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1. 发明授权

US5145849A Indolylpropanols and preparations containing the compounds 失效
标题翻译：包含化合物的吲哚酚和制剂
公开(公告)号：US5145849A
公开(公告)日：1992-09-08
申请号：US637385
申请日：1991-01-03
申请人： Wolfgang Stenzel , Ben Armah
发明人： Wolfgang Stenzel , Ben Armah
IPC分类号： A61K31/40 , A61P9/00 , C07D401/14 , C07D403/12 , C07D409/14
CPC分类号： C07D403/12
摘要： Indolylpropanols of the formula I ##STR1## in which R.sup.1 and R.sup.2, which can be identical or different, in each case denote a 2-, 3- or 4-pyridinyl or a 2- or 3-thienyl radical, phenyl or phenyl which is optionally monosubstituted or identically or differently disubstituted by halogen, alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxy, where alkyl denotes straight-chain alkyl having 1 to 6 carbon atoms or branched alkyl having 3 to 6 carbon atoms, and their salts and acid addition salts, tautomers and optical isomers show positive inotropic and antiarrhythmic activity.
摘要翻译：式I的吲哚基丙醇（I）其中可以相同或不同的R 1和R 2各自表示2-，3-或4-吡啶基或2-或3-噻吩基，苯基或苯基，其任选被卤素，烷基，C 3-7 - 环烷基或C 1-6 - 烷氧基任意单取代或相同或不同二取代，其中烷基表示具有1至6个碳原子的直链烷基或具有3至6个碳原子的支链烷基，其盐和酸加成盐，互变异构体和旋光异构体显示出正性肌力和抗心律失常活性。

2. 发明授权

US5028711A Novel benzopyran derivatives, processes for their preparation and their use and preparations containing the compounds 失效
标题翻译：新型苯并吡喃衍生物，其制备方法及其用途和含有化合物的制剂
公开(公告)号：US5028711A
公开(公告)日：1991-07-02
申请号：US376328
申请日：1989-07-06
申请人： Wolfgang Stenzel , Theo Schotten , Ben Armah
发明人： Wolfgang Stenzel , Theo Schotten , Ben Armah
IPC分类号： C07D311/68 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/425 , A61K31/426 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/45 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/00 , C07D311/22 , C07D311/70 , C07D311/72 , C07D405/04 , C07D413/04 , C07D417/04 , C07D493/04
CPC分类号： C07D405/04 , C07D311/22 , C07D311/70 , C07D311/72 , C07D413/04 , C07D417/04 , C07D493/04
摘要： Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.
摘要翻译：公开了通式I（I）的苯并吡喃衍生物。这些化合物是治疗活性化合物。

3. 发明授权

US4594419A Substituted 5-phenylthio-6-amino-pyrimidinones, a process for their preparation and their use, and formulations containing these compounds 失效
公开(公告)号：US4594419A
公开(公告)日：1986-06-10
申请号：US503469
申请日：1983-06-13
申请人： Erich Cohnen , Ben Armah
发明人： Erich Cohnen , Ben Armah
IPC分类号： A61K31/505 , A61P3/00 , A61P7/10 , A61P9/12 , A61P19/06 , C07D239/56 , C07D239/60 , C07D239/10
CPC分类号： C07D239/56 , C07D239/60
摘要： Substituted 5-phenylthio-6-aminopyrimidinones of the general formula I ##STR1## in which R denotes an amino or hydroxyl group, and their tautomeric forms and acid addition salts thereof, have diuretic, saluretic and uricosuric actions. They can be used as medicaments for the treatment of hypertension, hyperuricemia and edemas.

4. 发明授权

US4935414A New indolylpropanols, processes for their preparation and their use, and preparations containing the compounds 失效
公开(公告)号：US4935414A
公开(公告)日：1990-06-19
申请号：US207997
申请日：1988-06-17
申请人： Wolfgang Stenzel , Ben Armah , Thomas Beuttler
发明人： Wolfgang Stenzel , Ben Armah , Thomas Beuttler
IPC分类号： C07D409/14 , A61K31/40 , A61K31/403 , A61K31/495 , A61K31/55 , A61P9/00 , A61P9/06 , A61P9/12 , C07D209/12 , C07D209/34 , C07D209/42 , C07D209/43 , C07D403/12 , C07D409/12
CPC分类号： C07D209/42 , C07D209/12 , C07D209/34
摘要： Substituted indolylpropanols of the formula I ##STR1## in which R.sup.1 denotes a cyano, carboxamido, alkoxycarbonyl, hydroxyl or acetyl group,Y stands for the group A ##STR2## wherein n is the number 2 or 3, or the group B, ##STR3## R.sup.2 stands for R.sup.2 ' where Y denotes the group A and for R.sup.2 " when Y denotes the group B, whereR.sup.2 ' denotes pyridinyl, thienyl or substituted phenyl which is monosubstituted or disubstituted by difluoromethoxy, difluoromethylthio, trifluoromethoxy, trifluoromethylthio, trifluoroethoxy, alkoxyalkoxy, cycloalkylalkoxy, alkoxyalkyl, alkylthioalkoxy, alkylsulphinylalkoxy, alkylsulphonylalkoxy, alkoxyalkylthio, alkoxyalkylsulphinyl, alkoxyalkylsulphonyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl and dialkylaminoalkoxy, andR.sup.2 " denotes pyridinyl, thienyl, phenyl or substituted phenyl which is monosubstituted or disubstituted by halogen, alkyl, cycloalkyl, alkoxy, difluoromethoxy, difluoromethylthio, trifluoromethoxy, trifluoromethylthio, trifluoroethoxy, alkoxyalkoxy, cycloalkylalkoxy, alkoxyalkyl, alkylthioalkoxy, alkylsulphinylalkoxy, alkylsulphonylalkoxy, alkoxyalkylthio, alkoxyalkylsulphinyl, alkoxyalkylsulphonyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl and dialkylaminoalkoxy, andR.sup.3 stands for R.sup.3 ' when Y denotes the group A and for R.sup.3 " when R denotes the group B, whereR.sup.3 ' denotes hydrogen, difluoromethoxy, difluoromethylthio, trifluoromethoxy, trifluoromethylthio, trifluoroethoxy, alkoxylalkoxy, alkoxyalkyl, alkylthioalkoxy, alkylsulphinylalkoxy, alkylsulphonylalkoxy, alkoxyalkylthio, alkoxyalkylsulphinyl, alkoxyalkylsulphonyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl or dialkylaminoalkoxy, andR.sup.3 " denotes hydrogen, alkoxy, halogen, difluoromethoxy, difluoromethylthio, trifluoromethoxy, trifluoromethylthio, trifluoroethoxy, alkoxyalkoxy, alkoxyalkyl, alkylthioalkoxy, alkylsulphinylalkoxy, alkylsulphonylalkoxy, alkoxyalkylthio, alkoxyalkylsulphinyl, alkoxyalkylsulphonyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl or dialkylaminoalkoxy,or a physiologically tolerable hydrolysable derivative thereof, in which the hydroxyl group in the 2-position of the 3-aminopropoxy side chain is present in esterified form, and also their tautomeric forms and their salts and also acid addition salts, where in all cases previously mentioned alkyl of the alkyl groups or of alkyl moieties or alkylene moieties of groups in each case denotes straight-chain or branched alkyl or alkylene having 1 to 6 carbon atoms and cycloalkyl has 3 to 7 carbon atoms, with the proviso that if R.sup.2 ' denotes pyridinyl or thienyl, R.sup.3 ' does not denote hydrogen, but one of the other R.sup.3 radicals mentioned show positive inotropic, vasodilatory and antiarrhythmic action and are suitable for the treatment of cardiac insufficiency, cardiac arrhythmias and hypertonia, coronary heart disease and peripheral and central arterial circulatory disturbances.

5. 发明授权

US4526897A Hypertensive isoindolin-2-yl-aminoimidazolines and isoindolin-2-yl-guanidines 失效
标题翻译：高血压异二氢吲哚-2-基 - 氨基咪唑啉和异吲哚啉-2-基 - 胍
公开(公告)号：US4526897A
公开(公告)日：1985-07-02
申请号：US407972
申请日：1982-08-13
申请人： Erich Cohnen , Ben Armah
发明人： Erich Cohnen , Ben Armah
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61P9/00 , A61P9/02 , C07D209/44 , C07D209/48 , C07D403/12
CPC分类号： C07D209/48 , C07D209/44
摘要： New isoindolin-2-yl-guanidines and isoindolin-2-yl-aminoimidazolines of the general formula ##STR1## in which R.sup.1 and R.sup.2 can be identical or different and either hydrogen or a halogen, alkyl, or alkoxy, each with 1 to 4 carbon atoms,R.sup.3 and R.sup.4 can be identical or different and either a hydrogen or an alkyl with 1 to 4 carbon atoms, andR.sup.5, R.sup.6, R.sup.7, and R.sup.8 can be identical or different and either hydrogen or an alkyl with 1 to 4 carbon atoms, or in whichR.sup.5 and R.sup.6 together represent the ethylene group,and their salts have an .alpha.-sympathomimetic and vasoconstrictive action that makes them appropriate as drugs for the treatment of hypotonic and rhinological states.
摘要翻译：新的异吲哚啉-2-基 - 胍和异吲哚啉-2-基 - 氨基咪唑衍生物，其中R 1和R 2可以相同或不同，或者是氢或卤素，烷基或烷氧基，各自具有 1至4个碳原子，R 3和R 4可以相同或不同，并且氢或具有1至4个碳原子的烷基，R 5，R 6，R 7和R 8可以相同或不同，并且氢或烷基与1 至4个碳原子，或者其中R 5和R 6一起代表亚乙基，并且它们的盐具有α-舒张模拟和血管收缩作用，使其适合用作治疗低渗和犀牛状态的药物。

6. 发明授权

US5096914A Novel benzopyran derivatives, processes for their preparation and their use and preparations containing the compounds 失效
标题翻译：新的苯并噻吩衍生物，其制备方法及其使用和制备化合物
公开(公告)号：US5096914A
公开(公告)日：1992-03-17
申请号：US620513
申请日：1990-11-30
申请人： Wolfgang Stenzel , Theo Schotten , Ben Armah
发明人： Wolfgang Stenzel , Theo Schotten , Ben Armah
IPC分类号： C07D311/68 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/425 , A61K31/426 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/45 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/00 , C07D311/22 , C07D311/70 , C07D311/72 , C07D405/04 , C07D413/04 , C07D417/04 , C07D493/04
CPC分类号： C07D405/04 , C07D311/22 , C07D311/70 , C07D311/72 , C07D413/04 , C07D417/04 , C07D493/04
摘要： Benzopyran derivatives of the general formula I ##STR1## wherein the substituents are as defined herein are provided. The compounds show vasodilating and vascular spasmolytic activity and are useful in treating hypertension.

7. 发明授权

US4777181A Alpha-2-antagonistic substituted 4-fluoro-isoindolines 失效
标题翻译： α-2-拮抗性取代的4-氟 - 异吲哚啉
公开(公告)号：US4777181A
公开(公告)日：1988-10-11
申请号：US942137
申请日：1986-12-16
申请人： Erich Cohnen , Ben Armah
发明人： Erich Cohnen , Ben Armah
IPC分类号： C07D403/12 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/535 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , A61P25/02 , A61P25/04 , A61P27/02 , A61P27/06 , C07D209/44 , C07D405/12
CPC分类号： A61K31/535 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/54
摘要： Substituted 4-fluoro-isoindolines of the general formula I ##STR1## in which R denotes hydrogen or an acyl group, and their tautomeric forms and their acid addition salts have an alpha.sub.2 -antagonistic action.
摘要翻译：其中R表示氢或酰基的通式I（I）的取代的4-氟 - 异吲哚啉及其互变异构形式及其酸加成盐具有α2-拮抗作用。

8. 发明授权

US4686223A Substituted 5-phenylthio-6-amino-pyrimidinones, a process for their preparation and their use, and formulations containing these compounds 失效
标题翻译：取代的5-苯硫基-6-氨基 - 嘧啶酮，其制备方法及其应用，以及含有这些化合物的制剂
公开(公告)号：US4686223A
公开(公告)日：1987-08-11
申请号：US804423
申请日：1985-12-04
申请人： Erich Cohnen , Ben Armah
发明人： Erich Cohnen , Ben Armah
IPC分类号： A61K31/505 , A61P3/00 , A61P7/10 , A61P9/12 , A61P19/06 , C07D239/56 , C07D239/60
CPC分类号： C07D239/56 , C07D239/60
摘要： Substituted 5-phenylthio-6-aminopyrimidinones of the general formula I ##STR1## in which R denotes an amino or hydroxyl group, and their tautomeric forms and acid addition salts thereof, have diuretic, saluretic and uricosuric actions. They can be used as medicaments for the treatment of hypertension, hyperuricemia and edemas.
摘要翻译：其中R表示氨基或羟基的通式I（I）的取代的5-苯硫基-6-氨基嘧啶酮及其互变异构形式及其酸加成盐具有利尿，盐析和尿酸作用。它们可以用作治疗高血压，高尿酸血症和水肿的药物。

9. 发明授权

US4323570A Substituted aminopyrimidines 失效
标题翻译：取代氨基嘧啶
公开(公告)号：US4323570A
公开(公告)日：1982-04-06
申请号：US92134
申请日：1979-11-07
申请人： Wolfgang Stenzel , Wolfgang Fleck , Erich Cohnen , Ben Armah
发明人： Wolfgang Stenzel , Wolfgang Fleck , Erich Cohnen , Ben Armah
IPC分类号： C07D239/30 , C07D239/36 , C07D239/42 , C07D239/20
CPC分类号： C07D239/30 , C07D239/36 , C07D239/42
摘要： The present invention is directed to certain aminopyrimidines of the general formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are hydrogen, halogen, alkoxy, alkylthio, or alkyl having 1 to 4 carbon atoms, or cycloalkyl having 3 to 5 carbon atoms and R.sup.4 is hydrogen or an aliphatic or aromatic acyl group, as well as physiologically compatible acid addition salts thereof. Compounds of the present invention are useful as blood pressure lowering agents and in the treatment of glaucoma.
摘要翻译：本发明涉及某些具有通式（I）的氨基嘧啶，其中R 1，R 2和R 3是氢，卤素，烷氧基，烷硫基或具有1至4个碳原子的烷基，或具有3至5个碳原子的环烷基原子和R 4是氢或脂族或芳族酰基，以及其生理上相容的酸加成盐。本发明的化合物可用作降压药和治疗青光眼。

10. 发明授权

US4318915A Substituted guandines and methods of preparation thereof 失效
标题翻译：取代的甘氨酸及其制备方法
公开(公告)号：US4318915A
公开(公告)日：1982-03-09
申请号：US167992
申请日：1980-07-14
申请人： Erich Cohnen , Ben Armah , Eva Hofferber
发明人： Erich Cohnen , Ben Armah , Eva Hofferber
IPC分类号： A61K31/155 , A61P9/12 , C07C57/58 , C07C57/76 , C07C59/64 , C07C279/22 , C07C335/38 , C07D233/48 , C07C129/12
CPC分类号： C07D233/48 , C07C279/22 , C07C335/38 , C07C57/58 , C07C57/76 , C07C59/64
摘要： A compound of the formula ##STR1## wherein R.sup.1 is chlorine, bromine, or methoxy; and R.sup.2, R.sup.3, and R.sup.4 are individually hydrogen or methyl, at least one of R.sup.2, R.sup.3, and R.sup.4 being hydrogen; or R.sup.2 and R.sup.3 together are an ethylene group and R.sup.4 is hydrogen, or a pharmaceutically acceptable acid addition salt thereof. Such compounds are useful as anti-hypertensive agents. Methods of preparation and certain novel intermediates are also disclosed.
摘要翻译：式IMA的化合物，其中R 1是氯，溴或甲氧基; R2，R3和R4分别为氢或甲基，R2，R3和R4中的至少一个为氢; 或R 2和R 3一起为亚乙基，R 4为氢，或其药学上可接受的酸加成盐。这些化合物可用作抗高血压药。还公开了制备方法和某些新型中间体。

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