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11 条记录 (耗时 0.031 秒)

    [1,2,4]-Triazolo[1,5-a]and pyrazolo[2,3-a][1,3,5]triazine derivatives
    1.
    发明授权
    [1,2,4]-Triazolo[1,5-a]and pyrazolo[2,3-a][1,3,5]triazine derivatives 失效
    [1,2,4]三唑并[1,5-a]和吡唑并[2,3-a] [1,3,5]三嗪衍生物

    公开(公告)号：US5270311A

    公开(公告)日：1993-12-14

    申请号：US708265

    申请日：1991-05-28

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/08 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  A61P43/00 ,  C07D487/04 ,  C07D403/14

    CPC分类号： C07D487/04

    摘要： The invention concerns novel, pharmaceutically useful compounds of formula I in which Q is a 5-membered heteroaryl optionally bearing 1 or 2 substituents independently selected from (1-4C)alkyl and halogeno;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is hydrogen, (3-12C)cycloalkyl, (3-6C)alkenyl, phenyl(3-6C)alkenyl, tetrafluorophenyl, pentafluorophenyl, 5- or 6-membered heteroaryl, optionally substituted (1-6C)alkyl or optionally substituted phenyl;X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a 4 to 6-membered saturated heterocyclic ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists. The invention further provides novel intermediates useful in the manufacture of the compounds of formula I. ##STR1##

    Heterocyclic compounds
    2.
    发明授权
    Heterocyclic compounds 失效

    公开(公告)号：US5246932A

    公开(公告)日：1993-09-21

    申请号：US887211

    申请日：1992-05-21

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D487/04 ,  C07D519/00

    CPC分类号： C07D519/00

    摘要： A compound of the formula I ##STR1## wherein: A.sup.1 and A.sup.2 are each independently N or CT in which T is hydrogen or (1-4C)alkyl;R.sup.1 and R.sup.2 are each independently hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;X.sup.1 and X.sup.2 are each independently O, S or NH; andL is a (3-7C)cycloalkylene group or a (1-8C)alkylene chain optionally interrupted or extended by a group selected from phenylene, phenyleneoxy or oxyphenyleneoxy, the phenylene portion of said group being unsubstituted or substituted by one of halogen, hydroxy and (1-4C)alkoxy, provided that all heteroatoms in the group X.sup.1 --L--X.sup.2 are separated from one another by at least two carbon atoms; or a pharmaceutically acceptable salt thereof, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

    Azole derivatives
    3.
    发明授权
    Azole derivatives 失效
    唑衍生物

    公开(公告)号：US5290776A

    公开(公告)日：1994-03-01

    申请号：US886798

    申请日：1992-05-21

    申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

    IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  C07D487/04 ,  C07D405/14 ,  A51K31/53

    CPC分类号： C07D487/04

    摘要： A compound of the formula I ##STR1## wherein: R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is phenyl, a C-linked aromatic 5- or 6-membered heterocyclic ring containing one of oxygen and sulphur and/or one or two nitrogen, or (1-8C)alkyl, alkenyl or alkynyl unsubstituted or substituted by a phenyl or a C-linked aromatic 5- or 6-membered heterocylic ring containing one of oxygen and sulphur and/or one or two nitrogen, any phenyl being unsubstituted or substituted by one, two or three of (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, hydroxy, benzyloxy and (1-5C)alkanoyloxy;A is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof, processes for the manufacture of the compounds, and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

    摘要翻译： 式I化合物（*化学结构*）Ⅰ其中：R1为氢，（1-6C）烷基或（1-4C）烷酰基; R2是苯基，含有氧和硫之一和/或一个或两个氮的C-连接的芳香族5-或6-元杂环，或未被取代或被苯基取代或（1-8C）烷基， 含有一个氧和硫和/或一个或两个氮的C连接的芳族5-或6-元杂环，任何未被取代或被一个，两个或三个（1-4C）烷基取代的苯基（1-4C ）烷氧基，卤素，三氟甲基，羟基，苄氧基和（1-5C）烷酰氧基; A是N或CT，其中T是氢或（1-4C）烷基; 或其药学上可接受的盐，用于制备化合物的方法和含有它们的药物组合物。 这些化合物可用作腺苷拮抗剂。

    1,3-Dioxan-5-ylalkenoic acids
    6.
    发明授权
    1,3-Dioxan-5-ylalkenoic acids 失效
    1,3-二恶烷-5-基链烯酸

    公开(公告)号：US4567197A

    公开(公告)日：1986-01-28

    申请号：US492247

    申请日：1983-05-06

    申请人： Andrew G. Brewster ,  Peter W. R. Caulkett

    发明人： Andrew G. Brewster ,  Peter W. R. Caulkett

    IPC分类号： C07D319/06 ,  A61K31/335 ,  A61K31/35 ,  A61K31/357 ,  A61K31/36 ,  A61P7/02 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C20060101 ,  C07C59/48 ,  C07C69/732 ,  C07D309/06 ,  C07D317/54 ,  C07D319/04 ,  C07D319/08 ,  C07D325/00 ,  C07D407/04 ,  C07D407/10 ,  C07D413/06

    CPC分类号： C07D319/08 ,  C07D319/06 ,  C07D407/04

    摘要： The invention concerns novel 4-phenyl-1,3-dioxan-5-ylalkenoic acid derivatives of the formula I having cis relative stereochemistry at positions 4 and 5 of the dioxane ring and wherein Ra and Rb are variously hydrogen, alkyl, halogenoalkyl, alkenyl, and optionally substituted aryl or arylalkyl, Rc is hydroxy, alkoxy or alkanesulphonamido, n is 1 or 2, A is ethylene or vinylene, Y is (2-5C)polymethylene optionally substituted by alkyl, and benzene ring B is optionally substituted phenyl, or, when Rc is hydroxy, a salt thereof. The acid derivatives antagonize one or more of the actions of thromboxane A.sub.2 (TXA.sub.2) and are expected to be of value in those disease conditions in which TXA.sub.2 is involved. The invention also provides pharmaceutical compositions containing an acid derivative of formula I, and processes for their chemical production.

    摘要翻译： 本发明涉及式I的4-苯基-1,3-二恶烷-5-基亚烯基酸衍生物，其在二恶烷环的4和5位具有顺式相对立体化学，其中Ra和Rb分别为氢，烷基，卤代烷基，烯基 和任选取代的芳基或芳基烷基，R c是羟基，烷氧基或烷基磺酰胺基，n是1或2，A是亚乙基或亚乙烯基，Y是任选被烷基取代的（2-5C）聚亚甲基，苯环B是任选取代的苯基， 或当Rc为羟基时，其盐。 酸衍生物拮抗血栓素A2（TXA2）的一种或多种作用，并且预期在涉及TXA2的那些疾病状况下具有价值。 本发明还提供含有式I酸衍生物的药物组合物及其化学生产方法。

    Heterocyclic derivatives as inhibitors of factor Xa
    7.
    发明授权
    Heterocyclic derivatives as inhibitors of factor Xa 失效
    杂环衍生物作为因子Xa的抑制剂

    公开(公告)号：US06723723B1

    公开(公告)日：2004-04-20

    申请号：US09913071

    申请日：2001-11-15

    申请人： Peter W. R. Caulkett

    发明人： Peter W. R. Caulkett

    IPC分类号： C07D40114

    CPC分类号： C07D401/14

    摘要： The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, of formula (I) wherein: A is an optionally substituted 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms selected from oxygen, nitrogen and sulphur atoms; which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to phaautical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

    摘要翻译： 本发明涉及式（I）的杂环衍生物或其药学上可接受的盐，其中：A是任选取代的含有1,2或3个选自氧，氮和硫的环杂原子的5-或6-元单环芳环 原子 其具有抗血栓和抗凝血性质，因此可用于治疗人或动物的方法。 本发明还涉及制备杂环衍生物的方法，含有它们的航空组合物及其在制备用于制备抗血栓形成或抗凝血作用的药物中的用途。