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    Thiadizines
    2.
    发明授权
    Thiadizines 失效

    公开(公告)号：US4423045A

    公开(公告)日：1983-12-27

    申请号：US321899

    申请日：1981-11-16

    申请人： David Brown ,  Robert I. Dowell ,  Rodney B. Hargreaves ,  Brian G. Main

    发明人： David Brown ,  Robert I. Dowell ,  Rodney B. Hargreaves ,  Brian G. Main

    IPC分类号： C07D417/04 ,  A61K31/53 ,  A61K31/535 ,  A61K31/54 ,  A61P9/04 ,  A61P9/08 ,  C07C327/38 ,  C07D253/06 ,  C07D273/04 ,  C07D285/16 ,  C07D285/18 ,  C07D295/084 ,  C07D295/194 ,  C07D317/00 ,  C07D417/02

    CPC分类号： C07D253/06 ,  C07C255/00 ,  C07D273/04 ,  C07D285/16 ,  C07D295/092 ,  C07D295/194 ,  Y10S514/929

    摘要： Novel heterocyclic compounds of the formula: ##STR1## wherein either X is --CR.sup.1 R.sup.2 -- and Y is oxygen, sulphur or --NR.sup.3, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or --NH-- and Y is --CH.sub.2 --; wherein R.sup.4 and R.sup.5, which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in claim 1, provided that R.sup.4 and R.sup.5 are not both hydrogen; or wherein R.sup.4 and R.sup.5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate.These compounds possess cardiotonic properties, and some of them possess peripheral vasodilator properties, and they are useful for the treatment of acute or chronic heart failure. Representative of the compounds is N,N-dimethyl-p-(5,6-dihydro-5-oxo-4H-1,3,4-thiadiazin-2-yl)benzamide. Also disclosed are processes for the manufacture of the compounds and pharmaceutical compositions containing them.

    摘要翻译： 下式的新型杂环化合物：其中X为-CR 1 R 2 - 且Y为氧，硫或-NR 3，其中R 1，R 2和R 3可以相同或不同，各自为氢或直至 4个碳原子; 或X是氧，硫或-NH-，Y是-CH 2 - ; 其中R4和R5可以相同或不同，各自为氢，氰基，硝基，氨基或羟基或至多4个碳原子的烷硫基，或具有权利要求1中定义的各种其它含义，条件是R4和R5为 不是氢; 或其中R4和R5连接在一起，使得与苯环A形成如权利要求1所定义的苯并杂环; 其中苯环A可任选地具有一个或多个其它取代基; 或其盐。 这些化合物具有强心性质，其中一些具有外周血管扩张剂特性，可用于治疗急性或慢性心力衰竭。 化合物的代表是N，N-二甲基 - 对 - （5,6-二氢-5-氧代-4H-1,3,4-噻二嗪-2-基）苯甲酰胺。 还公开了制备含有它们的化合物和药物组合物的方法。

    Heterocyclic 5-lipoxygenase inhibitors
    5.
    发明授权
    Heterocyclic 5-lipoxygenase inhibitors 失效
    杂环5-脂氧合酶抑制剂

    公开(公告)号：US5276037A

    公开(公告)日：1994-01-04

    申请号：US45725

    申请日：1993-04-14

    申请人： Robert I. Dowell ,  Philip N. Edwards ,  Keith Oldham

    发明人： Robert I. Dowell ,  Philip N. Edwards ,  Keith Oldham

    IPC分类号： A61K31/35 ,  A61K31/351 ,  A61K31/40 ,  A61P29/00 ,  A61P37/08 ,  C07D309/10 ,  C07D309/12 ,  C07D405/10 ,  C07D405/12 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/10 ,  C07D405/12

    摘要： The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.3 is oxy, thio, sulphinyl or sulphonyl;which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.

    摘要翻译： 本发明涉及式I的芳基衍生物，其中Ar 1为任选取代的苯基，萘基或杂环部分，X 1为氧基，硫基，亚磺酰基，磺酰基，二氟亚甲基，亚氨基，（1-4C）烷基亚氨基或 任选取代的（1-4C）亚烷基，或X1是式-X4-CR2-或-CR2-X4-的基团，其中X4是氧基，硫基，亚磺酰基，磺酰基或羰基，每个R是氢，甲基或乙基; Ar 2和Ar 3各自为任选取代的亚苯基; X2是氧基，硫基，亚磺酰基或磺酰基; R1是（1-4C）烷基; 并且R2和R3一起形成式-A1-X3-A2-的基团，其与A1和A2所连接的碳原子一起定义为具有5至7个环原子的环，其中A1和A2各自为（1 -3C）亚烷基，X 3为氧基，硫基，亚磺酰基或磺酰基; 哪些化合物是5-脂氧合酶的抑制剂，并且可用于治疗炎性或过敏性疾病。

    Pyran derivatives and their use as inhibitors of 5-lipoxygenase
    7.
    发明授权
    Pyran derivatives and their use as inhibitors of 5-lipoxygenase 失效
    吡喃衍生物及其作为5-脂氧合酶抑制剂的用途

    公开(公告)号：US5407945A

    公开(公告)日：1995-04-18

    申请号：US99435

    申请日：1993-07-30

    申请人： Pierre A. R. Bruneau ,  Robert I. Dowell ,  David Waterson

    发明人： Pierre A. R. Bruneau ,  Robert I. Dowell ,  David Waterson

    IPC分类号： C07D309/08 ,  C07D405/12 ,  A61K31/47

    CPC分类号： C07D405/12 ,  C07D309/08

    摘要： The invention concerns a cyclic ether derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted phenylene or pyridylene;R.sup.1 includes hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl and (1-4C)alkylthio; 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, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

    摘要翻译： 本发明涉及式I的环醚衍生物，其中Ar 1是任选取代的苯基，萘基或9-或10-元双环杂环部分; A1是与X1或（1-3C）亚烷基的直接键; X1是氧基，硫基，亚磺酰基，磺酰基或亚氨基; Ar2是任选取代的亚苯基或亚吡啶基; R1包括氢，（1-4C）烷基，（1-4C）烷氧基羰基和（1-4C）烷硫基; 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定义为具有5至7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，亚磺酰基或磺酰基; 或其药学上可接受的盐。 本发明的化合物是5-脂氧合酶的抑制剂。

    Hydrazinopyridazine compounds
    8.
    发明授权
    Hydrazinopyridazine compounds 失效
    肼基哒嗪化合物

    公开(公告)号：US4711887A

    公开(公告)日：1987-12-08

    申请号：US479913

    申请日：1983-03-28

    申请人： Malcolm T. Briggs ,  Robert I. Dowell ,  Craig W. Thornber

    发明人： Malcolm T. Briggs ,  Robert I. Dowell ,  Craig W. Thornber

    IPC分类号： A61K31/50 ,  A61K31/502 ,  A61P9/12 ,  C07D237/14 ,  C07D237/18 ,  C07D237/20 ,  C07D237/22 ,  C07D237/24 ,  C07D237/32 ,  C07D237/34

    CPC分类号： C07D237/20 ,  C07D237/14 ,  C07D237/18 ,  C07D237/22 ,  C07D237/24 ,  C07D237/32 ,  C07D237/34

    摘要： Hydrazinopyridiazine derivatives of the formula: ##STR1## wherein A is alkylene, wherein either R.sup.1 is hydrogen and R.sup.2 is hydrogen, alkoxycarbonyl or aralkoxycarbonyl, or R.sup.1 and R.sup.2 together form alkylidene, aralkylidene, alkoxycarbonylalkylidene or aralkoxycarbonylalkylidene, wherein either R.sup.3 and R.sup.4, which may be the same or different, each is hydrogen, halogen, hydroxy, amino, nitro, trifluoromethyl, carbamoyl, cyano, alkyl, hydroxyalkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, cycloalkoxy, alkenyloxy, alkynyloxy, alkanoyl, aryl, aryloxy or dialkylamino, or R.sup.3 and R.sup.4 together with the adjacent benzene ring form indanyl, 5,6,7,8-tetrahydronaphthyl, 5-oxo-5,6,7,8-tetrahydronaphthyl, indenyl, 5,8-dihydronaphthyl or naphthyl, wherein either R.sup.5 and R.sup.6, which may be the same or different, each is hydrogen or alkyl, or R.sup.5 and R.sup.6 together with the adjacent pyridazine ring form phthalazinyl, and wherein X is oxygen or --NHCO--, --NHCO--A.sup.1 -- or --NHCO--A.sup.1 --O-- wherein A.sup.1 is alkylene, acid-addition salts thereof, processes for their manufacture and pharmaceutical composition containing them. The compounds possess antihypertensive activity.

    摘要翻译： 其中A是亚烷基，其中R 1是氢，R 2是氢，烷氧基羰基或芳烷氧基羰基，或者R 1和R 2一起形成亚烷基，亚烷叉基，烷氧羰基亚烷基或芳烷氧羰基亚烷基，其中R 3 硝基，三氟甲基，氨基甲酰基，氰基，烷基，羟基烷基，环烷基，烯基，炔基，烷氧基，烷硫基，环烷氧基，烯氧基，炔氧基，烷酰基 ，芳基，芳氧基或二烷基氨基，或R 3和R 4与相邻苯环一起形成茚满基，5,6,7,8-四氢萘基，5-氧代-5,6,7,8-四氢萘基，茚基， 二氢萘基或萘基，其中R 5和R 6可以相同或不同，各自为氢或烷基，或R 5和R 6与相邻哒嗪环一起形成酞嗪基，其中X为氧或-NHCO-，-NHCO- A1-或-NHCO-Al-O-，其中A1是亚烷基， 其加成盐，其制备方法和含有它们的药物组合物。 该化合物具有抗高血压活性。

    5-lipoxygenase inhibitors
    9.
    发明授权
    5-lipoxygenase inhibitors 失效
    5-脂氧合酶抑制剂

    公开(公告)号：US5272173A

    公开(公告)日：1993-12-21

    申请号：US45715

    申请日：1993-04-14

    申请人： Robert I. Dowell ,  Philip N. Edwards ,  Keith Oldham

    发明人： Robert I. Dowell ,  Philip N. Edwards ,  Keith Oldham

    IPC分类号： C07D309/10 ,  C07D405/12 ,  C07D521/00 ,  A61K31/35

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/10 ,  C07D405/12

    摘要： The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --wherein X.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.3 is oxy, thio, sulphinyl or sulphonyl; which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.

    摘要翻译： 本发明涉及式I的芳基衍生物，其中Ar 1为任选取代的苯基，萘基或杂环部分，X 1为氧基，硫基，亚磺酰基，磺酰基，二氟亚甲基，亚氨基，（1-4C）烷基亚氨基或 任选取代的（1-4C）亚烷基，或X1是式-X4-CR2-或-CR2-X4-的基团，其中X4是氧基，硫基，亚磺酰基，磺酰基或羰基，每个R是氢，甲基或乙基; Ar 2和Ar 3各自为任选取代的亚苯基; X2是氧基，硫基，亚磺酰基或磺酰基; R1是（1-4C）烷基; 并且R2和R3一起形成式-A1-X3-A2-的基团，其与A1和A2所连接的碳原子一起定义为具有5至7个环原子的环，其中A1和A2各自为（1 -3C）亚烷基，X 3为氧基，硫基，亚磺酰基或磺酰基; 哪些化合物是5-脂氧合酶的抑制剂，并且可用于治疗炎性或过敏性疾病。

    Pyran derivatives and their use as inhibitors of 5-lipoxygenase
    10.
    发明授权
    Pyran derivatives and their use as inhibitors of 5-lipoxygenase 失效
    吡喃衍生物及其作为5-脂氧合酶抑制剂的用途

    公开(公告)号：US5254581A

    公开(公告)日：1993-10-19

    申请号：US12810

    申请日：1993-02-02

    申请人： Pierre A. R. Bruneau ,  Robert I. Dowell ,  David Waterson

    发明人： Pierre A. R. Bruneau ,  Robert I. Dowell ,  David Waterson

    IPC分类号： C07D309/08 ,  C07D405/12 ,  A61K31/35 ,  C07D309/06

    CPC分类号： C07D405/12 ,  C07D309/08

    摘要： The invention concerns a cyclic ether derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted phenylene or pyridylene;R.sup.1 includes hydrogen, (1-4C)alkyl, (1-4C)alkcxycarbonyl and (1-4C)alkylthio; 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, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

    摘要翻译： 本发明涉及式I的环醚衍生物，其中Ar 1是任选取代的苯基，萘基或9-或10-元双环杂环部分; A1是与X1或（1-3C）亚烷基的直接键; X1是氧基，硫基，亚磺酰基，磺酰基或亚氨基; Ar2是任选取代的亚苯基或亚吡啶基; R1包括氢，（1-4C）烷基，（1-4C）烷氧羰基和（1-4C）烷硫基; 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定义为具有5至7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，亚磺酰基或磺酰基; 或其药学可接受的盐。 本发明的化合物是5-脂氧合酶的抑制剂。