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1. 发明授权

US4931429A .alpha.-aminoacyl .beta.-aminoacyl aminodiols as anti-hypertensive agents 失效
标题翻译： α-氨基酰基β-氨基酰基氨基二醇作为抗高血压药
公开(公告)号：US4931429A
公开(公告)日：1990-06-05
申请号：US103615
申请日：1987-10-01
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31/395 , A61K31/16 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/46 , A61K31/47 , A61K31/535 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61P9/12 , A61P43/00 , C07C67/00 , C07C237/00 , C07C237/12 , C07C237/20 , C07C237/22 , C07C237/36 , C07C253/00 , C07C255/60 , C07C271/06 , C07D207/08 , C07D207/12 , C07D209/08 , C07D209/10 , C07D209/30 , C07D209/44 , C07D215/08 , C07D233/64 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D263/04 , C07D265/30 , C07D265/36 , C07D277/06 , C07D279/04 , C07D279/16 , C07D295/20 , C07D451/02 , C07D498/08 , C12N9/99
CPC分类号： A61K31/16 , C07C237/00 , C07C271/06 , Y10S530/86
摘要： Compounds characterized generally as .alpha.-aminoacyl .beta.-aminoactyl aminodiols are useful as renin inhibitors for the treatment of hypertension.

2. 发明授权

US4925969A Process for preparing ethyl-alpha-amino-gamma-oxo-gamma-phenybutyrate derivatives 失效
标题翻译：制备乙基-γ-氨基-γ-氧代-γ-苯基丁酸酯衍生物的方法
公开(公告)号：US4925969A
公开(公告)日：1990-05-15
申请号：US324497
申请日：1989-03-16
申请人： Satomi Takahashi , Yasuyoshi Ueda , Kazuhiko Yamada , Yukio Yamada , Takehiko Yamane , Yoshifumi Yanagita , Yoshio Shimada , Kiyoshi Watanabe , Michio Nomura , Takehisa Ohashi , Kenji Inoue
发明人： Satomi Takahashi , Yasuyoshi Ueda , Kazuhiko Yamada , Yukio Yamada , Takehiko Yamane , Yoshifumi Yanagita , Yoshio Shimada , Kiyoshi Watanabe , Michio Nomura , Takehisa Ohashi , Kenji Inoue
IPC分类号： C07C227/08 , C07C233/46 , C07C271/06
CPC分类号： C07C233/46 , C07C227/08 , C07C271/06
摘要： Ethyl-.beta.-benzoyacrylate is reacted with an alkali metal salt of (S)-alanine or an alkali metal salt of N.sup.6 -trifluoroacetyl-L-lysine to form the corresponding Michael addition product, and not less than an equivalent amount of acid is added after completion of the Michael addition to prevent conversion of the (S,S) form of the product to the (R,S) form.
摘要翻译：乙基-β-苯甲酸酯与（S） - 丙氨酸的碱金属盐或N6-三氟乙酰基-L-赖氨酸的碱金属盐反应形成相应的迈克尔加成产物，加入不少于等量的酸完成迈克尔加成以防止（S，S）形式的产物转化为（R，S）形式。

3. 发明授权

US4883903A Novel procedure for the preparation of activated nitrosocarbamates 失效
标题翻译：用于制备活性亚硝基氨基甲酸酯的新方法
公开(公告)号：US4883903A
公开(公告)日：1989-11-28
申请号：US184915
申请日：1988-04-22
申请人： Pierre Roger , Jean-Paul Fournier , Rolande Leroy
发明人： Pierre Roger , Jean-Paul Fournier , Rolande Leroy
IPC分类号： C07C281/02 , C07C67/00 , C07C239/00 , C07C271/06
CPC分类号： C07C271/06
摘要： The subject of the invention is a novel procedure for the preparation of the compounds of formula I: ##STR1## in which n varies in particular from 2 to 5 and R represents Cl, Br or FZ represents in particular hydrogen, characterized in that the halogenoformate of formula II: ##STR2## R and n having the meanings indicated above, Y representing a halogen, is made to react with NH.sub.2 CH.sub.2 CH.sub.2 Cl to form the compound of formula Ia: ##STR3## in which R has the meanings indicated above, and in that the compound Ia is treated directly with nitrosylsulfuric acid.
摘要翻译：本发明的主题是制备式I化合物的新方法：其中n特别从2至5变化，R表示Cl，Br或FZ特别表示氢，其特征在于卤代甲酸酯式II的化合物：将具有上述含义的Y表示卤素的Y与NH 2 CH 2 CH 2 Cl反应形成式Ia化合物：其中R具有上述含义，其中化合物Ia直接用亚硝酰基硫酸处理。

4. 发明授权

US4709073A Process for the preparation of urethanes 失效
标题翻译：制备聚氨酯的方法
公开(公告)号：US4709073A
公开(公告)日：1987-11-24
申请号：US744951
申请日：1985-06-17
申请人： John H. Grate , David R. Hamm
发明人： John H. Grate , David R. Hamm
IPC分类号： B01J23/46 , B01J31/20 , C07C271/06 , C07C125/065 , C07C125/073
CPC分类号： C07C271/06
摘要： A process for preparing urethanes by reacting a solution of a nitrogen-containing organic compound and a hydroxyl-containing organic compound with carbon monoxide in the presence of a catalyst comprising rhodium, as a metal or compound, and essentially free of redox-active metal halide components is disclosed. In the process of this invention, the rate of conversion and selectivity to urethane is increased by providing a primary amine in the reaction solution.
摘要翻译：一种通过使含氮有机化合物和含羟基的有机化合物的溶液与一氧化碳在催化剂存在下制备聚氨酯的方法，所述催化剂包含铑作为金属或化合物，并且基本上不含氧化还原活性金属卤化物公开了组件。在本发明的方法中，通过在反应溶液中提供伯胺来提高转化率和对氨基甲酸酯的选择性。

5. 发明授权

US4694097A Carbamate ester production 失效
标题翻译：氨基甲酸酯生产
公开(公告)号：US4694097A
公开(公告)日：1987-09-15
申请号：US856665
申请日：1986-04-25
申请人： Howard Alper , David J. H. Smith
发明人： Howard Alper , David J. H. Smith
IPC分类号： C07B61/00 , B01J23/00 , B01J27/00 , C07C67/00 , C07C239/00 , C07C269/04 , C07C271/06 , C07C125/065
CPC分类号： C07C271/06
摘要： Carbamate esters are produced by reacting at ambient or elevated temperature an amine with carbon monoxide and an alcohol in the presence of a protonic acid, a dehydrating agent, for example a molecular sieve, and a catalyst comprising (a) at least one metal selected from the group palladium, rhodium, ruthenium, iridium and cobalt, and (b) at least one of the metals copper, molybdenum and iron, the components (a) and (b) being in the form of elemental metals or compounds thereof. The presence of the dehydrating agent reduces the formation of by-product carbon dioxide.
摘要翻译：氨基甲酸酯是通过在环境温度或升高温度下，在质子酸，脱水剂，例如分子筛和催化剂的存在下，将胺与一氧化碳和醇反应制备的，所述催化剂包含（a）至少一种选自钯，铑，钌，铱和钴组合，和（b）金属铜，钼和铁中的至少一种，组分（a）和（b）为元素金属或其化合物。脱水剂的存在降低副产物二氧化碳的形成。

6. 发明授权

US4687872A Process for the preparation of urethanes 失效
标题翻译：制备聚氨酯的方法
公开(公告)号：US4687872A
公开(公告)日：1987-08-18
申请号：US806389
申请日：1985-12-09
申请人： John H. Grate , David R. Hamm
发明人： John H. Grate , David R. Hamm
IPC分类号： C07C271/06 , C07C125/065 , C07C125/073
CPC分类号： C07C271/06
摘要： A process for preparing urethanes by reacting a solution of a nitrogen-containing organic compound and a hydroxyl-containing organic compound with carbon monoxide in the presence of a catalyst comprising rhodium, as a metal or compound, is disclosed. In the process of this invention, the rate of conversion and selectivity to urethane is increased by providing a rhodium catalyst comprising a polyamino ligand having at least two tertiary amino groups capable of coordinating with rhodium.
摘要翻译：在含有铑作为金属或化合物的催化剂的存在下，通过使含氮有机化合物和含羟基的有机化合物的溶液与一氧化碳反应来制备聚氨酯的方法。在本发明的方法中，通过提供包含具有至少两个能够与铑配位的叔氨基的聚氨基配位体的铑催化剂来提高转化率和对氨基甲酸酯的选择性。

7. 发明授权

US4681973A Direct n-acylation of amino acids 失效
标题翻译：氨基酸直接正酰化
公开(公告)号：US4681973A
公开(公告)日：1987-07-21
申请号：US833706
申请日：1986-02-27
申请人： Martin L. Kantor
发明人： Martin L. Kantor
IPC分类号： C07C271/06 , C07C125/06
CPC分类号： C07C271/06
摘要： Acylated amino acids having the general formula ##STR1## are prepared by reacting a compound of formula II ##STR2## with a compound of formula IIIROCOClwherein R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein.
摘要翻译：具有通式“I”的酰化氨基酸通过使式II化合物与式III化合物ROCOCl反应制备，其中R，R 1，R 2和R 3如本文所定义。

8. 发明授权

US4476317A Process for the production of methylenedicarbanilates 失效
标题翻译：生产甲基二甲苯胺化物的方法
公开(公告)号：US4476317A
公开(公告)日：1984-10-09
申请号：US458410
申请日：1983-01-17
申请人： Keisuke Wada
发明人： Keisuke Wada
IPC分类号： C07C271/06 , C07C125/07
CPC分类号： C07C271/06
摘要： A process is described for producing methylenedicarbanilates by reacting carbanilates with formaldehyde in the presence of a specific catalyst. The catalyst is selected from (1) a cation exchanger containing sulfonic acid groups which has a proton exchange capacity of at least 0.1 meq/g, (2) a clay having an acidity of at least 0.1 meq/g at an acidic site, the acid strength of the acidic site being -3.0 or less as a value of acidity function H.sub.o, (3) a mixed oxide having an acidity of at least 0.1 meq/g at an acidic site, the acid strength of the acidic site being -3.0 or less as a value of acidity function H.sub.o, (4) heteropolymolybdic acid, and (5) heteropolytungstic acid.
摘要翻译：描述了通过在特定催化剂存在下使氨基苯甲酸酯与甲醛反应制备亚甲基二甲苯二酸酯的方法。催化剂选自（1）含有质子交换容量至少为0.1meq / g的磺酸基的阳离子交换剂，（2）在酸性位置具有至少0.1meq / g的酸度的粘土，酸性部位的酸强度为酸性函数Ho的-3.0以下，（3）酸性部位酸度为0.1meq / g以上的混合氧化物，酸性部位的酸强度为-3.0 或以下的酸度函数Ho，（4）杂多钼酸和（5）杂多钨酸的值。

9. 发明授权

US4430505A Process for the preparation of N,O-disubstituted urethanes useful for the preparation of isocyanates 失效
标题翻译：用于制备可用于制备异氰酸酯的N，O-二取代的聚氨酯的方法
公开(公告)号：US4430505A
公开(公告)日：1984-02-07
申请号：US197032
申请日：1980-10-15
申请人： Peter Heitkamper , Klaus Konig , Kurt Findeisen , Rudolf Fauss , Rudolf Sundermann
发明人： Peter Heitkamper , Klaus Konig , Kurt Findeisen , Rudolf Fauss , Rudolf Sundermann
IPC分类号： C07C269/00 , C07C67/00 , C07C241/00 , C07C265/00 , C07C269/04 , C07C271/06 , C07C271/08 , C07C271/28 , C07C271/32 , C07C301/00 , C07C303/30 , C07C303/34 , C07C309/02 , C07C311/00 , C07C313/00 , C07C323/44 , C07C325/00 , C07C331/10 , C07C331/12 , C07C125/065 , C07C125/073
CPC分类号： C07C271/06
摘要： A process for the preparation of N,O-disubstituted urethanes. Urea or polyurets, primary amines and alcohols are reacted at 120.degree.-350.degree. C. in the presence of N-substituted urethanes and/or N-mono- or N,N'-disubstituted ureas or polyureas. In a preferred embodiment, the reactants further include catalysts known to be useful in esterification of carboxylic acids. The urethanes produced in accordance with this process are particularly useful as starting materials for preparation of isocyanates.
摘要翻译：制备N，O-二取代的聚氨酯的方法。在N-取代的氨基甲酸酯和/或N-单或N，N'-二取代的脲或聚脲的存在下，将脲或聚脲，伯胺和醇在120-350℃下反应。在优选的实施方案中，反应物还包括已知可用于羧酸酯化的催化剂。根据该方法制备的聚氨酯特别可用作制备异氰酸酯的原料。

10. 发明授权

US4338455A Novel process and intermediates useful in the preparation of sympathomimetic amines 失效
标题翻译：用于制备拟交感胺的新型方法和中间体
公开(公告)号：US4338455A
公开(公告)日：1982-07-06
申请号：US233457
申请日：1981-02-11
申请人： Jacob A. Zupan
发明人： Jacob A. Zupan
IPC分类号： C07C271/06 , C07C125/065
CPC分类号： C07C271/06 , Y02P20/55
摘要： The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.
摘要翻译：本发明涉及可用于拟交感神经胺的新方法和新型中间体。作为单 - 和二羟基芳族胺（例如儿茶酚胺）的酰基衍生物的药理学上有用的最终产物可以通过使相应的一羟基或二羟基芳族胺与能够形成N的试剂反应，以光学活性或外消旋形式制备 - 叔丁氧羰基衍生物; 将由此获得的新型中间体与酰氧基甲基氯反应，得到相应的新的单酰基或二酰化N-保护的芳族胺; 并从其中除去N-保护基。

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