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公开(公告)号:US06479519B1
公开(公告)日:2002-11-12
申请号:US09558812
申请日:2000-04-26
申请人: Peter Charles Astles , David Edward Clark , Alan John Collis , Paul Joseph Cox , Paul Robert Eastwood , Neil Victor Harris , Justine Yeun Quai Lai , Andrew David Morley , Barry Porter
发明人: Peter Charles Astles , David Edward Clark , Alan John Collis , Paul Joseph Cox , Paul Robert Eastwood , Neil Victor Harris , Justine Yeun Quai Lai , Andrew David Morley , Barry Porter
IPC分类号: C07C27538
CPC分类号: C07D213/75 , C07C275/42 , C07D211/62 , C07D213/71 , C07D213/81 , C07D213/82 , C07D213/89 , C07D233/84 , C07D237/24 , C07D261/18 , C07D309/06 , C07D333/38
摘要: The invention is directed to physiologically active compounds of formula (I): wherein: R1 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR10; and one of X3, X4 and X5 represents CR11 and the others independently represents N or CR10; where R10 is hydrogen, amino, halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, nitro or trifluoromethyl; and R11 represents a group —L1—Ar1—L2—Y; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).
摘要翻译: 本发明涉及式(I)的生理活性化合物:其中:R 1是氢,卤素,羟基,低级烷基或低级烷氧基; X 1,X 2和X 6独立地表示N或CR 10; X 3,X 4和X 5的一方表示CR 11,其余独立地表示N或CR 10;其中R 10为氢,氨基,卤素,羟基,低级烷基,低级烷氧基,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,硝基或三氟甲基; R11表示基团-L1-Ar1-L2-Y; 和相应的N-氧化物及其前药; 和这些化合物及其N-氧化物和前药的药学上可接受的盐和溶剂化物。 这些化合物具有有价值的药物性质,特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4(α4β1)的相互作用的能力。
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公开(公告)号:US07687540B2
公开(公告)日:2010-03-30
申请号:US11775547
申请日:2007-07-10
CPC分类号: C07F9/65517 , C07F9/3211
摘要: The present invention relates to certain esters of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1 and R2 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
摘要翻译: 本发明涉及式I的取代的3-氨基丙烷次膦酸衍生物的某些酯:其中R,R 1和R 2如本文所定义。 本发明的化合物可用于治疗各种疾病,包括但不限于抑郁,焦虑,某些精神症状,认知障碍和精神分裂症。
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公开(公告)号:US6048864A
公开(公告)日:2000-04-11
申请号:US67588
申请日:1998-04-28
IPC分类号: A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/505 , A61K31/535 , A61K31/55 , A61K31/551 , A61P13/02 , A61P13/08 , A61P15/00 , C07D401/04 , C07D403/04 , C07D405/14 , C07D471/04 , C07D239/94 , C07D239/95
CPC分类号: C07D401/04 , C07D403/04 , C07D405/14
摘要: Compounds of formula I, ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms;R.sup.2 and R.sup.3 independently represent H or C.sub.1-6 alkoxy (which is optionally substituted);R.sup.4 represents a 4-, 5-, 6- or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic, the ring system as a whole being optionally substituted;X represents CH or N; andL is absent,or represents a cyclic group of formula Ia, ##STR2## or represents a chain of formula Ib, ##STR3## and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.
摘要翻译: 式I化合物,其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R2和R3独立地表示H或C1-6烷氧基(其任选被取代); R4表示4-,5-,6-或7-元杂环,该环任选地与苯环或5-或6-元杂环稠合,该环系统作为整体任选被取代; X表示CH或N; 并且L不存在,或表示式Ia的环状基团,或表示式Ib的链及其药学上可接受的盐可用于治疗,特别是治疗良性前列腺增生。
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公开(公告)号:US06750214B2
公开(公告)日:2004-06-15
申请号:US10455546
申请日:2003-06-04
IPC分类号: A01N31519
CPC分类号: C07D401/04 , C07D215/42 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D497/04
摘要: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and the pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of inter alia benign prostatic hyperplasia.
摘要翻译: 本发明提供式(I)化合物,其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2表示任选被一个或多个氟原子取代的H或C 1-6烷氧基; R 3表示独立地选自H,卤素,C 1-4烷氧基和CF 3的一个或多个基团; 此外,R 2和一个R 3基团可以一起表示-OCH 2 - ,亚甲基连接到侧基苯环的邻位; R 4表示含有1或2个选自N,O和S的杂原子的4-,5-或6-元杂环,该环任选地与苯环稠合或含有5或6元杂环 1或2个选自N,O和S的杂原子,整个环系统任选被取代; X表示CH或N; 且L不存在或表示环状基团或开链基团; 及其药学上可接受的盐。 式(I)化合物可用于治疗特别是良性前列腺增生。
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公开(公告)号:US06642242B2
公开(公告)日:2003-11-04
申请号:US09812083
申请日:2001-03-19
IPC分类号: A61K31517
CPC分类号: C07D401/04 , C07D215/42 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D497/04
摘要: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of inter alia benign prostatic hyperplasia.
摘要翻译: 本发明提供式(I)化合物,其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2表示任选被一个或多个氟原子取代的H或C 1-6烷氧基; R 3表示独立地选自H,卤素,C 1-4烷氧基和CF 3的一个或多个基团; 此外,R 2和一个R 3基团可以一起表示-OCH 2 - ,亚甲基连接到侧基苯环的邻位; R 4表示含有1或2个选自N,O和S的杂原子的4-,5-或6-元杂环,该环任选地与苯环稠合或含有5或6元杂环 1或2个选自N,O和S的杂原子,整个环系统任选被取代; X表示CH或N; 且L不存在或表示环状基团或开链基团; 及其药学上可接受的盐。 式(I)化合物可用于治疗特别是良性前列腺增生。
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公开(公告)号:US6103738A
公开(公告)日:2000-08-15
申请号:US91370
申请日:1998-06-17
IPC分类号: A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/535 , A61K31/5355 , A61K31/55 , A61P7/00 , A61P9/06 , A61P9/12 , A61P13/02 , A61P15/00 , C07D215/42 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D497/04 , C07D513/04
CPC分类号: C07D401/04 , C07D215/42 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D497/04
摘要: The invention provides compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms; R.sup.2 represents H or C.sub.1-6 alkoxy optionally substituted by one or more fluorine atoms; R.sup.3 represents one or more groups independently selected from H, halogen, C.sub.1-4 alkoxy and CF.sub.3 ; in addition, R.sup.2 and one R.sup.3 group may together represent --OCH.sub.2 --, the methylene group being attached to the ortho-position of the pendant phenyl ring; R.sup.4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of inter alia benign prostatic hyperplasia.
摘要翻译: PCT No.PCT / EP96 / 05609 Sec。 371日期1998年6月17日第 102(e)1998年6月17日PCT 1996年12月5日PCT PCT。 公开号WO97 / 23462 日期:1997年7月3日本发明提供式(I)化合物,其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2表示H或任选被一个或多个氟原子取代的C 1-6烷氧基; R 3表示独立地选自H,卤素,C 1-4烷氧基和CF 3的一个或多个基团; 此外,R 2和R 3基团可以一起表示-OCH 2 - ,亚甲基连接到侧基苯环的邻位; R4代表含有1或2个选自N,O和S的杂原子的4-,5-或6-元杂环,该环任选地与苯环或含有1或2的5-或6-元杂环稠合 选自N,O和S的杂原子,所述环系统作为整体任选被取代; X表示CH或N; 且L不存在或表示环状基团或开链基团; 及其药学上可接受的盐。 式(I)化合物可用于治疗特别是良性前列腺增生。
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公开(公告)号:US08828974B2
公开(公告)日:2014-09-09
申请号:US13454643
申请日:2012-04-24
申请人: Yong Mi Choi-Sledeski , Julian Levell , Gregory Bernard Poli , Mark Czekaj , Alan John Collis , Roy Vaz
发明人: Yong Mi Choi-Sledeski , Julian Levell , Gregory Bernard Poli , Mark Czekaj , Alan John Collis , Roy Vaz
IPC分类号: A01N57/00 , A61K31/675 , C07C229/00 , C07F9/28 , C07F9/06 , C07F9/02 , C07F9/547 , C07F9/6506 , C07K5/08 , C07F9/30 , C07K5/06 , C07F9/6503 , C07F9/572 , A61K38/00
CPC分类号: C07K5/0827 , A61K38/00 , C07F9/301 , C07F9/303 , C07F9/572 , C07F9/5728 , C07F9/65031 , C07F9/6506 , C07K5/06191
摘要: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
摘要翻译: 本发明涉及一系列式I的取代的3-氨基丙烷次膦酸衍生物:其中R,R1,P1,P2和P3如本文所定义。 本发明的化合物可用于治疗各种疾病,包括但不限于抑郁,焦虑,某些精神症状,认知障碍和精神分裂症。
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公开(公告)号:US08183231B2
公开(公告)日:2012-05-22
申请号:US11552346
申请日:2006-10-24
申请人: Yong Mi Choi-Sledeski , Julian Levell , Gregory Bernard Poli , Mark Czekaj , Alan John Collis , Roy Vaz
发明人: Yong Mi Choi-Sledeski , Julian Levell , Gregory Bernard Poli , Mark Czekaj , Alan John Collis , Roy Vaz
IPC分类号: A61K31/675 , A61K31/66 , C07F9/30
CPC分类号: C07K5/0827 , A61K38/00 , C07F9/301 , C07F9/303 , C07F9/572 , C07F9/5728 , C07F9/65031 , C07F9/6506 , C07K5/06191
摘要: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
摘要翻译: 本发明涉及一系列式I的取代的3-氨基丙烷次膦酸衍生物:其中R,R1,P1,P2和P3如本文所定义。 本发明的化合物可用于治疗各种疾病,包括但不限于抑郁,焦虑,某些精神症状,认知障碍和精神分裂症。
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公开(公告)号:US06649620B2
公开(公告)日:2003-11-18
申请号:US10252852
申请日:2002-09-23
申请人: Alan John Collis , David Nathan Fox
发明人: Alan John Collis , David Nathan Fox
IPC分类号: C07D23994
CPC分类号: C07D401/04 , C07D239/95 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D471/04
摘要: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.
摘要翻译: 式I化合物,其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2表示任选被C 1-4烷基或SO 2 NH 2取代的芳基或杂芳基; R 3, 表示含有至少一个选自N,O和S的杂原子的4-,5-,6-或7-元杂环,所述环任选地与苯环稠合或含有5或6元杂环 至少一个选自N,O和S的杂原子,整个环系统任选被取代; X代表CH或N; 或不代表式Ia的环状基团,或表示式Ib的链和其药学上可接受的盐可用于治疗各种障碍,包括良性前列腺增生。
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公开(公告)号:US06417194B1
公开(公告)日:2002-07-09
申请号:US09499623
申请日:2000-02-07
IPC分类号: A61K3147
CPC分类号: C07D401/04 , C07D403/04 , C07D405/14
摘要: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally substituted); R4 represents a 4-, 5-, 6- or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.
摘要翻译: 式I化合物,其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2和R 3独立地表示H或C 1-6烷氧基(其任选被取代); R 4表示4-,5-,6-或 所述环任选地与苯环或5-或6-元杂环稠合,所述环系统作为整体任选被取代; X表示CH或N; 并且L不存在,或表示式Ia的环状基团,或表示式Ib的链及其药学上可接受的盐; 可用于治疗,特别是治疗良性前列腺增生。
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