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1. 发明授权

US4698346A Thiazolo[5,4-h]quinoline compounds useful as anti-allergy agents 失效
标题翻译：噻唑并[5,4-h]喹啉化合物可用作抗过敏剂
公开(公告)号：US4698346A
公开(公告)日：1987-10-06
申请号：US889021
申请日：1986-07-24
申请人： John H. Musser , Richard E. Brown
发明人： John H. Musser , Richard E. Brown
IPC分类号： C07D215/28 , C07D498/04 , A61K31/425 , C07D513/04
CPC分类号： C07D215/28
摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.
摘要翻译：新喹啉化合物及相应的1,2-; 1,3- 和1,4-苯并二嗪，喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷酰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氧，硫，氮或R 3 N，其中R 3为氢低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X是氰基，烷氧羰基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1，可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

2. 发明授权

US4522947A Certain 1,3-oxazolo[4,5H]quinolines useful as anti-allergy agents 失效
标题翻译：某些用作抗过敏剂的1,3-恶唑并[4,5H]喹啉
公开(公告)号：US4522947A
公开(公告)日：1985-06-11
申请号：US476673
申请日：1983-03-18
申请人： John H. Musser , Richard E. Brown
发明人： John H. Musser , Richard E. Brown
IPC分类号： C07D215/28 , C07D498/04 , A61K31/47
CPC分类号： C07D215/28
摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.
摘要翻译：新喹啉化合物及相应的1,2-; 1,3- 和1,4-苯并二嗪，喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷酰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氧，硫，氮或R 3 N，其中R 3为氢低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X是氰基，烷氧羰基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1，可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

3. 发明授权

US4656281A Imidazo quinoline compounds useful as anti-allergy agents 失效
标题翻译：咪唑喹啉化合物可用作抗过敏剂
公开(公告)号：US4656281A
公开(公告)日：1987-04-07
申请号：US731689
申请日：1985-05-08
申请人： John H. Musser , Richard E. Brown
发明人： John H. Musser , Richard E. Brown
IPC分类号： C07D215/28 , C07D498/04 , C07D471/04
CPC分类号： C07D215/28
摘要： The quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or intermediates in the preparation of compounds useful for treating asthma.
摘要翻译：喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基，芳基/低级亚烷基，硝基低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷氧基羰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氮或R3N，其中R3为氢，低级烷基，烯基，炔基，芳基芳烷基，酰基，氨基烷基或羧基烷基，Z是氮，X是氰基，甲酰氧基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1，可用作药物，特别是用于治疗哮喘和/ 可用于治疗哮喘的化合物的制备。

4. 发明授权

US4563463A 2-Oxo-1,3-oxazolo[4,5-h] quinolines useful as anti-allergy agents 失效
标题翻译：可用作抗过敏剂的2-氧代-1,3-恶唑并[4,5-h]喹啉
公开(公告)号：US4563463A
公开(公告)日：1986-01-07
申请号：US667667
申请日：1984-11-02
申请人： John H. Musser , Richard E. Brown
发明人： John H. Musser , Richard E. Brown
IPC分类号： C07D215/28 , C07D498/04 , A61K31/47
CPC分类号： C07D215/28
摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formulae: ##STR1## and salts thereof, wherein R is hydrogen, acyl, carboethoxy,(3-methoxyphen)acetyl,(2-phenyl)propionyl, dimethylcarbamoyl or methyl,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxy, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.
摘要翻译：新喹啉化合物及相应的1,2-; 1,3- 其中R为氢，酰基，乙酰乙氧基，（3-甲氧基苯基）乙酰基，（2-苯基）丙酰基，二甲基氨基甲酰基或甲基，R 1，R 2，氰基，芳基，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷氧基羰基，低级烷基氨基，低级烷基氨基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y是氧，硫，氮或R3N，其中R3是氢，低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X为氰基，烷氧羰基，羧基，甲酰肟基，四唑基，碳烷氧基烷基或羧基烷基，m为0或1，可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

5. 发明授权

US4307091A Process for treatment of allergic conditions with benzoxazinediones 失效
标题翻译：用苯并恶嗪酮治疗过敏症状的方法
公开(公告)号：US4307091A
公开(公告)日：1981-12-22
申请号：US149078
申请日：1980-05-12
申请人： Richard E. Brown , Vasil St. Georgiev , Bernard Loev , Robert Mack
发明人： Richard E. Brown , Vasil St. Georgiev , Bernard Loev , Robert Mack
IPC分类号： C07D265/36 , C07D267/14
CPC分类号： C07D265/36 , C07D267/14
摘要： Therapeutic compositions containing as active principle, a benzoxazindione or pharmaceutically-acceptable acid addition salt thereof are useful in the treatment of allergy.
摘要翻译：含有作为活性成分的苯并恶嗪二酮或其药学上可接受的酸加成盐的治疗组合物可用于治疗过敏。

6. 发明授权

US4179513A Indole-2-carboxylic acids to effect CNS depressant activity 失效
标题翻译：吲哚-2-羧酸以影响CNS抑制活性
公开(公告)号：US4179513A
公开(公告)日：1979-12-18
申请号：US895201
申请日：1978-04-10
申请人： Richard E. Brown
发明人： Richard E. Brown
IPC分类号： C07D209/42 , C07D498/04 , A61K31/40
CPC分类号： C07D209/42
摘要： This invention relates to substituted indolobenzoxazepines which act as central nervous system depressants and as such are useful as tranquillizers.
摘要翻译：本发明涉及作为中枢神经系统抑制剂的取代的吲哚并苯并氮杂，因此可用作镇静剂。

7. 发明授权

US4148806A Process for the preparation of indolopyrones 失效
标题翻译：制备吲哚并呋喃的方法
公开(公告)号：US4148806A
公开(公告)日：1979-04-10
申请号：US860504
申请日：1977-12-14
申请人： Richard E. Brown , Paul C. Unangst , Frank Fontsere , Arthur C. Fabian
发明人： Richard E. Brown , Paul C. Unangst , Frank Fontsere , Arthur C. Fabian
IPC分类号： C07D209/36 , C07D491/04 , C07D491/052
CPC分类号： C07D491/04 , C07D209/36
摘要： This invention relates to a novel process for preparing a group of novel substituted indolopyrones.
摘要翻译：本发明涉及制备一组新型取代的吲哚吡酮的新方法。

8. 发明授权

US4013671A Substituted benzopyrano[3,4-c]pyridines and process for their preparation 失效
标题翻译：取代的苯并吡喃（3,4-C）吡啶及其制备方法
公开(公告)号：US4013671A
公开(公告)日：1977-03-22
申请号：US666829
申请日：1976-03-15
申请人： Richard E. Brown , John Shavel, Jr.
发明人： Richard E. Brown , John Shavel, Jr.
IPC分类号： A61K31/535 , C07D491/052 , C07D311/06 , C07D311/76
CPC分类号： C07D491/052 , A61K31/535
摘要： Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##STR1## In the above formula, R.sub.1 R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; R.sub.3 is hydrogen or a lower alkyl group of from 1 to 6 carbon atoms and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c] pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.

9. 发明授权

US3984546A Substituted benzopyrano [3,4-c]pyridines for the treatment of bronchial asthma 失效
标题翻译：取代的苯并吡喃并[8,3-c {9吡啶用于治疗支气管哮喘
公开(公告)号：US3984546A
公开(公告)日：1976-10-05
申请号：US622547
申请日：1975-10-15
申请人： Richard E. Brown , John Shavel, Jr.
发明人： Richard E. Brown , John Shavel, Jr.
IPC分类号： A61K31/535 , A61K31/54 , A61K31/44 , A61K31/445
CPC分类号： C07D491/052 , A61K31/535 , A61K31/54 , Y10S514/826
摘要： Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##SPC1##In the above formula, R.sub.1 and R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c]pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.
摘要翻译：公开了具有以下结构式的取代的苯并吡喃并[3,4-c]吡啶：在上式中，R 1和R 2是氢，羟基或具有1至6个碳原子的低级烷氧基; X为氧原子，硫原子，亚甲基或被氢取代的氮原子，1〜6个碳原子的低级烷基或1〜6个碳原子的低级烷酰基。本发明化合物是通过在酸催化剂存在下使R1，R2取代的苯酚与3-乙酯基-4-哌啶酮反应得到中间体R1，R2取代的苯并吡喃并[3,4-c]吡啶。通过用适当取代的烷基卤处理苯并吡喃并[3,4-c]吡啶得到N-氨基烷基苯并吡喃并[3,4-c]吡啶。本发明的化合物可用作治疗支气管哮喘的支气管扩张剂。

10. 发明授权

US3961057A Benzopyrano(3,4-C)pyridine bronchodilators 失效
标题翻译：苯并吡喃（3,4-C）吡啶支气管扩张剂
公开(公告)号：US3961057A
公开(公告)日：1976-06-01
申请号：US538424
申请日：1975-01-03
申请人： Richard E. Brown , John Shavel, Jr.
发明人： Richard E. Brown , John Shavel, Jr.
IPC分类号： A61K31/535
CPC分类号： C07D491/052 , A61K31/535 , Y10S514/826
摘要： Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##SPC1##In the above formula, R.sub.1 and R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; R.sub.3 is hydrogen or a lower alkyl group of from 1 to 6 carbon atoms and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c]pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.
摘要翻译：公开了具有以下结构式的取代的苯并吡喃并[3,4-c]吡啶：在上式中，R 1和R 2是氢，羟基或具有1至6个碳原子的低级烷氧基; R3是氢或1〜6个碳原子的低级烷基，X是氧原子，硫原子，亚甲基或被氢取代的氮原子，1〜6个碳原子的低级烷基或 1至6个碳原子的低级烷酰基。本发明化合物是通过在酸催化剂存在下使R1，R2取代的苯酚与3-乙酯基-4-哌啶酮反应得到中间体R1，R2取代的苯并吡喃并[3,4-c]吡啶。通过用适当取代的烷基卤处理苯并吡喃并[3,4-c]吡啶得到N-氨基烷基苯并吡喃并[3,4-c]吡啶。本发明的化合物可用作治疗支气管哮喘的支气管扩张剂。

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