Aminoalcohol derivatives
    2.
    发明授权
    Aminoalcohol derivatives 失效
    氨基醇衍生物

    公开(公告)号:US07629366B2

    公开(公告)日:2009-12-08

    申请号:US11304632

    申请日:2005-12-16

    IPC分类号: A61K31/44 C07D211/82

    摘要: The present invention relates to a compound formula [I]: wherein  ect., X is bond, —CH2—,  etc., Y is bond, —O—(CH2)n— (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

    摘要翻译: 本发明涉及化合物式[I]:其中,X为键,-CH 2 - 等,Y为键,-O-(CH 2)n - (其中n为1,2,3或 4)等,Z是氰基,四唑基等,R 1是氢,低级烷基等,R 2是氢或氨基保护基,R 3是氢或低级烷基,R 4是氢或低级烷基,R 5和 R8各自独立地为氢,卤素,羟基,低级烷基等,R6为氢,低级烷基等,R9为氢或低级烷基,i为1或2,或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

    Aminoalcohol derivatives
    3.
    发明申请
    Aminoalcohol derivatives 失效
    氨基醇衍生物

    公开(公告)号:US20060100252A1

    公开(公告)日:2006-05-11

    申请号:US11304632

    申请日:2005-12-16

    摘要: The present invention relates to a compound formula [I]: wherein ect., X is bond, —CH2—, etc., Y is bond, —O—(CH2)n— (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

    摘要翻译: 本发明涉及化合物式[I]:其中,X是键,-CH 2 - 等,Y是键,-O-(CH 2 CH 2) (其中n为1,2,3或4)等,Z为氰基,四唑基等,R 1为氢, 低级烷基等,R 2是氢或氨基保护基,R 3是氢或低级烷基,R 4是氢或 低级烷基,R 5和R 8各自独立地为氢,卤素,羟基,低级烷基等,R 6为氢,低级 烷基等,R 9是氢或低级烷基,i是1或2,或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

    Aminoalcohol derivatives
    4.
    发明授权
    Aminoalcohol derivatives 失效
    氨基醇衍生物

    公开(公告)号:US07037938B2

    公开(公告)日:2006-05-02

    申请号:US10603943

    申请日:2003-06-26

    IPC分类号: A61K31/195 C07C229/34

    摘要: The present invention relates to a compound formula [I]: wherein Y is bond, —O—(CH2)n— (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

    摘要翻译: 本发明涉及化合物式[I]:其中Y是键,-O-(CH 2)n - (其中n是1,2,3) 或4)等,Z是氰基,四唑基等,R 1是氢,低级烷基等,R 2是氢或氨基保护基 R 3是氢或低级烷基,R 4是氢或低级烷基,R 5和R 8, 各自独立地为氢,卤素,羟基,低级烷基等,R 6为氢,低级烷基等,R 9为氢或低级烷基,且i 为1或2,或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

    Aminoalcohol derivatives
    5.
    发明申请
    Aminoalcohol derivatives 失效
    氨基醇衍生物

    公开(公告)号:US20050137236A1

    公开(公告)日:2005-06-23

    申请号:US11016886

    申请日:2004-12-21

    摘要: The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

    摘要翻译: 本发明涉及化合物式[I]:其中X是键,-CH 2 - , - O-或-NH-,R 1和R 2 > 12个各自独立地为氢,卤素,低级烷基等,R 2为氢或任选取代的低级烷基,R 3为氢或氨基 保护基,R 4,R 5和R 6各自独立地为氢或任选取代的低级烷基,R 7 O 其中Z为键,等等,R 13为羧基,低级烷氧基羰基,(低级烷基磺酰基)氨基甲酰基或低级烷酰基氨磺酰基,R 0为 其中Y为键,-CH 2 - , - O - , - S-等,其中R为 - 低级烷基,环(低级)烷基等,R 11是氢,低级烷基,低级烷氧基等,或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

    Aminoalcohol derivatives
    6.
    发明授权
    Aminoalcohol derivatives 失效
    氨基醇衍生物

    公开(公告)号:US07417060B2

    公开(公告)日:2008-08-26

    申请号:US11016886

    申请日:2004-12-21

    IPC分类号: A61K31/44 A61K31/195

    摘要: The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

    摘要翻译: 本发明涉及化合物式[I]:其中X是键,-CH 2 - , - O-或-NH-,R 1和R 2 > 12个各自独立地为氢,卤素,低级烷基等,R 2为氢或任选取代的低级烷基,R 3为氢或氨基 保护基,R 4,R 5和R 6各自独立地为氢或任选取代的低级烷基,R 7 O 其中Z为键,等等,R 13为羧基,低级烷氧基羰基,(低级烷基磺酰基)氨基甲酰基或低级烷酰基氨磺酰基,R 0为 其中Y为键,-CH 2 - , - O - , - S-等,其中R为 - 低级烷基,环(低级)烷基等,R 11是氢,低级烷基,低级烷氧基等,或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

    4,5-diaryloxazole compounds
    8.
    发明授权
    4,5-diaryloxazole compounds 失效
    4,5-二碘唑化合物

    公开(公告)号:US06297267B1

    公开(公告)日:2001-10-02

    申请号:US09529405

    申请日:2000-04-26

    IPC分类号: A61K3142

    摘要: A compound of the formula: wherein R1 is a hydrogen atom or a carboxy protective group, R2, R5, R6 and R7 are each a hydrogen atom or a hydroxy group, R3 and R4 are each a hydrogen atom, or are combined together to form an epoxy group or a single bond. R8 and R9 are each an optionally substituted aryl group, and X is a single bond or a methylene group, in addition to the above definitions. R2 and R3 may be combined together to form a single bond; provided that when R2, R5, R6 and R7 are each a hydrogen atom, then R3 and R4 are combined together to form an epoxy group; when R3 and R4 are combined together to form a single bond, then at least one of R2, R5, R6 and R7 is a hydroxy group and the others are hydrogen; and when R3 and R4 are each a hydrogen atom, then at least one of R2, R5, R6 and R7 is a hydroxy group and the others are hydrogen, and X is a methylene group, or its salt.

    摘要翻译: 下式的化合物:其中R 1是氢原子或羧基保护基,R 2,R 5,R 6和R 7各自是氢原子或羟基,R 3和R 4各自是氢原子,或者组合在一起形成 环氧基或单键。 除上述定义之外,R 8和R 9各自为任选取代的芳基,X为单键或亚甲基。 R2和R3可以组合在一起形成单键; 条件是当R 2,R 5,R 6和R 7各自为氢原子时,则R 3和R 4组合在一起形成环氧基; 当R3和R4组合在一起形成单键时,R 2,R 5,R 6和R 7中的至少一个是羟基,而其余的是氢; 当R 3和R 4各自为氢原子时,R 2,R 5,R 6和R 7中的至少一个为羟基,其余为氢,X为亚甲基或其盐。

    Ornithine derivatives as prostaglandin e2 agonists or antagonists
    10.
    发明申请
    Ornithine derivatives as prostaglandin e2 agonists or antagonists 审中-公开
    鸟氨酸衍生物作为前列腺素e2激动剂或拮抗剂

    公开(公告)号:US20070142638A1

    公开(公告)日:2007-06-21

    申请号:US10584146

    申请日:2004-12-17

    IPC分类号: C07D215/38 C07D209/42

    摘要: Ornithine derivatives of the formula (I): wherein X is —CO— or —(CH2)k— (wherein k is 1, 2 or 3); Y is Z-(CH2)n—, and the like; {wherein Z is R1—CO—NR4—, and the like, (wherein R1 is aryl, and the like; and R4 is hydrogen, or lower alkyl); and n is 1, 2, 3, 4, 5 or 6}; R2 is aryl-(lower alkyl), and the like; R3 is -Q-R7, [wherein Q is —CO— or —SO2—, R is heterocyclyl], and the like; and R5 and R6 are independently hydrogen or lower alkyl; or a pharmaceutically acceptable salt thereof, which are useful as medicament.

    摘要翻译: 式(I)的鸟氨酸衍生物:其中X是-CO-或 - (CH 2 CH 2)n - (其中k是1,2或3); Y是Z-(CH 2)n - 等等; {其中Z是R 1 -CO-NR 4 - 等,(其中R 1是芳基等)和 R 4是氢或低级烷基); n为1,2,3,4,5或6}; R 2是芳基 - (低级烷基)等; R 3是-Q-R 7,[其中Q是-CO-或-SO 2 - ,R是杂环基]等; R 5和R 6独立地是氢或低级烷基; 或其药学上可接受的盐,其可用作药物。