Substituted propane phosphinic acid esters
    2.
    发明授权
    Substituted propane phosphinic acid esters 有权
    取代的丙烷次膦酸酯

    公开(公告)号:US07687540B2

    公开(公告)日:2010-03-30

    申请号:US11775547

    申请日:2007-07-10

    IPC分类号: A61K31/34 C07F9/28

    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。

    Quinoline and quinazoline compounds useful in therapy
    4.
    发明授权
    Quinoline and quinazoline compounds useful in therapy 失效
    喹啉和喹唑啉化合物可用于治疗

    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

    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。

    Quinoline and quinazoline compounds useful in therapy
    5.
    发明授权
    Quinoline and quinazoline compounds useful in therapy 失效
    喹啉和喹唑啉化合物可用于治疗

    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

    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。

    Quinoline and quinazoline compounds useful in therapy
    9.
    发明授权
    Quinoline and quinazoline compounds useful in therapy 失效
    喹啉和喹唑啉化合物可用于治疗

    公开(公告)号:US06649620B2

    公开(公告)日:2003-11-18

    申请号:US10252852

    申请日:2002-09-23

    IPC分类号: C07D23994

    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。

    Quinolines and quinazolines useful in therapy
    10.
    发明授权
    Quinolines and quinazolines useful in therapy 失效
    喹啉和喹唑啉可用于治疗

    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

    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。