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1. 发明授权

US4042706A Novel anti-inflammatory pyrazole derivatives and preparation thereof 失效
标题翻译：新型抗炎吡唑衍生物及其制备方法
公开(公告)号：US4042706A
公开(公告)日：1977-08-16
申请号：US712659
申请日：1976-08-09
申请人： Hanns Ahrens , Henning Koch , Eberhard Schroder , Helmut Biere , Joachim-Friedrich Kapp
发明人： Hanns Ahrens , Henning Koch , Eberhard Schroder , Helmut Biere , Joachim-Friedrich Kapp
IPC分类号： A61K31/40 , A61K31/415 , A61P29/00 , C07D231/12 , C07D231/14 , C07D295/145
CPC分类号： C07D231/12 , C07C251/72 , C07D231/14 , C07D295/145
摘要： Pyrazole compounds of the formula ##STR1## wherein n is 1, 2, 3, or 4; R.sub.1, R.sub.2, R.sub.3, and R.sub.4, which can be in the ortho, meta or para position, each are hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, nitro or amino; X is cyano, aminocarbonyl, lower alkoxycarbonyl, carboxy and physiologically acceptable salts thereof, have anti-inflammatory activity.
摘要翻译：吡唑类化合物，其中n为1,2,3或4; 可以在邻位，间位或对位的R 1，R 2，R 3和R 4各自为氢，卤素，烷基，烷氧基，三氟甲基，硝基或氨基; X是氰基，氨基羰基，低级烷氧基羰基，羧基及其生理上可接受的盐具有抗炎活性。

2. 发明授权

US4057640A 5,6,7,8:Tetrahydrocarbazole-1-carboxylic acid derivatives 失效
标题翻译： 5,6,7,8：四氢咔唑-1-羧酸衍生物
公开(公告)号：US4057640A
公开(公告)日：1977-11-08
申请号：US683752
申请日：1976-05-06
申请人： Helmut Biere , Hanns Ahrens , Clemens Rufer , Eberhard Schroder , Henning Koch
发明人： Helmut Biere , Hanns Ahrens , Clemens Rufer , Eberhard Schroder , Henning Koch
IPC分类号： A61K31/405 , C07D209/88 , A61K31/40
CPC分类号： C07D209/88 , A61K31/405
摘要： Carbazoles of the formula ##STR1## wherein R.sub.1 is hydroxymethyl, alkanoyloxymethyl, tetrazolyl, cyano, oximinocarbonyl, aminocarbonyl, carboxyl and salts thereof with physiologically acceptable bases and the esters thereof with physiologically acceptable alcohols and amides thereof with physiologically acceptable amines,R.sub.2 through R.sub.6 each are a hydrogen atom, halogen atom, lower alkyl, trifluoromethyl, or lower alkoxy, orR.sub.5 and R.sub.6 collectively are a five- or six-membered isocyclic ring, andR.sub.7 is a hydrocarbon of 3-8 carbon atoms or, when at least one of the R.sub.2 through R.sub.6 is other than a hydrogen atom, a hydrogen atom, methyl or ethyl,And the corresponding compounds wherein R.sub.7 is a hydrogen atom, methyl or ethyl,And the 5,6,7,8-tetrahydrocarbazoles, possess topical anti-inflammatory activity.
摘要翻译：其中R 1为羟甲基，烷酰氧基甲基，四唑基，氰基，肟基羰基，氨基羰基，羧基及其盐与生理上可接受的碱，其酯与其生理上可接受的醇和酰胺与生理上可接受的胺，R 2至R 6各自相同是氢原子，卤素原子，低级烷基，三氟甲基或低级烷氧基，或者R5和R6共同是五元或六元的环状环，而R7是3-8个碳原子的烃，或者当至少一个 R 2至R 6不是氢原子，氢原子，甲基或乙基，并且R 7是氢原子，甲基或乙基的相应化合物，以及5,6,7,8-四氢四硼化物，POSSESS主题抗体 -INFLAMMATORY活动。

3. 发明授权

US3956295A Carbazole derivatives 失效
标题翻译：咔唑衍生物
公开(公告)号：US3956295A
公开(公告)日：1976-05-11
申请号：US489162
申请日：1974-07-17
申请人： Helmut Biere , Hanns Ahrens , Clemens Rufer , Eberhard Schroder , Henning Koch
发明人： Helmut Biere , Hanns Ahrens , Clemens Rufer , Eberhard Schroder , Henning Koch
IPC分类号： A61K31/405 , C07D209/88 , C07D209/82
CPC分类号： C07D209/88 , A61K31/405 , Y10S514/887
摘要： Carbazoles of the formula ##SPC1##Wherein R.sub.1 is hydroxymethyl, alkanoyloxymethyl, tetrazolyl, cyano, oximinocarbonyl, aminocarbonyl, carboxyl and salts thereof with physiologically acceptable bases and the esters thereof with physiologically acceptable alcohols and amides thereof with physiologically acceptable amines,R.sub.2 through R.sub.6 each are a hydrogen atom, halogen atom, lower alkyl, trifluoromethyl, or lower alkoxy, orR.sub.5 and R.sub.6 collectively are a five- or six-membered isocyclic ring, andR.sub.7 is a hydrocarbon of 3-8 carbon atoms or, when at least one of the R.sub.2 through R.sub.6 is other than a hydrogen atom, a hydrogen atom, methyl or ethyl,And the corresponding compounds wherein R.sub.7 is a hydrogen atom, methyl or ethyl,And the 5,6,7,8-tetrahydrocarbazoles, possess topical anti-inflammatory activity.
摘要翻译：式VIII的咔唑，其中R1是羟甲基，烷酰氧基甲基，四唑基，氰基，肟基羰基，氨基羰基，羧基及其盐与生理上可接受的碱，其酯与其生理上可接受的醇和酰胺与生理上可接受的胺，R2至R6各自为氢原子，卤素原子，低级烷基，三氟甲基或低级烷氧基，或者R5和R6共同是五元或六元的环状环，并且R 7是3-8个碳原子的烃，或者当R2中的至少一个通过R6不同于氢原子，氢原子，甲基或乙基，以及其中R7是氢原子，甲基或乙基的相应化合物，以及5,6,7,8-四氢四硼化物，POSSESS局部抗炎活性。

4. 发明授权

US3962471A Indolylacetylamino acid derivatives, process for their preparation, and pharmaceutical compositions 失效
标题翻译：吲哚乙酰氨基酸衍生物，其制备方法和药物组合物
公开(公告)号：US3962471A
公开(公告)日：1976-06-08
申请号：US557515
申请日：1975-03-12
申请人： Helmut Biere , Hanns Ahrens , Clemens Rufer , Eberhard Schroder , Henning Koch
发明人： Helmut Biere , Hanns Ahrens , Clemens Rufer , Eberhard Schroder , Henning Koch
IPC分类号： C07C67/00 , C07C237/22 , C07C241/00 , C07C251/76 , C07D209/26 , C07D209/28
CPC分类号： C07D209/28 , C07D209/26
摘要： Indolylacetylamino acids of the formula ##SPC1##Wherein R is H or CH.sub.3, physiologically acceptable salts thereof and the corresponding amides, alkyl and benzyl esters and alkyl and benzyl ethers thereof, possess anti-inflammatory activity.
摘要翻译：式WHEREIN R为H或CH3的吲哚基乙酰氨基酸，其生理学上可接受的盐及其相应的酰胺，烷基和苄基酯及其烷基和苄基醚具有抗炎活性。

5. 发明授权

US3962453A Novel pyrazolyloxyacetic acid derivatives and process for the preparation thereof 失效
标题翻译：新型吡唑氧基乙酸衍生物及其制备方法
公开(公告)号：US3962453A
公开(公告)日：1976-06-08
申请号：US505208
申请日：1974-09-12
申请人： Hans Ahrens , Helmut Biere , Clemens Rufer , Eberhard Schroder , Henning Koch
发明人： Hans Ahrens , Helmut Biere , Clemens Rufer , Eberhard Schroder , Henning Koch
IPC分类号： C07D231/20 , A61K31/415 , A61P29/00 , C07D231/22 , C07D231/18
CPC分类号： C07D231/22
摘要： Compounds of the formula ##SPC1##Wherein X and Y each are a bond or methylene, R is H or lower-alkyl and Z is a carboxyl, amide, nitrile or alkoxycarbonyl of 1-6 carbon atoms in the alkoxy group and the corresponding compounds bearing 1-2 halogen, lower-alkyl or lower-alkoxy groups on one or both benzene rings and, when Z is carboxyl, salts thereof with physiologically acceptable bases, possess anti-inflammatory and antipyretic activities.
摘要翻译：式WHEREIN X和Y各自为键或亚甲基的化合物，R为H或低级烷基，Z为烷氧基中1-6个碳原子的羧基，酰胺，腈或烷氧基羰基，一个或两个苯环上的2个卤素，低级烷基或低级烷氧基，当Z为羧基时，其盐与生理上可接受的碱基具有抗炎和解热活性。

6. 发明授权

US4117135A Novel 5,6,7,8-tetrahydro-5-quinolines and their use as anti-inflammatory agents 失效
标题翻译：新型5,6,7,8-四氢-5-喹啉及其作为抗炎剂的用途
公开(公告)号：US4117135A
公开(公告)日：1978-09-26
申请号：US620777
申请日：1975-10-08
申请人： Eberhard Schroder , Henning Koch
发明人： Eberhard Schroder , Henning Koch
IPC分类号： C07D213/80 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/48 , C07D221/04 , C07D401/04 , C07D471/10 , C07D215/16 , A61K31/47
CPC分类号： C07D213/80 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/48 , C07D221/04 , C07D471/10
摘要： Pyridine derivatives of the formula ##STR1## wherein R.sub.1 is an alkyl, aliphatic, a cycloalkyl, or a substituted or unsubstituted hydrocarbon aryl and the substituent is halogen, alkoxy or methylenedioxy; R.sub.2 is H or Cl; X is CN, 5-tetrazolyl, or COOH or a carboxylic acid derivative; Y is H, OH, OCOR.sub.7, NH.sub.2, NHCOR.sub.8, R.sub.9, COOH or COOR.sub.10 and R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are alkyl groups of 1-10 carbon atoms; A is methylene or a carbon-to-carbon bond; and R.sub.3 and R.sub.4 are each H or alkyl groups of 1-4 carbon atoms, are useful as anti-inflammatory agents.

7. 发明授权

US3968219A Hydroxy phenylbutazone derivatives and their preparation 失效
标题翻译：羟基保泰松衍生物及其制备方法
公开(公告)号：US3968219A
公开(公告)日：1976-07-06
申请号：US599397
申请日：1975-07-28
申请人： Dieter Rahtz , Henning Koch , Erich Gerhards
发明人： Dieter Rahtz , Henning Koch , Erich Gerhards
IPC分类号： C07D231/36 , C07D231/32 , C07D231/34 , A61K31/415
CPC分类号： C07C243/00 , C07D231/34
摘要： Bis-hydroxyphenylbutazone esters of alkanedioic acids of the formula ##SPC1##Wherein n is an integer from 1 to 18, inclusive; R.sub.1 is hydrocarbon of 3-9 carbon atoms, optionally substituted by oxo or interrupted by thia, sulfinyl, or sulfonyl; and R.sub.2 is a hydrogen atom, a fluorine atom, a chlorine atom, lower alkyl of 1-4 carbon atoms, or trifluoromethyl, preferably in the ortho or para position, possess topical anti-inflammatory activity.
摘要翻译：具有下式的链烷二酸的双羟基保泰松酯，其中N是1至18的整数，包含; R 1是3-9个碳原子的烃，任选被氧代取代或被硫杂，亚磺酰基或磺酰基中断; R2为氢原子，氟原子，氯原子，1-4个碳原子的低级烷基或三氟甲基，优选为邻位或对位，具有局部抗炎活性。

8. 发明授权

US4012510A Novel methylene steroids 失效
标题翻译：新亚甲基类固醇
公开(公告)号：US4012510A
公开(公告)日：1977-03-15
申请号：US630627
申请日：1975-11-10
申请人： Rudolf Wiechert , Klaus Kieslich , Henning Koch
发明人： Rudolf Wiechert , Klaus Kieslich , Henning Koch
IPC分类号： C12P33/02 , A61K31/57 , A61P17/00 , A61P29/00 , C07J51/00 , C07J53/00 , C12P33/08 , C12R1/07 , C12R1/15 , C12R1/645 , C12R1/66 , A61K31/56
CPC分类号： C07J51/00 , C07J53/008
摘要： Methylene steroids of the formula ##STR1## wherein X is H, F or CH.sub.3 ; Y is hydroxymethylene, alkanoyloxymethylene or carbonyl; R.sub.1 is H, OH or alkanoyloxy; and R.sub.2 is H, OH or esterified OH, possess topical anti-inflammatory activity.
摘要翻译：其中X为H，F或CH 3的式IMAMA的亚甲基类固醇; Y是羟基亚甲基，烷酰氧基亚甲基或羰基; R1是H，OH或烷酰氧基; R2为H，OH或酯化OH，具有局部抗炎活性。

9. 发明授权

US4011322A Benzimidazole derivatives and process for the production thereof 失效
标题翻译：苯并咪唑衍生物及其生产方法
公开(公告)号：US4011322A
公开(公告)日：1977-03-08
申请号：US599398
申请日：1975-07-28
申请人： Dieter Rahtz , Hans Wendt , Henning Koch
发明人： Dieter Rahtz , Hans Wendt , Henning Koch
IPC分类号： C07D235/14 , A61K31/4184 , C07D235/10 , C07D403/04 , C07D403/06
CPC分类号： C07D235/10
摘要： Benzimidazoles of the formula ##STR1## wherein R.sub.1 is o-hydroxyphenyl, a p-chlorophenyl, or p-fluorophenyl, and R.sub.2 is an alkyl of 2-4 carbon atoms, and physiologically acceptable acid addition salts thereof possess topical anti-inflammatory activity.

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