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92 条记录 (耗时 0.037 秒)

    FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
    1.
    发明申请
    FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY 有权
    具有腺苷A2a受体拮抗剂活性的融合三聚体化合物

    公开(公告)号：US20120232086A1

    公开(公告)日：2012-09-13

    申请号：US13510094

    申请日：2010-11-12

    申请人： Joel M. Harris ,  Bernard R. Neustadt ,  Andrew W. Stampford

    发明人： Joel M. Harris ,  Bernard R. Neustadt ,  Andrew W. Stampford

    IPC分类号： A61K31/4985 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04 ,  A61P25/16 ,  A61P25/24

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.

    摘要翻译： 本发明涉及式（I）（本文中也称为“熔融三环化合物”）的某些稠合三环杂芳基环化合物，其中M，Q，U，W，X，Y，Z，R 1，R 2， 和R 3，环C和D如本文所述。 本发明还提供了包含至少一种熔融三环化合物的组合物，以及这些化合物在治疗中枢神经系统疾病或障碍如帕金森病中的用途。

    [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists
    5.
    发明授权
    [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists 有权
    [1,2,4] - 三唑双环腺苷A2a受体拮抗剂

    公开(公告)号：US07078408B2

    公开(公告)日：2006-07-18

    申请号：US10973642

    申请日：2004-10-26

    申请人： Bernard R. Neustadt ,  Hong Liu

    发明人： Bernard R. Neustadt ,  Hong Liu

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/24 ,  A61P25/16

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds having the structural formula Iwherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1–C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted-aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations

    摘要翻译： 具有结构式I的化合物，其中：n为0,1,2或3; A是C（R 1）或N; R 1和R 2是H，（C 1 -C 6 -C 6） - 烷基，卤素，CN或 -CF 3 N 3; X是-C（O） - ， - O - ， - SO 2 - 或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二基; Y是-O-，-SO 0-2 - 或任选取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有一定条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的 - 芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基; 其用于治疗帕金森病，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合的组分的试剂盒

    [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists
    6.
    发明授权
    [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists 有权
    Ä1,2,4'-三唑双环腺苷A2a受体拮抗剂

    公开(公告)号：US06875772B2

    公开(公告)日：2005-04-05

    申请号：US10304939

    申请日：2002-11-26

    申请人： Bernard R. Neustadt ,  Hong Liu

    发明人： Bernard R. Neustadt ,  Hong Liu

    IPC分类号： A61K31/519 ,  A61P25/00 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1-C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

    摘要翻译： 具有结构式I的化合物，其中n为0,1,2或3; A为C（R 1）或N; R 1和R 1a为H，（C 1 -C 6） - 烷基，卤代 ，CN或-CF 3; X是-C（O） - ， - O - ， - SO 2 2-或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二; Y是-O-，-SOO- 取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有某些条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基;它们用于治疗帕金森病，单独或与其它用于治疗帕金森病的药物组合，其包含它们的药物组合物和包含 组合。

    Benzimidazole compounds that are vitronectin receptor antagonists
    7.
    发明授权
    Benzimidazole compounds that are vitronectin receptor antagonists 失效
    作为玻连蛋白受体拮抗剂的苯并咪唑化合物

    公开(公告)号：US06204282B1

    公开(公告)日：2001-03-20

    申请号：US09450235

    申请日：1999-11-29

    申请人： Bernard R. Neustadt ,  Elizabeth M. Smith

    发明人： Bernard R. Neustadt ,  Elizabeth M. Smith

    IPC分类号： A61K314184

    CPC分类号： C07D235/14

    摘要： The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y1 each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, —CF3, and —C(O)OH; R1, R2, R3 and R4 are as defined herein; R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from H or C1-C3 alkyl; and wherein are positioned meta or para relative to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.

    摘要翻译： 本发明提供了具有式n，p，q和r各自独立地选自0或1的化合物; a，b，c和d各自独立地表示碳原子或氮原子，条件是不大于2个 a，b，c和d是氮原子; Y和Y1各自独立地表示1-4个选自烷基，烷氧基，卤素，-CF 3和-C（O）OH的任选取代基; R 1，R 2，R 3和R 4是 如本文所定义; R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12独立地选自H或C 1 -C 3烷基;并且其中相对于彼此定位为间位或对位;或其不可生物酯， 其可接受的盐。 还提供了使用这些化合物治疗玻连蛋白介导的病症例如癌症，视网膜病变，动脉粥样硬化，血管再狭窄和骨质疏松症的方法。