有权杂芳基磺酰胺衍生物和含有它们的药物组合物公开(公告)号：US06218405B1
公开(公告)日：2001-04-17
申请号：US09331064
申请日：1999-06-16
IPC分类号： A61K31445
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendrocrine system, stress, and spasticity.
摘要翻译： 式（I）化合物及其药学上可接受的盐，其中A是亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3形成杂芳族或杂脂族链; g为0,1或2; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T是任选取代的芳基或杂芳基，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍 ，吸毒成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常， 神经分泌系统紊乱，压力和痉挛状态。
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公开(公告)号：US20090099209A1
公开(公告)日：2009-04-16
申请号：US12333533
申请日：2008-12-12
IPC分类号： A61K31/506 , A61K31/4152 , C07D231/18 , C07D413/06 , C07D401/06 , C07D417/06 , A61K31/4196 , A61K31/4245 , A61K31/4155 , A61K31/433 , A61K31/4192 , A61K31/427 , A61K31/4439 , A61K31/422 , A61K31/4178 , C07D403/06
CPC分类号： C07D231/28 , C07D231/18 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D413/06 , C07D417/06
摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中：R 1表示H，C 1-6烷基，C 1-6烷氧基，C 3-8环烷基或卤素; R 2表示H，C 1-6烷基（任选被R 3取代），苯基（任选被CN取代）或Het; R3表示OH，CN，Het，-R4-C1-6烷基或CONR5R6; R 4表示-CO 2 - 或-O-; R5和R6独立地表示H，C 1-6烷基（任选被OR 7取代）或C 3-8环烷基; R 7表示H或C 1-6烷基; Het表示含有（i）1-4个氮杂原子或（ii）一个或两个氮杂原子和一个氧或一个硫杂原子的五元或六元芳族杂环基，或（iii）一个或两个氧 或硫杂原子，所述杂环基团任选被一个或多个选自CN和C 1-6烷基的基团取代; R 8表示C 1-6烷基，C 1-6烷氧基，C 3-8环烷基或卤素; 且R 9和R 10独立地表示H，C 1-6烷基，C 1-6烷氧基，CN，CF 3或卤素; 可能有助于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。
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公开(公告)号：US06353002B2
公开(公告)日：2002-03-05
申请号：US09748153
申请日：2000-12-27
IPC分类号： A61K31445
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, and spasticity.
摘要翻译： 式I化合物及其药学上可接受的盐，其中A是亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3形成杂芳族或杂脂族链; g为0,1或2; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T是任选取代的芳基或杂芳基，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍 ，吸毒成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常， 神经内分泌系统疾病，压力和痉挛状态。
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公开(公告)号：US07425569B2
公开(公告)日：2008-09-16
申请号：US11870451
申请日：2007-10-11
IPC分类号： A61K31/44
CPC分类号： C07D231/18 , C07D401/12
摘要： Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中R 1和R 3独立代表H，C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基，CF 3或芳基; a代表1或2; R 4，R 5，R 7和R 8独立地表示H，C 1-6 C 1-6烷基，C 1-6烷氧基，CN或卤素，或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H，CN或卤素，条件是当X表示N时，R 6不存在。 这些化合物可用于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。
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公开(公告)号：US07309712B2
公开(公告)日：2007-12-18
申请号：US11592574
申请日：2006-11-03
IPC分类号： A61K31/44 , C07D401/00 , C07D231/10
CPC分类号： C07D231/18 , C07D401/12
摘要： Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中R 1和R 3独立代表H，C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基，CF 3或芳基; a代表1或2; R 4，R 5，R 7和R 8独立地表示H，C 1-6 C 1-6烷基，C 1-6烷氧基，CN或卤素，或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H，CN或卤素，条件是当X表示N时，R 6不存在。 这些化合物可用于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。
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公开(公告)号：US07482375B2
公开(公告)日：2009-01-27
申请号：US11408286
申请日：2006-04-18
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D231/28 , C07D231/18 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D413/06 , C07D417/06
摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii)one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中：R 1表示H，C 1-6 - 烷基，C 1-6烷氧基，C 3-8环烷基或卤素; R 2表示H，C 1-6烷基（任选被R 3取代），苯基（任选被CN取代）或Het; R3表示OH，CN，Het，-R4-C1-6烷基或CONR5R6; R 4表示-CO 2 - 或-O-; R5和R6独立地表示H，C 1-6烷基（任选被OR 7取代）或C 3-8环烷基; R 7表示H或C 1-6烷基; Het表示含有（i）1-4个氮杂原子或（ii）一个或两个氮杂原子和一个氧或一个硫杂原子的五元或六元芳族杂环基，或（iii）一个或两个氧 或硫杂原子，所述杂环基团任选被一个或多个选自CN和C 1-6烷基的基团取代; R 8表示C 1-6烷基，C 1-6烷氧基，C 3-8环烷基或卤素; R 9和R 10独立地表示H，C 1-6烷基，C 1-6烷氧基，CN，CF 3或卤素; 可能有助于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。
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公开(公告)号：US06201004B1
公开(公告)日：2001-03-13
申请号：US09380375
申请日：1999-09-01
IPC分类号： A61K3140
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, and spasticity.
摘要翻译： 式I化合物及其药学上可接受的盐，其中A是亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3形成杂芳族或杂脂族链; g为0,1或2; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T是任选取代的芳基或杂芳基，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍 ，吸毒成瘾，药物滥用，认知障碍，阿尔茨海默病，老年痴呆，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常， 神经内分泌系统疾病，压力和痉挛状态。
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公开(公告)号：US6107310A
公开(公告)日：2000-08-22
申请号：US91129
申请日：1998-06-16
IPC分类号： A61K31/00 , A61K31/365 , A61K31/366 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/10 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/12 , A61P15/00 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D491/04 , C07D491/056 , C07D493/04 , C07D498/04 , C07D513/04 , C07D401/14
CPC分类号： C07D491/04
摘要： Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; G.sub.1 --G.sub.2 --G.sub.3 are absent or form a heteroaromatic chain; g is 0,1,2,3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO. HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mrellitus, hyperglvcaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
摘要翻译： PCT No.PCT / EP96 / 05637 371日期：1998年6月16日 102（e）日期1998年6月16日PCT 1996年12月16日PCT公布。 公开号WO97 / 23485 日期：1997年7月3日，式I化合物及其药学上可接受的盐，其中A为亚甲基或-O-; B是亚甲基或-O-; G1-G2-G3不存在或形成杂芳族链; g为0,1,2,3或4; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T代表CO。HET可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍，药物成瘾， 药物滥用，认知障碍，阿尔茨海默病，老年痴呆症，强迫症，惊恐发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管疾病，非胰岛素依赖型糖尿病，高血糖，便秘，心律失常，神经内分泌紊乱 系统，压力，前列腺肥大和痉挛状态。
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