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1. 发明申请

WO2008146063A1 NEW BENZOFURAN DERIVATIVES AS SELECTIVE 5HT6 RECEPTOR INHIBITORS AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：作为选择性5HT6受体抑制剂的新型苯并呋喃衍生物及其制备方法
公开(公告)号：WO2008146063A1
公开(公告)日：2008-12-04
申请号：PCT/HU2008/000060
申请日：2008-05-30
申请人： EGIS GYÓGYSZERGYÁR Nyilvánosan Müködö Részvénytársagág , RIVÓ, Endre , PRAUDA, Ibolya , REITER, József , BARKÓCZY, József , GACSÁLYI, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
发明人： RIVÓ, Endre , PRAUDA, Ibolya , REITER, József , BARKÓCZY, József , GACSÁLYI, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
IPC分类号： A61K31/343 , A61K31/496 , C07D307/83 , C07D405/12 , A61P9/00 , A61P25/00
CPC分类号： C07D307/86
摘要： The present invention relates to new selective 5HT 6 receptor binding benzofuran derivatives of general formula (I) wherein, Z represents a hydrogen atom, C 1-4 acyl group, C 1-6 alkyl sulfonyl group, phenyl sulfonyl group substituted with one or more halogen atom; or naphthyl sulfonyl group optionally substituted with a halogen atom, tetrahydro naphthyl sulfonyl group, (lS)(+)-10-camphor-sulfonyl group, (lR)(-)-10-camphor-sulfonyl group or benzofuranyl sulfonyl group, substituted with a halogen atom and C 1 -4 alkyl group, Y represents C 2-6 alkylene group, R 1 and R 2 represent, independently, a hydrogen atom, C 1-4 alkyl group, benzyl group, or together with one or more halogen atoms, trifluoromethyl group, or C 1-4 alkoxy group substituted 4-phenyl-piperazine-l-yl group; and/or their pharmaceutically suitable acid addition salts, to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in treatment and/or prevention of disorders of the central nervous system and cardiovascular system.
摘要翻译：本发明涉及通式（I）的新的选择性5HT6受体结合苯并呋喃衍生物，其中Z表示氢原子，C1-4酰基，C1-6烷基磺酰基，被一个或多个卤素原子取代的苯基磺酰基; 或（R）（ - ） - 10-樟脑磺酰基，或被苯并呋喃基磺酰基取代的苯并呋喃基磺酰基，或者被卤素原子取代的萘基磺酰基，四氢萘基磺酰基，（1S）（+） - 10-樟脑磺酰基，（1R）卤素原子和C1〜4烷基，Y表示C2-6亚烷基，R1和R2独立地表示氢原子，C1-4烷基，苄基或与一个或多个卤素原子一起形成的三氟甲基，或C 1-4烷氧基取代的4-苯基 - 哌嗪-1-基; 和/或其药学上合适的酸加成盐，用于制备所述化合物的方法，含有所述化合物的药物组合物及其在治疗和/或预防中枢神经系统和心血管系统疾病中的用途。

2. 发明申请

WO2008146064A1 NEW BENZOFURAN DERIVATIVES AS SELECTIVE 5HT7 RECEPTOR INHIBITORS AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：作为选择性5HT7受体抑制剂的新型苯佐衍生物及其制备方法
公开(公告)号：WO2008146064A1
公开(公告)日：2008-12-04
申请号：PCT/HU2008/000061
申请日：2008-05-30
申请人： EGIS GYÓGYSZERGYÁR , PRAUDA, Ibolya , RIVÓ, Endre , REITER, József , BARKÖCZY, József , GACSÁLYL, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
发明人： PRAUDA, Ibolya , RIVÓ, Endre , REITER, József , BARKÖCZY, József , GACSÁLYL, István , KOMPAGNE, Hajnalka , SZIRAY, Nóra , PALLAGI, Katalin , EGYED, András , HEGEDÜS, Endre , LÉVAY, György , HÁRSING, László Gábor
IPC分类号： C07D307/86 , C07D405/12 , A61K31/4525 , A61P25/00
CPC分类号： C07D405/12 , C07D307/86
摘要： The present invention relates to new selective 5HT 7 receptor binding benzofuran derivatives of general formula (I), wherein X represents a halogen atom or SO 2 NR 1 R 2 group, wherein R 1 and R 2 represent, independently, a hydrogen atom, C 1-6 alkyl group, C 3-6 cycloalkyl group, phenyl group substituted with one or more halogen atom(s) or 1,7.7-trimethyl-bicyclo[2,2,1]hept-2-yl group, Y represents C 2-6 alkylene group, optionally substituted with hydroxy group, A represents carbon atom, nitrogen atom or CH group, B represents CH or CH 2 group, Q represents C 1-4 alkyl group, a phenyl group optionally substituted with one or more halogen atom(s), C 1-4 alkoxy group or trifluoromethyl group; phenylamino group substituted with a halogen atom or trifluoromethyl group; pyridine heterocycle; benzisoxazole or benzisothiazole heterocycle, optionally substituted with a halogen atom; benzimidazole or benzimidazolone heterocycle, optionally substituted with a halogen atom or trifluoromethyl group on the benzene ring, or optionally substituted on one of the N atoms with an C 1-4 alkyl group; benzodioxane heterocycle, optionally substituted with a halogen atom on the benzene ring; pyridazinone heterocycle substituted with a halogen atom; dibenzothiazepine heterocycle or Q together with groups A and B represents a thiophene ring and their pharmaceutically suitable acid addition salts, with the proviso that if Y represents 2-hydroxy propylene group, A represents a carbon atom, B represents CH group, and Q represents 3-trifluoro-methyl-phenyl group, then X does not represent bromo atom. The invention extends to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in treatment and/or prevention of disorders of the central nervous system and cardiovascular system.
摘要翻译：本发明涉及通式（I）的新的选择性5HT7受体结合苯并呋喃衍生物，其中X表示卤素原子或SO2NR1R2基团，其中R1和R2独立地表示氢原子，C1-6烷基，C3-6 环烷基，被一个或多个卤素原子或1,7,7-三甲基 - 双环[2,2,1]庚基取代的苯基，Y表示任选被羟基取代的C 2-6亚烷基 A表示碳原子，氮原子或CH基，B表示CH或CH2基，Q表示C1-4烷基，任选被一个或多个卤素原子取代的苯基，C 1-4烷氧基或三氟甲基 ; 被卤素原子或三氟甲基取代的苯基氨基; 吡啶杂环; 苯并异恶唑或苯并异噻唑杂环，任选被卤素原子取代; 苯并咪唑或苯并咪唑酮杂环，任选被苯环上的卤素原子或三氟甲基取代，或任选地在一个N原子上被C 1-4烷基取代; 苯并二恶烷杂环，任选被苯环上的卤素原子取代; 用卤素原子取代的哒嗪酮杂环; 二苯并硫氮杂环或Q与A和B组一起代表噻吩环及其药学上合适的酸加成盐，条件是如果Y表示2-羟基丙基，则A表示碳原子，B表示CH基，Q表示3 三氟甲基 - 苯基，则X不表示溴原子。本发明涉及生产所述化合物的方法，含有所述化合物的药物组合物及其在治疗和/或预防中枢神经系统和心血管系统疾病中的用途。

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