公开(公告)号：US5414020A

公开(公告)日：1995-05-09

申请号：US160453

申请日：1993-12-01

申请人： Harold Heller ,  Friedrich Werner ,  Alfred Mitschker ,  Axel Ingendoh

发明人： Harold Heller ,  Friedrich Werner ,  Alfred Mitschker ,  Axel Ingendoh

IPC分类号： B01J41/14 ,  C08F8/00 ,  C08F8/32 ,  B01J41/08 ,  B01J41/12

CPC分类号： B01J41/14 ,  C08F8/32

摘要： According to the process according to the invention for the preparation of anion exchange resins of the poly(meth)acrylamide type by aminolysis of bead polymers of cross-linked poly(meth)acrylic acid esters with excess polyamine, subsequent separation of the anion exchange resins from the liquid phase containing the unreacted polyamine, washing the anion exchangers free of amine with water and recovering the polyamines from the washing waters, the liquid phase containing the unreacted polyamine and the polyamine-containing washing waters are immediately mixed with the bead polymer of cross-linked poly(meth)acrylic acid ester to be subjected to aminolysis, the amount of fresh polyamine necessary for the establishment of the desired polyamine excess is added to the mixture, the mixture thus obtained is distillatively dewatered until its water content has fallen to a value of

摘要翻译： 根据本发明的制备聚（甲基）丙烯酰胺型阴离子交换树脂的方法，通过交联聚（甲基）丙烯酸酯与多余多胺的珠粒聚合物的分解，随后分离阴离子交换树脂 从含有未反应的多胺的液相中，用水洗涤不含胺的阴离子交换剂并从洗涤水中回收多胺，将含有未反应的多胺和含多胺洗涤水的液相立即与交叉的珠聚合物 连接的聚（甲基）丙烯酸酯进行氨解，将所需多胺过量所需的新鲜多胺的量加入混合物中，将得到的混合物进行蒸馏脱水，直到其含水量降至 值为<7重量％，并且在该蒸馏脱水后残留的混合物在该溶液中进行氨解 玛丽的样子

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.

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。