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1. 发明授权

US4634710A Tricyclic imidazole derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US4634710A
公开(公告)日：1987-01-06
申请号：US720775
申请日：1985-04-08
申请人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
发明人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
IPC分类号： A61K31/4184 , A61K31/44 , A61K31/4427 , A61P1/04 , C07D213/06 , C07D213/127 , C07D213/26 , C07D213/68 , C07D213/89 , C07D317/00 , C07D401/12 , C07D491/04 , C07D491/056 , A61K31/415
CPC分类号： C07D213/06 , C07D213/26 , C07D213/68 , C07D213/89 , C07D401/12 , C07D491/04
摘要： Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl and R.sup.8 is hydrogen or lower alkyl, and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increased gastric acid secretion.
摘要翻译：式I的三环咪唑衍生物其中R 1和R 3之一是低级烷基，另一个是氢或低级烷基，R 2是低级烷基，n是数字0或1，A是R 4，R 5， R6和R7各自为低级烷基，R8为氢或低级烷基，并描述其酸加成盐。这些化合物可用作控制或预防溃疡和增加胃酸分泌的药剂。

2. 发明授权

US4981861A Tricyclic imidazole derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US4981861A
公开(公告)日：1991-01-01
申请号：US463879
申请日：1990-01-05
申请人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
发明人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
IPC分类号： A61K31/4184 , A61K31/44 , A61K31/4427 , A61P1/04 , C07D213/06 , C07D213/127 , C07D213/26 , C07D213/68 , C07D213/89 , C07D317/00 , C07D401/12 , C07D491/04 , C07D491/056
CPC分类号： C07D213/06 , C07D213/26 , C07D213/68 , C07D213/89 , C07D401/12 , C07D491/04
摘要： Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl land R.sup.8 is hydrogen nor lower alkyl,and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increaased gastric acid secretion.

3. 发明授权

US4599347A Tetrahydro-naphth (2.3-d) imidazole derivatives 失效
标题翻译：四氢 - 萘（2.3-d）咪唑衍生物
公开(公告)号：US4599347A
公开(公告)日：1986-07-08
申请号：US560699
申请日：1983-12-12
申请人： Anna Krasso , Henri Ramuz
发明人： Anna Krasso , Henri Ramuz
IPC分类号： C07D401/12 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07C37/20 , C07C45/00 , C07C45/68 , C07C205/06 , C07D209/08 , C07D231/10 , C07D235/02 , C07D235/28 , C07D317/46 , C07D319/08 , C07D401/14 , C07D487/04 , C07D491/04 , C07D491/056
CPC分类号： C07D235/02 , C07C205/06 , C07C205/45 , C07C37/50 , C07C45/00 , C07C45/68 , C07D209/08 , C07D231/10 , C07D317/46 , C07D319/08 , C07D487/04 , C07D491/04 , C07C2102/08 , Y10S514/926 , Y10S514/927
摘要： Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 to 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
摘要翻译：其中R 1为任选被低级烷基或低级烷氧基取代的2-吡啶基，n为0至1的整数，R 2为氢或低级烷基，R 3和R 4独立地为氢或低级烷基，A是下式的基团：其中m是整数2或3，R5，R6，R7和R8独立地是氢或低级烷基，R9是氢，R10 如果A为式-CH = CH-CH = CH-或 - （CH 2）4 - 的基团，则R 3和R 4中的至少一个为低级烷基，，及其药学上可接受的酸加成盐。式I的化合物抑制胃酸分泌并防止胃溃疡的形成。

4. 发明授权

US4554280A Pyridyl methyl thio or sulfinyl indeno(5,6-d)imidazoles 失效
标题翻译：吡啶基甲基硫代或亚磺酰基茚并（5,6-d）咪唑
公开(公告)号：US4554280A
公开(公告)日：1985-11-19
申请号：US560698
申请日：1983-12-12
申请人： Anna Krasso , Henri Ramuz
发明人： Anna Krasso , Henri Ramuz
IPC分类号： C07D401/12 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07C37/20 , C07C45/00 , C07C45/68 , C07C205/06 , C07D209/08 , C07D231/10 , C07D235/02 , C07D235/28 , C07D317/46 , C07D319/08 , C07D401/14 , C07D487/04 , C07D491/04 , C07D491/056
CPC分类号： C07D235/02 , C07C205/06 , C07C205/45 , C07C37/50 , C07C45/00 , C07C45/68 , C07D209/08 , C07D231/10 , C07D317/46 , C07D319/08 , C07D487/04 , C07D491/04 , C07C2102/08 , Y10S514/926 , Y10S514/927
摘要： Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
摘要翻译：其中R 1为任选被低级烷基或低级烷氧基取代的2-吡啶基，n为0或1的整数，R 2为氢或低级烷基，R 3和R 4独立地为氢或低级烷基，A是下式的基团：其中m是整数2或3，R5，R6，R7和R8独立地是氢或低级烷基，R9是氢，R10 如果A为式-CH = CH-CH = CH-或 - （CH 2）4 - 的基团，则R 3和R 4中的至少一个为低级烷基，，及其药学上可接受的酸加成盐。式I的化合物抑制胃酸分泌并防止胃溃疡的形成。

5. 发明授权

US4435406A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US4435406A
公开(公告)日：1984-03-06
申请号：US290032
申请日：1981-08-05
申请人： Anna Krasso , Henri Ramuz
发明人： Anna Krasso , Henri Ramuz
IPC分类号： C07D401/12 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07C37/20 , C07C45/00 , C07C45/68 , C07C205/06 , C07D209/08 , C07D231/10 , C07D235/02 , C07D235/28 , C07D317/46 , C07D319/08 , C07D401/14 , C07D487/04 , C07D491/04 , C07D491/056 , C07D491/14
CPC分类号： C07D235/02 , C07C205/06 , C07C205/45 , C07C37/50 , C07C45/00 , C07C45/68 , C07D209/08 , C07D231/10 , C07D317/46 , C07D319/08 , C07D487/04 , C07D491/04 , C07C2102/08 , Y10S514/926 , Y10S514/927
摘要： Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
摘要翻译：其中R 1为任选被低级烷基或低级烷氧基取代的2-吡啶基，n为0或1的整数，R 2为氢或低级烷基，R 3和R 4独立地为氢或低级烷基，A是下式的基团：其中m是整数2或3，R5，R6，R7和R8独立地是氢或低级烷基，R9是氢，R10 如果A为式-CH = CH-CH = CH-或 - （CH 2）4 - 的基团，则R 3和R 4中的至少一个为低级烷基，，及其药学上可接受的酸加成盐。式I的化合物抑制胃酸分泌并防止胃溃疡的形成。

6. 发明授权

US5389616A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5389616A
公开(公告)日：1995-02-14
申请号：US99028
申请日：1993-07-29
申请人： Quirico Branca , Werner Neidhart , Jenri Ramuz , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
发明人： Quirico Branca , Werner Neidhart , Jenri Ramuz , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
IPC分类号： C07C215/26 , C07C237/00 , C07C317/44 , C07D233/54 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12 , A61K37/00
CPC分类号： C07D233/64 , C07C215/26 , C07C237/00 , C07C317/44 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：其中A，R 1，R 2，R 3，R 4，R 5和R 6如上所述的式Ⅺ化合物被描述。式I的化合物对天然酶肾素具有抑制活性，因此可以以用于控制或预防高血压和心脏功能不全的药物制剂的形式使用。

7. 发明授权

US5302727A Multidrug resistance modifying dithianes 失效
标题翻译：多药耐药修饰二硫丹
公开(公告)号：US5302727A
公开(公告)日：1994-04-12
申请号：US914241
申请日：1992-07-15
申请人： James F. Eliason , Henri Ramuz , Franz A. Kaufmann-Schmid, deceased
发明人： James F. Eliason , Henri Ramuz , Franz A. Kaufmann-Schmid, deceased
IPC分类号： A61K31/385 , A61P33/02 , A61P35/00 , C07D339/08 , C07D409/04 , C07D409/12 , C07D409/14
CPC分类号： C07D409/04 , C07D339/08 , C07D409/12
摘要： Compounds of the formula ##STR1## wherein R is a residue of the formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and Z are as described, with the exception of rac-N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-.beta.,N-dimethyl-m-dithiane-2-propanamine, as well as their acid addition salts, in particular for use in eliminating cytostatic resistance in tumor treatment and chloroquine resistance in malaria.
摘要翻译：其中R是式的残基的化合物，其中R是R 1，R 2，R 3，R 4，R 5，R 6，R 7，X，Y和Z的残基，除了rac-N - （3,4-二甲氧基苯乙基）-2-（3,4-二甲氧基苯基）-β，N-二甲基-m-二噻烷-2-丙胺，以及它们的酸加成盐，特别是用于消除细胞生长抑制疟疾中的肿瘤治疗和氯喹抗性。

8. 发明授权

US5120759A Tetrahydronaphthalene derivatives for improving short-term memory 失效
标题翻译：用于改善短期记忆的四氢萘并噻唑衍生物
公开(公告)号：US5120759A
公开(公告)日：1992-06-09
申请号：US690408
申请日：1991-04-23
申请人： Urs Hengartner , Henri Ramuz
发明人： Urs Hengartner , Henri Ramuz
IPC分类号： A61K31/215 , A61K31/357 , A61K31/36 , A61P25/28 , A61P33/02 , A61P35/00 , C07C35/52 , C07C57/58 , C07C57/76 , C07C59/48 , C07C69/732 , C07C215/42 , C07C219/24 , C07C323/52 , C07D317/58 , C07D319/18
CPC分类号： C07C57/76 , C07C219/24 , C07C35/52 , C07C57/58 , C07D317/58 , C07D319/18 , C07C2102/10
摘要： Novel compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkylthio-lower-alkyl or furyl, R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylenedioxy or ethylenoxy and n is an integer from 1 to 3, have a pronounced activity in counteracting cerebral insufficiency or improving cognitive functions and also reduce the multiple-resistance towards cytostatics in the treatment of tumors or of chloroquine resistance in the treatment of malaria. They can accordingly be used as medicaments, especially for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions. The novel compounds of formula I can be manufactured by O-acylating a likewise novel compound of the formula ##STR2## wherein R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylendioxy or ethylenoxy and n is an integer from 1 to 3.
摘要翻译：下式的新型化合物其中R 1为低级烷基，低级烷氧基 - 低级 - 烷基，低级 - 烷硫基 - 低级 - 烷基或呋喃基，R 2为低级烷基，苯基 - 低级 - 烷基或环己基 - 低级 - 烷基，R 3和R 6各自独立地为氢或氟，R 4和R 5各自独立地为氢或低级烷氧基或一起为亚甲二氧基，亚乙二氧基或乙烯氧基，n为1至3的整数，在抵抗脑中具有明显的活性功能不全或提高认知功能，并且还可减少治疗疟疾时治疗肿瘤或氯喹抗药性细胞抑制剂的多重阻力。因此，它们可以用作药物，特别是用于控制或预防脑功能不全或改善认知功能。式I的新化合物可以通过O-酰化类似新颖的式II化合物来制备，其中R 2是低级烷基，苯基 - 低级烷基或环己基 - 低级烷基，R 3和R 6各自独立地是氢或氟，R 4和R 5各自独立地为氢或低级烷氧基或一起为亚甲二氧基，乙二氧基或亚乙氧基，n为1至3的整数。

9. 发明授权

US4360521A 7[3,6-Dihydro-1(2H)-p yridyl]-2-oxo-2H-[1,2,4]oxadiazolo[2,3-c]pyrimidine-5-carbamate compounds 失效
标题翻译： 7 [3,6-二氢-1（2H） - 吡啶基] -2-氧代-2H- [1,2,4]恶二唑并[2,3-c]嘧啶-5-氨基甲酸酯化合物
公开(公告)号：US4360521A
公开(公告)日：1982-11-23
申请号：US327384
申请日：1982-12-04
申请人： Urs Hengartner , Jean-Claude Muller , Henri Ramuz
发明人： Urs Hengartner , Jean-Claude Muller , Henri Ramuz
IPC分类号： A61K31/505 , C07D235/06 , C07D498/04 , C07D521/00 , C07D498/22
CPC分类号： C07D235/06 , A61K31/505 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.
摘要翻译：描述了其中R是烷基，烯基，炔基或烷氧基烷基的式[IMAGE] I的恶二唑并[2,3-c]嘧啶衍生物及其盐。式I的化合物具有有价值的，持久的血管扩张和/或降血压性质，并且可用于治疗血管性高血压或作为外周血供应障碍中的血管扩张剂。化合物特别是通过氨基甲酰化制备含有游离氨基和任选的盐形成的相应衍生物。

10. 发明授权

US4073797A Sulphur containing derivatives 失效
标题翻译：含硫衍生物
公开(公告)号：US4073797A
公开(公告)日：1978-02-14
申请号：US728668
申请日：1976-10-01
申请人： Henri Ramuz
发明人： Henri Ramuz
IPC分类号： C07C45/46 , C07D339/06 , C07D339/08
CPC分类号： C07D339/08 , C07C45/46 , C07D339/06
摘要： A novel class of dithiane and disulfone compound is described. These compounds are pharmaceutically active as coronary dilating agents and thus can be used therapeutically in cases of insufficient cardiac blood supply, i.e., in the treatment of angina pectoris. A preferred compound is N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-N-methyl-m-dithiane-2-propylamine-1,1-3,3-tetraoxide.
摘要翻译：描述了一种新型的二噻吩和二砜化合物。这些化合物作为冠状动脉扩张剂是药学活性的，因此可以在心脏血供不足的情况下，即治疗心绞痛的情况下治疗。优选的化合物是N-（3,4-二甲氧基苯乙基）-2-（3,4-二甲氧基苯基）-N-甲基-m-二噻烷-2-丙胺-1,1-33,3-四氧化物。

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