2,3,4-cyclopentan-2,3,4-triol-1-yl compounds
    5.
    发明授权
    2,3,4-cyclopentan-2,3,4-triol-1-yl compounds 失效
    2,3,4-环戊烷-2,3,4-三醇-1-基化合物

    公开(公告)号:US06844348B2

    公开(公告)日:2005-01-18

    申请号:US10399748

    申请日:2001-11-07

    CPC classification number: C07D487/04 A61K31/519

    Abstract: The invention provides a compound of formula (I): wherein R1 is alkyl C1-6 or alkenyl C2-6, both independently optionally substituted by one or more groups selected from alkyl C1-5 or halogen; R2 is cycloalkyl C3-8, optionally substituted by R3; R3 is phenyl, optionally substituted by one or more groups selected from alkyl C1-6 or halogen; R4 and R5 are alkyl C1-6 or together cycloalkyl C3-6. These compounds are useful for the treatment of stable and unstable angina.

    Abstract translation: 本发明提供式(I)的化合物:其中R 1为烷基C 1-6或烯基C 2-6,两者独立地任选被一个或多个选自烷基C 1-5或卤素的基团取代; R 2是任选被R 3取代的环烷基C3-8; R 3是任选被一个或多个选自烷基C 1-6或卤素的基团取代的苯基; R 4和R 5是烷基C 1-6或环烷基C 3-6。 这些化合物可用于治疗稳定和不稳定的心绞痛。

    Thienopyridazinones and their use in modulation of autoimmune disease
    6.
    发明申请
    Thienopyridazinones and their use in modulation of autoimmune disease 失效
    噻吩并哒嗪酮及其在调节自身免疫性疾病中的应用

    公开(公告)号:US20060135539A1

    公开(公告)日:2006-06-22

    申请号:US10542457

    申请日:2004-01-15

    CPC classification number: C07D495/04

    Abstract: The invention relates to thienopyridazinones compound of formula (I) wherein: R1, R2 and Q are as defined in the specification, and Ar and Ar2 are selected from certain aromatic ring systems which may be optionally substituted, as defined in the specification. Processes for the preparation of compounds of formula (I), pharmaceutical compositions containing them and their use in therapy is also described and claimed.

    Abstract translation: 本发明涉及式(I)的噻吩并哒嗪酮化合物,其中:R 1,R 2和Q如说明书中所定义,Ar和Ar 2, 选自某些芳族环系统,其可以任选地被取代,如说明书中所定义的。 还描述和要求保护制备式(I)化合物的方法,含有它们的药物组合物及其在治疗中的用途。

    Novel compounds
    7.
    发明申请
    Novel compounds 失效
    新型化合物

    公开(公告)号:US20060052380A1

    公开(公告)日:2006-03-09

    申请号:US10542194

    申请日:2004-01-15

    CPC classification number: C07D495/04

    Abstract: The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.

    Abstract translation: 本发明涉及式(I)的噻吩并哒嗪酮:其中:R 1是C 1-6烷基,C 2-6链烯基或C 任选被C 1-6烷基取代的,任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G,其中G是含有氮原子的5-或6-元环,和选自氧和/ 硫邻近氮,并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5,其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮,氧和硫的杂原子的5至10元单环或双环芳族环系统,所述环系统如上所述被任选地取代 在本说明书及其药学上可接受的盐和溶剂化物中。 还描述了其制备方法,含有它们的药物组合物及其在治疗中的用途,特别是在调节自身免疫疾病中

    Thienopyriminediones and their use in the modulation of autoimmune disease
    10.
    发明申请
    Thienopyriminediones and their use in the modulation of autoimmune disease 有权
    噻吩并嘧啶及其在调节自身免疫性疾病中的应用

    公开(公告)号:US20060052400A1

    公开(公告)日:2006-03-09

    申请号:US10542197

    申请日:2004-01-15

    Applicant: Simon Guile

    Inventor: Simon Guile

    CPC classification number: C07D495/04

    Abstract: The invention relates to thienopyrimidinediones of formula (1) wherein R1 and R2 each independently represent a C1-6akyl, C3-6alkyl, C3-6alkenyl, C3-5cycloalkylC1-3alkyl or C3-6cycloalkyl; each of which may be optionally substituted by 1 to 3 halogen atoms R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen; the ring being substituted by at least one group as defined in the specification, Q is CR4R5 where R4 is hydrogen, fluorine or C1-6 alkyl and R5 is hydrogen, fluorine or hydroxy; and Ar is a 5-10-membered aromatic ring system wherein up to 4 ring atoms may be heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted by one or more groups defined in the specification; as well as pharmaccutically acceptable salts and solvates thereof. Processes for their preparation of the compounds, pharmaceutical compositions containing them and their use in therapy, in particular in immunosuppressive therapy are also described.

    Abstract translation: 本发明涉及式(1)的噻吩并嘧啶二酮,其中R 1和R 2各自独立地表示C 1-6烷基,C 3-6个环烷基; 其中每个可以被1至3个卤素原子任选取代。R 3是基团CO-G或SO 2 -G,其中G是5-或6-元 环,其含有氮原子和与氮相邻的选自氧和硫的第二杂原子; 该环被说明书中定义的至少一个基团取代,Q是CR 4,其中R 4是氢,氟或 C 1-6烷基和R 5是氢,氟或羟基; 并且Ar是5-至10-元芳族环系统,其中至多4个环原子可以是独立地选自氮,氧和硫的杂原子,该环系统任选被说明书中定义的一个或多个基团取代; 以及其药学上可接受的盐和溶剂化物。 还描述了它们制备化合物的方法,含有它们的药物组合物及其在治疗中的用途,特别是在免疫抑制治疗中的用途

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