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91. 发明申请

WO1997010246A1 INDENO[1,2-e]PYRAZIN-4-ONES, PREPARATION THEREOF AND MEDICAMENTS CONTAINING SAME 审中-公开
标题翻译： INDENO [1,2-e]吡嗪-4-酮，其制备方法和含有其的药物
公开(公告)号：WO1997010246A1
公开(公告)日：1997-03-20
申请号：PCT/FR1996001404
申请日：1996-09-12
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , DAMOUR, Dominique , HARDY, Jean-Claude , JIMONET, Patrick , MIGNANI, Serge , MANFRE, Franco , NEMECEK, Patrick
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of formula (I), wherein R is a C=CH-R2, C(R3)R4, CH-NH2, CH-CH(OH)-COOH or CH-CH(OH)-COOalk radical, R1 is an -alk-NH2 or alk-NH-CO-R5 radical, R2 is a -COOH or -COOalk radical, R3 is an alkyl, -alk-Ar or -alk-Het radical, R4 is an -NH2, -NH-alk, -N(alk)-alk', -NH-CO-alk, -NH-CO-Ar', -NH-CO-ALK-Ar', -NH-CO-Het, -NH-CO-alk-Het, -NH-CO-alk-COOH, -NH-CO-alk-COOalk', -alk-COOH, -alk-COOalk', -NH-CO-NH2, -NH-CO-NH-alk, -NH-CO-NH-Ar' or -NH-CO-NH-alk-Ar' radical, or R3 and R4, together with the carbon atom to which they are attached, form a 2- or 3-pyrrolidine, 2- or 4-piperidine or 2-azacycloheptane substituted or unsubstituted ring, R5 is an -NH2, -NH-alk, -NH-Ar', -NH-cycloalkyl, -NH-alk-Ar' or -N(alk)-alk' radical, the salts thereof, the preparation thereof and medicaments containing same are described.
摘要翻译：式（I）化合物，其中R是C = CH-R 2，C（R 3）R 4，CH-NH 2，CH-CH（OH）-COOH或CH-CH（OH）烷基-NH2或烷基-NH-CO-R5基，R2是-COOH或-COOalk基，R3是烷基，-alk-Ar或-alk-Het基，R4是-NH2，-NH-alk， -N（烷基）-alk'，-NH-CO-烷基，-NH-CO-Ar'，-NH-CO-ALK-Ar'，-NH-CO-Het，-NH-CO- -NH-CO-alk-COOH，-NH-CO-alk-COOalk'，-alk-COOH，-alk-COOalk'，-NH-CO-NH2，-NH-CO-NH- -NH-Ar'或-NH-CO-NH-alk-Ar'基团，或者R 3和R 4与它们所连接的碳原子一起形成2-或3-吡咯烷，2-或4-哌啶或2-氮杂环庚烷取代或未取代的环，R5是-NH2，-NH-alk，-NH-Ar'， - NH-环烷基，-NH-alk-Ar'或-N（alk）-alk'基团，其盐，其制备方法和含有它们的药物。

92. 发明申请

WO1997005110A1 PERHYDROISOINDOLE DERIVATIVES AS SUBSTANCE P AND NEUROKININE A ANTAGONISTS 审中-公开
标题翻译：作为物质P和神经氨酸的拮抗剂衍生物
公开(公告)号：WO1997005110A1
公开(公告)日：1997-02-13
申请号：PCT/IB1996000783
申请日：1996-07-25
申请人： RHONE-POULENC RORER S.A. , MALLERON, Jean-Luc , PEYRONEL, Jean-François , SABUCO, Jean-François
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D209/44
CPC分类号： C07D209/44
摘要： Compounds are described having formula (I) and salts and solvates thereof wherein R represents phenyl optionally substituted in the ring 2 or 3 position with fluorine, chlorine or methyl, R represents a group -NR R or an ammonio radical of structure (II), R represents phenyl optionally substituted by one or more of halogen, C1-4alkyl, trifluoromethyl or C1-4alkyloxy, and n represents an integer from 2 to 4. The novel compounds according to the invention simultaneously antagonize the effects of tachykinins on NK1 and NK2 receptors and are particularly advantageous therapeutic agents for the treatment of a variety of diseases and disorders, including those of the respiratory system.
摘要翻译：具有式（I）的化合物及其盐和溶剂化物，其中R表示在环2或3位上被氟，氯或甲基任选取代的苯基，R 1表示基团-NR a R b或结构（II）的铵基，R 2表示任选被一个或多个卤素，C 1-4烷基，三氟甲基或C 1-4烷氧基取代的苯基，n表示2-4的整数。根据发明同时拮抗速激肽对NK1和NK2受体的作用，并且是用于治疗各种疾病和病症（包括呼吸系统疾病和病症）的特别有利的治疗剂。

93. 发明申请

WO1997003050A1 4,9-ETHANO-BENZO(F)ISOINDOLE DERIVATIVES AS FARNESYL TRANSFERASE INHIBITORS 审中-公开
标题翻译： 4,9-ETHANO-BENZO（F）作为FARNESYL转移酶抑制剂的ISO衍生物
公开(公告)号：WO1997003050A1
公开(公告)日：1997-01-30
申请号：PCT/FR1996001062
申请日：1996-07-08
申请人： RHONE-POULENC RORER S.A. , COMMERÇON, Alain , LEBRUN, Alain , MAILLIET, Patrick , PEYRONEL, Jean-François , SOUNIGO, Fabienne , TRUCHON, Alain , ZUCCO, Martine
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D209/72
CPC分类号： C07D209/72 , C07F9/5728
摘要： Novel products of general formula (I), preparation thereof and pharmaceutical compositions containing said products are disclosed. In general formula (I), R is a radical of general formula -(CH2)m-X1-(CH2)n-Z, where X1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH2 radicals being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR4, where R4 is alkyl, or CON(R5)(R6), where R5 is hydrogen or alkyl and R6 is hydrogen or optionally substituted alkyl, or else R5 is hydrogen or alkyl and R6 is hydroxy, optionally substituted alkyloxy or amino, or PO(OR7)2, where R7 is hydrogen or alkyl; or a radical -NH-CO-T where T is hydrogen or optionally substituted alkyl; or else a radical (a); R1 and R2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R1 and R2 in ortho positions form a heterocyclic ring containing 1 or 2 optionally substituted heteroatoms, or R1 is hydrogen or halogen or optionally substituted alkyloxy or alkyl, and R2 is thioalkyl; R3 is hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; X is O or S or -NH-, -CO-, methylene, ethylene, alkylidene or 1,1-cycloalkyl; and Y is O or S. The novel products of general formula (I) are farnesyl transferase inhibitors having remarkable antitumoral and antineoplastic properties.
摘要翻译：公开了通式（I）的新产品，其制备方法和含有所述产物的药物组合物。在通式（I）中，R为通式 - （CH2）m-X1-（CH2）nZ的基团，其中X1为单键或O或S，n为0或1，n为0,1或 2，CH2基任选被羧基，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，氨基，烷基氨基或二烷基氨基取代，Z是羧基，COOR4，其中R4是烷基或CON（R5）（R6），其中R5是氢或烷基，R 6是氢或任选取代的烷基，或者R 5是氢或烷基，R 6是羟基，任选取代的烷氧基或氨基或PO（OR 7）2，其中R 7是氢或烷基; 或其中T为氢或任选取代的烷基的基团-NH-CO-T; 或者一个激进的（a）; R 1和R 2是氢或卤素或任选取代的烷氧基或烷基，或者R 1和R 2在邻位形成含有1或2个任选取代的杂原子的杂环，或R 1是氢或卤素或任选取代的烷氧基或烷基，R 2是硫代; R3是氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基; X是O或S或-NH-，-CO-，亚甲基，亚乙基，亚烷基或1,1-环烷基; 并且Y是O或S.通式（I）的新产物是具有显着抗肿瘤和抗肿瘤性质的法呢基转移酶抑制剂。

94. 发明申请

WO1996038447A1 2-AZABICYCLO[2.2.1]HEPTANE DERIVATIVES, PREPARATION AND APPLICATION THEREOF 审中-公开
标题翻译： 2-氨基甲酰氯[2.2.1]庚烷衍生物，其制备和应用
公开(公告)号：WO1996038447A1
公开(公告)日：1996-12-05
申请号：PCT/FR1996000793
申请日：1996-05-28
申请人： RHONE-POULENC RORER S.A.
发明人： RHONE-POULENC RORER S.A. , LARGEAU, Denis , LEON, Patrick
IPC分类号： C07D471/08
CPC分类号： C07D209/02 , C07D209/52
摘要： Novel 1R or 1S 2-azabicyclo[2.2.1]heptane derivatives of general formula (I) or (I'), wherein R is a hydrogen atom or a radical of formula (II) or (II') respectively, where R1 is an alkyl radical containing 1-4 carbon atoms and Ar is an optionally substituted phenyl or alpha - or beta -naphthyl radical, and preparation and application thereof. The novel products of general formula (I) are particularly useful for preparing adenosine agonists.
摘要翻译：通式（I）或（I'）的新型1R或1S 2-氮杂双环[2.2.1]庚烷衍生物，其中R分别是氢原子或式（II）或（II'）的基团，其中R1是含有1-4个碳原子的烷基，Ar是任选取代的苯基或α-或β-萘基，及其制备和应用。通式（I）的新产品对于制备腺苷激动剂特别有用。

95. 发明申请

WO1996018744A2 PURIFICATION OF A TRIPLE HELIX FORMATION WITH AN IMMOBILIZED OLIGONUCLEOTIDE 审中-公开
标题翻译：用固定化的寡核苷酸修饰三螺旋形成
公开(公告)号：WO1996018744A2
公开(公告)日：1996-06-20
申请号：PCT/FR1995001468
申请日：1995-11-08
申请人： RHONE-POULENC RORER S.A. , CROUZET, Joël , SCHERMAN, Daniel , WILS, Pierre
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C12Q01/68
CPC分类号： C12Q1/6839 , Y10S977/924 , C12Q2565/137
摘要： Method for double-stranded DNA purification, by which a solution containing said DNA in a mixture with other components is passed over a support on which is covalently coupled an oligonucleotide capable of hybridizing with a specific sequence present on said DNA to form a triple helix.
摘要翻译：通过双链DNA纯化方法，将含有与其它组分的混合物中的所述DNA的溶液通过其上共价偶联能够与存在于所述DNA上的特定序列杂交的寡核苷酸以形成三螺旋的载体上。

96. 发明申请

WO1996016169A1 PEPTIDES CAPABLE OF BINDING TO THE GAP PROTEIN SH3 DOMAIN, NUCLEOTIDE SEQUENCES CODING THEREFOR, AND PREPARATION AND USE THEREOF 审中-公开
标题翻译：能够与GAP蛋白SH3结合的肽，其核苷酸序列编码及其制备和使用
公开(公告)号：WO1996016169A1
公开(公告)日：1996-05-30
申请号：PCT/FR1995001539
申请日：1995-11-22
申请人： RHONE-POULENC RORER S.A. , DUCHESNE, Marc , FAUCHER, Didier , PARKER, Fabienne , SCHWEIGHOFFER, Fabien , TOCQUE, Bruno
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C12N15/12
CPC分类号： C07K14/4706 , A61K38/00 , C07K14/4702 , C07K14/4703 , C07K2319/00
摘要： Peptides capable of interacting with the GAP protein SH3 domain, nucleic acid sequences coding therefor, and pharmaceutical compositions containing same, are disclosed.
摘要翻译：能够与GAP蛋白SH3结构域相互作用的肽，其编码的核酸序列和含有该肽的药物组合物被公开。

97. 发明申请

WO1996013596A1 VIABLE CONTAMINANT PARTICLE FREE ADENOVIRUSES, THEIR PREPARATION AND USE 审中-公开
标题翻译：可视污染物颗粒免费腺病毒，其制备和使用
公开(公告)号：WO1996013596A1
公开(公告)日：1996-05-09
申请号：PCT/FR1995001415
申请日：1995-10-25
申请人： RHONE-POULENC RORER S.A. , YEH, Patrice , PERRICAUDET, Michel , ORSINI, Cécile
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C12N15/86
CPC分类号： C12N15/86 , A61K48/00 , A61L2/0023 , A61L2/04 , C07K14/005 , C07K14/75 , C12N2710/10322 , C12N2710/10343 , C12N2830/002
摘要： Novel adenovirus-derived viral vectors, the preparation thereof, and their use in gene therapy, are disclosed. In particular, recombinant adenoviruses including an adenovirus genome wherein (i) the E1 region is inactivated, (ii) the genomic organisation is modified, and (iii) optional recombination with the producing line genome generates non-viable viral particles, are disclosed.
摘要翻译：公开了新型腺病毒衍生的病毒载体，其制备及其在基因治疗中的用途。特别地，公开了包括腺病毒基因组的重组腺病毒，其中（i）E1区失活，（ii）基因组组织被修饰，并且（iii）与生产线基因组任选的重组产生非活的病毒颗粒。

98. 发明申请

WO1996013494A1 NOVEL TAXOIDS, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新型紫杉醇，其制剂及含有其的药物组合物
公开(公告)号：WO1996013494A1
公开(公告)日：1996-05-09
申请号：PCT/FR1995001393
申请日：1995-10-23
申请人： RHONE-POULENC RORER S.A. , BOUCHARD, Hervé , BOURZAT, Jean-Dominique , COMMERÇON, Alain , TERRIER, Corinne , ZUCCO, Martine
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： Novel taxoids of general formulas (I) and (II), preparation thereof, and pharmaceutical compositions containing same. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy or alkoxyacetoxy and Rb is hydrogen, or Ra and Rb, taken together with the carbon atom to which they are attached, form a ketone function; Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl, thenoyl or furoyl radical or a radical R2-O-CO- where R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or naphthyl radical; R4 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl or heterocyclyl radical; and R5 is an optionally substituted cycloalkenyl, alkyl, alkenyl, alkynyl or cycloalkyl radical. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antineoplastic properties.
摘要翻译：通式（I）和（II）的新型紫杉烷类，其制备方法和含有它们的药物组合物。在通式（I）中，R a是氢，羟基，烷氧基，酰氧基或烷氧基乙酰氧基，R b是氢，或者R a和R b与它们所连接的碳原子一起形成酮官能团; Z是氢原子或通式（II）的基团，其中R 1是任选取代的苯甲酰基，噻吩甲酰基或糠基或基团R 2 -O-CO-，其中R 2是烷基，烯基，炔基，环烷基，环烯基，任选取代的苯基或杂环基; R3是芳族杂环，烷基，烯基，炔基，环烷基，苯基或萘基; R4是烷基，烯基，炔基，环烷基，环烯基，双环烷基，芳基或杂环基; 并且R 5是任选取代的环烯基，烷基，烯基，炔基或环烷基。通式（I）的新产物，其中Z为通式（II）的基团，具有显着的抗肿瘤和抗肿瘤性质。

99. 发明申请

WO1996002536A1 4-HYDROXY-3-PHENYL-INDENO(1,2-B)PYRIDINE-2(1H)-ONE DERIVATIVES AS NMDA ANTAGONISTS 审中-公开
标题翻译： 4-羟基-3-苯基 - 茚满（1,2-B）吡啶-2（1H） - 酮衍生物作为NMDA拮抗剂
公开(公告)号：WO1996002536A1
公开(公告)日：1996-02-01
申请号：PCT/FR1995000952
申请日：1995-07-17
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D405/04
CPC分类号： C07D495/04 , C07D221/16
摘要： Derivatives of formula (I), wherein R is a methylene radical, N-alk, NH or an oxygen or sulphur atom, R1 and R2, which are the same or different, are a hydrogen or halogen atom or a hydroxy, alkoxy, alkyl, nitro, amino, monoalkylamino, dialkylamino, cyano, polyfluoroalkyl, polyfluoroalkoxy or phenoxy radical, R3 and R4, which are the same or different, are a hydrogen or halogen atom or an alkyl radical; tautomeric forms thereof, salts thereof, preparation thereof and drugs containing said derivatives.
摘要翻译：式（I）的衍生物，其中R是亚甲基，N-alk，NH或氧或硫原子，R 1和R 2相同或不同，是氢或卤素原子或羟基，烷氧基，烷基硝基，氨基，单烷基氨基，二烷基氨基，氰基，多氟烷基，多氟烷氧基或苯氧基，R 3和R 4相同或不同，为氢或卤素原子或烷基; 其互变异构体，其盐，其制备物和含有所述衍生物的药物。

100. 发明申请

WO1995035314A1 THIAZOLIDINE DERIVATIVES, THEIR PREPARATION AND DRUGS CONTAINING SAME 审中-公开
标题翻译：噻唑烷衍生物，其制备和含有其的药物
公开(公告)号：WO1995035314A1
公开(公告)日：1995-12-28
申请号：PCT/FR1995000808
申请日：1995-06-19
申请人： RHONE-POULENC RORER S.A. , CAPET, Marc , DUBROEUCQ, Marie-Christine , GUYON, Claude , MANFRE, Franco
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07K05/062
CPC分类号： C07K5/06034 , A61K38/00 , C07K5/06026 , C07K5/06191
摘要： Thiazolidine derivatives of formula (I), in which R1, R2, R3, R4 and R5 are as defined in the specification. The invention also concerns the salts of these derivatives, the preparation thereof and drugs containing same.
摘要翻译：式（I）的噻唑烷衍生物，其中R1，R2，R3，R4和R5如说明书中所定义。本发明还涉及这些衍生物的盐，其制备方法和含有它们的药物。

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