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1.发明授权
公开(公告)号：US5391810A
公开(公告)日：1995-02-21
申请号：US121569
申请日：1993-09-16
申请人： So Abe , Shinichi Kishimoto , Toshihisa Kato , Hideo Takeda
发明人： So Abe , Shinichi Kishimoto , Toshihisa Kato , Hideo Takeda
IPC分类号： C07K5/072 , C07K5/075 , C07C101/02
CPC分类号： C07K5/0613
摘要： In crystallizing .alpha.-APM from a water solution or a mixed solvent solution of water and a lower alcohol in a crystallizer, the pressure in the crystallizer is held at not higher than atmospheric pressure, a water or water/alcohol mixed solution of .alpha.-APM is fed into the crystallizer with stirring so that the solvent is vaporized, and the crystallization solution is cooled and crystallized by the latent heat of vaporization or is heated so as to prevent supercooling.
摘要翻译： 在结晶器中从水溶液或水和低级醇的混合溶剂溶液中结晶α-APM时，将结晶器中的压力保持在不高于大气压的水溶液或水/乙醇混合的α-APM溶液 在搅拌下进料到结晶器中，使溶剂蒸发，并将结晶溶液冷却并通过蒸发潜热结晶或加热，以防止过冷。
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公开(公告)号：US4820729A
公开(公告)日：1989-04-11
申请号：US248172
申请日：1981-03-30
IPC分类号： C07D209/20 , A61K38/00 , A61K38/55 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C239/00 , C07C271/22 , C07C279/18 , C07C313/00 , C07C323/58 , C07C323/60 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , A61K31/215 , A61K31/195 , C07C61/08 , C07C101/02 , C07C101/72
摘要： Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy or lower alkoxy,R.sub.1 and R.sub.2 are hydrogen or lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hygrogen or lower alkyl,R.sub.6 is cycloalkly having from 3 to 20 carbon atoms, aryl or aryl-lower alkyl, and the aryl group contains from 6 to 10 carbon atoms, and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts possess antihypertensive activity.
摘要翻译： 其中R和R9独立地是羟基或低级烷氧基，R1和R2是氢或低级烷基，具有7-12个碳原子的芳基 - 低级烷基或具有6-12个碳原子的杂环低级烷基的化合物 原子，R 3，R 4，R 5，R 7和R 8是氢或低级烷基，R 6是具有3至20个碳原子的环烷基，芳基或芳基 - 低级烷基，并且芳基含有6至10个碳原子， 可接受的无毒酸加成盐，其中R或R9或两者均为羟基，其药学上可接受的无毒碱性盐具有抗高血压活性。
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3.发明授权Process for the production of n-formyl-aspartyl-phenylalanine or its methyl ester 失效N-甲酰基 - 天冬氨酰 - 苯丙氨酸或其甲酯的制备方法
公开(公告)号：US4810816A
公开(公告)日：1989-03-07
申请号：US99733
申请日：1987-09-22
申请人： Toshiaki Tsuji , Shinichi Kishimoto
发明人： Toshiaki Tsuji , Shinichi Kishimoto
CPC分类号： C07K5/0613
摘要： A process for producing N-formyl-aspartylphenylalanine or its methyl ester, wherein aspartic acid is reacted with formic acid and acetic anhydride in approximately stoichiometric quantities in the presence or absence of a catalyst and phenylalanine or its methyl ester is directly added to the dehydration mixture. This process has a higher yield of the desired N-formyl-dipeptide and minimizes the amount of by-products and unreacted starting materials.
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公开(公告)号：US4806282A
公开(公告)日：1989-02-21
申请号：US106057
申请日：1987-10-07
申请人： Maria O. Tinti , Domenico Misiti
发明人： Maria O. Tinti , Domenico Misiti
IPC分类号： C07C20060101 , C07C229/12 , C07C101/02
CPC分类号： C07C229/12
摘要： Gamma-butyrobetaine is prepared via a process whose characterizing step comprises hydrogenating crotonoylbetaine chloride to gamma-butyrobetaine chloride is a strongly acidic environment (pH 1-4), at 15-60 psi (1.05-4.21 kg/cm.sup.2) in the presence of 10% Pd/C or PtO.sub.2 as hydrogenation catalyst.
摘要翻译： 通过一种方法制备γ-丁基甜菜碱，该方法的特征步骤包括在10-60秒存在下，在15-60psi（1.05-4.21kg / cm 2）下，将巴豆酰基甜菜碱氯化物氢化为γ-丁酸丁酯氯化物是强酸性环境（pH 1-4） ％Pd / C或PtO 2作为氢化催化剂。
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公开(公告)号：US4730076A
公开(公告)日：1988-03-08
申请号：US942146
申请日：1986-12-16
IPC分类号： C07K5/075 , C07C101/02
CPC分类号： C07K5/0613
摘要： The present invention relates to a process for producing .alpha.-aspartyl-phenylalanine ester represented by the general formula ##STR1## wherein R' represents an alkyl group having 1 to 4 carbon atoms, by reducing an N-protected-N-hydroxymethyl-.alpha.-aspartyl-phenylalanine ester represented by the general formula ##STR2## wherein R represents an organic mioety which can be substituted reductively by hydrogen, and R' is as defined above, with hydrogen gas or formic acid, in the presence of a reduction catalyst and an aromatic primary amine. According to the present invention, there can be obtained a high purity .alpha.-aspartyl-phenylalanine ester with a high yield.
摘要翻译： 本发明涉及通过还原N-保护的N-羟甲基-α-谷氨酰胺来制备由通式“IMAGE”表示的α-天门冬酰胺 - 苯丙氨酸酯的方法，其中R'代表具有1至4个碳原子的烷基， 由通式
表示的天冬氨酰基 - 苯丙氨酸酯，其中R表示可在氢还原催化剂和还原催化剂存在下用氢气或甲酸还原的氢被还原反应的R'和R'定义的有机二氧化物， 芳族伯胺。 根据本发明，可以高产率地得到高纯度的α-天冬氨酰基苯丙氨酸酯。 -
6.发明授权
公开(公告)号：US3471548A
公开(公告)日：1969-10-07
申请号：US3471548D
申请日：1964-06-30
申请人： CIBA GEIGY CORP
IPC分类号： A61K31/195 , C07D207/26 , C07D211/88 , C07C101/00 , C07C101/02
CPC分类号： C07D207/26 , A61K31/195 , C07D211/88 , Y10S514/906
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7.发明授权Process for the production of N-formyl-alpha-L-aspartyl-L-phenylalanine methyl ester 失效制备N-甲酰基-α-L-天冬氨酰基-L-苯丙氨酸甲酯的方法
公开(公告)号：US4820861A
公开(公告)日：1989-04-11
申请号：US931123
申请日：1986-11-17
CPC分类号： C07K5/0613
摘要： N-formyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester is obtained by reacting L-phenylalanine methyl ester with N-formyl-L-aspartic acid anhydride in a reaction solvent containing acetic acid or acetic acid and formic acid in a complete mixing type continuous reaction mode.
摘要翻译： N-甲酰基-α-天冬氨酰基-L-苯丙氨酸甲酯通过L-苯丙氨酸甲酯与N-甲酰基-L-天冬氨酸酐在含有乙酸或乙酸的反应溶剂和甲酸的完全反应溶液中反应得到 混合型连续反应方式。
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公开(公告)号：US4801721A
公开(公告)日：1989-01-31
申请号：US943798
申请日：1986-12-19
申请人： James W. Ryan , Alfred Chung
发明人： James W. Ryan , Alfred Chung
IPC分类号： C07D207/16 , C07K1/107 , C07K5/062 , C07D209/54 , C07C101/02 , C07C101/26 , C07C103/00 , C07C103/19 , C07C103/20 , C07C125/06 , C07D207/00
CPC分类号： C07K5/06026 , C07D207/16 , C07K1/1077 , C07K5/06104
摘要： Methods for the alkylation of substituted amines with trifluorate esters is disclosed.
摘要翻译： 公开了用三氟酸酯烷基化取代的胺的方法。
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9.发明授权Substituted oxime-ethers and their use as bioregulators to lower the endogenous ethylene level in plants 失效取代的肟醚及其作为生物调节剂用于降低植物内源乙烯含量的用途
公开(公告)号：US4744811A
公开(公告)日：1988-05-17
申请号：US35730
申请日：1987-04-08
申请人： Guenter Schulz , Wolfgang Will , Johann Jung , Hansjoerg Fritsch
发明人： Guenter Schulz , Wolfgang Will , Johann Jung , Hansjoerg Fritsch
IPC分类号： A01N3/02 , A01N37/36 , C07C67/00 , C07C239/00 , C07C251/60 , A01N37/00 , C07C69/74 , C07C101/02
CPC分类号： A01N37/36
摘要： Substituted oxime-ethers of the formulae ##STR1## where R.sup.1 and R.sup.2 independently of one another are C.sub.1 -C.sub.6 -alkyl, n is 2 or 3 and R.sup.3 is hydrogen or C.sub.1 -C.sub.6 -alkyl.
摘要翻译： 式（Ia）的取代的肟 - 醚（Ⅰb）其中R1和R2彼此独立地是C1-C6-烷基，n是2或3，R3是氢或C1-C6-烷基。
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10.发明授权Amino acid derivatives and their use as antidepressives and hypotensive agents 失效氨基酸衍生物及其作为抗抑郁药和降血压药的用途
公开(公告)号：US4738803A
公开(公告)日：1988-04-19
申请号：US900814
申请日：1986-08-22
IPC分类号： A61K31/195 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/445 , A61K31/66 , A61K38/00 , A61P1/12 , A61P25/04 , A61P25/24 , A61P25/26 , C07C67/00 , C07C231/00 , C07C233/51 , C07C237/12 , C07C237/20 , C07C239/20 , C07C239/22 , C07C259/06 , C07C291/04 , C07C301/00 , C07C309/53 , C07C313/00 , C07C317/28 , C07C323/25 , C07C323/59 , C07C323/60 , C07D207/16 , C07D209/20 , C07D295/08 , C07D295/088 , C07F9/22 , C07F9/24 , C07F9/38 , C07F9/40 , C07F9/547 , C07F9/572 , C07F9/59 , C07K5/02 , C07K5/06 , C07K14/575 , C07K14/655 , C07K14/81 , C07C101/02 , C07C101/24 , C07C101/42
CPC分类号： C07D295/088 , C07D207/16 , C07D209/20 , C07F9/222 , C07F9/2458 , C07F9/2475 , C07F9/3808 , C07F9/3882 , C07K5/06191 , A61K38/00
摘要： Derivatives having the general formula: ##STR1## in which the various radicals, A,B,X,R.sub.1, R.sub.2, R.sub.3 and n have indicated definitions. These compounds have in particular enkephalinase-inhibiting, antalgic, antidepressive, antidiarrhea and hypotensive activities.
摘要翻译： 具有以下通式的衍生物：其中各种基团A，B，X，R 1，R 2，R 3和n表示定义。 这些化合物特别是脑啡肽酶抑制，止痛药，抗抑郁药，止泻药和降血压活性。
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