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    Aminoguanidine bicarbonate with particular properties and method for making same
    24.
    发明授权
    Aminoguanidine bicarbonate with particular properties and method for making same 有权
    具有特殊性质的氨基胍碳酸氢盐及其制备方法

    公开(公告)号：US06884912B1

    公开(公告)日：2005-04-26

    申请号：US10031113

    申请日：2000-06-08

    申请人： Jean-Michel Bossoutrot ,  Paul Bourdauducq

    发明人： Jean-Michel Bossoutrot ,  Paul Bourdauducq

    IPC分类号： C07C277/08 ,  C07C277/02 ,  C07C279/02 ,  C07C281/16

    CPC分类号： C07C277/02 ,  C07C279/02

    摘要： The invention concerns a method for making aminoguanidine bicarbonate from an aqueous solution of cyanamide and an aqueous solution of hydrazine in the presence of CO2. The invention is characterised in that it consists in proceeding with an amount of cyamide slightly higher than the stoichiometric quantity. The invention also concerns quasi-spherical agglomerates of aminoguanidine bicarbonate crystals.

    摘要翻译： 本发明涉及一种在CO 2 2存在下由氨腈水溶液和肼水溶液制备氨基胍碳酸氢盐的方法。 本发明的特征在于其进行量稍高于化学计量的cyamide。 本发明还涉及氨基胍碳酸氢盐晶体的准球形附聚物。

    Preparation of N-acyl amino carboxylic acids, amino carboxylic acids and their derivatives by metal-catalyzed carboxymethylation in the presence of a promoter
    25.
    发明申请
    Preparation of N-acyl amino carboxylic acids, amino carboxylic acids and their derivatives by metal-catalyzed carboxymethylation in the presence of a promoter 审中-公开
    在助催化剂存在下，通过金属催化的羧甲基化制备N-酰基氨基羧酸，氨基羧酸及其衍生物

    公开(公告)号：US20020058834A1

    公开(公告)日：2002-05-16

    申请号：US09871869

    申请日：2001-06-01

    发明人： Thaddeus S. Franczyk II

    IPC分类号： C07C277/02

    CPC分类号： C07F9/3813 ,  C07C227/20 ,  C07C231/08 ,  C07C273/18 ,  C07C229/12 ,  C07C229/16 ,  C07C233/47

    摘要： A process for the preparation of amino carboxylic acids, N-acyl amino carboxylic acids, or derivatives thereof by carboxymethylation of an amide, amide precursor or amide source compound in the presence of a carboxymethylation catalyst precursor and a promoter is provided. A carboxymethylation reaction mixture is formed by introducing a promoter, an amide, amide precursor or amide source compound, carbon monoxide, hydrogen, an aldehyde or aldehyde source compound, and a carboxymethylation catalyst precursor into a carboxymethylation reaction zone. In a preferred embodiment, the promoter is a supported noble metal promoter. In another preferred embodiment, the amide compound and aldehyde are selected to yield an N-acyl amino carboxylic acid which is readily converted to N-phosphonomethyl)glycine, or a salt or ester thereof.

    摘要翻译： 提供了在羧甲基化催化剂前体和助催化剂存在下通过酰胺，酰胺前体或酰胺源化合物的羧甲基化制备氨基羧酸，N-酰基氨基羧酸或其衍生物的方法。 通过将助催化剂，酰胺，酰胺前体或酰胺源化合物，一氧化碳，氢，醛或醛源化合物和羧甲基化催化剂前体引入到羧甲基化反应区中形成羧甲基化反应混合物。 在优选的实施方案中，促进剂是负载的贵金属助催化剂。 在另一个优选的实施方案中，选择酰胺化合物和醛以产生N-酰基氨基羧酸，其易于转化为N-膦酰基甲基）甘氨酸或其盐或酯。

    Method for producing N-alkyl-N'-nitroguanidines
    26.
    发明授权
    Method for producing N-alkyl-N'-nitroguanidines 有权
    制备N-烷基-N'-硝基胍的方法

    公开(公告)号：US6114581A

    公开(公告)日：2000-09-05

    申请号：US381675

    申请日：1999-09-22

    申请人： Reinhard Lantzsch

    发明人： Reinhard Lantzsch

    IPC分类号： C07C277/08 ,  C07C279/36 ,  C07C277/02

    CPC分类号： C07C277/08

    摘要： The invention relates to a novel process for the preparation of N-alkyl-N'-nitroguanidines of the formula (I) ##STR1## in which R is C.sub.1 -C.sub.6 -alkyl,by neutralizing alkylamine with nitric acid, then reacting it with cyanamide, and dehydrating the alkylguanidine nitrate formed.

    摘要翻译： PCT No.PCT / EP98 / 01428 371日期1999年9月22日 102（e）1999年9月22日PCT 1998年3月12日PCT PCT。 第WO98 / 43951号公报 日期1998年10月8日本发明涉及一种制备式（I）的N-烷基-N'-硝基胍的新方法，其中R为C1-C6烷基，通过用硝酸中和烷基胺，然后使其反应 与氰胺反应，并使形成的硝酸烷基胍脱水。

    Process for the production of guanidine derivatives
    27.
    发明授权
    Process for the production of guanidine derivatives 失效
    生产胍衍生物的方法

    公开(公告)号：US5276186A

    公开(公告)日：1994-01-04

    申请号：US981683

    申请日：1992-11-25

    申请人： Rudolf Waditschatka

    发明人： Rudolf Waditschatka

    IPC分类号： C07C277/08 ,  C07C279/18 ,  C07C277/02

    CPC分类号： C07C277/08

    摘要： A process for the production of phenylguanidine carbonate and hydrogencarbonate by reacting aqueous cyanamide with aniline hydrochloride within a specified pH range, combining the reaction mixture with an alkali metal carbonate or hydrogencarbonate, and separating the crystalline product.

    摘要翻译： 通过将氰氨水与苯胺盐酸盐在规定的pH范围内反应生产苯基碳酸胍和碳酸氢盐的方法，将反应混合物与碱金属碳酸盐或碳酸氢盐结合，并分离结晶产物。

    Antihypertensive pyridylguanidine compounds
    28.
    发明授权
    Antihypertensive pyridylguanidine compounds 失效
    抗高血压吡啶胍化合物

    公开(公告)号：US4057636A

    公开(公告)日：1977-11-08

    申请号：US636747

    申请日：1975-12-01

    申请人： Hans Jorgen Petersen

    发明人： Hans Jorgen Petersen

    IPC分类号： C07D213/53 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/47 ,  A61P9/12 ,  C07C277/02 ,  C07D213/72 ,  C07D213/75 ,  C07D215/38 ,  C07D211/00

    CPC分类号： C07D215/38 ,  C07D213/72 ,  C07D213/75

    摘要： The invention relates to a series of new compounds, to methods for preparing the compounds, to compositions containing said compounds which are useful in the human and veterinary medical practice, and to methods for treating patients suffering from certain illnesses with said compounds, the new compounds having the general formula I ##STR1## or the tautomeric forms thereof in which the R.sup.1 -substituted cyano-guanidyl radical is placed in the 2-, 3- or 4-position of the pyridine ring, and in which R.sup.1 stands for a straight or branched, saturated or unsaturated, aliphatic hydrocarbon radical having from 1 to 8 carbon atoms, a cycloalkyl or cycloalkenyl radical having from 3 to 7 carbon atoms, an aryl or an aralkyl radical, and R.sup.2 stands for hydrogen, halogen, hydroxy, lower alkyl or alkoxy radicals; and in the case of the present compounds containing one or more asymmetric carbon atoms, also the stereoisomers thereof and racemic mixtures of same; and salts of the compounds of formula I with nontoxic, pharmaceutically acceptable acids.The new compounds of the invention have surprisingly shown to be highly potent hypotensive compounds giving rise to a pronounced reduction of the blood pressure. They have a low toxicity and consequently a high therapeutic ratio.

    摘要翻译： 本发明涉及一系列新化合物，制备化合物的方法，含有可用于人和兽医医学实践中的所述化合物的组合物，以及用所述化合物治疗患有某些疾病的患者的方法，新化合物 具有通式I“I”或其互变异构形式，其中R1取代的氰基胍基置于吡啶环的2-，3-或4-位，其中R1代表直链 或具有1至8个碳原子的支链，饱和或不饱和的脂族烃基，具有3至7个碳原子的环烷基或环烯基，芳基或芳烷基，R 2代表氢，卤素，羟基，低级烷基 或烷氧基; 在本发明化合物含有一个或多个不对称碳原子的情况下，其立体异构体及其外消旋混合物也是如此; 和式I化合物的盐与无毒的药学上可接受的酸形成的盐。

    Process for the preparation of the compound N-(3,5-dimethylphenyl)-N′-(2-trifluoromethylphenyl) guanidine
    30.
    发明授权
    Process for the preparation of the compound N-(3,5-dimethylphenyl)-N′-(2-trifluoromethylphenyl) guanidine 有权

    公开(公告)号：US10343984B2

    公开(公告)日：2019-07-09

    申请号：US15751437

    申请日：2016-08-10

    申请人： CHEMO RESEARCH, S.L.

    发明人： José Amato

    IPC分类号： C07C277/08 ,  C07C277/02 ,  C07C279/18 ,  C07C277/06

    摘要： The present invention relates to a process for the preparation of the compound N-(3,5-dimethylphenyl)-N′-(2-trifluoromethylphenyl) guanidine of formula (I) which comprises reacting a salt of a compound of formula (II) or a mixture of the salt of the compound of formula (II) and a compound of formula (II) with a compound of formula (III), in the presence of a polar organic solvent; a crystalline solid form of the compound of formula (I), in particular crystalline solid form A; to a pharmaceutical composition comprising them; and to their use as a medicament, in particular to the treatment of a condition mediated by Rho-GTPase cell proteins.