专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5063230A Substituted saturated and unsaturated indole quinoline and benzazepine carboxamides and their use as pharmacological agents 失效
标题翻译：取代的饱和和不饱和吲哚喹啉和苯并氮杂甲酰胺及其作为药物代用品的用途
公开(公告)号：US5063230A
公开(公告)日：1991-11-05
申请号：US489646
申请日：1990-04-06
申请人： Jeffrey C. Pelletier , Raymond D. Youssefyeh , Henry F. Campbell
发明人： Jeffrey C. Pelletier , Raymond D. Youssefyeh , Henry F. Campbell
IPC分类号： C07D209/08 , C07D215/48 , C07D223/16 , C07D453/02 , C07D471/08
CPC分类号： C07D223/16 , C07D209/08 , C07D215/48 , C07D453/02 , C07D471/08
摘要： This invention relates to a series of bicyclic benzomonoazacyclic carboxamide compounds of the general formula: ##STR1## Where Z is tertiary amine, which are useful for the method of treating patients suffering from gastrointestinal disorders, and of pharmaceutical composition including an effective 5HT3 - antagonists amount of said compounds therein.
摘要翻译：本发明涉及以下通式的一系列双环苯并偶氮环状羧酰胺化合物：其中Z是叔胺，其可用于治疗患有胃肠道疾病的患者的方法，以及包含有效的5HT3拮抗剂量的药物组合物的所述化合物。

2. 发明授权

US4933445A Heteroazabenzobicyclic carboxamide 5-HT.sub.3 antagonists 失效
标题翻译：杂环氮杂双环羧酰胺5-HT3拮抗剂
公开(公告)号：US4933445A
公开(公告)日：1990-06-12
申请号：US277610
申请日：1988-11-29
申请人： Jeffrey C. Pelletier , Raymond D. Youssefyeh , Henry F. Campbell
发明人： Jeffrey C. Pelletier , Raymond D. Youssefyeh , Henry F. Campbell
IPC分类号： C07D453/02 , C07D471/08
CPC分类号： C07D471/08 , C07D453/02
摘要： This invention relates to heteroazabenzo-bicyclic substituted carboxamide compounds of the formula: ##STR1## where W is O, S or NR.sub.5 andZ is ##STR2## 3-quinuclidine, 4-quinuclidine,4-(1-azabicyclo[3.3.1]nonane),3-(9-methylazabicyclo[3.3.1]nonane),7-(3-oxo-9-methylazabicyclo[3.3.1]nonane) or4-[3-methoxy-1-(3-[4-fluorophenoxy[propyl)piperidine];which exhibit 5-HT.sub.3 antagonist properties including CNS, anti-emetic and gastric prokinetic activity. This invention further relates to pharmaceutical compositions and methods for the treatment of the above disorders.
摘要翻译：本发明涉及下式的杂氮杂苯并双环取代的甲酰胺化合物：其中W是O，S或NR5，Z是3-奎宁环，4-奎宁环，4-（1-氮杂双环[3.3.1] 壬烷），3-（9-甲基偶氮二环[3.3.1]壬烷），7-（3-氧代-9-甲基偶氮二[3.3.1]壬烷）或4- [3-甲氧基-1-（3- [4- 氟苯氧基[丙基]哌啶]; 其显示5-HT3拮抗剂性质，包括CNS，抗呕吐和胃动力活性。本发明还涉及用于治疗上述疾病的药物组合物和方法。

3. 发明授权

US4625034A 1,2-Dihydro; 1,2,3,4-tetrahydro; 5,8 dihydro; and 5,6,7,8-tetrahydroquinoline derivatives 失效
标题翻译： 1,2-二氢; 1,2,3,4-四氢 5,8二氢; 和5,6,7,8-四氢喹啉衍生物
公开(公告)号：US4625034A
公开(公告)日：1986-11-25
申请号：US697999
申请日：1985-02-04
申请人： Edward S. Neiss , Rohit M. Desai , Raymond D. Youssefyeh
发明人： Edward S. Neiss , Rohit M. Desai , Raymond D. Youssefyeh
IPC分类号： A61K31/045 , A61K31/075 , A61K31/085 , A61K31/47 , A61P29/00 , A61P37/08 , A61P43/00 , C07C17/00 , C07C17/093 , C07C22/04 , C07C27/00 , C07C33/18 , C07C33/34 , C07C41/00 , C07C43/23 , C07C43/253 , C07C67/00 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/60 , C12N9/99
CPC分类号： C07D215/233 , C07C17/093 , C07C309/00 , C07C33/34 , C07C43/23 , C07D215/14 , C07D215/20 , C07D215/60
摘要： This invention relates to novel lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic activities. The present new compounds are di- and tetra-hydroquinoline or di- and tetra-hydronapthalene derivatives, more particularly, 1,2-, 1,4-, 5,6-, or 7,8-dihydro; 1,2,3,4-tetrahydro-; 5,8-dihydro-; or 5,6,7,8-tetrahydroquinoline or napthalene derivatives of a compound of the formula: ##STR1## and oxides, quaternary ammonium salts and acid salts thereof; wherein A is CH or N;Z is an alkylene chain containing up to 10 carbon atoms in the principal chain and a total of up to 12 carbon atoms and the said alkylene chain may be attached to the phenyl group through an oxygen atom;R is the substituent OR.sub.6 attached to one of the carbon atoms of Z in which R.sub.6 is H, lower alkyl or phenyl;X is --O(CHR.sub.5).sub.m --, alkylene of up to 2 carbon atoms in the principal chain and up to a total of 4 carbon atoms or ##STR2## wherein R.sub.5 is H or CH.sub.3 ;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each H or OH;n'=1 or 2; andm=1 or 2.
摘要翻译：本发明涉及具有抗炎和抗过敏活性的新型脂氧合酶抑制剂。本发明新的化合物是二 - 和四 - 氢喹啉或二 - 和四 - 氢化萘衍生物，更具体地，1,2-，1,4-，5,6-或7,8-二氢; 1,2,3,4-四氢 - 5,8-二氢 - 或下式化合物的5,6,7,8-四氢喹啉或萘衍生物及其氧化物，季铵盐及其酸盐; 其中A为CH或N; Z是在主链中含有至多10个碳原子的亚烷基链，总共多达12个碳原子，所述亚烷基链可以通过氧原子连接到苯基上; R是连接到Z的一个碳原子上的取代基OR 6，其中R 6是H，低级烷基或苯基; X是-O（CHR 5）m - ，主链中最多2个碳原子的亚烷基和总共4个碳原子，或者其中R 5是H或CH 3; R1，R2，R3和R4各自为H或OH; n'= 1或2; m = 1或2。

4. 发明授权

US4619944A Antihypertensive compounds 失效
标题翻译：抗高血压化合物
公开(公告)号：US4619944A
公开(公告)日：1986-10-28
申请号：US703054
申请日：1985-02-19
申请人： Raymond D. Youssefyeh , Howard Jones
发明人： Raymond D. Youssefyeh , Howard Jones
IPC分类号： A61K31/215 , A61K31/24 , A61K31/265 , A61K31/275
CPC分类号： A61K31/215 , A61K31/24 , A61K31/265 , A61K31/275
摘要： Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.2 R, wherein R is hydrogen, alkyl, or aryl, and where Y is hydroxy, their pharmaceutically acceptable, nontoxic alkali metal, alkaline earth metal, and amine salts.
摘要翻译：本发明提供了下式的抗高血压化合物：其中R1，R2，R3，R4，R5和R6是氢，烷基，烯基，炔基，苯基 - 烷基或环烷基，并且可以相同或不同，m是 0〜2的整数，n为0〜4的整数，M为烯基，炔基，环烷基，环烷基 - 烷基，多环烷基，多环烷基 - 烷基，芳基，芳烷基，杂芳基，杂芳基 - 烷基，杂环烷基，稠合的芳基 - 环烷基，稠合的芳基 - 环烷基 - 烷基，稠合的杂芳基 - 环烷基，稠合的杂芳基 - 环烷基 - 烷基，烷氧基烷基，烷基硫代烷基，烷基氨基 - 烷基或二烷基氨基烷基。 Y是羟基，烷氧基，氨基或取代的氨基，氨基烷酰基，芳氧基，氨基烷氧基或羟基烷氧基，R7是烷基，芳基，芳烷基，环烷基，环烷基 - 烷基，杂环基，-CO-SR，-CS-SR，其中R是氢，烷基或芳基，并且其中Y（CH 2 CO 2 R）， - 是羟基，它们的药学上可接受的，无毒的碱金属，碱土金属和胺盐。

5. 发明授权

US4239887A Pyridothienotriazines 失效
标题翻译：吡哆噻嗪三嗪
公开(公告)号：US4239887A
公开(公告)日：1980-12-16
申请号：US89853
申请日：1979-10-31
申请人： Raymond D. Youssefyeh , Jeffrey D. Wilson
发明人： Raymond D. Youssefyeh , Jeffrey D. Wilson
IPC分类号： A61K31/53 , A61P37/08 , C07D495/04 , C07D495/14 , C07D513/14
CPC分类号： C07D495/04 , C07D495/14
摘要： New pyridothienotriazines are described. These compounds are useful as anti-allergic reagents.
摘要翻译：描述了新的吡啶并噻吩三嗪。这些化合物可用作抗过敏试剂。

6. 发明授权

US5246942A Pharmaceutically useful dibenzofurancarboxamides of specific stereo-configuration 失效
标题翻译：具有特定立体结构的药学上有用的二苯并呋喃甲酰胺
公开(公告)号：US5246942A
公开(公告)日：1993-09-21
申请号：US887594
申请日：1992-05-29
申请人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla , John E. Airey , Scott I. Klein , Matthew R. Powers
发明人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla , John E. Airey , Scott I. Klein , Matthew R. Powers
IPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08 , C07D498/08
CPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08
摘要： This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinctic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.
摘要翻译：本发明涉及某些二苯并呋喃甲酰胺及其作为5HT3拮抗剂的用途，其具有独特的CNS，抗呕吐和胃原性活性，没有任何显着的D2受体结合性质。本发明还描述了其制备所需的新方法。

7. 发明授权

US4863921A Dibenzofurancarboxamides and their pharmaceutical compositions and methods 失效
标题翻译：二苯并呋喃甲酰胺及其药物组合物和方法
公开(公告)号：US4863921A
公开(公告)日：1989-09-05
申请号：US186824
申请日：1988-04-27
申请人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla
发明人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla
IPC分类号： C07D307/91 , A61K31/435 , A61K31/443 , A61K31/445 , A61P1/00 , A61P1/08 , C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08 , C07D491/08 , C07D498/08
CPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08
摘要： This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.

8. 发明授权

US4839367A Antihypertensive amide compounds 失效
标题翻译：抗高血压酰胺化合物
公开(公告)号：US4839367A
公开(公告)日：1989-06-13
申请号：US895107
申请日：1986-08-11
申请人： Raymond D. Youssefyeh , Howard Jones
发明人： Raymond D. Youssefyeh , Howard Jones
IPC分类号： A61K31/47 , C07D209/02 , C07D209/36 , C07D211/72
CPC分类号： A61K31/47 , C07D209/02 , C07D209/36 , C07D211/72
摘要： Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl,Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.2 CO.sub.2 R, wherein R is hydrogen, alkyl, or aryl, and where Y is hydroxy, their pharmaceutically acceptable, nontoxic alkali metal, alkaline earth metal, and amine salts.
摘要翻译：本发明提供了下式的抗高血压化合物：其中R1，R2，R3，R4，R5和R6是氢，烷基，烯基，炔基，苯基 - 烷基或环烷基，并且可以相同或不同，m是 0〜2的整数，n为0〜4的整数，M为烷基，炔基，环烷基，环烷基 - 烷基，多环烷基，多环烷基 - 烷基，芳基，芳烷基，杂芳基，杂芳基 - 烷基，杂环烷基，稠合芳基 - 环烷基，稠合芳基 - 环烷基 - 烷基，稠合的杂芳基 - 环烷基，稠合的杂芳基 - 环烷基 - 烷基，烷氧基烷基，烷硫基烷基，烷基氨基 - 烷基或二烷基氨基烷基，Y是羟基，烷氧基，氨基或取代氨基，氨基烷酰基，芳氧基，氨基烷氧基或羟基烷氧基，R7是烷基，芳基，芳烷基，环烷基，环烷基 - 烷基，杂环基，-CO-SR，-CS-SR，CH2COR，-CHM-CO2R，-CH2 -CO-SR，-CN， -CO-NH-CH 2 CO 2 R，IMA或-CO-CO 2 CO 2 R，其中R是氢，烷基或芳基，并且其中Y是羟基，药学上可接受的，无毒的碱金属，碱土金属和胺盐。

9. 发明授权

US4728668A Aryl and heteroaryl ethers as agents for the treatment of hypersensitive ailments 失效
标题翻译：芳基和杂芳基醚作为治疗过敏性疾病的药剂
公开(公告)号：US4728668A
公开(公告)日：1988-03-01
申请号：US877570
申请日：1986-06-23
申请人： Utpal R. Chakraborty , Raymond D. Youssefyeh
发明人： Utpal R. Chakraborty , Raymond D. Youssefyeh
IPC分类号： C07C43/23 , C07D215/14 , C07D257/04 , C07D309/22 , C07D401/12 , C07D405/12 , A61K31/36
CPC分类号： C07D257/04 , C07C43/23 , C07D215/14 , C07D309/22 , C07D401/12 , C07D405/12
摘要： The present invention is concerned with the therapeutic composition comprising as an active ingredient a compound of the formula:(R.sub.1)(R.sub.2) Ar--Z--M--Ar.sub.1 (R.sub.3)(R.sub.4) Iand salts thereof;whereinAr and Ar.sub.1 are independently phenyl, naphthyl or a nitrogen, oxygen, or sulfur heterocyclic ring;Z is an alkylene chain containing from 1 to 5 carbon atoms in the principal chain and up to a total of 10 carbon atoms;M is oxygen, sulfur, or NR.sub.5 ;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently H, lower alkyl, lower alkoxy, hydroxy, halo, trihalomethyl, hydroxy lower alkyl, carboxy, formyl, aryl, aryloxy, benzyloxy, lower alkanoyl, carboxy lower alkoxy, nitro, amino, lower alkylamino, dilower alkylamino, cyano, lower alkanoyloxy, carbamoyl, lower alkoxy-alkoxy, carbo-lower alkoxy-alkoxy, or tetrahydropyranylmethyl; andR.sub.5 is hydrogen or lower alkyl.
摘要翻译：本发明涉及包含下式化合物作为活性成分的治疗组合物：（R1）（R2）Ar-Z-M-Ar1（R3）（R4）I及其盐; 其中Ar和Ar 1独立地是苯基，萘基或氮，氧或硫杂环; Z是在主链中含有1至5个碳原子并且总共10个碳原子的亚烷基链; M是氧，硫或NR5; R 1，R 2，R 3和R 4各自独立地为H，低级烷基，低级烷氧基，羟基，卤素，三卤甲基，羟基低级烷基，羧基，甲酰基，芳基，芳氧基，苄氧基，低级烷酰基，羧基低级烷氧基，硝基，烷基氨基，二元烷基氨基，氰基，低级烷酰氧基，氨基甲酰基，低级烷氧基 - 烷氧基，碳 - 低级烷氧基 - 烷氧基或四氢吡喃基甲基; R5是氢或低级烷基。

10. 发明授权

US4920227A Benzobicyclic carboxamide 5-HT3 antagonists 失效
标题翻译：苯环双羧酰胺5-HT3拮抗剂
公开(公告)号：US4920227A
公开(公告)日：1990-04-24
申请号：US277611
申请日：1988-11-29
申请人： Jeffrey C. Pelletier , Raymond D. Youssefyeh , Henry F. Campbell
发明人： Jeffrey C. Pelletier , Raymond D. Youssefyeh , Henry F. Campbell
IPC分类号： C07D451/02 , C07D453/02
CPC分类号： C07D453/02 , C07D451/02
摘要： Certain specific substituted benzobicyclic carboxamides and their valuable use as 5-HT3 antagonists having CNS and gastric prokenetic activity void of any significant D.sub.2 receptor binding activity are disclosed.
摘要翻译：公开了某些特异性取代的苯并双环羧酰胺及其作为具有CNS的5-HT 3拮抗剂和没有任何显着的D2受体结合活性的胃发育活性的有价值的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式