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

US4088653A Tetrahydropyridyl derivatives 失效
标题翻译：四氢吡啶基衍生物
公开(公告)号：US4088653A
公开(公告)日：1978-05-09
申请号：US716676
申请日：1976-08-23
申请人： Edward E. Knaus , Kinfe Redda , Frank W. Wandelmaier
发明人： Edward E. Knaus , Kinfe Redda , Frank W. Wandelmaier
IPC分类号： C07D211/98 , C07D213/89 , C07D311/72 , C07D401/12 , A61K31/44
CPC分类号： C07D213/89 , C07D311/72 , Y10S514/866
摘要： Pharmaceutical compounds of the general formula ##STR1## and non-toxic pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen, lower alkyl having from 1 to 4 carbon atoms, lower alkoxy having from 1 to 4 carbon atoms and hydroxy lower alkyl having from 1 to 4 carbon atoms, and if R.sub.1 or R.sub.2 is other than hydrogen, the other substituent is hydrogen; and R.sub.3 is a member selected from the group consisting of pyridyl, phenyl, lower alkyl substituted pyridyl, lower alkoxy substituted pyridyl, lower alkyl substituted phenyl and lower alkoxy substituted phenyl, the lower alkyl and alkoxy substituents having from 1 to 4 carbon atoms. These compounds exhibit an analgesic, hyperglycemic or anti-inflammatory activity.
摘要翻译：通式为“IMAGE”的药物化合物及其无毒的药学上可接受的盐，其中R 1和R 2选自氢，具有1至4个碳原子的低级烷基，具有1至4个碳原子的低级烷氧基和具有1至4个碳原子的羟基低级烷基，如果R1或R2不是氢，另一个取代基是氢; 并且R 3是选自吡啶基，苯基，低级烷基取代的吡啶基，低级烷氧基取代的吡啶基，低级烷基取代的苯基和低级烷氧基取代的苯基的成员，低级烷基和烷氧基取代基具有1至4个碳原子。这些化合物表现出镇痛，高血糖或抗炎活性。

2. 发明授权

US4338445A N-(Carbonylamino)-tetrahydropyridyl derivatives 失效
标题翻译： N-（羰基氨基） - 四氢吡啶基衍生物
公开(公告)号：US4338445A
公开(公告)日：1982-07-06
申请号：US179249
申请日：1980-08-18
申请人： Edward E. Knaus , Linda A. Corleto , Kinfe Redda
发明人： Edward E. Knaus , Linda A. Corleto , Kinfe Redda
IPC分类号： C07D211/70 , C07D211/78 , C07D211/90 , C07D213/89
CPC分类号： C07D213/89 , C07D211/70 , C07D211/78 , C07D211/90
摘要： Pharmaceutical compounds of the general formula ##STR1## and non-toxic pharmaceutically-acceptable salts thereof wherein R.sup.1 is inter alia alkyl, cycloalkyl, aralkyl, or certain pyridyl or phenyl radicals, and with provisoR.sup.2 is selected from hydrogen, lower alkyl, lower alkoxy, amino, hydroxyl, halogen, carboxyl, amido, and --CON(lower alkyl).sub.2. Methods of preparing these compounds are described. The compounds exhibit analgesic, anti-inflammatory, hyperglycemic and/or hypoglycemic activity.
摘要翻译：通式为（IMAGE）（1）的药物化合物及其无毒的药学上可接受的盐，其中R 1特别是烷基，环烷基，芳烷基或某些吡啶基或苯基，条件是R2选自氢，低级烷基，低级烷氧基，氨基，羟基，卤素，羧基，酰氨基和-CON（低级烷基）2。描述了制备这些化合物的方法。该化合物显示镇痛，抗炎，高血糖和/或降血糖活性。

3. 发明申请

US20090186859A1 DIAZENIUMDIOLATED NON-STEROIDAL ANTI-INFLAMMATORY DRUGS, COMPOSITIONS THEREOF, AND RELATED METHODS 审中-公开
标题翻译：二氮芥非甾体抗炎药，其组合物及相关方法
公开(公告)号：US20090186859A1
公开(公告)日：2009-07-23
申请号：US12298322
申请日：2007-04-24
申请人： Carlos A. Velázquez , Joseph E. Saavedra , Larry Keefer , Brett Showalter , Edward E. Knaus
发明人： Carlos A. Velázquez , Joseph E. Saavedra , Larry Keefer , Brett Showalter , Edward E. Knaus
IPC分类号： A61K31/655 , C07C245/24 , A61P19/02
CPC分类号： C07D403/12 , C07D207/50
摘要： Disclosed are compounds that release nitric oxide, e.g., a compound of Formula (I) wherein R1-10, X, and n are as described herein, which are NSAID derivatives comprising a diazeniumdiolate moiety N2O2−. The compounds are chemopreventive agents with gastric-sparing, analgesic, cardioprotective, and/or anti-inflammatory properties. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed is a method of preventing or treating cancer or treating inflammation or an inflammation-related condition in a mammal comprising administering an effective amount of a compound of the invention to the mammal.
摘要翻译：公开了释放一氧化氮的化合物，例如其中R1-10，X和n如本文所述的式（I）化合物，其是包含二氮烯二硫酸盐部分N 2 O 2的NSAID衍生物。这些化合物是具有胃保存，镇痛，心脏保护和/或抗炎特性的化学预防剂。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。还公开了一种预防或治疗癌症或治疗哺乳动物的炎症或炎症相关病症的方法，包括向哺乳动物施用有效量的本发明化合物。

4. 发明授权

US4771057A Reduced pyridyl derivatives with cardiovascular regulating properties 失效
标题翻译：具有心血管调节特性的还原吡啶衍生物
公开(公告)号：US4771057A
公开(公告)日：1988-09-13
申请号：US824920
申请日：1986-02-03
申请人： Edward E. Knaus , Michael W. Wolowyk , Lina Dagnino , Moy C. Li-Kwong-Ken , Donald A. Soboleski , Hla Wynn
发明人： Edward E. Knaus , Michael W. Wolowyk , Lina Dagnino , Moy C. Li-Kwong-Ken , Donald A. Soboleski , Hla Wynn
IPC分类号： A61K31/455 , A61P9/12 , C07D211/90 , C07D401/04 , A61K31/44
CPC分类号： C07D401/04 , C07D211/90
摘要： Pharmaceutical compounds of the general formula (1): ##STR1## have been prepared and non-toxic pharmaceutically acceptable salts thereof, wherein the ring system is a 1,2- or 1,4-dihydropyridyl radical; R.sub.1 is a hydrogen, lower alkyl, lower alkyl carbonyl or lower alkoxy carbonyl substituent; R.sub.2 is a lower alkly or phenyl substituent; R.sub.3 is a lower alkoxy carbonyl, (N,N-lower dialkylamino) lower alkoxy carbonyl, (N-lower alkyl-N-phenyl lower alkyl amino) lower alkoxy carbonyl, lower alkoxy lower alkoxy carbonyl, nitro, or cyano substituent; R.sub.4 is a member selected from the group consisting of pyridyl, N-lower alkoxy carbonyl-1,2-dihydropyridyl, N-lower alkyl carbonyl-1,2-dihydropyridyl, N-phenyloxy carbonyl-1,2-dihydropyridyl, N-lower alkoxy carbonyl-1,6-dihydropyridyl, N-lower alkyl carbonyl-1,6-dihydropyridyl, N-lower alkyl carbonyl-1,6-dihydropyridyl, N-phenyloxy carbonyl-1,6-dihydropyridyl, N-lower alkoxy carbonyl-1,4-dihydropyridyl, N-lower alkyl carbonyl-1,4-dihydropyridyl, N-phenyloxy carbonyl-1,4-dihydropyridyl, N-lower alkyl 1,2,3,6-tetrahydropyridyl, N-lower alkoxy carbonyl-1,2,3,6-tetrahydropyridyl, N-lower alkyl carbonyl-1,2,3,6-tetrahydropyridyl, nitro substituted phenyl or trifluoromethyl substituted phenyl; R.sub.5 is a lower alkoxy carbonyl, (N,N-lower dialkylamino) lower alkoxy carbonyl, (N-lower alkyl-N-phenyl lower alkyl amino) lower alkoxy carbonyl, lower alkoxy lower alkoxy carbonyl, nitro, or cyano substitutent; R.sub.6 is a lower alkyl, or phenyl substituent, lower denoting a straight or branched chain having from 1-6 carbon atoms. These compounds regulate cardiovascular activity due to their ability to induce cerebral and peripheral vasodilation, decrease heart rate, and/or increase cardiac contractility, and are useful in the treatment of angina, arrhythmias, cerebralvascular disease and hypertension.

5. 发明申请

US20080214646A1 Novel Nsaids Possessing a Nitric Oxide Donor Diazen-1-Ium-1,2-Diolate Moiety 审中-公开
标题翻译：具有一氧化氮供体的新型Nsaids二氮烯-1-I-1,2-Diolate部分
公开(公告)号：US20080214646A1
公开(公告)日：2008-09-04
申请号：US11914430
申请日：2006-05-16
申请人： Edward E. Knaus , Carlos Velazquez
发明人： Edward E. Knaus , Carlos Velazquez
IPC分类号： A61K31/404 , C07C243/06 , A61K31/131 , C07D207/50 , A61P29/00 , A61K31/40 , C07D209/42
CPC分类号： C07D295/30 , C07C245/24 , C07D209/28 , C07D403/12
摘要： This invention provides a prodrug that help arthritis patients without increasing cardiovascular and gastrointestinal risk. A novel group of hybrid nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs), moiety attached via a one -carbon methylene spacer to the carboxylic acid group of the traditional NSAIDs aspirin, ibuprofen and indomethacin were synthesized. The ester prodrugs showed equipotent anti-inflammatory activities in vivo to that of the parent aspirin, ibuprofen and indomethacin. The simultaneous release of parent drug and nitric oxide from the NO- prodrugs constitutes a potentially beneficial property for the prophylactic prevention of thrombus formation and adverse cardiovascular events such as stroke and myocardial infarction. Data acquired in an in vivo ulcer index (UI) assay showed that this group of ester prodrugs in which no lesions were observed when compared to the parent drugs at equivalent doses. Accordingly, these hybrid NO-NSAID prodrugs possessing a diazen-1-ium-1,2-diolate moiety, represents a new approach for the rational design of anti-inflammatory drugs with reduced gastric ulcerogenicity.
摘要翻译：本发明提供一种前体药物，其可帮助关节炎患者不增加心血管和胃肠道风险。合成了一组新型的混合一氧化氮释放非甾体抗炎药（NO-NSAIDs），通过单碳亚甲基间隔物连接到传统NSAIDs阿司匹林，布洛芬和吲哚美辛的羧酸基上。酯前药在体内显示与母体阿司匹林，布洛芬和吲哚美辛的等效抗炎活性。母体药物和一氧化氮从NO前药同时释放构成预防性血栓形成和不良心血管事件如卒中和心肌梗塞的潜在有益的性质。在体内溃疡指数（UI）测定中获得的数据显示，与相同剂量的母体药物相比，这组酯前体药物没有观察到病变。因此，具有二氮嗪-1- ium-1,2-二醇化物部分的这些杂合NO-NSAID前药代表了胃溃疡发生率降低的抗炎药合理设计的新方法。

6. 发明授权

US4468403A Analgesic substituted piperidylidene-2-sulfon(cyan)amide derivatives 失效
标题翻译：镇痛取代的哌啶亚基-2-磺酸（青）酰胺衍生物
公开(公告)号：US4468403A
公开(公告)日：1984-08-28
申请号：US399994
申请日：1982-07-20
申请人： Edward E. Knaus , Brent K. Warren , Theodore A. Ondrus
发明人： Edward E. Knaus , Brent K. Warren , Theodore A. Ondrus
IPC分类号： C07D211/72 , C07D211/74 , C07D401/12 , A61K31/445
CPC分类号： C07D401/12 , C07D211/72 , C07D211/74
摘要： Pharmaceutical compounds of the general formula (1) have been prepared ##STR1## and non-toxic pharmaceutically acceptable salts thereof, wherein R.sub.1 is a lower alkyl, phenyl lower alkyl, amino substituted phenyl lower alkyl, nitro substituted phenyl lower alkyl, cycloalkyl lower alkyl or a lower alkenyl substituent, R.sub.2 is a member selected from the group consisting of a cyano, pyridylsulfonyl, lower alkyl substituted sulfonyl, phenylsulfonyl, lower alkyl substituted phenylsulfonyl, lower alkoxy substituted phenylsulfonyl, halogen substituted phenylsulfonyl, nitro substituted phenylsulfonyl, amino substituted phenylsulfonyl and lower alkyl amido substituted phenylsulfonyl; R.sub.3 is a hydrogen or halogen atom; and R.sub.4 is a hydrogen, lower alkyl or lower alkoxy substituent, lower denoting a straight or branched chain having from 1-4 carbon atoms. These compounds exhibit analgesic agonist activity or analgesic agonist-antagonist activities.
摘要翻译：制备通式（1）的药物化合物及其无毒的药学上可接受的盐，其中R 1为低级烷基，苯基低级烷基，氨基取代的苯基低级烷基，硝基取代的苯基低级烷基，环烷基低级烷基或低级烯基取代基，R2是选自氰基，吡啶基磺酰基，低级烷基取代的磺酰基，苯基磺酰基，低级烷基取代的苯基磺酰基，低级烷氧基取代的苯基磺酰基，卤素取代的苯基磺酰基，硝基取代的苯磺酰基，氨基取代的苯基磺酰基和低级烷基酰氨基取代的苯磺酰基; R3是氢或卤素原子; 并且R 4是氢，低级烷基或低级烷氧基取代基，较低表示具有1-4个碳原子的直链或支链。这些化合物表现出镇痛激动剂活性或镇痛激动剂 - 拮抗剂活性。

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