公开(公告)号：EP1014990A1

公开(公告)日：2000-07-05

申请号：EP98906594.1

申请日：1998-02-17

申请人： Sanofi-Synthelabo, Inc.

发明人： DEXTER, Daniel, L. ,  JUNIEWICZ, Paul, E. ,  RAKE, James, B. ,  VON HOFF, Daniel, D.

IPC分类号： A61K31/53 ,  A61K31/335 ,  A61K33/24

CPC分类号： A61K31/555 ,  A61K33/24 ,  A61K31/335 ,  A61K31/53 ,  A61K2300/00

摘要： In accordance with the present invention there is provided a method of treating a mammal having a solid tumor, the method comprising: a) administering to the mammal an effective amount of 3-amino-1,2,4-benzotriazine 1,4-dioxide; b) administering to the mammal an effective amount of paclitaxel; and c) administering to the mammal an effective amount of a platinum complex. The method provides unexpected synergistic efficacy. The invention further provides a kit for treatment of a mammalian tumor comprising 3-amino-1,2,4-benzotriazine 1,4-dioxide, paclitaxel and a platinum complex.

公开(公告)号：EP0979079A1

公开(公告)日：2000-02-16

申请号：EP98921552.0

申请日：1998-04-17

申请人： SANOFI-SYNTHELABO

发明人： BOURRIE, Bernard ,  CASELLAS, Pierre ,  MAFFRAND, Jean-Pierre

IPC分类号： A61K31/44

CPC分类号： A61K31/444 ,  A61K31/4418

摘要： The invention concerns the use of tetrahydropyridine derivatives of formula (I) in which: R1 represents a halogen or a CF3, (C1-C4) alkyl or (C1-C4)alkoxy group; Y represents a nitrogen atom or a CH group; Z' and Z' represent each hydrogen or a (C1-C3) alkyl group, or one represents hydrogen and the other a hydroxy group, or both together represent an oxo group; Z represents a phenyl radical; a phenyl radical monosubstituted by a substituent X, X being (a) a (C1-C6)alkyl, (C1-C6)alkoxy (C3-C7)carboxyalkyl, (C1-C4)alkoxycarbonyl(C1-C6)alkyl, (C3-C7)carboxyalkoxy or (C1-C4)-alkoxycarbonyl(C1-C6) alkoxy group; (b) a group selected among a (C3-C7)cycloalkyl, (C3-C7)cycloalkoxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl group, said group capable of being substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino, mono- or di-(C1-C4)alkylamino; or (c) a group selected among a phenyl, phenoxy, phenylamino, N-(C1-C3)alkylphenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulphonyl, phenylsulphinyl or styryl group, said group can be mono- or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl; a phenyl radical disubstituted by a substituent R2, R2 being a halogen or a hydroxy, methyl, ethyl, (C3-C6)alkyl, (C1-C4)alkoxy or trifuoromethyl group and by a substituent X, X being as defined above; a 1-naphthyl or 2-naphthyl radical; a 1-naphthyl or 2-naphthyl radical, substituted in positions 5, 6, 7 and/or 8 by one or two hydroxyl groups, one or two (C1-C4) alkoxy groups, or a 6,7-methylenedioxy group; or Z' is hydrogen and Z and Z' represent, each independently, a phenyl group non-substituted or mono-, di- or trisubstituted; or one of its pharmaceutically acceptable salts or solvates, for preparing pharmaceutical compositions to fight against diseases causing demyelination.

公开(公告)号：EP1465893A1

公开(公告)日：2004-10-13

申请号：EP03712202.5

申请日：2003-01-03

申请人： SANOFI-SYNTHELABO

发明人： GALLI, Frédéric ,  LECLERC, Odile ,  LOCHEAD, Alistair ,  NEDELEC, Alain

IPC分类号： C07D471/08 ,  A61K31/439 ,  A61P25/00

CPC分类号： C07D471/08

摘要： The invention relates to compounds having general formula (I), wherein R denotes a halogen atom, a phenyl group which is substituted by one or more groups selected from among halogen atoms and the (Cl-C6) alkyl, (C1-C6) alcoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, a pyridinyl group, a thienyl group, a indolyl group, or a pyrimidinyl group which is optionally substituted by one or more (C1-C6) alcoxy groups. Moreover, among the two carbon-carbon bonds denoted by ----, one is simple and the other can be simple or double. The inventive compounds are nicotinic receptor ligands.

公开(公告)号：EP1460076A1

公开(公告)日：2004-09-22

申请号：EP03290728.9

申请日：2003-03-21

申请人： SANOFI-SYNTHELABO ,  Mitsubishi Pharma Corporation

发明人： Lochead, Alistair W. ,  Saady, Mourad ,  Slowinski, Franck ,  Yaiche, Philippe

IPC分类号： C07D487/04

CPC分类号： A61K31/519 ,  C07D487/04

摘要： The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:

X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom;
Y represents a bond, a carbonyl group, a methylene group optionally substituted;
R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted;
R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted;
R3 represents a hydrogen atom or a C 1-6 alkyl group;
R4 represents a C 1-2 perhalogenated alkyl group or a C 1-3 halogenated alkyl group;
R5 represents a hydrogen atom; a C 1-6 alkyl group or a halogen atom;
n represents 0 to 3; and p+q=0-3.

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）表示的取代嘧啶酮衍生物或其盐：其中：X表示两个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Y表示键，羰基，任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R2表示苯基或萘环; 苯基和萘环任选被取代; R3表示氢原子或C1-6烷基; R4表示C1-2全卤代烷基或C1-3卤代烷基; R5表示氢原子; C 1-6烷基或卤素原子; n表示0〜3; 和p + q = 0-3。 本发明还涉及包含所述衍生物或其盐作为活性成分的药物，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。

公开(公告)号：EP1458721A1

公开(公告)日：2004-09-22

申请号：EP02796852.8

申请日：2002-11-20

申请人： SANOFI-SYNTHELABO

发明人： BURNIER, Philippe ,  FROISSANT, Jacques ,  MARABOUT, Benoît ,  MARGUET, Frank ,  PUECH, Frédéric

IPC分类号： C07D487/04 ,  A61K31/50 ,  A61P25/02 ,  A61P25/28

CPC分类号： C07D487/04 ,  C07D209/42

摘要： The invention concerns compounds of general formula (I), wherein: X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3, represent each, independently of each other, a hydrogen atom or a (C1-C4)alkyl group, or R2 and R3 form, with the atom which bears them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl, pyridazinyl type, the heteroaromatic group may represent one or several halogen atoms and/or one or several (C1-C4)alkyl, (C1-C4)alkoxyl groups; in the form of bases, addition salts to acids, solvates or hydrates. The invention also concerns pharmaceutical compositions containing same, methods for preparing same and synthesis intermediates.

公开(公告)号：EP1454908A1

公开(公告)日：2004-09-08

申请号：EP03290571.3

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： C07D471/08 ,  C07D487/08 ,  A61K31/40 ,  A61K31/435

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 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, 3 or 4-pyridine 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，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全卤代烷基的取代基取代 ，C 1-3卤代烷基，羟基，C 1-4烷氧基，硝基，氰基，氨基，C 1-6单烷基氨基或C 2-10二烷基氨基; 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2,3或4-吡啶环; 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。

公开(公告)号：EP1451197A1

公开(公告)日：2004-09-01

申请号：EP02803450.2

申请日：2002-11-20

申请人： SANOFI-SYNTHELABO

发明人： GALLI, Frédéric ,  LECLERC, Odile ,  LOCHEAD, Alistair

IPC分类号： C07D519/00 ,  A61K31/551 ,  A61P25/28 ,  A61P25/16

CPC分类号： C07D519/00

摘要： The invention concerns a compound of general formula (I), wherein R2 represents a chlorine atom, a methyl group or a thien-3-yl group. The invention has therapeutic uses.

公开(公告)号：EP1194131B1

公开(公告)日：2004-09-01

申请号：EP00949361.0

申请日：2000-06-27

申请人： SANOFI-SYNTHELABO

发明人： ANDRE, Frédéric ,  LEWIS, Gareth ,  MIGNONNEAU, Jérôme ,  RIBARDIERE, Agnès

IPC分类号： A61K9/50

CPC分类号： A61K9/5078 ,  A61K9/5015 ,  A61K9/5026

摘要： The present invention relates to delayed release coated cores comprising an active substance in their core and a polymer coating comprising at least one or more ammonio methacrylate copolymer, characterised in that the core comprises at least a surfactant; to monolithic or multiparticulate pharmaceutical dosage forms comprising such delayed release coated cores and to their method of manufacture.

公开(公告)号：EP1448550A1

公开(公告)日：2004-08-25

申请号：EP02803433.8

申请日：2002-11-18

申请人： SANOFI-SYNTHELABO

发明人： BARONI, Marco ,  BOURRIE, Bernard ,  CASELLAS Pierre ,  PULEO, Letizia

IPC分类号： C07D401/10 ,  A61K31/4523 ,  A61K31/4545 ,  A61P25/00

CPC分类号： C07D401/10

摘要： The invention concerns a compound 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 C1-C4 alkyl group; R4 represents a hydrogen atom or a C1-C4 alkyl group; n is 0 or 1; A represents a heterocycle selected among pyridine, pyrimidine, pyrazine and pyridazine optionally mono-or di-substituted by a C1-C4 alkyl or C1-C4 alkoxy group; and their N-oxides and their salts or solvates.

公开(公告)号：EP1446131A1

公开(公告)日：2004-08-18

申请号：EP02787601.0

申请日：2002-11-07

申请人： SANOFI-SYNTHELABO

发明人： LENSING, Anthonie Wilhelmus A.,c/o N.V. Organon

IPC分类号： A61K31/7024 ,  A61P9/10

CPC分类号： A61K31/7024

摘要： The invention relates to the use of a dose of 2.5 mg of the pentasaccharide methyl O-(2-deoxy-2-sulfoamino-6-O-sulfo-α-D-glucopyranosyl)-(1-4)-O-(β-D-glucopyranosyl uronic acid)-(1-4)-O-(2-deoxy-2-sulfoamino-3,6-di-O-sulfo-α-D-glucopyranosyl)-(1-4)-O-(2-O-sulfo-α-L-idopyranosyl uronic acid)-(1-4)-2-deoxy-2-sulfoamino-6-O-sulfo-α-D-glucopyranoside or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of Acute Coronary Syndromes (ACS).