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1. 发明授权

US4585772A Agents for combating circulatory illnesses and their use 失效
标题翻译：防治循环系统疾病及其用途的药剂
公开(公告)号：US4585772A
公开(公告)日：1986-04-29
申请号：US512582
申请日：1983-07-11
申请人： Bodo Junge , Siegfried Goldmann , Gunter Thomas , Bernward Garthoff
发明人： Bodo Junge , Siegfried Goldmann , Gunter Thomas , Bernward Garthoff
IPC分类号： A61K31/505 , A61P7/02 , A61P9/08 , A61P9/10 , C07D233/24 , C07D413/14 , C07D471/14 , C07D487/04 , C07D487/14 , A61K31/535
CPC分类号： C07D471/14 , C07C255/00 , C07D233/24 , C07D487/04
摘要： The invention relates to pharmaceutical compositions containing active ingredients of Formula (I) and methods for the use of said compositions to treat cardiac insufficiencies. Also included in the invention are methods of the manufacture of said active ingredients of Formula (I). The invention includes, additionally, compounds of Formula (I).
摘要翻译：本发明涉及含有式（I）的活性成分的药物组合物和使用所述组合物治疗心功能不全的方法。本发明还包括制备式（I）的所述活性成分的方法。另外，本发明还包括式（I）的化合物。

2. 发明授权

US4582840A 1,4-dihydro-2,6-dimethyl-4-nitrophenyl-3,5-pyridinedicarboxylic acid esters useful for treating renal insufficiency 失效
标题翻译：可用于治疗肾功能不全的1,4-二氢-2,6-二甲基-4-硝基苯基-3,5-吡啶二羧酸酯
公开(公告)号：US4582840A
公开(公告)日：1986-04-15
申请号：US726879
申请日：1985-04-25
申请人： Bernward Garthoff , Stanislav Kazda , Andreas Knorr , Gunter Thomas
发明人： Bernward Garthoff , Stanislav Kazda , Andreas Knorr , Gunter Thomas
IPC分类号： C07D211/90 , A61K31/44 , A61K31/455 , A61P7/10 , C07D213/55
CPC分类号： A61K31/44
摘要： A method of combating a disorder of the salt balance in a patient afflicted therewith comprising administering to such patient a salt-balance restoring effective amount of a vasodilating 1,4-dihydropyridine of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is alkyl with 1 to 4 carbon atoms, and the nitro radical is in the ortho- or meta-position of the phenyl radical.The salt balance disorder may accompany the hypertensive disease or may also be aggravated by administering to such a patient a hypertension reducing agent.
摘要翻译：一种防治患病患者的盐平衡紊乱的方法，其包括向所述患者施用盐平衡恢复有效量的式“IMAGE”的血管舒张性1,4-二氢吡啶，其中R 1和R 2各自独立地为烷基具有1至4个碳原子，并且硝基在苯基的邻位或间位。盐平衡障碍可伴随高血压疾病，或者也可通过向这样的患者施用高血压减轻剂而加重。

3. 发明授权

US4567188A Hypotensive 2-nitro-1,1-ethenediamines 失效
标题翻译：低血压2-硝基-1,1-乙烯二胺
公开(公告)号：US4567188A
公开(公告)日：1986-01-28
申请号：US522069
申请日：1983-08-10
申请人： Ekkehard Niemers , Andreas Knorr , Bernward Garthoff
发明人： Ekkehard Niemers , Andreas Knorr , Bernward Garthoff
IPC分类号： A61K31/04 , A61K31/13 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P9/08 , A61P9/12 , C07C67/00 , C07C209/00 , C07C209/22 , C07C211/29 , C07C211/44 , C07C211/52 , C07C215/76 , C07C217/84 , C07C323/36 , C07D213/38 , C07D213/40 , C07D213/74 , C07D213/75 , A61K31/135 , C07C87/60
CPC分类号： C07D213/74 , C07D213/38
摘要： Compounds of the formula ##STR1## in which R.sup.1 is an optionally substituted aryl or heteroaryl radical,R.sup.2 is an alkyl or alkenyl radical which is optionally substituted by alkoxy or cycloalkyl, or an optionally substituted aryl or heteroaryl radical, and X is an optionally aklyl-substituted methylene radical or a direct bond, but if X is a direct bond R.sup.2 is not aryl,or physiologically acceptable acid addition salts thereof, exhibit activity on the circulation system particularly as hypotensive agents.
摘要翻译：其中R 1为任选取代的芳基或杂芳基，R 2为任选被烷氧基或环烷基取代的烷基或烯基，或任选取代的芳基或杂芳基，且X为任选取代的烷基或烯基 - 取代的亚甲基或直接键，但是如果X是直接键，则R2不是芳基或其生理上可接受的酸加成盐，在循环系统上表现出特别是作为降压剂的活性。

4. 发明授权

US4659737A Substituted aminomethyl benzopyrans having anti-hypertensive activities 失效
标题翻译：具有抗高血压活性的取代的氨基甲基苯并吡喃
公开(公告)号：US4659737A
公开(公告)日：1987-04-21
申请号：US715434
申请日：1985-03-25
申请人： Hans-Joachim Kabbe , Ulrich Niewohner , Arno Widdig , Andreas Knorr , Bernward Garthoff , Stanislav Kazda
发明人： Hans-Joachim Kabbe , Ulrich Niewohner , Arno Widdig , Andreas Knorr , Bernward Garthoff , Stanislav Kazda
IPC分类号： A61K31/35 , A61K31/352 , A61K31/357 , A61K31/40 , A61K31/4025 , A61K31/495 , A61P9/00 , C07D311/58 , C07D311/96 , C07D317/00 , C07D405/12 , C07D407/12 , A61K31/355
CPC分类号： C07D405/12 , C07D311/58 , C07D311/96 , C07D407/12
摘要： Substituted benzopyrans of the formula ##STR1## in which --A-- is a single or double bond,X is a direct bond, optionally substituted methylene, oxygen or optionally substituted --NH--, and the various other radicals can have various meanings,or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.
摘要翻译：取代的苯并吡喃，其中-A-是单键或双键，X是直接键，任选取代的亚甲基，氧或任选取代的-NH-，并且各种其它基团可以具有各种含义或药学上具有抗高血压活性的可接受的加成盐。

5. 发明授权

US4657905A Novel hypotensive imidazothiadiazolealkanecarboxamides 失效
标题翻译：新型降压咪唑并噻二唑烷烃酰胺
公开(公告)号：US4657905A
公开(公告)日：1987-04-14
申请号：US789689
申请日：1985-10-21
申请人： Axel Ingendoh , Horst Meyer , Bernward Garthoff
发明人： Axel Ingendoh , Horst Meyer , Bernward Garthoff
IPC分类号： A61K31/415 , A61K31/445 , A61P7/10 , A61P9/12 , C07D513/04 , A61K31/41 , A61K31/535 , A61K31/55
CPC分类号： C07D513/04 , Y10S514/869
摘要： Imidazothiadiazolealkenecarboxamides of the formula ##STR1## in which R.sup.1 is hydrogen, aryl, substituted aryl or a cyclic or aliphatic hydrocarbon radical which is optionally interrupted by O, S, N, N-alkyl, N-aryl or N-aralkyl and which is optionally substituted,R.sup.8 having the meaning indicated for R.sup.1, andX representing oxygen, sulphur or the radical NR.sup.9 R.sup.10,the other radical having various definitions, and acid addition salts thereof, exhibit hypotensive activity.
摘要翻译：其中R 1是氢，芳基，取代的芳基或任选地被O，S，N，N-烷基，N-芳基或N-芳烷基中断的环状或脂族烃基的咪唑并噻二唑烯烃酰胺，其任选地取代的R 8具有R1表示的含义，X代表氧，硫或NR9R10基团，另一个具有不同定义的基团及其酸加成盐，表现为降血压活性。

6. 发明授权

US4703038A Combination of dihydropyridines with angiotensin converting enzymes-inhibitors 失效
标题翻译：二氢吡啶与血管紧张素转换酶抑制剂的组合
公开(公告)号：US4703038A
公开(公告)日：1987-10-27
申请号：US785182
申请日：1985-10-07
申请人： Bernward Garthoff , Stanislav Kazda , Andreas Knorr
发明人： Bernward Garthoff , Stanislav Kazda , Andreas Knorr
IPC分类号： C07D211/90 , A61K31/455 , A61K38/00 , A61K38/55 , A61P9/12 , A61K31/44 , A61K37/02 , C07C103/52
CPC分类号： A61K38/556
摘要： The invention concerns a combination of dihydropyridine derivatives with compounds which inhibit the formation of enzymes which control the conversion of angiotensin I into angiotensin II and their use as antihypertensive agents.
摘要翻译：本发明涉及二氢吡啶衍生物与抑制血管紧张素I转化为血管紧张素II的酶的形成的化合物的组合以及它们作为抗高血压药物的用途。

7. 发明授权

US4647579A Circulation active novel substituted 4-hydroxy-benzopyrans 失效
标题翻译：循环活性新型取代的4-羟基 - 苯并吡喃
公开(公告)号：US4647579A
公开(公告)日：1987-03-03
申请号：US714340
申请日：1985-03-21
申请人： Hans-Joachim Kabbe , Arno Widdig , Ulrich Niewohner , Andreas Knorr , Bernward Garthoff , Stanislav Kazda
发明人： Hans-Joachim Kabbe , Arno Widdig , Ulrich Niewohner , Andreas Knorr , Bernward Garthoff , Stanislav Kazda
IPC分类号： A61K31/35 , A61K31/352 , A61K31/357 , A61P9/00 , C07D311/22 , C07D311/96 , C07D317/00 , C07D407/12
CPC分类号： C07D311/96 , C07D311/22
摘要： Novel substituted 4-hydroxy-benzopyrans of the formula ##STR1## in which X is a single bond, ##STR2## and the other radicals can have various meanings, or pharmaceutically acceptable addition salts thereof, which are active on the circulation system.
摘要翻译：新颖的取代的4-羟基 - 苯并吡喃，其中X是单键，其它基团可以具有各种含义，或其药学上可接受的加成盐，其在循环系统上是有活性的。

8. 发明授权

US4621082A Pyridopyrimidines, pharmaceutical compositions and use 失效
标题翻译：吡啶并嘧啶，药物组合物和用途
公开(公告)号：US4621082A
公开(公告)日：1986-11-04
申请号：US816594
申请日：1986-01-07
申请人： Horst Meyer , Egbert Wehinger , Bernward Garthoff , Stanislav Kazda
发明人： Horst Meyer , Egbert Wehinger , Bernward Garthoff , Stanislav Kazda
IPC分类号： A61K31/435 , A61P7/10 , A61P9/08 , A61P13/02 , A61P15/00 , C07D211/90 , C07D471/04 , A61K31/505 , A61K31/535
CPC分类号： C07D471/04 , C07D211/90
摘要： Pyridopyrimidines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heterocyclic,exhibit circulation active properties, especially renal vasodilating and diuretic action.
摘要翻译：其中R1是任选取代的芳基或杂环的式“IMAGE”的吡啶并嘧啶具有循环活性，特别是肾血管扩张和利尿作用。

9. 发明授权

US4859665A Antihypertensive combination products containing a dihydropyridine and a pyridazodiazepine 失效
标题翻译：含有二氢吡啶和吡咯并二氮杂的抗高血压组合产品
公开(公告)号：US4859665A
公开(公告)日：1989-08-22
申请号：US937867
申请日：1986-12-02
申请人： Bernward Garthoff , Marcel Gerold , Fridolin Hefti , Stanislav Kazda , Andreas Knorr
发明人： Bernward Garthoff , Marcel Gerold , Fridolin Hefti , Stanislav Kazda , Andreas Knorr
IPC分类号： A61K31/50 , A61K31/55 , A61P9/12
CPC分类号： A61K31/55 , Y10S514/929
摘要： Compositions for treating hypertension comprising an effective amount of a dihydropyridine of the formula ##STR1## in which X is 1 or 2 identical or different substituents from the group consisting of nitro, chlorine and trifluoromethyl, or together with the phenyl ring, the group ##STR2## R.sup.1 is alkyl of 1 to 4 C atoms, which is optionally substituted by alkoxy of 1 to 4 C atoms,R.sup.2 is alkyl of 1 to 12 C atoms, which is optionally substituted by alkoxy of 1 to 3 C atoms, fluorine or N-methyl-N-benzylamino andR.sup.3 is alkyl of 1 to 4 C atoms, cyano or hydroxymethyl, and a pyridazodiazepine of the formula ##STR3## in which R.sup.4 is aralkyl,R.sup.5 is hydrogen or alkyl of 1 to 8 C atoms,R.sup.6 is hydrogen or alkyl of 1 to 8 C atoms andR.sup.7 and R.sup.8 are hydrogen, or together, an oxo group, are described.
摘要翻译：用于治疗高血压的组合物，其包含有效量的式“IMAGE”的二氢吡啶，其中X是与硝基，氯和三氟甲基相同或不同的取代基，或与苯环一起，组IMA IMA > R 1为1〜4个C原子的烷基，其任选被1〜4个C原子的烷氧基取代，R 2为1〜12个C原子的烷基，其任选被1〜3个C原子的烷氧基取代，氟或N - 甲基-N-苄基氨基，R3为1-4个C原子的烷基，氰基或羟甲基，以及其中R 4为芳烷基，R 5为氢或1至8个C原子的烷基的式“IMAGE”的吡咯并二氮杂为R6 氢或1〜8个碳原子的烷基，R7和R8为氢，或一起为氧代基。

10. 发明授权

US4709031A Imidazothiadiazolealkylene carboxylic acids 失效
公开(公告)号：US4709031A
公开(公告)日：1987-11-24
申请号：US884561
申请日：1986-07-11
申请人： Axel Ingendoh , Horst Meyer , Bernward Garthoff
发明人： Axel Ingendoh , Horst Meyer , Bernward Garthoff
IPC分类号： A61K31/415 , A61K31/445 , A61P7/10 , A61P9/12 , C07D513/04 , A61K31/425 , C07D285/12
CPC分类号： C07D513/04 , Y10S514/869
摘要： An alkenecarboxylic acid of the formula ##STR1## in which R.sup.1 denotes hydrogen, aryl, substituted aryl or a straight-chain or cyclic, saturated or unsaturated aliphatic hydrocarbon radical, which is optionally interrupted by O, S, N, N-alkyl, N-aryl or N-aralkyl, and which is optionally substituted by hydroxyl, alkoxy, alkyl, trifluoromethyl, halogen, phenyl, alkoxycarbonyl or dialkylamino, the two alkyl radicals together with the nitrogen atom optionally forming a 5 to 7-membered ring, which optionally contains a heteroatom from the group comprising O, S, NH or N-alkyl and these aforementioned alkyl and phenyl radicals in turn optionally being substituted by halogen, trifluoromethyl, alkyl, aryl, aralkyl, alkoxy, alkylmercapto or SO.sub.2 -alkyl,R.sup.2 represents the radical CXR.sup.8, R.sup.8 having the meaning indicated for R.sup.1 and being identical to or different from R.sup.1, andX representing oxygen, sulphur or the radical NR.sup.9 R.sup.10, R.sup.9 and R.sup.10 being identical or different and each having the meanings of R.sup.1 and being identical to or different from R.sup.1 ; or represents the radical SO.sub.n R.sup.11, n denoting 1 or 2 and R.sup.11 having the meaning indicated for R.sup.1 and being identical to or different from R.sup.1, orR.sup.1 and R.sup.2 together represents a group of the general formula .dbd.C(R.sup.12)(Y--R.sup.13), Y representing oxygen, sulphur, NH or N-alkyl, and R.sup.12 and R.sup.13 each having the meaning indicated for R.sup.1, being identical to or different from one another and R.sup.1, and optionally together forming, with inclusion of .dbd.C--Y, a 5 to 7-membered ring, which optionally contains a heteroatom from the group comprising O, S, NH or N-alkyl,R.sup.3 has the meaning indicated for R.sup.1 and is identical to or different from R.sup.1, or represents furyl, phenyl, thienyl, pyrimidyl, pyrazinyl, quinolinyl, isoquinolinyl or pyridyl, the rings optionally being substituted by 1, 2 or 3 identical or different substituents from the group comprising alkyl, aryl, alkoxy, halogen, nitro, trifluoromethyl, SO.sub.n -alkyl (n=0, 1 or 2) or NR.sup.9 R.sup.10, R.sup.9 and R.sup.10 having the meaning indicated above, R.sup.4 represents hydrogen, trifluoromethyl or alkyl, and R.sup.5 represents hydrogen, alkyl, cyano, halogen, nitro, SO.sub.n -alkyl (n=0, 1 or 2) or CXR.sup.8. These alkene carboxylic acids can be reacted with amine of the formula HNR.sup.6 R.sup.7 to give amides which are useful as antihypertnsives, diuretics and uricosuric agents.

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