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    Thiazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
    3.
    发明授权
    Thiazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes 失效
    可用作PDE4同功酶抑制剂的噻唑基酰胺衍生物

    公开(公告)号：US06559168B2

    公开(公告)日：2003-05-06

    申请号：US10062145

    申请日：2002-01-31

    申请人： Anthony Marfat ,  Michael William McKechney

    发明人： Anthony Marfat ,  Michael William McKechney

    IPC分类号： C07D41710

    CPC分类号： C07D417/12 ,  C07D277/56

    摘要： This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recited, optionally one carbon atom of said carbon ring system may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; E is selected from: and all other substituents shown above are as defined in the specification.

    摘要翻译： 本申请涉及可用作PDE4抑制剂的化合物，用于治疗由下列通式的嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺疾病的活化和脱颗粒调节的疾病，其中Y = C（R 1a） - 或 - [Nsquare（O）k] - 其中k是0或1; G 1是饱和或不饱和的碳环体系，其是3-至7-元单环，或者是7-12元稠合多环 ; 条件是G1不是如G2定义的不连续或限制性的联芳基部分; 其中任选地一个碳原子可以被选自N，O和S的杂原子取代; 其中任选地，其第二个碳原子和其另外任选的第三个碳原子可以被N取代; -G2是饱和或不饱和的碳环体系，其为3-至7-元单环; 或者是7-12元稠合的多环; 或者是7至18元不连续或限制性的联芳基部分; 其中对于所述碳环体系中的每一个，所述碳环体系的任选一个碳原子可被选自N，O和S的杂原子代替; 其中任选地，其第二个碳原子和其另外任选的第三个碳原子可以被N取代; E选自：和上述所有其它取代基如说明书中所定义。

    Indazole bioisostere replacement of catechol in therapeutically active compounds
    4.
    发明授权
    Indazole bioisostere replacement of catechol in therapeutically active compounds 失效
    吲唑生物电子替代治疗活性化合物中的儿茶酚

    公开(公告)号：US06391872B1

    公开(公告)日：2002-05-21

    申请号：US09381425

    申请日：1999-09-20

    申请人： Anthony Marfat

    发明人： Anthony Marfat

    IPC分类号： A61K314155

    CPC分类号： C07D231/56

    摘要： Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I1) or (I2): or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment RC is hydrogen; RA is cyclohexyl; and RB is ethyl. Ra and Rb are each individually and independently hydrogen or non-catechol substituents of said compounds resulting directly from an indazole-for-catechol bioisostere replacement of said catechol-containing compound having said therapeutic activity, where said non-catechol substituents are the same or homologous before and after said replacement, provided that both of Ra and Rb cannot be hydrogen at the same time. The therapeutic activity involved may comprise cholinesterase inhibitory activity, adrenergic &agr;1-antagonist and &bgr;1-agonist activity, calcium channel inhibitory activity, antineoplastic activity, and phosphodiesterase type IV inhibitory activity.

    摘要翻译： 描述了物质及其成员物质的治疗活性组合物，其包含含吲唑的化合物，所述化合物及其直接由具有相同治疗活性的含儿茶酚的化合物的吲唑类邻苯二酚生物电子替代产生的治疗活性， 邻苯二酚取代基在所述置换之前和之后是相同或同源的，并且其中所述物质组合物包含式（I 1）或（I 2）的化合物或其药学上可接受的盐，其中在优选的实施方案中，RC为氢; RA为环己基; 而RB是乙基。 R a和R b各自独立地和独立地是所述化合物的氢或非邻苯二酚取代基，其直接由具有所述治疗活性的所述含儿茶酚的化合物的吲唑 - 邻苯二酚生物电子替代物取代，其中所述非邻苯二酚取代基相同或同源 在所述替换之前和之后，条件是Ra和Rb两者不能同时为氢。 所涉及的治疗活性可包括胆碱酯酶抑制活性，肾上腺素能α1-拮抗剂和β1-激动剂活性，钙通道抑制活性，抗肿瘤活性和磷酸二酯酶IV抑制活性。

    Substituted indazole derivatives and related compounds
    5.
    发明授权
    Substituted indazole derivatives and related compounds 失效
    取代的吲唑衍生物和相关化合物

    公开(公告)号：US06211222B1

    公开(公告)日：2001-04-03

    申请号：US08963904

    申请日：1997-11-04

    申请人： Anthony Marfat

    发明人： Anthony Marfat

    IPC分类号： A61K31415

    CPC分类号： C07D231/56 ,  C07D409/08

    摘要： The invention relates to compounds of the formula I and pharmaceutically acceptable salts thereof, wherein R2a and R2b are independently selected from the group consisting essentially of hydrogen and hereinafter recited substituents, provided that one, but not both of R2a and R2b must be independently selected as hydrogen, wherein said substituents comprise: wherein the dashed lines in formulas (Ia) and (Ib) independently and optionally represent a single or double bond, provided that in formula (Ia) both dashed lines cannot both represent double bonds at the same time; and R, R1, R3, R4, R5, R6, R7, R18 and m are as defined. The invention further relates to intermediates for the preparation of the compounds of formula I, and to pharmaceutical compositions containing, and methods of using, the compounds of formula I, or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.

    摘要翻译： 本发明涉及式I化合物及其药学上可接受的盐，其中R 2a和R 2b独立地选自氢和下文所述的取代基，条件是R 2a和R 2b之一必须独立地选自氢， 其中所述取代基包括：其中式（Ia）和（Ib）中的虚线独立地且任选地表示单键或双键，条件是在式（Ia）中，两条虚线不能同时表示双键; R，R 1，R 3，R 4，R 5，R 6，R 7，R 18和m如上所定义。 本发明还涉及用于制备式I化合物的中间体，以及含有式I化合物或其可接受的盐用于抑制IV型磷酸二酯酶（PDE）或其制备方法的药物组合物和 在哺乳动物中产生肿瘤坏死因子（TNF）。