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1. 发明授权

US5371227A Quinoline derivatives, process for their preparation, and their therapeutic applications 失效
标题翻译：喹啉衍生物，其制备方法及其治疗应用
公开(公告)号：US5371227A
公开(公告)日：1994-12-06
申请号：US39828
申请日：1993-03-30
申请人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
发明人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
IPC分类号： C07D215/12 , C07D401/14
CPC分类号： C07D401/14 , C07D215/12
摘要： The present invention provides a compound which is a quinoline derivative of the formula (I) ##STR1## in which R.sub.1 represents either 1H-tetrazol-5-yl, or CO.sub.2 H,R.sub.2 represents either (C.sub.1-7)alkyl or (C.sub.2-6)alkenyl,R.sub.3 and R.sub.4 represent, independently of each other, hydrogen, halogen, cyano group, (C.sub.1-7)alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-4)alkyl, aryl, aryl(C.sub.1-4)alkyl, aryl(C.sub.2-6)alkenyl, --(CH.sub.2).sub.m --COR.sub.5 in which m=0 to 4 and R.sub.5 represents hydrogen, --OH, --(C.sub.1-6)alkoxy, or --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 representing, independently of each other, hydrogen or --(C.sub.1-4)alkyl group, or a --(CH.sub.2).sub.n --R.sub.6 group in which n=1 to 4 and R.sub.6 represents --OH, --(C.sub.1-6)alkoxy, --(C.sub.1-4)alkoxy --(C.sub.1-4)alkoxy, or (C.sub.3-7)cycloalkyl(C.sub.1-4)alkoxy group, or a pharmaceutically acceptable salt thereof and their therapeutic applications.
摘要翻译：本发明提供一种化合物，其为式（I）的喹啉衍生物，其中R 1表示1H-四唑-5-基或CO 2 H，R 2表示（C 1-7）烷基或（ C2-6）烯基，R3和R4彼此独立地表示氢，卤素，氰基，（C1-7）烷基，（C3-7）环烷基（C1-4）烷基，芳基，芳基（C1-4 ）烷基，芳基（C2-6）烯基， - （CH2）m-COR5，其中m = 0至4，R5表示氢，-OH， - （C1-6）烷氧基或-NR7R8，R7和R8表示，氢或 - （C1-4）烷基或其中n = 1-4的R6为R6，R6为-OH的 - （CH2）n-R6基， - （C1-6）烷氧基， - （C1 -4）烷氧基 - （C 1-4）烷氧基或（C 3-7）环烷基（C 1-4）烷氧基或其药学上可接受的盐及其治疗应用。

2. 发明授权

US5432283A Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US5432283A
公开(公告)日：1995-07-11
申请号：US295469
申请日：1994-08-25
申请人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
发明人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
IPC分类号： C07D215/12 , C07D401/14 , C07D403/10 , C07D215/16
CPC分类号： C07D401/14 , C07D215/12
摘要： The present invention provides a compound which is a quinoline derivative of the formula (I) ##STR1## in which R.sub.1 represents either 1H-tetrazol-5-yl, or CO.sub.2 H,R.sub.2 represents either (C.sub.1-7)alkyl or (C.sub.2-6)alkenyl,R.sub.3 and R.sub.4 represent, independently of each other, hydrogen, halogen, cyano group, (C.sub.1-7)alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-4)alkyl, aryl, aryl(C.sub.1-4)alkyl, aryl(C.sub.2-6)alkenyl, --(CH.sub.2).sub.m --COR.sub.5 in which m=0 to 4 and R.sub.5 represents hydrogen, --OH, --(C.sub.1-6)alkoxy, or --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 representing, independently of each other, hydrogen or --(C.sub.1-4)alkyl group, or a --(CH.sub.2).sub.n --R.sub.6 group in which n=1 to 4 and R.sub.6 represents --OH, --(C.sub.1-6)alkoxy, --(C.sub.1-4)alkoxy(C.sub.1-4)alkoxy, or (C.sub.3-7)cycloalkyl(C.sub.1-4)alkoxy group, or a pharmaceutically acceptable salt thereof and their therapeutic applications.
摘要翻译：本发明提供一种化合物，其为式（I）的喹啉衍生物，其中R 1表示1H-四唑-5-基或CO 2 H，R 2表示（C 1-7）烷基或（ C2-6）烯基，R3和R4彼此独立地表示氢，卤素，氰基，（C1-7）烷基，（C3-7）环烷基（C1-4）烷基，芳基，芳基（C1-4 ）烷基，芳基（C2-6）烯基， - （CH2）m-COR5，其中m = 0至4，R5表示氢，-OH， - （C1-6）烷氧基或-NR7R8，R7和R8表示，氢或 - （C1-4）烷基或其中n = 1-4的R6为R6，R6为-OH的 - （CH2）n-R6基， - （C1-6）烷氧基， - （C1 -4）烷氧基（C 1-4）烷氧基或（C 3-7）环烷基（C 1-4）烷氧基或其药学上可接受的盐及其治疗应用。

3. 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。

4. 发明授权

US4187124A Process for doping semiconductors 失效
标题翻译：掺杂半导体工艺
公开(公告)号：US4187124A
公开(公告)日：1980-02-05
申请号：US887076
申请日：1978-03-15
申请人： Jean-Claude Muller , Jean-Pierre Ponpon , Joseph Kurek , Paul Siffert
发明人： Jean-Claude Muller , Jean-Pierre Ponpon , Joseph Kurek , Paul Siffert
IPC分类号： C30B31/22 , H01J37/317 , H01L21/265 , H01L21/263 , H01J37/30
CPC分类号： H01J37/3171 , C30B31/22 , H01L21/265 , H01L21/26513 , Y10S438/961
摘要： A process and apparatus for doping a substrate by ion implantation or discharge. The process comprises the steps of maintaining an electric discharge in an evacuated enclosure containing a gaseous compound of a dopant for creating ions of said dopant; extracting and accelerating a beam of said ions from said atmosphere toward said substrate under a voltage selected for achieving a predetermined doping profile; and circulating said substrate transversely to said beam.
摘要翻译：用于通过离子注入或放电掺杂衬底的工艺和装置。该方法包括以下步骤：在包含掺杂剂的气体化合物的真空外壳中保持放电，以产生所述掺杂剂的离子; 在选择用于实现预定掺杂分布的电压下，将所述离子束从所述气氛中提取并加速到所述衬底; 并使所述衬底横向于所述光束循环。

5. 发明授权

US4549019A Pyrimidinecarbamate derivatives as intermediates 失效
标题翻译：嘧啶甲酸衍生物作为中间体
公开(公告)号：US4549019A
公开(公告)日：1985-10-22
申请号：US394392
申请日：1982-07-01
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： C07D239/48 , C07D401/04 , C07D498/04 , C07D239/34
CPC分类号： C07D239/48 , C07D401/04
摘要： 2,4-Disubstituted 6-[3,6-dihydro-1(2H)-pyridyl]pyrimidine-3-oxides of the formula ##STR1## wherein R.sup.1 is lower alkyl or lower alkoxy-lower alkyl, R.sup.2 is hydrogen or --COOR.sup.3 wherein R.sup.3 is lower alkyl or lower alkoxy-lower alkyl,which are important for the preparation of therapeutically valuable 1,2,5,6-tetrahydropyridyl-substituted 2-oxo-2H-[1,2,4]oxadiazolopyrimidinecarbamates, are described. The foregoing oxides of formula I can be prepared by reacting the corresponding arylsulfonyloxy- or alkylsulfonyl-substituted derivatives with 1,2,5,6-tetrahydropyridine.
摘要翻译： 2,4-二取代的6- [3,6-二氢-1（2H） - 吡啶基]嘧啶-3-氧化物，其中R1是低级烷基或低级烷氧基 - 低级烷基，R2是氢或 - 描述了对于制备治疗有价值的1,2,5,6-四氢吡啶基取代的2-氧代-2H- [1,2,4]恶二唑并嘧啶碳酸氢盐重要的低级烷基或低级烷氧基 - 低级烷基的COOR 3 。上述式I的氧化物可以通过使相应的芳基磺酰氧基或烷基磺酰基取代的衍生物与1,2,5,6-四氢吡啶反应来制备。

6. 发明授权

US4336380A Oxadiazolotriazine derivatives 失效
标题翻译：恶二唑三嗪衍生物
公开(公告)号：US4336380A
公开(公告)日：1982-06-22
申请号：US234538
申请日：1981-02-17
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： C07D211/98 , C07D251/66 , C07D498/04
CPC分类号： C07D211/98 , C07D251/66
摘要： Oxadiazolotriazine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, are described.A process for preparing compounds of formula I wherein R.sup.1 is hydrogen, R.sup.2 is a group of the formula --COOR.sup.5, wherein R.sup.5 is as hereinafter set forth, and R.sup.3 is as hereinafter set forth, by cyclizing an intermediate of the formula ##STR2## wherein R.sup.3 and R.sup.5 are as hereinafter set forth, is also described. The compounds of formula I are useful in the treatment of vascular-condition hypertension or also as vasodilators in the case of peripheral blood supply disorders.
摘要翻译：其中R 1，R 2和R 3如下文所述，式ⅩⅧ的恶二唑三嗪衍生物被描述。制备式I化合物的方法，其中R 1是氢，R 2是式-COOR 5的基团，其中R 5如下文所述，并且R 3如下文所述，通过使式IV的中间体环化其中R3和R5如下文所述。式I化合物可用于治疗血管状态性高血压或在外周血供应障碍的情况下用作血管扩张剂。

7. 发明授权

US4150132A Oxadiazolopyrimidine derivatives 失效
标题翻译：恶二唑嘧啶衍生物
公开(公告)号：US4150132A
公开(公告)日：1979-04-17
申请号：US873182
申请日：1978-01-27
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： A61K31/505 , A61P9/08 , A61P9/12 , C07D498/04 , C07D498/22
CPC分类号： C07D498/04
摘要： Alkyl or alkoxyalkyl 5-[3,6-dihydro-1(2H)-pyridyl]-2-oxo-2H-[1,2,4]-oxadiazolo-[2,3-a]primidine-7-carbamates, prepared, inter alia, from the corresponding 6-[3,6-dihydro-1(2H)-pyridyl]-2,4-pyrimidine-dicarbamate-3-oxide, are described. The end products are useful in the treatment of vascular-conditioned hypertension or as vasodilators in the case of peripheral blood supply disorders.
摘要翻译： 5- [3,6-二氢-1（2H） - 吡啶基] -2-氧代-2H- [1,2,4] - 恶二唑并[2,3-a]脒基-7-氨基甲酸酯的烷基或烷氧基烷基酯，描述了由相应的6- [3,6-二氢-1（2H） - 吡啶基] -2,4-嘧啶二氨基甲酸酯-3-氧化物制备的。最终产品在外周血供给障碍的情况下可用于治疗血管性高血压或作为血管扩张剂。

8. 发明授权

US4743599A 1,5-benzothiazepine derivatives and compositions containing them 失效
标题翻译： 1,5-苯并硫氮杂衍生物和含有它们的组合物
公开(公告)号：US4743599A
公开(公告)日：1988-05-10
申请号：US38152
申请日：1987-04-14
申请人： Jean-Claude Muller , Andre Dumas
发明人： Jean-Claude Muller , Andre Dumas
IPC分类号： A61K31/55 , A61K31/554 , A61P3/00 , A61P9/00 , A61P25/24 , A61P25/26 , C07D281/10 , C07D417/06
CPC分类号： C07D281/10
摘要： Compounds which are 1,5-benzothiazepine derivatives of general formula (I) ##STR1## in which R denotes hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.1 and R.sub.2 either separately denote C.sub.1 -C.sub.4 alkyl groups or together denote a tetramethylene or pentamethylene group and their acid addition salts are therapeutically active as calcium antagonists.
摘要翻译：作为通式（I）的1,5-苯并硫氮杂衍生物的化合物，其中R表示氢或C1-C4烷基，R1和R2分别表示C1-C4烷基或一起表示四亚甲基或五亚甲基并且它们的酸加成盐作为钙拮抗剂是治疗活性的。

9. 发明授权

US4410698A Oxadiazolopyrimidine derivatives 失效
标题翻译：恶二唑嘧啶衍生物
公开(公告)号：US4410698A
公开(公告)日：1983-10-18
申请号：US407870
申请日：1982-08-13
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

US4276417A Oxadiazolotriazine derivatives 失效
标题翻译：恶二唑三嗪衍生物
公开(公告)号：US4276417A
公开(公告)日：1981-06-30
申请号：US61068
申请日：1979-07-26
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： C07D211/98 , C07D251/66 , C07D498/04
CPC分类号： C07D211/98 , C07D251/66
摘要： Oxadiazolotriazine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, are described. The compounds of formula I are useful in the treatment of vascular-condition hypertension or also as vasodilators in the case of peripheral blood supply disorders.
摘要翻译：其中R 1，R 2和R 3如下文所述，式ⅩⅧ的恶二唑三嗪衍生物被描述。式I化合物可用于治疗血管状态性高血压或在外周血供应障碍的情况下用作血管扩张剂。

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