公开(公告)号：US4755599A

公开(公告)日：1988-07-05

申请号：US10558

申请日：1987-02-03

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

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

IPC分类号： A61K31/135 ,  A61K31/10 ,  A61K31/137 ,  A61K31/21 ,  A61K31/22 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02 ,  C07C215/28 ,  C07C215/30 ,  C07C215/42 ,  C07C219/22 ,  C07C219/32 ,  C07C239/00 ,  C07C271/20 ,  C07C313/00 ,  C07C317/28 ,  C07C317/36 ,  C07C319/20 ,  C07C323/27 ,  C07C323/32 ,  C07C323/65 ,  C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/084 ,  C07D295/092 ,  C07D307/32 ,  C07F9/40 ,  C07D279/04 ,  C07C149/24 ,  C07D205/04 ,  C07D223/04 ,  C07D275/02 ,  C07D277/04 ,  C07D401/06

CPC分类号： C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/092 ,  C07D307/32 ,  C07F9/4006

摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups,(ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring,it being understood that the alkyl radicals and alkyl parts contains 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.

摘要翻译： 本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N， 或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基 ，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6 C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，且R7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2， 烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环包含5或6个C，任选地连接到苯环，应理解烷基和烷基 部分包含1至4 C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。 这些化合物可用作抗抑郁药。

公开(公告)号：US4618599A

公开(公告)日：1986-10-21

申请号：US630288

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： C07D498/14 ,  A61K31/435 ,  A61K38/00 ,  A61P31/04 ,  C07D20060101 ,  C07D213/65 ,  C07D273/00 ,  C07D498/18 ,  C07K7/00 ,  C07K7/06 ,  A61K37/02 ,  C07K5/12

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

摘要： The invention provides new synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 and (a) R.sub.1 and R.sub.2 =H and R=pyrrolidin-3-ylthio or piperidin-3-ylthio or piperidin-4-ylthio (optionally substituted by alkyl), or altenatively R=alkylthio substituted by 1 or 2 SO.sub.3 H radicals or alkylamino or dialkylamino radicals (optionally substituted) or by 1 or 2 piperazino rings (optionally substituted) or morpholino, thiomorpholino, piperidino, pyrrolidin-1-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl or pyrrolidin-2-yl or pyrrolidin-3-yl rings (these last 5 rings being optionally substituted by alkyl), or(b) R.sub.1 and R.sub.2 form a bond and R=pyrrolidin-3-ylamino, piperidin-3-ylamino or piperidin-4-ylamino, pyrrolidin-3-yloxy, piperidin-3-yloxy or piperidin-4-yloxy, pyrrolidin-3-ylthio, piperidin-3-ylthio or piperidin-4-ylthio (optionally substituted by alkyl), or alternatively R=alkylamino, alkoxy or alkylthio substituted by 1 or 2 SO.sub.3 H radicals, alkylamino or dialkylamino radicals (optionally substituted) or trialkylammonio or imidazol-4-yl or imidazol-5-yl radicals or by 1 or 2 piperazino rings (optionally substituted by alkyl) or morpholino, thiomorpholino, piperidino, pyrrolidin-1-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl or pyrrolidin-2-yl or pyrrolidin-3-yl rings (these last two rings being optionally substituted by alkyl), and their salts, their preparation, and the pharmaceutical compositions in which they are present. These compounds are useful as anitbacterial agents.

摘要翻译： 本发明提供下式的新增效剂衍生物：其中Y = H或N（CH 3）2和（a）R 1和R 2 = H，R =吡咯烷-3-基硫代或哌啶-3-基硫基 或哌啶-4-基硫代（任选被烷基取代），或惰性地R =被1或2个SO 3 H基团取代的烷硫基或烷基氨基或二烷基氨基（任选取代的）或1或2个哌嗪子基环（任选取代的）或吗啉代，硫代吗啉代， 哌啶子基，吡咯烷-1-基，哌啶-2-基，哌啶-3-基或哌啶-4-基或吡咯烷-2-基或吡咯烷-3-基环（这5个环任选被烷基取代） 或（b）R 1和R 2形成键，R =吡咯烷-3-基氨基，哌啶-3-基氨基或哌啶-4-基氨基，吡咯烷-3-基氧基，哌啶-3-基氧基或哌啶-4-基氧基，吡咯烷 -3-烷硫基（任选被烷基取代），或者R =被1或2个SO 3 H基取代的烷基氨基，烷氧基或烷硫基，烷基氨基或二烷基氨基 （任选取代的）或三烷基氨基或咪唑-4-基或咪唑-5-基或1或2个哌嗪子基环（任选被烷基取代）或吗啉代，硫代吗啉代，哌啶子基，吡咯烷-1-基，哌啶-2-基， 哌啶-3-基或哌啶-4-基或吡咯烷-2-基或吡咯烷-3-基环（这些最后两个环任选被烷基取代），及其盐，它们的制备和药物组合物 他们在场。 这些化合物可用作厌氧细菌剂。

公开(公告)号：US4617290A

公开(公告)日：1986-10-14

申请号：US630245

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： C07D498/14 ,  A61K31/435 ,  A61K38/00 ,  A61P31/04 ,  C07K7/06 ,  A61K37/02 ,  C07K5/12

CPC分类号： C07K7/06 ,  A61K38/00

摘要： The invention provides novel synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 : and R.sub.1 =H and R.sub.2 =OH or alkyl optionally substituted by COOH, alkoxycarbonyl or OH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 =cycloalkyl (of 3 to 7 carbons) or a heterocycle chosen from azetidine, pyrrolidine, piperidine or azepine (optionally substituted on the nitrogen by alkyl), or R.sub.1 =formyl or alkylcarbonyl and R.sub.2 =alkyl substituted by COOH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 is a heterocycle as defined above, or R.sub.1 and R.sub.2, which are identical or different, represent alkyl optionally substituted by COOH, alkoxycarbonyl, OH, alkylamino, or dialkylamino of which the alkyl radicals can form a heterocycle, or R.sub.1 and R.sub.2 form an azetidine, pyrrolidine, piperidine, morpholine or piperazine ring (optionally substituted by alkyl), all the alkyls having 1 to 5 carbon atoms. These compounds are useful as antibacterial agents.

摘要翻译： 本发明提供了下式的新型增效剂衍生物：其中Y = H或N（CH 3）2：和R 1 = H且R 2 = OH或任选被COOH，烷氧基羰基或OH取代的烷基或烷基氨基或 二烷基氨基，其烷基可以形成杂环，或R2 =环烷基（3至7个碳）或选自氮杂环丁烷，吡咯烷，哌啶或吖庚因的杂环（任选在氮上被烷基取代），或R1 =甲酰基或烷基羰基 并且R 2 =被COOH取代的烷基或被烷基氨基或二烷基氨基取代的烷基，其烷基可以形成杂环，或者R2是如上定义的杂环，或者相同或不同的R 1和R 2表示任选被COOH取代的烷基，烷氧基羰基 ，烷基氨基或二烷基氨基，其中烷基可形成杂环，或R 1和R 2形成氮杂环丁烷，吡咯烷，哌啶，吗啉或哌嗪环（任选被烷基取代），所有烷基具有1至5个碳原子。 这些化合物可用作抗菌剂。

公开(公告)号：US4576954A

公开(公告)日：1986-03-18

申请号：US582043

申请日：1984-02-21

申请人： Jean-Dominique Bourzat ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris ,  Gerard Taurand

发明人： Jean-Dominique Bourzat ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris ,  Gerard Taurand

IPC分类号： C07D339/04 ,  C07D409/04 ,  C07D413/04 ,  A61K31/47 ,  C07D215/02 ,  C07D217/02

CPC分类号： C07D409/04 ,  C07D339/04

摘要： New derivatives of the general formula (I) in which:R=H or Cl and either R.sub.1 and R.sub.2 form a tetrahydroquinoxaline, tetrahydroquinoline, tetrahydroisoquinoline, dihydrobenzoxazine, tetrahydro-1H-benzazepine or isoindoline ring, it being possible for all these rings to be substituted by one or more halogen, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano, nitro, alkoxy, alkylthio or alkyl, substituted by carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, hydroxyl, amino, alkylamino or dialkylamino, or R.sub.1 =alkyl and R.sub.2 =alkyl substituted by phenyl which is itself unsubstituted or substituted by one or more halogen, alkyl, alkoxy, alkylthio, hydroxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano or nitro, all the alkyls having 1 to 4 C in a straight or branched chain.These new products are used as antirheumatics. ##STR1##

摘要翻译： 通式（I）的新衍生物，其中：R = H或Cl，R 1和R 2形成四氢喹喔啉，四氢喹啉，四氢异喹啉，二氢苯并恶嗪，四氢-1H-苯并氮杂或异吲哚啉环，所有这些环都是可能的 被一个或多个卤素，羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，三氟甲基，氰基，硝基，烷氧基，烷硫基或被羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，羟基，氨基，烷基氨基或二烷基氨基取代的烷基取代， 烷基，烷氧基，烷硫基，羟基，氨基，烷基氨基，二烷基氨基，羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，三氟甲基，氰基或 硝基，所有烷基在直链或支链上具有1-4个碳原子。 这些新产品被用作抗风湿剂。 （一）

公开(公告)号：US06833382B2

公开(公告)日：2004-12-21

申请号：US09987614

申请日：2001-11-15

申请人： Véronique Blanc ,  Denis Thibaut ,  Nathalie Bamas-Jacques ,  Francis Blanche ,  Joël Crouzet ,  Jean-Claude Barriere ,  Laurent Debussche ,  Alain Famechon ,  Jean-Marc Paris ,  Gilles Dutruc-Rosset

发明人： Véronique Blanc ,  Denis Thibaut ,  Nathalie Bamas-Jacques ,  Francis Blanche ,  Joël Crouzet ,  Jean-Claude Barriere ,  Laurent Debussche ,  Alain Famechon ,  Jean-Marc Paris ,  Gilles Dutruc-Rosset

IPC分类号： A61K3140

CPC分类号： C07D295/155 ,  A61K38/00 ,  C07C229/36 ,  C07C229/42 ,  C07C233/15 ,  C07C233/25 ,  C07C323/63 ,  C07K7/06 ,  C12N15/52 ,  C12N15/76

摘要： Novel group B streptogramin-like compounds of general formula (I), and a method for preparing streptogramines by mutasynthesis using a mutated micro-organism to influence the biosynthesis of at least one of the precursors of group B streptogramins are disclosed. Novel nucleotide sequences involved in the biosynthesis of said precursors, and their uses, are also disclosed.

摘要翻译： 公开了通式（I）的新型B族链霉素样化合物，以及通过使用突变微生物进行突变的制备链霉菌素以影响至少一种B族链霉素前体的生物合成的方法。 还公开了涉及所述前体的生物合成的新型核苷酸序列及其用途。

公开(公告)号：US06352839B1

公开(公告)日：2002-03-05

申请号：US08765907

申请日：1997-03-20

申请人： Véronique Blanc ,  Denis Thibaut ,  Nathalie Bamas-Jacques ,  Francis Blanche ,  Joël Crouzet ,  Jean-Claude Barriere ,  Laurent Debussche ,  Alain Famechon ,  Jean-Marc Paris ,  Gilles Dutruc-Rosset

发明人： Véronique Blanc ,  Denis Thibaut ,  Nathalie Bamas-Jacques ,  Francis Blanche ,  Joël Crouzet ,  Jean-Claude Barriere ,  Laurent Debussche ,  Alain Famechon ,  Jean-Marc Paris ,  Gilles Dutruc-Rosset

IPC分类号： C12P100

CPC分类号： C07D295/155 ,  A61K38/00 ,  C07C229/36 ,  C07C229/42 ,  C07C233/15 ,  C07C233/25 ,  C07C323/63 ,  C07K7/06 ,  C12N15/52 ,  C12N15/76

摘要： The invention provides a method for preparing streptogramins using genetically-modified microorganisms to influence the biosynthesis of at least one of the precursors of the group B streptogramins. Cultures of the genetically-modified microorganisms are supplemented with a least one precursor that is different from the streptogramin precursor whose biosynthesis is altered and the streptogramins produced are recovered.

摘要翻译： 本发明提供了使用遗传修饰的微生物来制备链霉素的方法，所述基因修饰的微生物影响B群链霉素的至少一种前体的生物合成。 对经遗传修饰的微生物的培养物补充有至少一种不同于生物合成改变的链霉素前体的前体，并且生成的链霉蛋白酶被回收。

公开(公告)号：US5556861A

公开(公告)日：1996-09-17

申请号：US472766

申请日：1995-06-07

申请人： Eric Bacque ,  Michel Barreau ,  Jean-Francois Desconclois ,  Philippe Girard ,  Michel Kryvenko ,  Marc P. Lavergne ,  Jean-Marc Paris ,  Guy Picaut

发明人： Eric Bacque ,  Michel Barreau ,  Jean-Francois Desconclois ,  Philippe Girard ,  Michel Kryvenko ,  Marc P. Lavergne ,  Jean-Marc Paris ,  Guy Picaut

IPC分类号： C07D471/04 ,  A61K31/435

CPC分类号： C07D471/04

摘要： This invention relates to a novel 1,8 benzo[b]naphythyridine derivative of general formula (I), ##STR1## wherein R is H or a hydroxy, amino or alkylamino radical optionally substituted by amino or hydroxy, or R is dialkylamino of which the alkyl portions may form, with the nitrogen atom, a 5- or 6-membered heterocyclic ring which optionally contains a further heteroatom chosen from nitrogen, oxygen or sulphur, or R is C.sub.3-6 cycloalkylamino or an alkanylamino, N-alkyl N-alkanylamino or aminoalkylphenylamino radical; R.sub.1 and R.sub.2, which are the same or different, are in positions 2 and 3 and represent H, alkyl, C.sub.2-4 alkenyl, phenyl, or substituted phenyl, or R.sub.1 and R.sub.2 are in position 2 and represent alkyl; R.sub.3 is H or alkyl, fluoroalkyl, carboxyalkyl, C.sub.3-6 cycloalkyl, fluorophenyl, difluorophenyl, alkyloxy or alkylamino; and R.sub.4 is H or F, wherein the C.sub.1-4 alkanyl and alkyl radicals are linear or branched; stereoisomeric forms thereof or mixtures of these; and salts and hydrated forms thereof. These novel derivatives are useful as antimicrobials.

摘要翻译： 本发明涉及通式（I）的新颖的1,8-苯并[b]萘啶衍生物，其中R是H或羟基，任选被氨基或羟基取代的氨基或烷基氨基，或R是 烷基部分可以与氮原子形成的二烷基氨基，其任选地含有选自氮，氧或硫的另外的杂原子的5-或6-元杂环，或R是C 3-6环烷基氨基或烷基氨基， 烷基N-烷基氨基或氨基烷基苯基氨基; R1和R2相同或不同，位于2和3位，代表H，烷基，C2-4烯基，苯基或取代苯基，或R1和R2位于2位，代表烷基; R3是H或烷基，氟代烷基，羧基烷基，C3-6环烷基，氟苯基，二氟苯基，烷氧基或烷基氨基; R4是H或F，其中C1-4烷基和烷基是直链或支链的; 其立体异构形式或它们的混合物; 及其盐和水合形式。 这些新型衍生物可用作抗微生物剂。

公开(公告)号：US4686309A

公开(公告)日：1987-08-11

申请号：US702088

申请日：1985-02-15

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

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

IPC分类号： A61K31/135 ,  A61K31/10 ,  A61K31/137 ,  A61K31/21 ,  A61K31/22 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02 ,  C07C215/28 ,  C07C215/30 ,  C07C215/42 ,  C07C219/22 ,  C07C219/32 ,  C07C239/00 ,  C07C271/20 ,  C07C313/00 ,  C07C317/28 ,  C07C317/36 ,  C07C319/20 ,  C07C323/27 ,  C07C323/32 ,  C07C323/65 ,  C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/084 ,  C07D295/092 ,  C07D307/32 ,  C07F9/40 ,  C07C91/16 ,  C07C67/02 ,  C07D211/70

CPC分类号： C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/092 ,  C07D307/32 ,  C07F9/4006

摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups, (ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring, it being understood that the alkyl radicals and alkyl parts contain 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.

摘要翻译： 本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N， 或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基 ，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，R 7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2， 烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环含有5或6个C，任选地连接到苯环，应理解烷基和烷基 部分含有1至4个C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。 这些化合物可用作抗抑郁药。

公开(公告)号：US4775753A

公开(公告)日：1988-10-04

申请号：US70389

申请日：1987-07-07

申请人： Jean-Claude Barriere ,  Jean-Pierre Bastart ,  Jean-Marc Paris

发明人： Jean-Claude Barriere ,  Jean-Pierre Bastart ,  Jean-Marc Paris

IPC分类号： C07D498/18 ,  A61K31/42 ,  A61P31/04 ,  C07D498/14 ,  C07K5/06 ,  C07K5/078

CPC分类号： C07D498/14 ,  C07K5/06182

摘要： Pristinamycin II.sub.B derivatives of formula I in which R represents: ##STR1## either a 4- to 7-membered nitrogen-containing heterocyclic radical, optionally containing 1 or more other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl,or alkyl of 2 to 4 carbon atoms, substituted by 1 or 2 radicals chosen from phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino having 3 to 6 ring carbon atoms, alkylamino, dialkylamino or dialkylcarbamoyloxy (the alkyl parts of these last 2 radicals being optionally joined to form, with the nitrogen atom to which they are attached, a 4- to 7-membered saturated or unsaturated heterocycle optionally containing another hetero atom chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl) or a said alkyl substituted by one or more 4- or 7-membered nitrogen-containing heterocycles optionally containing 1 or 2 other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form and unsubstituted or substituted by an alkyl radical, the said heterocycles being attached to the alkyl via a carbon atom, at least one of the substituents carried by the alkyl being a nitrogen-containing substituent capable of forming salts,or a [(S)-1-methyl-2-pyrrolidinyl]methyl radical, the aforesaid alkyl radicals being straight-chain or branched and containing, unless otherwise stated, 1 to 10 carbon atoms each, including isomeric forms thereof and mixtures thereof, and the salts thereof, are made by oxidizing a pristinamycin II.sub.B derivative of formula II ##STR2## with potassium peroxymonosulphate.

摘要翻译： 式I的普瑞霉素IIB衍生物，其中R表示：（I）4-元至7-元含氮杂环基，任选地含有1或多个选自亚砜中的氮，氧和硫的其它杂原子，或 砜基形式，未取代的或被烷基取代或被2至4个碳原子的烷基取代，被1或2个选自苯基，环烷基氨基或具有3至6个环碳原子的N-烷基-N-环烷基氨基的基团取代，烷基氨基，二烷基氨基或 二烷基氨基甲酰氧基（这些最后2个基团的烷基部分任选地连接形成与它们所连接的氮原子一起形成4-7元饱和或不饱和的杂环，任选地含有另外选自氮，氧和硫的杂原子） 亚砜或砜形式，未取代或被烷基取代）或被一个或多个4-或7-元含氮杂环取代的所述烷基，任选地含有1或2个其它h 选自氮，氧和硫的亚杂原子或未被取代或被烷基取代的杂原子，所述杂环经由碳原子连接到烷基上，烷基所携带的至少一个取代基是氮 （S）-1-甲基-2-吡咯烷基]甲基，上述烷基是直链或支链的并且除非另有说明，含有各自为1-10个碳原子， 包括其异构体形式及其混合物及其盐通过用过氧单硫酸钾与过氧化硫酸盐钾一起氧化式II的嘌呤霉素IIB衍生物来制备。

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）