公开(公告)号：US4703125A

公开(公告)日：1987-10-27

申请号：US880752

申请日：1986-07-01

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 ,  C07D277/66

CPC分类号： C07D513/04 ,  Y10S514/869

摘要： A carbonyl compound 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, and X 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, or R.sup.1 and R.sup.2 together represent 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, and R.sup.4 represents hydrogen, trifluoromethyl or alkyl.These compounds are useful as intermediates in the preparation of alkene carboxamides which are useful as antihypertensives, diuretics and uricosuric agents.

公开(公告)号：US4588723A

公开(公告)日：1986-05-13

申请号：US634851

申请日：1984-07-26

申请人： Axel Ingendoh ,  Horst Meyer ,  Bernward Garthoff

发明人： Axel Ingendoh ,  Horst Meyer ,  Bernward Garthoff

IPC分类号： A61K31/41 ,  A61K31/445 ,  A61K31/535 ,  A61P7/10 ,  A61P9/12 ,  A61P19/06 ,  C07D513/04 ,  A61K31/425

CPC分类号： C07D513/04

摘要： The invention relates to aminoalkyl-imidazothiadiazole-alkenecarboxylic acid amides, processes for their preparation, intermediates which are used in their preparation, medicaments containing said active compounds for use as antihypertensive agents, diuretics and uricosuric agents. Also included in the invention are methods for use of said compounds and compositions for the above indicated indications. The active compounds are identified herein by formula (I) and the novel intermediates used in preparing the compounds of Formula (I) are those described herein under Formula (II).

摘要翻译： 本发明涉及氨基烷基 - 咪唑并噻二唑 - 烯烃羧酸酰胺，其制备方法，用于制备的中间体，含有用作抗高血压剂的活性化合物，利尿剂和尿酸营养剂的药物。 本发明还包括使用所述化合物和组合物用于上述适应症的方法。 活性化合物在本文中由式（I）鉴定，用于制备式（I）化合物的新中间体是本文在式（II）中所述的那些。

公开(公告)号：US4585873A

公开(公告)日：1986-04-29

申请号：US468737

申请日：1983-02-22

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 ,  C07D277/00 ,  C07D513/22

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 radicals 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，具有R1所示含义的R 8，X代表氧，硫或NR 9 R 10基团，其它具有各种定义的基团及其酸加成盐，表现为降血压活性。

公开(公告)号：US4444770A

公开(公告)日：1984-04-24

申请号：US263400

申请日：1981-05-13

申请人： Horst Meyer ,  Harald Horstmann ,  Eike Moller ,  Bernward Garthoff

发明人： Horst Meyer ,  Harald Horstmann ,  Eike Moller ,  Bernward Garthoff

IPC分类号： C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D277/60

CPC分类号： C07D487/04 ,  C07D513/04

摘要： The invention relates to imidazoazole-alkenoic acid amides of Formula (I) and methods for their production. Also included in the invention are compositions containing said alkenoic acid amides and methods for the use of said alkenoic acid amides and the compositions containing them. In addition, the invention includes the intermediate carbonyl compounds of Formula (II) and the intermediate alkenoic acids of Formula (V) as well as methods for their preparation.

摘要翻译： 本发明涉及式（I）的咪唑并 - 烯酸酰胺及其制备方法。 本发明还包括含有所述烯酸酰胺的组合物和使用所述烯酸酰胺的方法和含有它们的组合物。 此外，本发明包括式（II）的中间体羰基化合物和式（V）的中间体烯酸以及其制备方法。