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101. 发明专利

JPS5832803A NOVEL MICROBICIDE AND ALGICIDE 失效
公开(公告)号：JPS5832803A
公开(公告)日：1983-02-25
申请号：JP11411382
申请日：1982-07-02
申请人： HENKEL KGAA
发明人： HANSU UERUNERU ETSUKERUTO , GIYUNTERU KOTSUPENSHIYUTAINERU
IPC分类号： A01N37/20 , A01N37/18 , A01N37/44 , A61K31/16 , A61P31/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/14 , C07C237/10 , C07C237/12 , C07C237/22 , C08G69/14

102. 发明专利

JPS5748103B2 失效
公开(公告)号：JPS5748103B2
公开(公告)日：1982-10-14
申请号：JP7993878
申请日：1978-06-30
IPC分类号： A61K31/265 , A61P13/02 , A61P15/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C237/08 , C07C237/12 , C07C237/22 , C07C313/00 , C07C323/60 , C07D207/46

103. 发明专利

JPS57156449A PREPARATION OF ALPHA-AMINO ACID OR N-ACYL AMINO ACID 失效
公开(公告)号：JPS57156449A
公开(公告)日：1982-09-27
申请号：JP4108081
申请日：1981-03-20
申请人： MITSUBISHI CHEM IND
发明人： EGAMI FUJIO , YANAGAWA HIROSHI , MAKINO YUMIKO
IPC分类号： C07C227/08 , C07C67/00 , C07C227/00 , C07C229/02 , C07C231/00 , C07C231/10 , C07C231/14 , C07C233/47 , C07C233/56 , C07C237/12
摘要： PURPOSE:To prepare the titled compound through a novel reaction path, by reacting an aldehyde acid or an alpha-ketone acid with at least one compound selected from ammonium salts and primary amines, etc. CONSTITUTION:The titled compound is prepared by reacting (A) an aldehyde acid or an alpha-keto acid free of amino group, e.g. the compound of formula R COCO2H (R is H, organic group or -CH2CH2CO2H) with (B) at least one compound selected from ammonia, primary amines of formula R -NH2 (R is organic group) and primary amine salts, in an aqueous solution at 0-110 deg.C. When R is H, the compound of formula IV, and then the compound of formula II are produced through the path (i), however, when R is organic group, the path (ii) is predominant. When the reaction temperature is low, N-acylamino acid (the compound of formula IV or formula II) is the major product, and when it is >=60 deg.C, the production of alpha-amino acid (the compound of formula III) is predominant.

104. 发明专利

JPS57123157A Indane derivative and its preparation 失效
标题翻译：印度衍生物及其制备
公开(公告)号：JPS57123157A
公开(公告)日：1982-07-31
申请号：JP1054781
申请日：1981-01-26
申请人： Takeda Chem Ind Ltd
发明人： OKA YOSHIKAZU , NISHIKAWA KOUHEI , ITOU KATSUMI
IPC分类号： A61K31/195 , A61K31/22 , A61P9/12 , C07C67/00 , C07C231/00 , C07C231/02 , C07C237/12
摘要： NEW MATERIAL:A compound shown by the formula I(R
1 is H, lower alkyl, aralkyl; R
2 is H or lower alkyl; R
3 is aralkyl; R
4 is H or acyl derived from a carboxylic acid) or its salt.
EXAMPLE: N-(5-Benzamido-4-oxo-6-phenylhexanoyl)-N-(2-indanyl)glycine.
USE: Having inhibiting actions on an enzyme capable of converting angiotension or of decomposing bradykinin, a diagnosticum, preventive or remedy for hypertension, anodyme, and enhancer for analgesic action.
PROCESS: A compound shown by the formula II is reacted with a compound shown by the formula III or its reactive derivative at its carboxyl in a proper solvent at -20W150°C, to give a compound shown by the formula I. The compound shown by the formula II as the starting material is obtained by condensing 2-indanone with a compound shown by the formula IV or under reducing conditions in an organic solvent preferably at -20W100°C.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：由式I表示的化合物（R 1是H，低级烷基，芳烷基; R 2是H或低级烷基; R 3是芳烷基; R 4是H或衍生自羧酸）或其盐。实施例：N-（5-苯甲酰氨基-4-氧代-6-苯基己酰基）-N-（2,3-二氢化茚基）甘氨酸。使用：对能够转化血管紧张素或分解缓激肽的酶具有抑制作用，用于高血压，止痛剂和镇痛作用增强剂的诊断，预防或补救措施。方法：将式II化合物与式III化合物或其反应性衍生物在适当的溶剂中在-20-150℃下在羧基上反应，得到式I所示的化合物。通过将式Ⅱ化合物作为起始原料的化合物是通过将2-二氢茚酮与式IV所示化合物或还原条件下在有机溶剂中优选-20-100℃冷凝而获得的。

105. 发明专利

JPS5775955A Amide derivative, manufacture and pharmacetic composition containing same and having hypotensive activity 失效
标题翻译：酰胺衍生物，制造和含有相同活性的药物组合物
公开(公告)号：JPS5775955A
公开(公告)日：1982-05-12
申请号：JP11544481
申请日：1981-07-24
申请人： Ici Ltd
发明人： MAIKERU BARII GUREIBUSUTOTSUKU
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/40 , A61P9/12 , C07C20060101 , C07C45/88 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C237/08 , C07C237/12 , C07C237/16 , C07C237/20 , C07C237/22 , C07C273/10 , C07D20060101 , C07D207/08 , C07D207/16

106. 发明专利

JPS5759844A Trans-4-aminomethylcyclohexanecarboxylic acid derivative 失效
标题翻译：反式-4-氨基甲酰基环己基羧酸衍生物
公开(公告)号：JPS5759844A
公开(公告)日：1982-04-10
申请号：JP13700780
申请日：1980-09-29
申请人： Hisamitsu Pharmaceut Co Inc
发明人： NODA KANJI , NAKAGAWA AKIRA , MOTOMURA TOSHIHARU , MIYATA SATORU , INOUE TOSHITAKA , IDE HIROYUKI
IPC分类号： A61K31/195 , A61K31/27 , A61P1/04 , A61P7/00 , A61P35/00 , A61P37/00 , C07C67/00 , C07C237/12 , C07C239/00 , C07C271/22 , C07D207/16 , C07D209/20 , C07D233/64
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:A trans-4-aminomethylcyclohexanecarboxylic acid derivative of the formula (R is amino acid residue).
EXAMPLE: An L-seryl-trans-4-aminomethylcyclohexanecarboxylic acid derivative.
USE: Useful as a medicine having anticomplementary action, carcinostatic action, antiulcer action and antithrombotic action.
PROCESS: An N-protected amino acid is reacted with a chloride, e.g. SOCl
2 or PCl
5 , in an organic solvent, e.g. benzene, to synthesize an N-protected amino acid chloride, which is then condensed with an alkaline salt of trans-4-aminomethylcyclohexanecarboxylic acid in an aqueous solution in the presence of a base in an equivalent amount or a p-aminomethylcyclohexanecarboxylic ester in an organic solvent, e.g. THF, and if desired the protecting group is removed to give the compound of the formula.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式（R为氨基酸残基）的反式-4-氨基甲基环己烷羧酸衍生物。实施例：L-丝酰基反式-4-氨基甲基环己烷羧酸衍生物。用途：作为具有抗补体作用，抗癌作用，抗溃疡作用和抗血栓作用的药物。方法：将N-保护的氨基酸与氯化物反应，例如 SOCl 2或PCl 5，在有机溶剂中，例如苯，合成N-保护的氨基酰氯，然后将其与反式-4-氨基甲基环己烷羧酸的碱金属盐在水溶液中在等量的碱存在下或在有机物中的对氨基甲基环己烷羧酸酯溶剂，例如 THF，如果需要，除去保护基，得到下式的化合物。

107. 发明专利

JPS56110654A CARNITINE AMIDE DERIVATIVE OF AMINO ACID AND ITS MANUFACTURE 失效
公开(公告)号：JPS56110654A
公开(公告)日：1981-09-01
申请号：JP954981
申请日：1981-01-23
申请人： SIGMA TAU IND FARMACEUTI
发明人： PAORO DE UITSUTO , MARIA ORUNETSURA TEINTEI
IPC分类号： A61K20060101 , A61K31/16 , A61K31/205 , C07C20060101 , C07C237/12 , C07C323/25 , C07D233/58 , C07D233/64

108. 发明专利

JPS5697254A NOVEL PEPTIDE* PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND ITS PREPARATION 失效
公开(公告)号：JPS5697254A
公开(公告)日：1981-08-05
申请号：JP14088380
申请日：1980-10-07
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： HASHIMOTO SHINJI , KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HENMI KEIJI , ARAYA MATSUHIKO , TAKENO SHIYUUICHI , OKADA TATSU , TANAKA HIROKAZU
IPC分类号： A61K31/16 , A61K31/195 , A61K38/00 , A61K39/39 , A61P31/04 , A61P37/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C237/06 , C07C237/12 , C07C237/22 , C07C271/22 , C07K1/113 , C07K5/02
摘要： NEW MATERIAL:A peptide of formula I [R is H or acyl; R is optionally protected carboxyl or -CONH-Ra [Ra is optionally protected carboxy(lower)alkyl]; R is optionally protected carboxyl, lower alkyl, etc.; RP is optionally protected carboxyl, carbamoyl, etc.; l is 0 or an integer 2; m is an integer 1-3; n is 0 or 1] and a pharmaceutical salt thereof. EXAMPLE:The compound of formula IV. USE:A remedy for infectious diseases having an immune response enhancing action, a stimulating action on the reticuloendothelial system, a juvenizing activity and an infection protecting effect. PROCESS:A compound of formula II (R1P is protected carboxyl, carbamoyl, etc.) or a salt thereof is reacted with compound of formula III (Rc is a part of R ) or a salt thereof to give a compound of formula I or a salt thereof, which is subjected to the removal of the protecting groups and acylated if necessary to afford the desired compound.

109. 发明专利

JPS5665852A PRODUCTION OF CARBOXYLIC ACID AMIDE 失效
公开(公告)号：JPS5665852A
公开(公告)日：1981-06-03
申请号：JP14119479
申请日：1979-11-02
申请人： TOKYO DAIGAKU
发明人： MUKAIYAMA MITSUAKI , WATANABE YUTAKA , MORIFUJI NAOYA
IPC分类号： C07D201/08 , B01J31/00 , B01J31/02 , C07B61/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/83 , C07C237/12 , C07C237/22 , C07D223/10 , C07K1/10 , C07K5/06 , C07K5/08
摘要： PURPOSE:To condensation reaction of a single compound bearing carboxyl and amino groups or a plurality of compounds bearing these groups in different molecules is effected in the presence of an organophosphorous compound to produce the titled compound used as a medicine in various application. CONSTITUTION:In the presence of an organophosphorus compound of the formula (R , R are alkyl; R is aryloxy; X is S, O), a condensation reaction of a single compound bearing a carboxylic and an amino group such as an aminocarboxylic acid or between plural compounds bearing carboxyl and amino groups in different compounds such as carboxylic acid and organic amine or its salt is effected to produce a carboxylic acid amide. EFFECT:The objective compounds are obtained under mild reaction conditions by simple operations in a short time. The racemization can be prevented in the production of peptides. The starting materials are inexpensive, easy-to-handle because its crystallinity.

110. 发明专利

JPS55167262A ESTERS OF CARNITINE* ITS MANUFACTURE AND ITS USE 失效
公开(公告)号：JPS55167262A
公开(公告)日：1980-12-26
申请号：JP5482180
申请日：1980-04-23
申请人： SIGMA TAU IND FARMACEUTI
发明人： KURAUJIO KABAZA
IPC分类号： A61K31/16 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/255 , A61K31/44 , A61P9/00 , A61P9/04 , A61P25/24 , A61P25/26 , C07C67/00 , C07C227/16 , C07C229/22 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/18 , C07C233/89 , C07C237/06 , C07C237/12 , C07C273/10 , C07C311/46

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