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81. 发明申请

WO1997035002A1 PURIFICATION OF PHARMACEUTICAL-GRADE PLASMID DNA 审中-公开
标题翻译：药物级粒子DNA的纯化
公开(公告)号：WO1997035002A1
公开(公告)日：1997-09-25
申请号：PCT/FR1997000472
申请日：1997-03-17
申请人： RHONE-POULENC RORER S.A. , WILS, Pierre , OLLIVIER, Monique
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C12N15/10
CPC分类号： C12N15/101 , C12Q1/6806
摘要： A method for purifying pharmaceutical-grade plasmid DNA by means of at least one hydroxyapatite column chromatography step is disclosed.
摘要翻译：本发明涉及纯化双链DNA的方法，其包括使用陶瓷羟基磷灰石柱色谱法。本发明还涉及纯化的重组质粒DNA组合物，其包含小于或等于0.01％的染色体DNA含量以及包含通过前述方法制备的DNA的组合物。

82. 发明申请

WO1997032869A1 TAXOIDS, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：紫杉醇，其制备方法及含有其的药物组合物
公开(公告)号：WO1997032869A1
公开(公告)日：1997-09-12
申请号：PCT/FR1997000386
申请日：1997-03-05
申请人： RHONE-POULENC RORER S.A. , BOUCHARD, Hervé , BOURZAT, Jean-Dominique , COMMERCON, Alain
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D305/14
CPC分类号： C07D305/14 , Y02P20/55
摘要： Novel taxoids of general formula (I), the preparation thereof and pharmaceutical compositions containing same, are disclosed. In general formula (I), Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl 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 alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphthyl or aromatic heterocyclic radical; R4 is a hydroxy radical or an alkoxy, alkenyloxy, optionally substituted alkynyloxy, alkanoyloxy, alkenoyloxy, alkynyloxy, alkoxyacetyl or alkyloxycarbonyloxy radical, or a cycloalkyloxy, cycloalkenyloxy, arylcarbonyloxy or heterocyclylcarbonyloxy radical; and R5 is an optionally substituted alkoxy radical or a cycloalkyloxy or cycloalkenyloxy radical. The novel compounds of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antineoplastic properties.
摘要翻译：公开了通式（I）的新型紫杉烷类，其制备方法和含有其的药物组合物。在通式（I）中，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或基团R 2 -O-CO-，其中R 2是烷基，烯基，炔基，环烷基，环烯基，双环烷基，任选取代的苯基或杂环基; R3是烷基，烯基，炔基，环烷基，苯基，萘基或芳族杂环基; R4是羟基或烷氧基，烯氧基，任选取代的炔氧基，烷酰氧基，烯酰氧基，炔氧基，烷氧基乙酰基或烷氧基羰基氧基，或环烷氧基，环烯基氧基，芳基羰基氧基或杂环基羰基氧基; 并且R 5是任选取代的烷氧基或环烷氧基或环烯氧基。通式（I）的新化合物，其中Z为通式（II）的基团，具有显着的抗肿瘤和抗肿瘤性质。

83. 发明申请

WO1997029121A1 APPLICATION OF UREIDOACETAMIDES TO THE PREPARATION OF MEDICAMENTS INTENDED TO THE TREATMENT OF THE ABUSE OF DRUGS OR SUBSTANCES GIVING RISE TO PHARMACOMANIA OR TO AN EXCESSIVE USE 审中-公开
标题翻译：应用抗氧化剂对于制定治疗药物或物质滥用药物或过度使用的药物的准备
公开(公告)号：WO1997029121A1
公开(公告)日：1997-08-14
申请号：PCT/FR1997000208
申请日：1997-02-03
申请人： RHONE-POULENC RORER S.A. , BOHME, Andrees , DUBROEUCQ, Marie-Christine , FRATTA, Walter , GUYON, Claude , IMPERATO, Assunta
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07K05/06
CPC分类号： C07K5/06026 , A61K38/00
摘要： Application of ureidoacetamides having general formula (I), their racemic compounds and enantiomers when they comprise at least one asymmetric center and salts thereof, to the preparation of medicaments intended to the treatment of the abuse of drugs or substances giving rise to pharmacomania or to an excessive use.
摘要翻译：具有通式（I）的脲基乙酰胺，其外消旋化合物和对映异构体当其包含至少一个不对称中心及其盐时，可用于制备用于治疗滥用药物或引起药物性或药物滥用的物质的药物过度使用

84. 发明申请

WO1997020850A1 3,4-DIHYDRO[1,2,4]THIADIAZINO[3,4-b]BENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译： 3,4-二氢[1,2,4]噻二唑并[3,4-b]苯并噻唑衍生物，其制备方法和含有其的药物
公开(公告)号：WO1997020850A1
公开(公告)日：1997-06-12
申请号：PCT/FR1996001868
申请日：1996-11-26
申请人： RHONE-POULENC RORER S.A. , BOIREAU, Alain , DUBROEUCQ, Marie-Christine , IMPERATO, Assunta , JIMONET, Patrick , MIGNANI, Serge , RANDLE, John
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Compounds of formula (I), wherein R is a polyfluoroalkyl radical, R1 is an alkyl radical and Hal is a halogen atom, are disclosed. The compounds of formula (I) are useful for treating Parkinson's disease and parkinsonian syndromes.
摘要翻译：公开了式（I）化合物，其中R是多氟烷基，R 1是烷基，Hal是卤素原子。式（I）化合物可用于治疗帕金森病和帕金森综合征。

85. 发明申请

WO1997020557A1 USE OF 2-AMINOBENZOTHIAZOLES FOR TREATING PARKINSON'S DISEASE AND PARKINSONIAN SYNDROMES 审中-公开
标题翻译：用于治疗帕金森病和帕金森综合症的2-氨基苯唑胺的应用
公开(公告)号：WO1997020557A1
公开(公告)日：1997-06-12
申请号：PCT/FR1996001866
申请日：1996-11-26
申请人： RHONE-POULENC RORER S.A. , BOIREAU, Alain , DUBROEUCQ, Marie-Christine , IMPERATO, Assunta , JIMONET, Patrick , MIGNANI, Serge , RANDLE, John
发明人： RHONE-POULENC RORER S.A.
IPC分类号： A61K31/425
CPC分类号： A61K31/428
摘要： The use of 2-aminobenzothiazoles of formula (I), wherein R is a straight or branched C1-5 alkyl, trifluoromethyl, pentafluoroethyl or pentafluoroethoxy radical, and enantiomers and pharmaceutically acceptable salts thereof, for treating Parkinson's disease and parkinsonian syndromes, is disclosed.
摘要翻译：公开了用于治疗帕金森病和帕金森综合征的式（I）的2-氨基苯并噻唑，其中R是直链或支链C 1-5烷基，三氟甲基，五氟乙基或五氟乙氧基，及其对映异构体和药学上可接受的盐。

86. 发明申请

WO1997010343A1 CIRCULAR DNA MOLECULE WITH CONDITIONAL ORIGIN OF REPLICATION, METHOD FOR PREPARING SAME AND USE THEREOF IN GENE THERAPY 审中-公开
标题翻译：具有复制条件的圆形DNA分子，其制备方法及其在基因治疗中的用途
公开(公告)号：WO1997010343A1
公开(公告)日：1997-03-20
申请号：PCT/FR1996001414
申请日：1996-09-13
申请人： RHONE-POULENC RORER S.A. , CROUZET, Joël , SOUBRIER, Fabienne
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C12N15/69
CPC分类号： C12N15/70 , A61K48/00 , C07K14/501 , C07K14/82 , C12N15/69
摘要： A circular DNA molecule, useful for gene therapy, comprising at least one nucleic acid sequence of interest, characterised in that the region allowing the replication thereof has an origin of replication with a functionality in a host cell that requires the presence of at least one specific protein foreign to said host cell. A method for preparing same, cells incorporating said DNA molecules and uses thereof in gene therapy are also described.
摘要翻译：一种可用于基因治疗的环状DNA分子，其包含至少一种目标核酸序列，其特征在于允许其复制的区域具有在宿主细胞中具有功能性的复制起点，其需要存在至少一种特异性所述宿主细胞外源的蛋白质。还描述了其制备方法，并入所述DNA分子的细胞及其在基因治疗中的用途。

87. 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。

88. 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。

89. 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。

90. 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。

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