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1. 发明授权

EP1044005B1 1,2,4-BENZOTRIAZINE OXIDES FORMULATIONS 失效
标题翻译： 1,2,4-苯并三，含有氧化筹备工作
公开(公告)号：EP1044005B1
公开(公告)日：2006-07-05
申请号：EP98915529.6
申请日：1998-04-14
申请人： Sanofi-Synthelabo, Inc.
发明人： BROWN, Stephen , BAKER, Edward
IPC分类号： A61K31/53 , A61P35/00
CPC分类号： A61K47/12 , A61K9/0019 , A61K31/53
摘要： Disclosed are: aqueous parenteral formulations for the treatment of cancer tumors comprising 1,2,4-benzotriazine 1,4-dioxides in a citrate buffer; and method of cancer tumor treatment.

2. 发明公开

EP1454910A1 Substituted pyrimidinyl-2-(diaza-bicyclo-alkyl)-pyrimidone derivatives 审中-公开
标题翻译：取代基嘧啶基-2-（二氮杂 - 双环烷基） - 嘧啶酮
公开(公告)号：EP1454910A1
公开(公告)日：2004-09-08
申请号：EP03290570.5
申请日：2003-03-07
申请人： SANOFI-SYNTHELABO , Mitsubishi Pharma Corporation
发明人： Lochead, Alistair W. , Saady, Mourad , Slowinski, Franck , Yaiche, Philippe
IPC分类号： C07D487/08 , A61K31/506 , A61P25/28 , A61P35/00
CPC分类号： C07D487/08
摘要： The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:

R1 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom;
R2 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group or a C 1-4 alkoxy group; a C 1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C 1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring or an imidazole ring; the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a benzene ring, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-4 alkoxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group or a C 2-10 dialkylamino group;
R3 represents a 2, 4 or 5-pyrimidine ring optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom;
R4 represents a C 1-4 alkyl group optionally substituted by a hydroxyl group, a C 1-4 alkoxy group or a halogen atom and n represents 1 or 2.

The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
摘要翻译：本发明涉及由式（I）表示的2-（二氮杂双环烷基） - 嘧啶酮衍生物或其盐：其中：R1表示氢原子，C1-6烷基或卤素原子; R2表示氢原子，任选被1至4个选自卤素原子，羟基或C 1-4烷氧基的取代基取代的C 1-6烷基; C1-2全卤代烷基，苄基，苯乙基，苄氧基羰基，C1-4烷氧基羰基，苯环，萘环，喹啉环，酞嗪环，5,6,7 8-四氢萘环，吡啶环，吲哚环，吡咯环，噻吩环，苯磺酰基，苯甲酰基，哒嗪环，呋喃环或咪唑环; 苄基，苯乙基，苄氧基羰基，苯磺酰基，苯甲酰基和环任选被1〜4个选自C 1-6烷基，苯环，卤素原子，C1- 2个全卤代烷基，C1-3卤代烷基，羟基，C1-4烷氧基，硝基，氰基，氨基，C1-6单烷基氨基或C2-10二烷基氨基; R3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,4或5-嘧啶环; R 4表示任选被羟基，C 1-4烷氧基或卤素原子取代的C 1-4烷基，n表示1或2.本发明还涉及包含所述衍生物或盐的药物作为活性成分，其用于预防和/或治疗由GSK3β的异常活性如阿尔茨海默病引起的神经变性疾病。

3. 发明授权

EP1089994B1 NOUVELLE FORME DE L'IRBESARTAN, PROCEDES POUR OBTENIR LADITE FORME ET COMPOSITIONS PHARMACEUTIQUES EN CONTENANT 无效
标题翻译：厄贝沙坦的新形式，METHODS这种形式获得并含有YOU的药物组合物
公开(公告)号：EP1089994B1
公开(公告)日：2004-09-08
申请号：EP99923712.6
申请日：1999-06-10
申请人： SANOFI-SYNTHELABO
发明人： FRANC, Bruno , HOFF, Christian , KIANG, San , LINDRUD, Mark, D. , MONNIER, Olivier , WEI, Chenkou
IPC分类号： C07D403/10 , A61K31/415
CPC分类号： C07D403/10
摘要： The invention concerns irbesartan form A having a modified crystalline habit such that length/width ratio ranges between 1:1 and 10:1, preferably between 1:1 and 5:1 and a method for preparing said crystalline habit. The method is characterised in that it consists in either subjecting a crystalline suspension of irbesartan form A having acicular habit to at least a temperature oscillating step, or in subjecting a crystalline suspension of irbesartan form A having acicular habit to a mechanical shearing. The invention also concerns a pharmaceutical composition containing said irbesartan crystalline habit.

4. 发明授权

EP1165528B1 NOUVEAUX DERIVES DE MORPHOLINE, PROCEDE POUR LEUR PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT 有权
标题翻译：吗啉，方法用于产生和含YOU的药物组合物
公开(公告)号：EP1165528B1
公开(公告)日：2004-09-01
申请号：EP00911009.9
申请日：2000-03-21
申请人： SANOFI-SYNTHELABO
发明人： DUCOUX, Jean, Philippe , EMONDS-ALT, Xavier , GUEULE, Patrick , PROIETTO, Vincenzo
IPC分类号： C07D265/30 , C07D413/06 , A61K31/5375 , A61K31/5377 , A61P11/00 , A61P25/00
CPC分类号： C07D265/30

5. 发明授权

EP1226137B1 PHENYL- ET PYRIDYL-TETRAHYDRO-PYRIDINES POSSEDANT UNE ACTIVITE INHIBITRICE DE FNT 有权
标题翻译：苯基 - 吡啶基 - 四氢 - 吡啶类化合物活性活性抑制剂DE FNT
公开(公告)号：EP1226137B1
公开(公告)日：2004-07-21
申请号：EP00969646.9
申请日：2000-10-19
申请人： SANOFI-SYNTHELABO
发明人： BARONI, Marco , BOURRIE, Bernard , CARDAMONE, Rosanna , CASELLAS, Pierre , GUZZI, Umberto
IPC分类号： C07D401/06 , A61K31/4709 , A61K31/4725 , A61P9/00 , C07D401/14 , C07D217/02 , C07D215/14
CPC分类号： C07D401/06 , A43B7/125 , A43B9/02 , B29C2045/14844 , B29D35/0045 , B29D35/06 , B29D35/062 , B29D35/122 , B29D35/128 , B29D35/142 , C07D215/14 , C07D217/02 , C07D401/14
摘要： The invention concerns compounds of formula (I) wherein: X represents N or CH; R1 represents a hydrogen or halogen atom, or a CF3 group; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents a group of formula (a) or (b) wherein: R4 represents a hydrogen or halogen atom, a C1-C4 alkyl group, a CF3 group, an amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino; R5 represents a hydrogen or halogen atom, a (C1-C4)alkoxy group, a (C1-C4)alkyl group or a CF3 group; R6 represents a hydrogen atom, a (C1-C4)alkyl group or a (C1-C4)alkoxy group; and their salts or solvates, pharmaceutical compositions containing them, a method for preparing them and the synthesis intermediates in said method.
摘要翻译：本发明涉及式（I）的化合物，其中：X代表N或CH; R1代表氢或卤素原子或CF3基团; R2和R3独立地表示氢原子或甲基; n是0或1; A表示式（a）或（b）的基团，其中：R 4表示氢或卤素原子，C 1 -C 4烷基，CF 3基，氨基，单（C 1 -C 4）烷基氨基，二）烷基氨基; R5代表氢或卤素原子，（C1-C4）烷氧基，（C1-C4）烷基或CF3基团; R6代表氢原子，（C1-C4）烷基或（C1-C4）烷氧基; 及其盐或溶剂化物，含有它们的药物组合物，其制备方法和所述方法中的合成中间体。

6. 发明授权

EP1242404B1 PHENOXYPROPANOLAMINES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译： PHENOXYPROPANOLAMIN衍生物，生产和治疗用途
公开(公告)号：EP1242404B1
公开(公告)日：2004-07-07
申请号：EP00988936.1
申请日：2000-12-15
申请人： SANOFI-SYNTHELABO
发明人： BOVY, Philippe, R. , CECCHI, Roberto , VENIER, Olivier
IPC分类号： C07D401/04 , A61K31/4545 , A61K31/4523 , A61P1/00 , C07D401/14 , C07D211/58
CPC分类号： C07D401/04 , C07D401/14
摘要： The invention concerns phenoxypropanolamines of formula (I) wherein: R1 represents a hydrogen, a -S(O)z-(C1-C4)Alk-R' group, R' being H, phenyl or (C1-C4) alkoxy), -NHSO2-(C1-C4) Alk, NHCO(C1-C4) Alk; m and n are each independently 0, 1 or 2; R2 and R3 represent independently a hydrogen, a (C5-C6) alkyl, (C3-C6) cycloalkyl, (C1-C4) alkoxy, hydroxy(C1-C4)alkyl, (C1-C4) alkoxy-(C1-C4)alkyl, mono-or di-(C1-C4)Alk-amino(C1-C4)alkyl, pyrrolidino-(C1-C4)alkyl, phenylamino, (C2-C4)alkenyl group, or an aromatic or heteroaromatic group substituted or not with a group R4; R2 and R3 can also together constitute a saturated or unsaturated cycle of 3 to 6 atoms capable of bearing a (C1-C4) alkyl, amino(C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, a -CO(C1-C4)Alk group or a -NHSO2-(C1-C4)Alk group; a (C1-C4)Alk group, a (C1-C4)alkoxy group, a halogen, -COOH, -COO(C1-C4)Alk, -CN, -CONR3R4, -NO2, -SO2NH2, -NHSO2(C1-C4)Alk; z is 1 or 2; and their salts and solvates. Said compounds have an agonist activity with respect to β-3 adrenergic receptors.

7. 发明公开

EP1427720A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 有权
标题翻译： 3-取代的-4-嘧啶酮
公开(公告)号：EP1427720A1
公开(公告)日：2004-06-16
申请号：EP02772871.6
申请日：2002-09-20
申请人： Mitsubishi Pharma Corporation , SANOFI-SYNTHELABO
发明人： UEHARA, Fumiaki,MITSUBISHI PHARMA CORPORATION , ARITOMO, Keiichi,MITSUBISHI PHARMA CORPORATION , SHODA, Aya,MITSUBISHI PHARMA CORPORATION , HIKI, Shinsuke,MITSUBISHI PHARMA CORPORATION , OKUYAMA, Masahiro,MITSUBISHI PHARMA CORPORATION , USUI, Yoshihiro,MITSUBISHI PHARMA CORPORATION , OOIZUMI, Mitsuru,MITSUBISHI PHARMA CORPORATION , WATANABE, Kazutoshi,MITSUBISHI PHARMA CORPORATION , YAMAKOSHI, Koichi,MITSUBISHI PHARMA CORPORATION
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , A61K31/505 , A61P25/28
CPC分类号： C07D401/04 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/14 , C07D413/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:wherein R1 represents a C¿1?-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II):wherein R?2 and R3¿ independently represent a hydrogen atom or a C¿1?-C8 alkyl group; R?4¿ represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

8. 发明公开

EP1419150A2 DERIVES DE 1-PHENYLSULFONYL-1,3-DIHYDRO-2H-INDOL-2-ONE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译：苯磺酰基-1,3-二氢-2H-吲哚-2-酮衍生物，其制备及其治疗用途
公开(公告)号：EP1419150A2
公开(公告)日：2004-05-19
申请号：EP02774822.7
申请日：2002-07-15
申请人： SANOFI-SYNTHELABO
发明人： DI MALTA, Alain , GARCIA, Georges , ROUX, Richard , SCHOENTJES, Bruno , SERRADEIL-LE GAL, Claudine , TONNERRE, Bernard , WAGNON, Jean
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , A61K31/496 , A61P13/00
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention concerns compounds of formula (I), as well as their addition salts with acids or organic salts, their solvates and/or hydrate(s), exhibiting affinity and selectivity for arginine-vasopressin V1b receptors and/or for ocytocin receptors, and further, for certain compounds an affinity for V1a receptors. The invention also concerns the method for preparing them, intermediate compounds of formula (IV) useful for their preparation, pharmaceutical compositions containing them and their use for preparing medicines.

9. 发明授权

EP0917464B1 AMINES POUR LA FABRICATION DE MEDICAMENTS DESTINES A EMPECHER LA PROLIFERATION DE CELLULES TUMORALES 失效
标题翻译：胺药物的抑制肿瘤细胞增殖的生产
公开(公告)号：EP0917464B1
公开(公告)日：2004-05-12
申请号：EP97935643.3
申请日：1997-07-28
申请人： SANOFI-SYNTHELABO
发明人： BRELIERE, Jean-Claude , FERRARA, Pascual , LEBOUTEILLER, Christine , PAUL, Raymond , ROSENFELD, Jorge , VAN BROECK, Didier
IPC分类号： A61K31/135 , A61K31/55 , A61K31/445 , A61K31/535 , A61K31/40 , A61K31/495 , A61K31/35 , C07D211/14 , C07D211/70 , C07C211/29 , C07C211/41 , A61P35/00
CPC分类号： C07D221/20 , A61K31/137 , A61K31/35 , A61K31/40 , A61K31/445 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K31/55 , C07C211/29 , C07C2601/14 , C07D211/14 , C07D211/52 , C07D211/70 , C07D307/33
摘要： The use of compounds capable of displacing tritiated cis N-cyclohexyl N-ethyl-[3-(3-chloro-4-cyclohexylphenyl)allyl]amine from the receptors thereof, for preparing pharmaceutical compositions useful for preventing cell proliferation, is disclosed.

10. 发明授权

EP1009458B1 DISPOSITIF POUR DISTRIBUER UN PRODUIT FLUIDE OU PULVERULENT A UNE DISTANCE PREDETERMINEE 失效
标题翻译：装置，使液体或粉末产品在一定的距离
公开(公告)号：EP1009458B1
公开(公告)日：2004-04-28
申请号：EP98903081.2
申请日：1998-01-19
申请人： VALOIS S.A.S. , SANOFI-SYNTHELABO
发明人： ARGHYRIS, Laurent , BEDOS, Michel
IPC分类号： A61M11/00 , A61F9/00 , B05B15/08
CPC分类号： B05B11/3091 , B05B11/0005 , B05B11/0027 , B05B15/68
摘要： The invention concerns a device for spraying or dispensing a fluid or powdery product on a surface to be treated and/or an intake element (50), comprising: a dispensing member (1), including a dispensing opening (31), said dispensing member being associated with a reservoir (2 ) containing said product and being movable between an inoperative position and a dispensing position; and actuating means for moving said dispensing member (1) towards its dispensing position for delivering a dose of product: The invention is characterised in that the device further comprises: means for measuring distance (20) movable between an inoperative position and their useful position, and arranged in their useful position such that each time the device is used the dispensing opening (31) is located at a fixed predetermined distance from the surface to be treated and/or the intake element (50), the movement of said means for distance measuring (20) from their useful position towards their inoperative position bringing the said dispensing member (1) back towards its inoperative position.

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