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1. 发明申请

WO1998028329A1 CYCLOSPORIN DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：环磷酰胺衍生物，其制备和含有它们的药物组合物
公开(公告)号：WO1998028329A1
公开(公告)日：1998-07-02
申请号：PCT/FR1997002405
申请日：1997-12-23
申请人： RHONE-POULENC RORER S.A. , BARRIERE, Jean-Claude , BASHIARDES, Georges , CARRY, Jean-Christophe , EVERS, Michel , FILOCHE, Bruno , LECONTE, Jean-Pierre , MIGNANI, Serge
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07K07/64
CPC分类号： C07K7/645 , A61K38/00
摘要： The invention concerns cyclosporin derivatives characterised in that they comply with general formula (I) in which Alk is C2-C6 alkylene linear or branched or C3-C6 cycloalkylene and R is: either COOH or alkyloxycarbonyl, or -NR1R2 for which R1 and R2 identical or different are H, or alkyl, C2-C4 alkylene, C3-C6 cycloalkyl, phenyl optionally substituted (by halogen, alkyloxy, alkyloxycarbonyl, amino, alkylamino or dialkylamino) or are benzyl or saturated or unsaturated heterocyclic compound radicals containing 5 or 6 chains and 1 to 3 heteroatoms, or for which R1 and R2 form with the nitrogen atom to which they are bound a heterocyclic compound containing 4 to 6 chains capable of containing another heteroatom selected among N, O and S and optionally substituted by an alkyl, phenyl or benzyl, or a radical of general formula (I') for which R1 and R2 are defined as above, R3 is H or alkyl and n is a whole number from 2 to 4. The alkyl portions or radicals defined above are linear or branched and contain 1 to 4 carbon atoms as well as their pharmaceutically acceptable salts when they exist. These novel products are particularly useful for treating and or preventing retroviral infections.
摘要翻译：本发明涉及环孢菌素衍生物，其特征在于它们符合通式（I），其中Alk是直链或支链或C3-C6亚环烷基的C2-C6亚烷基，R是：COOH或烷氧基羰基，或-NR1R2，其中R1和R2相同或不同的是H或烷基，C 2 -C 4亚烷基，C 3 -C 6环烷基，任选被（卤素，烷氧基，烷氧基羰基，氨基，烷基氨基或二烷基氨基）取代的苯基）或是含有5或6个链的苄基或饱和或不饱和杂环化合物或1至3个杂原子，或者R1和R2与它们所连接的氮原子形成杂环化合物，该杂环化合物含有能够含有选自N，O和S中的另外的杂原子并且任选被烷基取代的4至6个链，苯基或苄基，或其中R 1和R 2如上定义的通式（I'）的基团，R 3为H或烷基，n为2至4的整数。上述烷基部分或自由基为直链或支链当它们存在时，它们含有1至4个碳原子以及它们的药学上可接受的盐。这些新产品对于治疗和/或预防逆转录病毒感染特别有用。

2. 发明申请

WO1997000073A1 NOVEL USE FOR PYRROLE DERIVATIVES 审中-公开
标题翻译：用于光子衍生物的新用途
公开(公告)号：WO1997000073A1
公开(公告)日：1997-01-03
申请号：PCT/FR1996000887
申请日：1996-06-12
申请人： RHONE-POULENC RORER S.A. , BACQUE, Eric , BASHIARDES, Georges , DEREU, Norbert , NEMECEK, Conception
发明人： RHONE-POULENC RORER S.A.
IPC分类号： A61K31/44
CPC分类号： C07D471/04 , A61K31/4439 , C07D487/04 , C07D513/04
摘要： A novel therapeutical use of pyrrole derivatives of general formula (I), wherein Het is a ring fused with pyrrole to form a pyrrolothiazole, tetrahydro-5,6,7,8-indolizine, dihydro-pyrrolothiazine or dihydropyrrolizine ring, R1 is a carboxamide, cyano, carboxy, alkyloxycarbonyl, acyl or imidazolylcarbonyl radical, R2 is a hydrogen or halogen atom or an alkyl, alkenyl, trihalomethyl or cyano radical, R3 is a hydrogen or halogen atom or a hydroxy or alkyl radical, and Het' is a pyridyl, pyridyl N-oxide or thiazolyl radical, the alkyl or acyl radicals being straight or branched and having 1-4 carbon atoms, and the alkenyl radicals being straight or branched and having 2-4 carbon atoms, and salts thereof, if any, for preparing a drug for treating conditions in which TNF is involved.
摘要翻译：通式（I）的吡咯衍生物的新型治疗用途，其中Het是与吡咯稠合形成吡咯噻唑，四氢-5,6,7,8-中氮茚，二氢吡咯并噻嗪或二氢吡咯烷环的环，R 1是甲酰胺，氰基，羧基，烷氧基羰基，酰基或咪唑基羰基，R2是氢或卤素原子或烷基，烯基，三卤甲基或氰基，R3是氢或卤素原子或羟基或烷基，Het'是吡啶基，N-氧化吡啶基或噻唑基，所述烷基或酰基为直链或支链并具有1-4个碳原子，所述链烯基为直链或支链并具有2-4个碳原子，及其盐（如果有的话），制备用于治疗涉及TNF的病症的药物。

3. 发明申请

WO2012001308A9 PROCEDE DE SYNTHESE D'ALCALOIDES DU TYPE ERGOLINE PAR DOUBLE CYCLISATION A PARTIR DE BICYCLES INDOLIQUES, PRODUITS OBTENUS ET PRODUITS INTERMEDIAIRES 审中-公开
公开(公告)号：WO2012001308A9
公开(公告)日：2012-01-05
申请号：PCT/FR2011/051524
申请日：2011-06-29
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , UNIVERSITE DE POITIERS , BASHIARDES, Georges , LECORNUÉ, Frédéric , PICARD, Sébastien
发明人： BASHIARDES, Georges , LECORNUÉ, Frédéric , PICARD, Sébastien
IPC分类号： A61P25/00 , C07D209/12 , C07D457/00 , C07D487/06 , A61P35/00 , A61K31/407
摘要： La présente invention concerne un procédé de préparation d'analogues structurels des alcaloïdes ergoline tétra- et penta- et polycycliques, en quatre étapes à partir d'un indole-3-carboxaldéhyde, dont les deux étapes- clé suivante : une étape de couplage d'un analogue indolique N-protégé 4-iodé et 3-fluoré avec un promoteur de fonction insaturée dipolarophile, notamment un organostannique, ce qui mène au 3-formyl-4-alcénylindole ou au 3-formyl-4-alcynylindole. Ces intermédiaires comportent d'une part une fonction aldéhyde, qui est transformée en ylure d'azométhine et d'autre part une fonction insaturée dipolarophile, ceci permettant la réaction dipolaire [3+2] de la seconde étape-clé, la réaction de cyclisation, cycloaddition, est conduite avec un composé α-amino-fonctionnalisé, par exemple du type α-aminoester et conduit après condensation et cycloaddition à des indoles tétra-, penta- et polycycliques attendus.

4. 发明申请

WO2012001308A1 METHOD FOR SYNTHESIZING ERGOLINE ALKALOIDS FROM INDOLIC BICYCLIC COMPOUNDS BY DOUBLE CYCLIZATION, RESULTING MATERIALS, AND INTERMEDIATE MATERIALS 审中-公开
标题翻译：通过双环化合成雌二醇生物碱的方法，催化材料和中间体材料
公开(公告)号：WO2012001308A1
公开(公告)日：2012-01-05
申请号：PCT/FR2011051524
申请日：2011-06-29
申请人： CENTRE NAT RECH SCIENT , UNIV POITIERS , BASHIARDES GEORGES , LECORNUE FREDERIC , PICARD SEBASTIEN
发明人： BASHIARDES GEORGES , LECORNUE FREDERIC , PICARD SEBASTIEN
IPC分类号： A61P25/00 , A61K31/407 , A61P35/00 , C07D209/12 , C07D457/00 , C07D487/06
CPC分类号： C07F7/0814 , C07D209/12 , C07D487/06 , C07D487/14 , C07F7/0812
摘要： The present invention relates to a method for preparing structural analogues of tetracyclic, pentacyclic, and polycyclic ergoline alkaloids, in four steps, from an indole-3-carboxaldehyde, wherein the method includes the following two key steps: a step of coupling an N-protected 4-iodized 3-fluorinated indolic analogue with an unsaturated dipolarophilic function promoter, in particular an organostannic compound, thus leading to 3-formyl-4-alkenylindole or 3-formyl-4-alkynylindole. Said intermediates comprise an aldehyde function, which is converted into azomethine ylide, as well as a dipolarophilic unsaturated function that enables the dipolar reaction [3+2] of the second key step. The cyclization reaction, i.e. cycloaddition, is performed with an a-amino-functionalized compound, for example an a-aminoester compound, and, after condensation and cycloaddition, results in anticipated tetracyclic, pentacyclic, and polycyclic indoles.
摘要翻译：本发明涉及由吲哚-3-甲醛分四个步骤制备四环，五环和多环麦角灵生物碱的结构类似物的方法，其中该方法包括以下两个关键步骤：用不饱和双亲性官能促进剂，特别是有机锡化合物，由此得到3-甲酰基-4-烯基吲哚或3-甲酰基-4-炔基吲哚。所述中间体包含转化为偶氮甲碱叶立德的醛官能团，以及能够进行第二关键步骤的偶极反应[3 + 2]的双亲水性不饱和官能团。用α-氨基官能化的化合物，例如α-氨基酯化合物进行环化反应，即环加成反应，并且在缩合和环加成后得到预期的四环，五环和多环吲哚。

5. 发明申请

WO1998028330A1 NOVEL CYCLOSPORIN DERIVATIVES, METHOD OF PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新型环磷酰胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：WO1998028330A1
公开(公告)日：1998-07-02
申请号：PCT/FR1997002406
申请日：1997-12-23
申请人： RHONE-POULENC RORER S.A. , BARRIERE, Jean-Claude , BASHIARDES, Georges , CARRY, Jean-Christophe , EVERS, Michel , FILOCHE, Bruno , MIGNANI, Serge
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07K07/64
CPC分类号： C07K7/645 , A61K38/00
摘要： The invention concerns cyclosporin derivatives of general formula (I) in which Alk is C2-C6 alkylene linear or branched or C3-C6 cycloalkylene and R is: either OH, COOH or alkyloxycarbonyl, or -NR1R2 for which R1 and R2 identical or different are H, or alkyl, C2-C4 alkylene, C3-C6 cycloalkyl, phenyl optionally substituted (by halogen, alkyloxy, alkyloxycarbonyl, amino, alkylamino or dialkylamino), or are benzyl or saturated or unsaturate heterocyclic compound containing 5 or 6 chains and 1 to 3 heteroatoms, or for which R1 and R2 form with the nitrogen atom to which they are bound a heterocyclic compound containing 4 to 6 chains capable of containing another heteroatom selected among N, O or S and optionally substituted by an alkyl, phenyl or benzyl, or a radical of general formula (I') for which R1 and R2 are as defined above, R3 is H or alkyl and n is a whole number from 2 to 4. The alkyl portions or radicals defined above are linear or branched and contain 1 to 4 carbon atoms, as well as their pharmaceutically acceptable salts when they do exist. These novel products are particularly useful for treating and/or preventing retroviral infections.
摘要翻译：本发明涉及通式（I）的环孢菌素衍生物，其中Alk是C2-C6亚烷基直链或支链或C3-C6亚环烷基，R是：OH，COOH或烷氧基羰基，或-NR1R2，其中R1和R2相同或不同 H或烷基，C 2 -C 4亚烷基，C 3 -C 6环烷基，任选被（卤素，烷氧基，烷氧基羰基，氨基，烷基氨基或二烷基氨基）取代的苯基，或者是含有5或6个链的苄基或饱和或不饱和杂环化合物， 3个杂原子，或其中R1和R2与其结合的氮原子形成的杂环化合物，其含有能够含有选自N，O或S中的另外的杂原子且任选被烷基，苯基或苄基取代的4至6个链的杂环化合物，或其中R 1和R 2如上所定义的通式（I'）基团，R 3为H或烷基，n为2至4的整数。上述烷基部分或自由基为直链或支链并含有1 至4个碳原子当它们确实存在时，作为其药学上可接受的盐。这些新产品对于治疗和/或预防逆转录病毒感染特别有用。

6. 发明申请

WO1998028328A1 CYCLOSPORIN DERIVATIVE, ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：环磷酰胺衍生物，其制备和含有相同的药物组合物
公开(公告)号：WO1998028328A1
公开(公告)日：1998-07-02
申请号：PCT/FR1997002404
申请日：1997-12-23
申请人： RHONE-POULENC RORER S.A. , BARRIERE, Jean-Claude , BASHIARDES, Georges , CARRY, Jean-Christophe , EVERS, Michel , FILOCHE, Bruno , MIGNANI, Serge
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07K07/64
CPC分类号： C07K7/645 , A61K38/00
摘要： The invention concerns a cyclosporin derivative of formula (I). This novel product is particularly useful for treating and/or preventing retroviral infections.
摘要翻译：本发明涉及式（I）的环孢菌素衍生物。该新产品对于治疗和/或预防逆转录病毒感染特别有用。

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