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71. 发明申请

WO1998003485A1 PHENOXYPROPANOLAMINES HAVING 'beta'3-ADRENERGIC ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有β3-ADRENERGIC ANTAGONIST活性的苯氧基丙氨酸
公开(公告)号：WO1998003485A1
公开(公告)日：1998-01-29
申请号：PCT/FR1997001360
申请日：1997-07-22
申请人： SANOFI , BADONE, Domenico , CECCHI, Roberto , CROCI, Tiziano , GUZZI, Umberto , MANARA, Luciano
发明人： SANOFI
IPC分类号： C07D213/74
CPC分类号： C07D213/74
摘要： Phenoxypropanolamines of formula (I), wherein R1 is a C3-7 alkyl group or a C3-7 cycloalkyl group, R2 is hydrogen or an electron accepting group, and Alk is a C2-3 alkylene group having beta 3-adrenergic receptor antagonist activity, salts thereof, a method for preparing same, pharmaceutical compositions containing such compounds, and synthesis intermediates therefor, are disclosed.
摘要翻译：式（I）的苯氧基丙醇胺，其中R1是C3-7烷基或C3-7环烷基，R2是氢或电子接受基团，Alk是具有β3-肾上腺素能受体拮抗剂活性的C2-3亚烷基，其盐，其制备方法，含有这些化合物的药物组合物及其合成中间体。

72. 发明申请

WO1997045110A1 PROCESS OF PREPARING 2,2'-(1-METHYL-1,2-ETHANEDIYLIDENE)BIS[HYDRAZINE CARBOXIMIDAMIDE] 审中-公开
标题翻译：制备2,2' - （1-甲基-1,2-乙二胺）二胺的方法[氢化卡西酰胺]
公开(公告)号：WO1997045110A1
公开(公告)日：1997-12-04
申请号：PCT/US1997008347
申请日：1997-05-19
申请人： SANOFI , PHILION, Richard , ELENBAAS, Steven, A.
发明人： SANOFI
IPC分类号： A61K31/155
CPC分类号： C07C281/18
摘要： Process for the preparation of 2,2'-(1-methyl-1,2-ethanediylidene)bis[hydrazine carboximidamide] by: a) reacting aminoguanidine hydrochloride with methylglyoxal aldehyde or methylglyoxal dimethyl acetal; and b) purifying the 2,2'-(1-methyl-1,2-ethanediylidene)bis[hydrazine carboximidamide] by crystallization from an acidic aqueous-isopropyl alcohol medium.
摘要翻译：通过以下方法制备2,2' - （1-甲基-1,2-乙二亚基）双[肼亚胺基酰胺]的方法：a）使氨基胍盐酸盐与甲基乙二醛醛或甲基乙二醛二甲基缩醛反应; 和b）通过从酸性含水异丙醇介质中结晶纯化2,2' - （1-甲基-1,2-亚乙基）双[肼亚胺脒]。

73. 发明申请

WO1997025315A1 NOVEL N-(ARYLSULPHONYL)AMINO ACID DERIVATIVES HAVING BRADYKININ RECEPTOR AFFINITY 审中-公开
标题翻译：具有BRADYKININ受体亲和力的新型N-（芳基磺酰基）氨基酸衍生物
公开(公告)号：WO1997025315A1
公开(公告)日：1997-07-17
申请号：PCT/FR1997000026
申请日：1997-01-07
申请人： SANOFI , FERRARI, Bernard , GOUGAT, Jean , MUNEAUX, Claude , MUNEAUX, Yvette , PERREAUT, Pierre , PLANCHENAULT, Claudine
发明人： SANOFI
IPC分类号： C07D233/26
CPC分类号： C07D239/06 , C07C311/19 , C07D233/22 , C07D233/24 , C07D233/26 , C07D295/185 , C07D403/12
摘要： Compounds of formula (I), wherein R1 to R9, R16 and R17 are as defined in claim 1, are disclosed. The compounds are pharmacologically active.
摘要翻译：公开了式（I）化合物，其中R 1至R 9，R 16和R 17如权利要求1中所定义。这些化合物具有药理活性。

74. 发明申请

WO1997019063A1 PYRAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID DERIVATIVES 审中-公开
标题翻译：吡唑衍生物，其制备方法和含有衍生物的药物组合物
公开(公告)号：WO1997019063A1
公开(公告)日：1997-05-29
申请号：PCT/FR1996001847
申请日：1996-11-21
申请人： SANOFI , BARTH, Francis , CONGY, Christian , MARTINEZ, Serge , RINALDI, Murielle
发明人： SANOFI
IPC分类号： C07D231/14
CPC分类号： C07D231/14
摘要： Compounds of formula (I), wherein R1 is fluorine, hydroxy, (C1-5) alkoxy, (C1-5) alkylthio, hydroxy(C1-5)alkoxy, a -NR10R11 group, cyano, (C1-5) alkylsulphonyl or (C1-5) alkylsulphinyl; R2 and R3 are each (C1-4) alkyl or, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- to 10-membered heterocyclic radical optionally substituted one or more times by (C1-3) alkyl or (C1-3) alkoxy; each of R4, R5, R6, R7, R8 and R9 is independently hydrogen, halogen or trifluoromethyl, and when R1 is fluorine, R4, R5, R6, R7, R8 and/or R9 may also be fluoromethyl; with the proviso that at least one of substituents R4 or R7 is other than hydrogen; each of R10 and R11 is independently hydrogen or (C1-5) alkyl, or R10 and R11, taken together with the nitrogen atom to which they are attached, form a heterocyclic radical selected from pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl optionally substituted by (C1-4) alkyl; a method for preparing same, and pharmaceutical compositions containing said compounds, are disclosed. Said compounds have very high affinity for central cannabinoid receptors.
摘要翻译：式（I）的化合物，其中R 1是氟，羟基，（C 1-5）烷氧基，（C 1-5）烷硫基，羟基（C 1-5）烷氧基，-NR 10 R 11基，氰基，（C 1-5）烷基磺酰基或（C 1-5）烷基亚磺酰基; R 2和R 3各自为（C 1-4）烷基，或与它们所连接的氮原子一起形成饱和或不饱和的5-至10-元杂环基，任选被（C 1-3）取代一次或多次）烷基或（C 1-3）烷氧基; R4，R5，R6，R7，R8和R9各自独立地是氢，卤素或三氟甲基，当R1是氟时，R4，R5，R6，R7，R8和/或R9也可以是氟甲基; 条件是取代基R4或R7中的至少一个不是氢; R 10和R 11各自独立地为氢或（C 1-5）烷基，或者R 10和R 11与它们所连接的氮原子一起形成选自吡咯烷-1-基，哌啶-1-基，任选被（C 1-4）烷基取代的吗啉-4-基或哌嗪-1-基; 公开了其制备方法和含有所述化合物的药物组合物。所述化合物对中枢大麻素受体具有非常高的亲和力。

75. 发明申请

WO1997017064A1 STABLE FREEZE-DRIED PHARMACEUTICAL FORMULATION 审中-公开
标题翻译：稳定的冷冻干燥药物制剂
公开(公告)号：WO1997017064A1
公开(公告)日：1997-05-15
申请号：PCT/FR1996001706
申请日：1996-10-30
申请人： SANOFI , BOULOUMIE, Colette , BREUL, Thierry , COLLIERE, Laurence , FAURE, Philippe
发明人： SANOFI
IPC分类号： A61K09/19
CPC分类号： A61K47/183 , A61K9/0019 , A61K9/19 , A61K47/26
摘要： A pharmaceutically acceptable freeze-dried formulation consisting of an amorphous phase and a crystalline phase and including at least one non-protein active principle. The formulation is characterised in that it contains mannitol and alanine in a ratio R of 0.1-1, where R is the weight of mannitol over the weight of alanine.
摘要翻译：由非晶相和结晶相组成且包含至少一种非蛋白质活性成分的药学上可接受的冷冻干燥制剂。该制剂的特征在于其含有甘露醇和丙氨酸，其比例R为0.1-1，其中R是甘露醇的重量比丙氨酸重量。

76. 发明申请

WO1997015304A1 USE OF 1-(2-NAPHTH-2-YLETHYL)-4-(3-TRIFLUOROMETHYLPHENYL)-1,2,3,6-TETRAHYDROPYRIDINE FOR PREPARING DRUGS FOR TREATING AMYOTROPHIC LATERAL SCLEROSIS 审中-公开
标题翻译： 1-（2-萘基-2-甲基乙基）-4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶的制备用于治疗左心室鳞状细胞癌的药物
公开(公告)号：WO1997015304A1
公开(公告)日：1997-05-01
申请号：PCT/FR1996001674
申请日：1996-10-25
申请人： SANOFI , DOUILLET, Patrice , FOURNIER, Jacqueline
发明人： SANOFI
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , A61K38/185 , A61K38/30 , A61K31/425 , A61K2300/00
摘要： The use of 1-(2-naphth-2-ylethyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydrop yridine, or pharmaceutically acceptable acid addition salts thereof, for preparing drugs for treating amyotrophic lateral sclerosis (ALS) is disclosed.
摘要翻译： 1-（2-萘-2-基乙基）-4-（3-三氟甲基苯基）-1,2,3,6-四氢化吖啶或其药学上可接受的酸加成盐用于制备治疗肌萎缩性侧索硬化症的药物（ALS）。

77. 发明申请

WO1997010809A1 LYOPHILIZED THIOXANTHENONE ANTIMUMOR AGENTS 审中-公开
标题翻译： LYOPHILIZED THIENHANTHENONE抗体药剂
公开(公告)号：WO1997010809A1
公开(公告)日：1997-03-27
申请号：PCT/IB1996000984
申请日：1996-09-12
申请人： SANOFI
发明人： SANOFI , BROWN, Stephen , SANDHU, Gurdial, Singh
IPC分类号： A61K09/14
CPC分类号： A61K31/67 , A61K9/0019 , A61K9/19 , A61K31/382 , A61K47/02 , A61K47/12 , A61K47/26 , Y10S514/908 , Y10S514/97
摘要： Disclosed are reconstituted lyophilized formulations for the treatment of mammalian tumors comprising a thioxanthenone antitumor agent in combination with mannitol or sucrose as a stabilizer in a lactate buffer.
摘要翻译：公开了用于治疗哺乳动物肿瘤的重组冻干制剂，其包含与甘露醇或蔗糖组合的噻吨酮抗肿瘤剂作为乳酸盐缓冲液中的稳定剂。

78. 发明申请

WO1997010243A1 2-(PYRAZOL-5-YL-OXYMETHYL)-1,2-BENZISOTHIAZOL-3(2H)-ONE 1,1-DIOXIDES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： 2-（PYRAZOL-5-YL-OXYMETHYL）-1,2-BENZISOTHIAZOL-3（2H） - 酮1,1-二氧化物和含有它们的药物组合物
公开(公告)号：WO1997010243A1
公开(公告)日：1997-03-20
申请号：PCT/IB1996000997
申请日：1996-09-12
申请人： SANOFI
发明人： SANOFI , EISSENSTAT, Michael, A. , KUO, Gee-Hong , DESAI, Ranjit, C. , HLASTA, Dennis, J. , COURT, John, J.
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , C07C69/38 , C07D417/14
摘要： 2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides of formula (I), pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
摘要翻译：式（I）的2-（吡唑-5-基 - 氧甲基）-1,2-苯并异噻唑-3（2H） - 酮1,1-二氧化物，含有它们的药物组合物和利用它们治疗退行性疾病的方法。

79. 发明申请

WO1997002031A1 PHARMACEUTICAL AMIODARONE COMPOSITION FOR PARENTERAL DELIVERY 审中-公开
标题翻译：用于家庭服务的药物AMIODARONE组合物
公开(公告)号：WO1997002031A1
公开(公告)日：1997-01-23
申请号：PCT/FR1996001010
申请日：1996-06-28
申请人： SANOFI , GAUTIER, Jean-Claude , BELLAMY, Régine
发明人： SANOFI
IPC分类号： A61K31/34
CPC分类号： A61K31/343 , A61K9/0019 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/44
摘要： A pharmaceutical composition for parenteral delivery including 1.5-8 wt % of an active principle consisting of amiodarone or a pharmaceutically acceptable salt thereof, a physiologically acceptable buffer solution capable of solubilising the active principle and keeping the pH of the composition at 2.4-3.8, and a non-ionic hydrophilic surfactant.
摘要翻译：一种用于胃肠外递送的药物组合物，包括由胺碘酮或其药学上可接受的盐组成的活性成分的1.5-8重量％，能够溶解活性成分并将组合物的pH保持在2.4-3.8的生理上可接受的缓冲溶液，以及非离子型亲水性表面活性剂。

80. 发明申请

WO1997000868A1 4-PHENYLAMINOTHIAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID DERIVATIVES 审中-公开
标题翻译： 4-苯基苯并噻唑衍生物，其制备方法和含有衍生物的药物组合物
公开(公告)号：WO1997000868A1
公开(公告)日：1997-01-09
申请号：PCT/FR1996000941
申请日：1996-06-18
申请人： SANOFI , GULLY, Danielle , ROGER, Pierre , WERMUTH, Camille, Georges
发明人： SANOFI
IPC分类号： C07D277/42
CPC分类号： C07D417/12 , C07D277/42
摘要： Aminothiazole derivatives of formula (I), wherein each of R1 and R2 is independently a halogen atom; a C1-5 hydroxyalkyl radical; C1-5 alkyl; C7-10 aralkyl; C1-5 alkoxy; trifluoromethyl; nitro; nitrile; a group -SR where R is hydrogen, a C1-5 alkyl radical or a C7-10 aralkyl radical; a group S-CO-R where R is a C1-5 alkyl radical or aralkyl in which the aryl portion is C6-8 and the alkyl portion is C1-4; a group -COOR' where R' is hydrogen or C1-5 alkyl; a group -CONR'R" where R' and R" are as defined above for R'; a group -NR'R" where R' and R" are as previously defined for R'; a group -CONRaRb or -NRaRb, where Ra and Rb, taken together with the nitrogen atom to which they are attached, form a 5- to 7-membered heterocyclic ring; or a group -NHCO-NR'R", where R' and R" are as defined above for R'; R3 is hydrogen or as defined above for R1 and R2; R4 is a hydrogen atom; C1-5 alkyl; halogen; a hydroxymethyl group; or a formyl group; R5 is C1-5 alkyl; a C3-7 cycloalkyl group; a cycloalkylalkyl group in which the cycloalkyl portion is C3-7 and the alkyl portion is C1-5; or C5-6 alkenyl; n is 0 or 1; R6 is C1-5 alkyl; alkoxyalkyl in which the alkyl portions are C1-5; C3-7 cycloalkyl; a cycloalkylalkyl group in which the cycloalkyl portion is C3-7 and the alkyl portion is C1-5; a cycloalkyloxyalkyl radical in which the cycloalkyl is C3-7 and the alkyl is C1-4; a hydroxyalkyloxyalkyl radical in which the alkyls are C2-10; or an alkoxyalkyloxyalkyl radical in which the alkyls are C3-12; and Z is an optionally substituted bi- or tricyclic aromatic or heteroaromatic group; and stereoisomers and/or addition salts thereof.
摘要翻译：式（I）的氨基噻唑衍生物，其中R 1和R 2各自独立地为卤素原子; C1-5羟基烷基; C 1-5烷基; C7-10芳烷基; C 1-5烷氧基三氟甲基; 硝基; 腈; 基团-SR，其中R是氢，C1-5烷基或C7-10芳烷基; 基团S-CO-R，其中R是C 1-5烷基或芳烷基，其中芳基部分是C6-8，烷基部分是C1-4; 基团-COOR'，其中R'是氢或C 1-5烷基; 基团-CONR'R“，其中R'和R”如上面对R'所定义; 基团-NR'R“，其中R'和R”如前面对R'所定义; 基团-CONR a R b或-NR a R b，其中R a和R b与它们所连接的氮原子一起形成5-至7-元杂环; 或基团-NHCO-NR'R“，其中R'和R”如上对R'所定义; R3是氢或如对于R1和R2所定义的; R4是氢原子; C 1-5烷基; 卤素; 羟甲基; 或甲酰基; R5是C1-5烷基; C3-7环烷基; 环烷基部分为C3-7，烷基部分为C1-5的环烷基烷基; 或C5-6烯基; n为0或1; R6是C1-5烷基; 烷基部分为C1-5的烷氧基烷基; C3-7环烷基; 环烷基部分为C3-7，烷基部分为C1-5的环烷基烷基; 环烷氧基烷基，其中环烷基是C3-7，烷基是C1-4; 烷基是C2-10的羟基烷氧基烷基; 或其烷基为C3-12的烷氧基烷氧基烷基; 并且Z是任选取代的双环或三环芳族或杂芳族基团; 及其立体异构体和/或其加成盐。

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