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    Ether derivatives having 5-lipoxygenase inhibitory activity
    1.
    发明授权
    Ether derivatives having 5-lipoxygenase inhibitory activity 失效
    具有5-脂氧合酶抑制活性的醚衍生物

    公开(公告)号：US5512594A

    公开(公告)日：1996-04-30

    申请号：US440132

    申请日：1995-05-12

    申请人： Thomas G. C. Bird ,  Graham C. Crawley ,  Michael S. Large ,  Patrick Ple

    发明人： Thomas G. C. Bird ,  Graham C. Crawley ,  Michael S. Large ,  Patrick Ple

    IPC分类号： A61K31/40 ,  A61K31/47 ,  A61K31/55 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D405/12 ,  C07D409/14 ,  C07D417/14 ,  C07D493/08 ,  A61K31/405 ,  C07D409/12

    CPC分类号： C07D405/12 ,  C07D409/14 ,  C07D417/14 ,  C07D493/08

    摘要： The invention concerns ether derivatives of the formula IQ.sup.1 -X-Ar-Q.sup.2 Iwherein Q.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; X is oxy, thio, sulphinyl or sulphonyl; Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl; and Q.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R.sup.2 is (1-4C)alkyl; and R.sup.3 is hydrogen or (1-4C)alkyl; or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

    摘要翻译： 本发明涉及式I Q1-X-Ar-Q2I的醚衍生物，其中Q1是含有一个或两个氮杂原子的任选取代的9,10或11元双环杂环部分，并任选地含有另外的选自氮， 氧和硫; X是氧基，硫基，亚磺酰基或磺酰基; Ar是任选取代的亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基，噻唑二基，恶唑二基，噻二唑二基或恶二唑二基。 和Q2选自式II和III的基团：其中R 1是氢，（2-5C）烷酰基或任选取代的苯甲酰基; R2是（1-4C）烷基; 并且R 3是氢或（1-4C）烷基; 或R 2和R 3连接形成亚甲基，亚乙烯基，亚乙基或三亚甲基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

    Ether derivatives having 5-lipoxygenase inhibitory activity
    2.
    发明授权
    Ether derivatives having 5-lipoxygenase inhibitory activity 失效
    具有5-脂氧合酶抑制活性的醚衍生物

    公开(公告)号：US5478842A

    公开(公告)日：1995-12-26

    申请号：US234148

    申请日：1994-04-28

    申请人： Thomas G. C. Bird ,  Graham C. Crawley ,  Michael S. Large ,  Patrick Ple

    发明人： Thomas G. C. Bird ,  Graham C. Crawley ,  Michael S. Large ,  Patrick Ple

    IPC分类号： A61K31/40 ,  A61K31/47 ,  A61K31/55 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D405/12 ,  C07D409/14 ,  C07D417/14 ,  C07D493/08 ,  C07D405/14

    CPC分类号： C07D405/12 ,  C07D409/14 ,  C07D417/14 ,  C07D493/08

    摘要： The invention concerns ether derivatives of the formula IQ.sup.1 --X--Ar--Q.sup.2 IwhereinQ.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;X is oxy, thio, sulphinyl or sulphonyl;Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazoiediyl, thiadiazoiediyl or oxadiazolediyl; andQ.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl;R.sup.2 is (1-4C)alkyl; andR.sup.3 is hydrogen or (1-4C)alkyl;or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

    摘要翻译： 本发明涉及式I Q1-X-Ar-Q2I的醚衍生物，其中Q1是含有一个或两个氮杂原子的任选取代的9,10或11元双环杂环部分，并任选地含有另外的选自氮， 氧和硫; X是氧基，硫基，亚磺酰基或磺酰基; Ar是任选取代的亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基，噻唑二基，恶唑二基，噻二唑基或恶二唑二基。 并且Q2选自式II和III的基团：其中R 1是氢，（2-5C）烷酰基或任选取代的苯甲酰基; R2是（1-4C）烷基; 并且R 3是氢或（1-4C）烷基; 或R 2和R 3连接形成亚甲基，亚乙烯基，亚乙基或三亚甲基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

    Oxime derivatives
    3.
    发明授权
    Oxime derivatives 失效
    肟衍生物

    公开(公告)号：US5482966A

    公开(公告)日：1996-01-09

    申请号：US240464

    申请日：1994-06-13

    申请人： Thomas G. C. Bird ,  Patrick Ple

    发明人： Thomas G. C. Bird ,  Patrick Ple

    IPC分类号： A61K31/425 ,  A61K31/505 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D239/42 ,  C07D307/20 ,  C07D309/08 ,  C07D309/10 ,  C07D317/22 ,  C07D405/04 ,  C07D409/02 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  A61K31/35 ,  A61K31/34

    CPC分类号： C07D405/04 ,  C07D307/20 ,  C07D309/10 ,  C07D317/22 ,  C07D409/04 ,  C07D417/04

    摘要： The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

    摘要翻译： 本发明涉及式I的肟衍生物，其中R 4包括氢，羧基，氨基甲酰基，氨基，氰基，三氟甲基，（1-4C）烷基氨基，二（1-4C）烷基氨基和（1-4C）烷基 ; R5包括氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，（2-5C）烷酰基，卤代 - （2-4C）烷基和羟基 - （2-4C）烷基; Ar1是亚苯基或杂芳基双基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基或杂芳基双基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起形成具有5或6个环原子的环，其中A2和A3各自为（1 -3C）亚烷基，X 2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

    Oxime derivatives
    4.
    发明授权
    Oxime derivatives 失效
    肟衍生物

    公开(公告)号：US5332757A

    公开(公告)日：1994-07-26

    申请号：US14564

    申请日：1993-02-08

    申请人： Thomas G. C. Bird ,  Patrick Ple

    发明人： Thomas G. C. Bird ,  Patrick Ple

    IPC分类号： A61K31/425 ,  A61K31/505 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D239/42 ,  C07D307/20 ,  C07D309/08 ,  C07D309/10 ,  C07D317/22 ,  C07D405/04 ,  C07D409/02 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  A61K31/35 ,  A61K31/34

    CPC分类号： C07D405/04 ,  C07D307/20 ,  C07D309/10 ,  C07D317/22 ,  C07D409/04 ,  C07D417/04

    摘要： The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

    摘要翻译： 本发明涉及式I的肟衍生物，其中R 4包括氢，羧基，氨基甲酰基，氨基，氰基，三氟甲基，（1-4C）烷基氨基，二（1-4C）烷基氨基和（1-4C）烷基 ; R5包括氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，（2-5C）烷酰基，卤代 - （2-4C）烷基和羟基 - （2-4C）烷基; Ar1是亚苯基或杂芳基双基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基或杂芳基双基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起形成具有5或6个环原子的环，其中A2和A3各自为（1 -3C）亚烷基，X 2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

    Quinazoline derivatives
    5.
    发明授权
    Quinazoline derivatives 失效
    喹唑啉衍生物

    公开(公告)号：US06806274B1

    公开(公告)日：2004-10-19

    申请号：US10019945

    申请日：2002-01-07

    申请人： Graham C Crawley ,  Laurent F A Hennequin ,  Darren McKerrecher ,  Patrick Ple ,  Jeffrey Philip Poyser ,  Christine M P Lambert

    发明人： Graham C Crawley ,  Laurent F A Hennequin ,  Darren McKerrecher ,  Patrick Ple ,  Jeffrey Philip Poyser ,  Christine M P Lambert

    IPC分类号： A61K31517

    CPC分类号： C07D231/12 ,  C07D215/54 ,  C07D233/56 ,  C07D239/94 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D487/04

    摘要： The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中Q 1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉环，或下式：Q 3 -X 1 - 的基团，其中 X 1包括直接键，O和Q 3包括芳基，芳基 - （1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R 2和R 3各自为氢或（1-6C）烷基; Z包括O，S和NH; 和Q 2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗温血动物中的T细胞介导的疾病或医学病症的药物中的用途。