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    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。

    Ether derivatives having 5-lipoxygenase inhibitory activity
    3.
    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。

    Hydroxylamine derivatives
    4.
    发明授权
    Hydroxylamine derivatives 失效
    羟胺衍生物

    公开(公告)号：US5334614A

    公开(公告)日：1994-08-02

    申请号：US59313

    申请日：1993-05-11

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/135 ,  A61K31/27 ,  A61K31/275 ,  A61K31/35 ,  A61K31/496 ,  A61K31/505 ,  A61P37/08 ,  A61P43/00 ,  C07C239/20 ,  C07D213/63 ,  C07D263/36 ,  C07D277/22 ,  C07D307/42 ,  C07D309/10 ,  C07D405/12 ,  C07D417/04 ,  A61K31/34 ,  C07D307/20

    CPC分类号： C07D405/12 ,  C07D309/10

    摘要： The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, cyclopentyl, cyclohexyl, tetrahydrofuran-3-yl, tetrahydropyran-4-yl, piperidin-4-yl, N-(1-4C)alkylpiperidin-4-yl, (2-5C)alkanoyl, (1-4C)alkylsulphonyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, phenyl, phenyl-(1-4C)alkyl, di-phenyl-(1-4C)alkyl, benzoyl, phenylsulphonyl or a heteroarylmethyl group;R.sup.5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;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, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (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 -wherein each of A.sup.2 and A.sup.3 is independently (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的羟胺衍生物，其中R 4是氢，氨基甲酰基，（1-4C）烷基，环戊基，环己基，四氢呋喃-3-基，四氢吡喃-4-基，哌啶-4-基，N （1-4C）烷基哌啶-4-基，（2-5C）烷酰基，（1-4C）烷基磺酰基，N-（1-4C）烷基氨基甲酰基，N，N-二（1-4C）烷基氨基甲酰基，苯基， 苯基 - （1-4C）烷基，二 - 苯基 - （1-4C）烷基，苯甲酰基，苯基磺酰基或杂芳基甲基; R5是氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，氰基 - （1-4C）烷基，苯基或苯基 - （1-4C）烷基; A4是（1-4C）亚烷基; Ar1是亚苯基，吡啶二基或嘧啶二基; 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，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; R1为氢，（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，其中A2和A3各自独立地为（1-3C）亚烷基，X2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。

    Oxides of 1,2,5-thiadiazoles, their use in pharmaceutical compositions
    5.
    发明授权
    Oxides of 1,2,5-thiadiazoles, their use in pharmaceutical compositions 失效
    1,2,5-噻二唑的氧化物，它们在药物组合物中的用途

    公开(公告)号：US4746672A

    公开(公告)日：1988-05-24

    申请号：US376395

    申请日：1982-05-10

    申请人： Tobias O. Yellin ,  Philip N. Edwards ,  Michael S. Large

    发明人： Tobias O. Yellin ,  Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/425 ,  A61P1/04 ,  A61P43/00 ,  C07D417/12 ,  A61K31/41

    CPC分类号： C07D417/12

    摘要： Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R.sup.3 is a variety of radicals described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes for the derivatives, intermediates and pharmaceutical compositions are also part of the invention.

    摘要翻译： 作为组胺H-2拮抗剂的硫衍生物，其抑制式I的胃酸分泌：其中R1和R2独立地为氢或1-10C烷基，3-8C环烷基或4-14C环烷基烷基，每个烷基 任选地携带一个或多个F，Cl或Br原子的环烷基或环烷基烷基，条件是R 1和R 2中的一个是卤素取代的; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基或1-8C亚烷基链，其中任选地插入一个或两个基团; p为1或2; R3是说明书中描述的各种基团; 及其药学上可接受的酸加成盐。 衍生物，中间体和药物组合物的制备方法也是本发明的一部分。

    Pyrrolidine derivatives
    6.
    发明授权
    Pyrrolidine derivatives 失效
    吡咯烷衍生物

    公开(公告)号：US5420298A

    公开(公告)日：1995-05-30

    申请号：US114187

    申请日：1993-09-01

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/40 ,  A61K31/4025 ,  A61K31/425 ,  A61K31/47 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D207/12 ,  C07D401/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D207/06 ,  C07D207/14

    CPC分类号： C07D401/12 ,  C07D207/12 ,  C07D409/12

    摘要： The invention concerns pyrrolidine derivatives of the formula ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl, naphthyl or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A is a direct link to the group X or A is (1-4C)alkylene;X is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, halogeno-(1-4C)alkyl, halogeno-(2-4C)alkenyl, halogeno-(2-4C)alkynyl, (1-4C)alkoxy-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, carboxy-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl or N,N-di-(1-4C)alkylcarbamoyl-(1-4C)alkyl; andn is 1 or 2 and each R.sup.3 is independently hydrogen, hydroxy, (1-4C)alkyl or (1-4C)alkoxy;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Ia的吡咯烷衍生物，其中Ar1是任选取代的苯基，萘基或含有一个或两个氮杂原子并且任选地含有另外选自氮，氧和硫的杂原子的10元双环杂环部分; A是直接连接到基团X或A是（1-4C）亚烷基; X是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; R2是（1-4C）烷基，（2-4C）烯基，（2-4C）炔基，卤代 - （1-4C）烷基，卤代 - （2-4C）烯基，卤代 - （2-4C） （1-4C）烷基，（2-4C）烷基，氰基 - （1-4C）烷基，羧基 - （1-4C）烷基，氨基甲酰基 - （1-4C） （1-4C）烷氧基羰基 - （1-4C）烷基，N-（1-4C）烷基氨基甲酰基 - （1-4C）烷基或N，N-二（1-4C）烷基氨基甲酰基 - （1-4C）烷基; 并且n为1或2，并且每个R 3独立地为氢，羟基，（1-4C）烷基或（1-4C）烷氧基; 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。

    Naphtho(2,1-b) furan derivatives
    9.
    发明授权
    Naphtho(2,1-b) furan derivatives 失效
    萘酚（2,1-b）呋喃衍生物

    公开(公告)号：US4916148A

    公开(公告)日：1990-04-10

    申请号：US267319

    申请日：1988-11-04

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/443 ,  A61K31/50 ,  A61P3/00 ,  C07D405/06 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06

    摘要： Naphtho[2,1-b]furan derivatives of the formula: ##STR1## wherein R.sup.1 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 3-pyridyl or 5-pyrimidinyl radical or a 1H-imidazol-1-yl radical optionally substituted in the 5-position by a 1-6C alkyl or halogenoalkyl radical;R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen or deuterium atom, a cyano radical, a 1-6C alkyl or halogenoalkyl radical, a phenyl radical optionally substituted by halogen, or one of R.sup.2 and R.sup.3 is a radical of the formula R.sup.1 as defined above, and the other is hydrogen;R.sup.4 and R.sup.5, which may be the same or different, are each a 1-2C alkyl, deuterioalkyl or halogenoalkyl radical;or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached form a 3-6C cycloalkyl radical;R.sup.6 and R.sup.7, which may be the same or different, are each a hydrogen or halogen atom, an amino, carboxy, carbamoyl, cyano, 1-cyano-1-methylethyl or nitro radical, a 1-6C alkyl or halogenoalkyl radical, a mono- or di-(1-6C)alkylcarbamoyl radical, a mono- or di-(1-6C)halogenoalkylcarbamoyl radical, a group of the formula --COR.sup.8, --SO.sub.n R.sup.8 or --OR.sup.8, in which n is 0, 1 or 2 and R.sup.8 is a 1-6C alkyl or halogenoalkyl radical, or a benzoyl radical optionally substituted by halogen;one of R.sup.9 and R.sup.10 is hydrogen and the other is a hydroxy or 1-6C alkoxy radical, or R.sup.9 and R.sup.10 together form an oxo radical;and the pharmaceutically acceptable acid addition salts thereof; processes for their manufacture; and pharmaceutical compositions containing them.

    Haloguanidine intermediates
    10.
    发明授权
    Haloguanidine intermediates 失效
    卤代中间体

    公开(公告)号：US4762932A

    公开(公告)日：1988-08-09

    申请号：US869615

    申请日：1986-06-02

    申请人： Tobias O. Yellin ,  Philip N. Edwards ,  Michael S. Large

    发明人： Tobias O. Yellin ,  Philip N. Edwards ,  Michael S. Large

    IPC分类号： C07D251/16 ,  C07C279/18 ,  C07C323/44 ,  C07C335/28 ,  C07D209/48 ,  C07D213/74 ,  C07D213/75 ,  C07D231/38 ,  C07D231/40 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D241/20 ,  C07D251/18 ,  C07D277/20 ,  C07D277/42 ,  C07D277/48 ,  C07D285/08 ,  C07D403/12 ,  C07D417/12 ,  G09F13/04 ,  C07D277/04

    CPC分类号： C07D209/48 ,  C07C323/44 ,  C07C335/28 ,  C07D213/75 ,  C07D231/40 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D241/20 ,  C07D251/18 ,  C07D277/48 ,  C07D285/08

    摘要： Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Processes for producing compounds of formula (I), pharmaceutical compositions containing them, methods of utilizing such compositions and intermediates useful for synthesizing compounds of formula (I) are also described.

    摘要翻译： 本发明涉及下式的胍：其中R 1和R 2为H，C 1-10烷基，C 3-8环烷基或环烷基烷基，其中烷基部分为C 1-6 并且环烷基部分为C3-8，烷基，环烷基和环烷基烷基中的每一个任选被一个或多个选自F，Cl和Br的卤素取代，条件是R 1和R 2中的至少一个为 卤素取代的烷基，环烷基或环烷基 - 烷基，条件是在直接与氮连接的碳上不存在卤素取代基;环X是携带1或2个任选的取代基或含有1或2个任选取代基的5-或6-元杂环芳环的苯基 ，选自O，N和S的2或3个杂原子，该杂环可以携带选自F，Cl，Br，I，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，三氟甲基 ，羟基和氨基; ... Y是O，S，直接键，亚甲基，亚乙烯基，SO或NR 4，其中R 4是H或C 1-6烷基; m是0-4， n为1至5，条件是当Y为O，SO或NR 4时，n为2至5; R 3具有各种含义; ...及其药学上可接受的酸加成盐。 还描述了制造方法和药物组合物。