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    • 3. 发明授权
    • New process for the preparation of pristinamycin II.sub.B derivatives
    • 制备原始蛋白霉素IIB衍生物的新方法
    • US4775753A
    • 1988-10-04
    • US70389
    • 1987-07-07
    • Jean-Claude BarriereJean-Pierre BastartJean-Marc Paris
    • Jean-Claude BarriereJean-Pierre BastartJean-Marc Paris
    • C07D498/18A61K31/42A61P31/04C07D498/14C07K5/06C07K5/078
    • C07D498/14C07K5/06182
    • 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.
    • 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。
    • 4. 发明授权
    • Pristinamycin derivatives, their preparation and their use
    • 普瑞霉素衍生物,其制备及其应用
    • US4590004A
    • 1986-05-20
    • US630284
    • 1984-07-12
    • Jean-Pierre CorbetClaude CotrelDaniel FargeJean-Marc Paris
    • Jean-Pierre CorbetClaude CotrelDaniel FargeJean-Marc Paris
    • C07D498/18A61K9/08A61K31/42A61K38/00A61P31/04C07D498/20C07K5/078C07K7/06C07K5/12
    • C07K5/06182C07K7/06A61K38/00Y10S930/19Y10S930/27
    • 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##
    • 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)
    • 6. 发明授权
    • Synergistine derivatives having anti-bacterial activity and their use
    • 具有抗菌活性的协同主义衍生物及其用途
    • US4618599A
    • 1986-10-21
    • US630288
    • 1984-07-12
    • Jean-Pierre CorbetClaude CotrelDaniel FargeJean-Marc Paris
    • Jean-Pierre CorbetClaude CotrelDaniel FargeJean-Marc Paris
    • C07D498/14A61K31/435A61K38/00A61P31/04C07D20060101C07D213/65C07D273/00C07D498/18C07K7/00C07K7/06A61K37/02C07K5/12
    • C07K7/06A61K38/00Y10S930/19Y10S930/27
    • 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.
    • 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。
    • 7. 发明授权
    • Synergistine derivatives, their preparation and pharmaceutical
compositions containing them
    • 协同三烯衍生物,它们的制备和含有它们的药物组合物
    • US4617290A
    • 1986-10-14
    • US630245
    • 1984-07-12
    • Jean-Pierre CorbetClaude CotrelDaniel FargeJean-Marc Paris
    • Jean-Pierre CorbetClaude CotrelDaniel FargeJean-Marc Paris
    • C07D498/14A61K31/435A61K38/00A61P31/04C07K7/06A61K37/02C07K5/12
    • C07K7/06A61K38/00
    • 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.
    • 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。
    • 8. 发明授权
    • Anti-rheumatic 5-(substituted amino)-1,2-dithiol-3-one compounds and
their use
    • 抗风湿5-(取代氨基)-1,2-二硫酚-3-酮化合物及其用途
    • US4576954A
    • 1986-03-18
    • US582043
    • 1984-02-21
    • Jean-Dominique BourzatClaude CotrelDaniel FargeJean-Marc ParisGerard Taurand
    • Jean-Dominique BourzatClaude CotrelDaniel FargeJean-Marc ParisGerard Taurand
    • C07D339/04C07D409/04C07D413/04A61K31/47C07D215/02C07D217/02
    • C07D409/04C07D339/04
    • 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##
    • 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)