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1. 发明授权

US4810719A Anti-inflammator 1,n-diarylpyrazol-3-amines 失效
标题翻译：抗炎剂1，正二芳基吡唑-3-胺
公开(公告)号：US4810719A
公开(公告)日：1989-03-07
申请号：US733591
申请日：1985-05-10
申请人： Richard A. Appleton , Sidney C. Burford , David N. Hardern , David Wilkinson
发明人： Richard A. Appleton , Sidney C. Burford , David N. Hardern , David Wilkinson
IPC分类号： A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/505 , A61P29/00 , C07D213/57 , C07D231/06 , C07D231/38 , C07D333/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/00 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/12
CPC分类号： C07D231/06 , C07C255/00 , C07D213/57 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D417/04 , C07D417/12
摘要： There are described compounds of formula I, ##STR1## in which either R.sub.2 represents hydrogen, alkyl or Ar.sub.2, andR.sub.3 represents hydrogen, alkyl or alkyl substituted by Ar.sub.3 ;or R.sub.2 and R.sub.3 together form the chain --(CH.sub.2).sub.m --;R.sub.4 and R.sub.5, which may be the same or different, each independently represent hydrogen, halogen, Ar, alkyl, or alkyl substituted by Ar,Ar.sub.1, Ar.sub.2 and Ar, which may be the same or different each independently represent aryl or aryl substituted by one or more ofhalogen, hydroxy, --CN, --COR.sub.6, trihalomethyl, alkoxy, alkoxy substituted by --COR.sub.6, alkoxy substituted by --NR.sub.7 R.sub.8, alkyl, alkyl substituted by --COR.sub.6, alkyl substituted by NR.sub.7 R.sub.8, alkoxy substituted by Ar.sub.3, S(O).sub.n R.sub.9, --NR.sub.7 R.sub.8 or OAr.sub.3 ;R.sub.6 represents --OR.sub.10, --NR.sub.7 R.sub.8, hydrogen or alkyl;R.sub.7 and R.sub.8, which may be the same or different, each independently represent hydrogen, alkyl, alkanoyl or Ar.sub.3 ;R.sub.9 represents alkyl or Ar.sub.3 ;R.sub.10 represents hydrogen, alkyl or Ar.sub.3 ;m represents an integer from 3 to 6 inclusive;n represents 0, 1 or 2; andAr.sub.3 represents unsubstituted aryl;or a pharmaceutically acceptable derivative thereof.There are also described compositions containing the compounds and methods for their preparation.The compounds are indicated for use as pharmaceutical, e.g. anti-inflammatory, agents.
摘要翻译：描述式I化合物，其中R 2表示氢，烷基或Ar 2，R 3表示氢，被Ar 3取代的烷基或烷基; 或R 2和R 3一起形成链 - （CH 2）m - ; R 4和R 5可以相同或不同，各自独立地表示氢，卤素，Ar，烷基或被Ar，Ar1，Ar2和Ar取代的烷基，它们可以相同或不同，各自独立地表示被一个或多个卤素，羟基，-CN，-COR 6，三卤代甲基，烷氧基，被-COR 6取代的烷氧基，被-NR 7 R 8取代的烷氧基，被-COR 6取代的烷基，被NR 7 R 8取代的烷基，被Ar 3取代的烷氧基，S（ O）n R 9，-NR 7 R 8或OAr 3; R6表示-OR10，-NR7R8，氢或烷基; R 7和R 8可以相同或不同，各自独立地表示氢，烷基，烷酰基或Ar 3; R9代表烷基或Ar3; R 10表示氢，烷基或Ar 3; m表示3〜6的整数， n表示0,1或2; 和Ar 3表示未取代的芳基; 或其药学上可接受的衍生物。还描述了含有这些化合物的组合物及其制备方法。化合物指示用作药物，例如，抗炎，药剂。

2. 发明授权

US5428044A Anti-inflammatory 4-aminophenyl derivatives 失效
标题翻译：抗炎4-氨基苯基衍生物
公开(公告)号：US5428044A
公开(公告)日：1995-06-27
申请号：US138375
申请日：1993-10-15
申请人： John R. Bantick , David N. Hardern , Richard A. Appleton , John Dixon , David J. Wilkinson
发明人： John R. Bantick , David N. Hardern , Richard A. Appleton , John Dixon , David J. Wilkinson
IPC分类号： A61K31/35 , A61K31/15 , A61K31/352 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/455 , A61K31/465 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/53 , A61P29/00 , A61P43/00 , C07D209/60 , C07D213/82 , C07D215/38 , C07D231/06 , C07D231/38 , C07D233/88 , C07D235/30 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D241/28 , C07D249/04 , C07D249/08 , C07D249/14 , C07D251/02 , C07D253/06 , C07D253/07 , C07D261/14 , C07D263/48 , C07D285/08 , C07D285/12 , C07D285/135 , C07D311/92 , C07D333/36 , C07D333/40 , C07D401/08 , C07D401/10 , C07D401/12 , C07D521/00 , A61K31/535 , A01N43/56
CPC分类号： C07D213/82 , C07D215/38 , C07D231/06 , C07D231/12 , C07D231/38 , C07D233/56 , C07D233/88 , C07D235/30 , C07D237/20 , C07D237/22 , C07D239/42 , C07D239/48 , C07D241/20 , C07D249/04 , C07D249/08 , C07D249/14 , C07D253/07 , C07D261/14 , C07D263/48 , C07D285/08 , C07D285/135 , C07D311/92 , C07D333/36 , C07D401/12
摘要： There are disclosed compounds of the formula (I): ##STR1## in which the variables R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and X are defined in the specification. The compounds are useful as pharmaceuticals, especially as anti-inflammatory agents.
摘要翻译：公开了式（I）化合物：其中变量R1，R2，R3，R4，R5，R6和X在本说明书中定义。这些化合物可用作药物，特别是作为抗炎剂。

3. 发明授权

US4803216A Pyrazole-3-amines as anti-inflammatory agents 失效
标题翻译：吡唑-3-胺作为抗炎剂
公开(公告)号：US4803216A
公开(公告)日：1989-02-07
申请号：US46656
申请日：1987-05-05
申请人： Richard A. Appleton , John Dixon , Sidney C. Burford
发明人： Richard A. Appleton , John Dixon , Sidney C. Burford
IPC分类号： A61K31/415 , C07D231/38
CPC分类号： C07D231/38
摘要： There are described compounds of formula I, ##STR1## in which R.sub.1 represents hydrogen, alkyl, alkanoyl or alkyl substituted by Ar.sub.1,R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, each independently represent hydrogen, alkyl or Ar.sub.3,Ar.sub.1, Ar.sub.2 and Ar.sub.3, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of alkyl, hydroxy, alkoxy, NR.sub.6 R.sub.7 or halogen,R.sub.6 and R.sub.7, which may be the same or different, independently represent hydrogen or alkyl,and pharmaceutically acceptable acid addition salts thereof.Compositions containing the compounds and methods for their preparation are also described.The compounds are indicated for use as pharmaceutical, e.g. anti-inflammatory, agents.

4. 发明授权

US4151179A 2-(4H-1-Benzopyran-6-yl)propionic acids 失效
标题翻译： 2-（4H-1-苯并吡喃-6-基）丙酸
公开(公告)号：US4151179A
公开(公告)日：1979-04-24
申请号：US712603
申请日：1976-08-09
申请人： Richard A. Appleton , Kevan Brown
发明人： Richard A. Appleton , Kevan Brown
IPC分类号： C07C41/26 , C07C43/23 , C07C45/54 , C07D311/22 , A61K31/35
CPC分类号： C07D311/22 , C07C41/26 , C07C45/54 , Y10S514/825 , Y10S514/87
摘要： There are described compounds of formula I, ##STR1## in which Ra is hydrogen, alkyl, alkenyl or phenyl, R.sub.3, R.sub.5, R.sub.7 and R.sub.8, which may be the same or different, are each hydrogen, alkyl, alkoxy, halogen, hydroxy, alkenyl or phenyl,Rx is hydrogen or alkyl,Ry and Rz are both hydrogen, or together represent a carbonyl oxygen atom,Rb and Rc are both hydrogen or together represent a carbon-carbon bond,Provided that when Rx is hydrogen, Ry and Rz together represent a carbonyl oxygen atom and R.sub.5, R.sub.7 and R.sub.8 are all hydrogen then Ra is other than methyl or phenyl,And pharmaceutically acceptable derivatives thereof.There are also described methods for making the compounds and pharmaceutical, e.g. anti-inflammatory, compositions containing the compounds.
摘要翻译：描述了式I的化合物，其中R a是氢，烷基，烯基或苯基，R 3，R 5，R 7和R 8可以相同或不同，各自为氢，烷基，烷氧基，卤素，羟基，烯基或苯基，Rx是氢或烷基，R y和R z都是氢或一起代表羰基氧原子，R b和R c都是氢或一起代表碳 - 碳键，当Rx是氢时，Ry 并且Rz一起表示羰基氧原子，R 5，R 7和R 8均为氢，则R a不是甲基或苯基，并且其药学上可接受的衍生物。

5. 发明授权

US4296114A 3,4-Dihydro-3-oxopyrido[2,3-b]-pyrazines, compositions and use thereof 失效
标题翻译： 3,4-二氢-3-氧代吡啶并[2,3-b] - 吡嗪的组合物及其用途
公开(公告)号：US4296114A
公开(公告)日：1981-10-20
申请号：US63357
申请日：1979-08-02
申请人： Richard A. Appleton , David Johnston
发明人： Richard A. Appleton , David Johnston
IPC分类号： C07D241/44 , C07D471/04 , A61K31/495 , A61K31/535 , C07D471/08
CPC分类号： C07D471/04 , C07D241/44
摘要： There are described compounds of formula I, ##STR1## in which R.sub.1 is phenyl substituted by halogen, alkoxy, alkyl, carboxy-alkyl, --NR.sub.4 R.sub.5, carboxy or alkoxy carbonyl,R.sub.3 is hydrogen, alkyl, mono- or di-carboxy alkyl, halo, alkoxy, phenyl, halo-phenyl, hydroxy, phenoxy, thiol, thioalkoxy, thiophenoxy, --NR.sub.4 R.sub.5, cyano, --COOH, carboxyureido, --CF.sub.3, --COR.sub.6, hydroxyalkyl, aminoalkyl, or alkoxy substituted by NR.sub.4 R.sub.5,ring A is a benzene or a pyridine ring which optionally carries up to 4 substituents R.sub.3, which may be the same or different,R.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, phenyl, halophenyl or alkyl, the alkyl optionally being substituted by alkoxy or by a mono- or di-alkyl or unsubstituted amino group; or R.sub.4 and R.sub.5, together with the nitrogen atom to which they are attached, form a piperidine, morpholine or an optionally alkyl substituted piperazine ring, andR.sub.6 is hydrogen or alkyl,provided that (i) when R.sub.1 is phenyl substituted by chlorine or bromine, ring A is not a benzene ring substituted by chlorine or bromine, or (ii) when R.sub.1 is phenyl substituted by methoxy R.sub.3 is not phenyl, and pharmaceutically acceptable salts, esters and amides thereof.There are also described methods for making the compounds and pharmaceutical, e.g. anti-inflammatory, compositions containing the compounds.
摘要翻译：描述了式I的化合物，其中R 1是被卤素，烷氧基，烷基，羧基 - 烷基，-NR 4 R 5，羧基或烷氧基羰基取代的苯基，R 3是氢，烷基，单 - 或二 - 羧基烷基，卤素，烷氧基，苯基，卤代苯基，羟基，苯氧基，硫醇，硫代烷氧基，硫代苯氧基，-NR4R5，氰基，-COOH，羧基脲基，-CF3，-COR6，羟基烷基，氨基烷基或被NR4R5取代的烷氧基，苯或吡啶环，其任选地带有至多4个可以相同或不同的取代基R 3，R 4和R 5可以相同或不同，各自表示氢，苯基，卤代苯基或烷基，所述烷基任选被烷氧基或被一或二烷基或未取代的氨基取代; 或R 4和R 5与它们所连接的氮原子一起形成哌啶，吗啉或任选的烷基取代的哌嗪环，并且R 6是氢或烷基，条件是（ⅰ）当R 1是被氯或溴取代的苯基时环A不是被氯或溴取代的苯环，或（ii）当R 1是被甲氧基取代的苯基不是苯基时，及其药学上可接受的盐，酯和酰胺。还描述了制备化合物和药物的方法。抗炎剂，含有这些化合物的组合物。

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