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    Heterocyclic nitriles
    4.
    发明授权
    Heterocyclic nitriles 失效
    杂环腈

    公开(公告)号：US4456758A

    公开(公告)日：1984-06-26

    申请号：US406998

    申请日：1982-08-10

    申请人： Jean-Claude Aloup ,  Jean Bouchaudon ,  Daniel Farge ,  Claude James

    发明人： Jean-Claude Aloup ,  Jean Bouchaudon ,  Daniel Farge ,  Claude James

    IPC分类号： C07D405/04 ,  C07D409/04 ,  C07D471/04 ,  C07D407/04

    CPC分类号： C07D405/04 ,  C07D409/04

    摘要： New heterocyclic nitriles of the formula: ##STR1## wherein (i) Het represents a heterocyclic radical of aromatic character containing one or two nitrogen atoms selected from pyrid-3-yl, pyrid-4-yl, pyridazinyl, pyrazinyl, pyrimidinyl, quinolyl, imidazolyl, naphthyridinyl, quinoxalinyl and quinazolinyl, X represents an oxygen atom and Y represents a valency bond or a methylene radical, or altenatively X represents a sulphur atom and Y represents a sulphur atom, a valency bond or a methylene radical, or(ii) Het represents the pyrid-2-yl radical, X represents an oxygen atom and Y represents a valency bond or a methylene radical, or alternatively X represents a sulphur atom and Y represents a sulphur atom or a methylene radical, are useful, in particular, as intermediates for the preparation of therapeutically useful heterocyclic thioformamides by converting the depicted cyano radical into a grouping --CSNHR wherein R represents a hydrogen atom or an alkyl (C.sub.1-4) radical.

    摘要翻译： 新的式（I）的杂环腈，其中（i）Het表示含有一个或两个选自吡啶-3-基，吡啶-4-基，哒嗪基，吡嗪基，嘧啶基的氮原子的芳族字符的杂环基 ，喹啉基，咪唑基，萘啶基，喹喔啉基和喹唑啉基，X表示氧原子，Y表示价键或亚甲基，或者说，X表示硫原子，Y表示硫原子，价键或亚甲基，或 （ii）Het表示吡啶-2-基，X表示氧原子，Y表示价键或亚甲基，或者X表示硫原子，Y表示硫原子或亚甲基， 特别是作为制备治疗上有用的杂环硫代甲酰胺的中间体，通过将所描绘的氰基转化成分组-CSNHR，其中R表示氢原子或烷基（C1-4）基团。

    2-(Pyrid-2-yl)tetrahydrothiophene derivatives
    5.
    发明授权
    2-(Pyrid-2-yl)tetrahydrothiophene derivatives 失效
    2-（吡啶-2-基）四氢噻吩衍生物

    公开(公告)号：US4272534A

    公开(公告)日：1981-06-09

    申请号：US134311

    申请日：1980-03-26

    申请人： Jean-Claude Aloup ,  Jean Bouchaudon ,  Daniel Farge ,  Claude James

    发明人： Jean-Claude Aloup ,  Jean Bouchaudon ,  Daniel Farge ,  Claude James

    IPC分类号： C07D213/26 ,  C07D213/32 ,  A61K31/44 ,  A61K31/495 ,  C07D413/14

    CPC分类号： C07D213/26 ,  C07D213/32

    摘要： Compounds of the formula: ##STR1## wherein R represents hydrogen or alkyl of 1 through 4 carbon atoms, and R.sub.1 and R.sub.2 represent hydrogen or alkyl of 1 through 15 carbon atoms, or alkyl of 1 through 15 carbon atoms substituted by one substituent selected from (i) hydroxy, (ii) alkylamino in which the alkyl radical is of 1 through 4 carbon atoms, (iii) dialkylamino in which the alkyl radicals are of 1 through 4 carbon atoms, (iv) phenyl, (v) carboxy, and (vi) alkoxycarbonyl in which the alkoxy radical is of 1 through 4 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached represent a five- or six-membered heterocyclic radical, are new compounds. They possess pharmacological properties and are particularly useful in the treatment of gastro-intestinal ulcers.

    摘要翻译： 下式的化合物：其中R表示氢或1至4个碳原子的烷基，R1和R2表示氢或1至15个碳原子的烷基，或1至15个碳原子的烷基，被一个选自 （i）羟基，（ii）其中烷基为1至4个碳原子的烷基氨基，（iii）烷基具有1至4个碳原子的二烷基氨基，（iv）苯基，（v）羧基和 （vi）其中烷氧基为1至4个碳原子的烷氧基羰基，或R1和R2与它们所连接的氮原子一起代表五或六元杂环基，是新的化合物。 它们具有药理学性质，特别可用于治疗胃肠溃疡。

    Peptides, their preparation and compositions containing them
    7.
    发明授权
    Peptides, their preparation and compositions containing them 失效
    肽，它们的制备和含有它们的组合物

    公开(公告)号：US4916119A

    公开(公告)日：1990-04-10

    申请号：US163878

    申请日：1980-06-27

    申请人： Jean Bouchaudon ,  Daniel Farge ,  Claude James

    发明人： Jean Bouchaudon ,  Daniel Farge ,  Claude James

    IPC分类号： C07K5/06 ,  A61K38/00 ,  A61K39/39 ,  A61P31/04 ,  A61P35/00 ,  A61P37/04 ,  A61P43/00 ,  C07K1/02 ,  C07K1/04 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02

    CPC分类号： C07K5/0215 ,  A61K38/00

    摘要： Tripeptides of the general formula: ##STR1## wherein the symbols R, which may be the same or different represent hydrogen or a fatty acid residue (at least one of them representing a fatty acid residue), R.sub.1 represents hydroxy, amino or alkoxy and R.sub.2 and R.sub.3, which may be the same or different, represent hydrogen, carboxy, carbamoyl or alkoxycarbonyl radical (with the proviso that R.sub.2 and R.sub.3 cannot simultaneously represent a hydrogen atom), the alanine moiety being in the L form, the glutamic acid moiety being in the D form, the lysine moiety (when R.sub.2 or R.sub.3 =a hydrogen atom) being in the L form and the 2,6-diaminopimelic acid moiety or its derivatives (when R.sub.2 and/or R.sub.3 =carboxy, carbamoyl or alkoxycarbonyl) being in the D,D, L,L, D,D/L,L (racemic) or D,L (meso) form, and salts thereof, possess immunological adjuvant and immunostimulant activity.

    摘要翻译： 具有以下通式的三肽：其中符号R可以相同或不同，表示氢或脂肪酸残基（其中至少一个代表脂肪酸残基），R1表示羟基，氨基或烷氧基， R2和R3可以相同或不同，表示氢，羧基，氨基甲酰基或烷氧基羰基（条件是R2和R3不能同时代表氢原子），丙氨酸部分为L形，谷氨酸部分 处于D形式时，赖氨酸部分（当R 2或R 3 =氢原子）为L形时，2,6-二氨基庚二酸部分或其衍生物（当R 2和/或R 3 =羧基，氨基甲酰基或烷氧羰基时） 在D，D，L，L，D，D / L，L（外消旋）或D，L（内消旋）形式及其盐具有免疫佐剂和免疫刺激活性。

    Tetrapeptides and pentapeptides, their preparation and compositions containing them
    8.
    发明授权
    Tetrapeptides and pentapeptides, their preparation and compositions containing them 失效
    四肽和五肽，它们的制备方法和含有它们的组合物

    公开(公告)号：US4742048A

    公开(公告)日：1988-05-03

    申请号：US163890

    申请日：1980-06-27

    申请人： Jean Bouchaudon ,  Daniel Farge ,  Claude James

    发明人： Jean Bouchaudon ,  Daniel Farge ,  Claude James

    IPC分类号： C07K1/113 ,  A61K38/00 ,  A61K39/39 ,  A61P31/04 ,  A61P35/00 ,  A61P37/04 ,  A61P43/00 ,  C07K1/02 ,  C07K1/04 ,  C07K1/06 ,  C07K5/02 ,  C07K5/10 ,  A61K37/02 ,  C07K5/08

    CPC分类号： C07K5/0215 ,  A61K38/00

    摘要： Tetrapeptides and pentapeptides of the formula: ##STR1## wherein R represents hydrogen or a fatty acid residue, R.sub.1 represents hydroxy, amino, alkoxy of 1 to 4 carbon atoms, optionally substituted by phenyl or nitrophenyl, one of R.sub.2 and R.sub.4 represents hydrogen, carboxy, carbamoyl, alkoxycarbonyl of 2 to 5 carbon atoms, optionally substituted by phenyl or nitrophenyl, or a N-carbonylglycine or N-carbonyl-D-alanine radical optionally esterified by alkyl of 1 to 4 carbon atoms (which is optionally substituted by phenyl or nitrophenyl) and the other symbol represents hydrogen, carboxy, carbamoyl, or alkoxycarbonyl fof 2 to 5 carbon atoms, optionally substituted by phenyl or nitrophenyl, and R.sub.3 represents hydrogen, a fatty acid residue or a glycyl or D-alanyl moiety in which the amine group is optionally substituted by a fatty acid residue, it being understood that R.sub.2 and R.sub.4 cannot simutaneously represent hydrogen, that at least one of R.sub.2, R.sub.3 and R.sub.4 represents a glycyl or D-alanyl moiety, that at least one of R and R.sub.3 represents or contains a fatty acid residue, and that the alanine moiety is in the L form, the glutamic acid moiety or its derivatives are in the D form, the lysine moiety or its derivatives, when one of the symbols R.sub.2 and R.sub.4 represents a hydrogen atom, are in the L form, and the 2,6-diaminopimelic acid moiety or fits derivatives, when R.sub.2 and R.sub.4 represent a carboxy, carbamoyl or alkoxycarbonyl radical, are in the D,D L,L,D,D/L,L (racemic) or D,L (meso) form, and salts thereof possess immunostimulant activity.

    摘要翻译： 下式的四肽和五肽：其中R表示氢或脂肪酸残基，R1表示羟基，氨基，1至4个碳原子的烷氧基，任选被苯基或硝基苯基取代，R2和R4之一表示氢，羧基 ，任选被苯基或硝基苯基取代的2-5个碳原子的氨基甲酰基，烷氧基羰基，或任选被1至4个碳原子的烷基酯化的N-羰基甘氨酸或N-羰基-D-丙氨酸基（其任选被苯基或 硝基苯基），另一个符号表示2-5个碳原子的氢，羧基，氨基甲酰基或烷氧基羰基，任选被苯基或硝基苯基取代，R3表示氢，脂肪酸残基或甘氨酰或D-丙氨酰部分，其中胺 基团任选被脂肪酸残基取代，应理解R 2和R 4不能同时代表氢，R 2，R 3和R 4中的至少一个代表甘氨酰或D-丙氨酰部分， R和R 3中的至少一个表示或含有脂肪酸残基，并且丙氨酸部分为L形式，当其中一个为谷氨酸部分或其衍生物时，谷氨酸部分或其衍生物为D形式，赖氨酸部分或其衍生物 当R 2和R 4表示羧基，氨基甲酰基或烷氧基羰基时，符号R 2和R 4表示氢原子，为L形，2,6-二氨基庚二酸部分或配合物衍生物在D，DL，L， D，D / L，L（外消旋）或D，L（内消旋）形式及其盐具有免疫刺激活性。

    Tri-, tetra, and penta-peptides, their preparation and compositions containing them
    9.
    发明授权
    Tri-, tetra, and penta-peptides, their preparation and compositions containing them 失效
    三肽，四肽和五肽，它们的制备方法和含有它们的组合物

    公开(公告)号：US4401658A

    公开(公告)日：1983-08-30

    申请号：US331593

    申请日：1981-12-17

    申请人： Jean Bouchaudon ,  Gilles Dutruc-Rosset ,  Daniel Farge ,  Claude James

    发明人： Jean Bouchaudon ,  Gilles Dutruc-Rosset ,  Daniel Farge ,  Claude James

    IPC分类号： C07K1/113 ,  A61K38/00 ,  A61K39/39 ,  A61P31/04 ,  A61P35/00 ,  A61P37/04 ,  C07K1/04 ,  C07K1/06 ,  C07K5/02 ,  C07C103/52 ,  A61K37/02

    CPC分类号： C07K5/0215 ,  A61K38/00

    摘要： The invention provides tri-, tetra- or penta-peptides of the general formula: ##STR1## in which RCO is a fatty acid residue, R.sub.1 is hydroxyl, amino, alkoxy or benzyloxy, R.sub.2 and R.sub.4 (identical or different) represent hydrogen, carboxyl, alkoxycarbonyl or benzyloxycarbonyl or an optionally esterified N-carbonylglycyl or N-carbonyl-D-alanyl radical, it being impossible for R.sub.2 and R.sub.4 simultaneously to represent hydrogen, R.sub.3 is hydrogen, or represents a glycyl or D-alanyl residue (in which case, only one of the radicals R.sub.2 and R.sub.4 can represent an N-carbonylglycyl or N-carbonyl-D-alanyl radical), X is a sulphur atom or methylene, and m and n=1 or 2, it being understood that if X is methylene, m and n are different from 1, their salts, their preparation and compositions containing them: the compounds are useful as vaccine adjuvants or as non-specific stimulants of anti-infectious or anti-tumoral activity.

    摘要翻译： 本发明提供以下通式的三 - ，四 - 或五肽 - 其中RCO是脂肪酸残基，R1是羟基，氨基，烷氧基或苄氧基，R2和R4（相同或不同）代表氢， 羧基，烷氧基羰基或苄氧基羰基或任选酯化的N-羰基甘氨酰或N-羰基-D-丙氨酰基，R2和R4同时代表氢，R3是氢，或代表甘氨酰或D-丙氨酰残基（其中 情况下，只有一个基团R 2和R 4可以表示N-羰基甘氨酰基或N-羰基-D-丙氨酰基），X是硫原子或亚甲基，m和n = 1或2，可以理解如果X 是亚甲基，m和n不同于1，它们的盐，它们的制备和含有它们的组合物：该化合物可用作疫苗佐剂或作为抗感染或抗肿瘤活性的非特异性兴奋剂。