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    Peptides, their preparation and compositions containing them
    54.
    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
    55.
    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。

    Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and method of use therefor
    56.
    发明授权
    Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and method of use therefor 失效

    公开(公告)号：US4684658A

    公开(公告)日：1987-08-04

    申请号：US684061

    申请日：1984-12-20

    申请人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    IPC分类号： A61K31/435 ,  A61K31/505 ,  A61P7/02 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/38 ,  C07D417/14

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

    摘要： The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.4), benzyl or phenyl radicals optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3 or NO.sub.2, or R.sub.2 =adamantyl, pyridyl or pyridylmethyl,or R.sub.1 and R.sub.2 =both unsubstituted alkylor R.sub.1 and R.sub.2 from a 4-phenylpiperazin-1-yl radical the phenyl part of which may be substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3 or NO.sub.2(2) or R=halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio, and Y=NH.sub.2or A is a heterocyclic ring such that it forms, with pyrrole, a 2,3-dihydro-1H-pyrrolizine substituted by OH, 2,3-dihydropyrrolo[2,1-b]thiazole or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, R=H, Y=NH.sub.2, n=0 or 1 or Het=5-thiazolyl or 3-pyridyl,or A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 1H,3H-pyrrolo[1,2-c]oxazole or 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-oxazine ring system, R=H, Y=NH.sub.2 andeither Het=5-thiazolyl and n=0 or 1or Het=3-pyridyl and n=1, the alkyl containing 1 to 4 C as a straight or branched chain, and their acid addition salts, pharmaceutical compositions containing the said pyrrole derivatives and process for their preparation. These pyrrole derivatives are useful in prophylactic and therapeutic treatment of thrombotic complaints.

    Pristinamycin derivatives, their preparation and their use
    57.
    发明授权
    Pristinamycin derivatives, their preparation and their use 失效
    普瑞霉素衍生物，其制备及其应用

    公开(公告)号：US4590004A

    公开(公告)日：1986-05-20

    申请号：US630284

    申请日：1984-07-12

    申请人： Jean-Pierre Corbet ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris

    发明人： Jean-Pierre Corbet ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris

    IPC分类号： C07D498/18 ,  A61K9/08 ,  A61K31/42 ,  A61K38/00 ,  A61P31/04 ,  C07D498/20 ,  C07K5/078 ,  C07K7/06 ,  C07K5/12

    CPC分类号： C07K5/06182 ,  C07K7/06 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27

    摘要： The invention provides new pristinamycin II.sub.B derivatives of the formula: ##STR1## in which R represents alkylthio substituted by (i) alkylamino or dialkylamino of which the alkyl parts can form a pyrrolidin-1-yl, piperidino, azetidin-1-yl, azepin-1-yl, morpholino, thiomorpholino or piperazin-1-yl ring (optionally substituted by alkyl), or (ii) pyrrolidin-2-yl or pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl, azetidin-2-yl or azetidin-3-yl or azepin-2-yl, azepin-3-yl or azepin-4-yl;a radical Het-S-, in which Het is pyrrolidin-3-yl, piperidin-3-yl or piperidin-4-yl, azetidin-3-yl or azepin-3-yl or azepin-4-yl optionally N-alkylsubstituted; ordialkylamino of which the alkyl parts can form a pyrrolidin-1-yl, piperidino, azetidin-1-yl, azepin-1-yl, morpholino, thiomorpholino or piperazin-1-yl ring (optionally substituted by alkyl), the said alkyls having 1 to 5 carbon atoms each in a linear or branched chain. The compounds of the formula (I) are useful as antimicrobial agents when used in association with known synergistines or synergistines of the formula: ##STR2##

    摘要翻译： 本发明提供了下式的新霉素霉素IIB衍生物：其中R表示被（i）烷基氨基或二烷基氨基取代的烷硫基，其烷基部分可以形成吡咯烷-1-基，哌啶子基，氮杂环丁烷-1-基， 哌嗪-1-基，吗啉代，硫代吗啉代或哌嗪-1-基环（任选被烷基取代），或（ii）吡咯烷-2-基或吡咯烷-3-基，哌啶-2-基，哌啶-3-基 - 基或哌啶-4-基，氮杂环丁烷-2-基或氮杂环丁烷-3-基或氮杂-2-基，吖庚因-3-基或氮杂-4-基; 基团Het-S-，其中Het是吡咯烷-3-基，哌啶-3-基或哌啶-4-基，氮杂环丁烷-3-基或吖庚因-3-基或氮杂-4-基任选N-烷基取代 ; 或其二烷基氨基，其烷基部分可以形成吡咯烷-1-基，哌啶子基，氮杂环丁烷-1-基，吖庚因-1-基，吗啉代，硫代吗啉代或哌嗪-1-基环（任选被烷基取代），所述烷基 具有1至5个碳原子，各自为直链或支链。 当与已知的下式的增效剂或增效剂结合使用时，式（I）的化合物可用作抗微生物剂：（V）

    1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and anti-inflammatory activity
    59.
    发明授权
    1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and anti-inflammatory activity 失效
    1H，具有抗过敏和抗炎活性的3H-吡咯并[1,2-c]噻唑衍生物

    公开(公告)号：US4529728A

    公开(公告)日：1985-07-16

    申请号：US569908

    申请日：1984-01-11

    申请人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    IPC分类号： C07D471/04 ,  A61K31/425 ,  A61K31/429 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/54 ,  A61P7/02 ,  A61P29/00 ,  A61P37/08 ,  C07D213/02 ,  C07D233/60 ,  C07D513/04 ,  C07D521/00 ,  A61K31/445

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D513/04

    摘要： New compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 =H or alkyl and(a) R=CN or alkylcarbonyl, or(b) R=CON(R.sub.3)R.sub.4, in which R.sub.3 =H and R.sub.4 =NH.sub.2, alkylamino, dialkylamino, phenylamino or diphenylamino; or R.sub.3 and R.sub.4 =H, alkyl (1 to 5 C) or substituted phenyl; or R.sub.3 =H and R.sub.4 =pyridyl or alkyl (1 to 5 C) substituted by COOH, NH.sub.2, alkylamino, dialkylamino, morpholino, piperidino, pyrrolidin-1-yl, piperazin-1-yl (optionally substituted by alkyl, pyridyl or optionally substituted phenyl or benzyl), optionally substituted phenyl, pyridyl or imidazolyl; or R.sub.3 and R.sub.4 form an imidazolyl radical or a 5-membered or 6-membered heterocycle which can contain an oxygen, sulphur or nitrogen atom and which is optionally substituted by alkyl, alkoxycarbonyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, pyridyl, pyrimidinyl, pyrazinyl, optionally substituted phenyl or optionally substituted benzyl; or(c) R=--C(.dbd.NOH)NH.sub.2 or --C[.dbd.NN(R'R")NH.sub.2 ], in which R' and R"=alkyl,the said alkyl radicals and alkyl portions being straight-chain or branched-chain and, unless mentioned otherwise, containing 1 to 4 carbon atoms, and the substituted phenyl and benzyl radicals carrying a halogen atom or an alkyl, alkoxy, alkylthio, trifluoromethyl or dialkylamino radical, and their tautomeric forms, addition salts with acids and the metals salts and the addition salts with nitrogen bases, are useful anti-allergic and anti-inflammatory agents. A variety of methods of making them are described.

    摘要翻译： 式（I）的新化合物，其中R 1和R 2 = H或烷基和（a）R = CN或烷基羰基，或（b）R = CON（R3）R4，其中R3 = H和R4 = NH 2，烷基氨基，二烷基氨基，苯基氨基或二苯基氨基; 或R 3和R 4 = H，烷基（1至5 C）或取代的苯基; 或R 3 = H和R 4 =被COOH，NH 2，烷基氨基，二烷基氨基，吗啉代，哌啶子基，吡咯烷-1-基，哌嗪-1-基取代的吡啶基或烷基（1至5 C）（任选地被烷基，吡啶基或任选地 取代的苯基或苄基），任选取代的苯基，吡啶基或咪唑基; 或R3和R4形成咪唑基或可含有氧，硫或氮原子的5元或6元杂环，并且其任选被烷基，烷氧基羰基，羟基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，吡啶基，嘧啶基， 吡嗪基，任选取代的苯基或任选取代的苄基; 或（c）R = -C（= NOH）NH 2或-C [= NN（R'R“）NH 2]，其中R'和R”=烷基，所述烷基和烷基部分为直链， 链或支链，除非另有说明，含有1至4个碳原子，并且取代的苯基和苄基带有卤素原子或烷基，烷氧基，烷硫基，三氟甲基或二烷基氨基，以及它们的互变异构形式，与 酸和金属盐和与氮碱的加成盐是有用的抗过敏和抗炎剂。 描述了制作它们的各种方法。