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1. 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。

2. 发明申请

WO1998025903A1 1-PHENYLALKYL-1,2,3,6-TETRAHYDROPYRIDINES FOR TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译： 1-苯甲酰基-1,2,3,6-四氢吡啶类药物治疗阿尔茨海默病
公开(公告)号：WO1998025903A1
公开(公告)日：1998-06-18
申请号：PCT/FR1997002286
申请日：1997-12-12
申请人： SANOFI , BARONI, Marco , CARDAMONE, Rosanna , FOURNIER, Jacqueline , GUZZI, Umberto
发明人： SANOFI
IPC分类号： C07D211/70
CPC分类号： C07D401/04 , C07D211/70
摘要： The invention concerns compounds of formula (I) in which Y represents -CH- or -N-; R1 represents hydrogen, a halogen, a CF3 group, (C1-C4)alkyl or (C1-C4)alcoxyl; R2 represents a methyl or ethyl group; R3 and R4 each represent hydrogen or a (C1-C3)alkyl; X represents (a) a (C1-C6)alkyl; a (C1-C6)alcoxyl; a (C3-C7)carboxyalkyl; a (C1-C4)alcoxycarbonyl(C1-C6)alkyl; a (C3-C7)carboxyalcoxyl; or a (C1-C4)alcoxycarbonyl(C1-C6)alcoxyl; (b) a radical selected among a (C3-C7)cycloalkyl, (C3-C7)cycloalkyloxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl, said radical can be substituted by a halogen, hydroxy, (C1-C4)alcoxy, carboxy, (C1-C4)alcoxycarbonyl, 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, phenylsuphonyl, phenylsulphinyl or styryl, said group can be mono- or poly-substituted by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alcoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alcoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl, hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl. The invention also concerns a method for preparing them and the pharmaceutical compositions containing them. These compounds have a neurotrophic and neuroprotecting activity.
摘要翻译：本发明涉及式（I）化合物，其中Y代表-CH-或-N-; R1表示氢，卤素，CF3基，（C1-C4）烷基或（C1-C4）烷氧基; R2表示甲基或乙基; R3和R4各自表示氢或（C1-C3）烷基; X表示（a）（C 1 -C 6）烷基; （C1-C6）烷基; （C 3 -C 7）羧基烷基; （C 1 -C 4）烷氧基羰基（C 1 -C 6）烷基; （C 3 -C 7）羧烷氧基; 或（C 1 -C 4）烷氧基羰基（C 1 -C 6）烷氧基; （c）选自（C 3 -C 7）环烷基，（C 3 -C 7）环烷氧基，（C 3 -C 7）环烷基甲基，（C 3 -C 7）环烷基氨基和环己烯基中的基团，所述基团可以被卤素，羟基，（ C1-C4）烷氧基，羧基，（C1-C4）烷氧基羰基，氨基，单 - 或二 - （C1-C4）烷基氨基; 或（c）选自苯基，苯氧基，苯基氨基，N-（C1-C3）烷基苯基氨基，苯基甲基，苯乙基，苯基羰基，苯硫基，苯基对苯基，苯基亚磺酰基或苯乙烯基中的基团，所述基团可以被单取代或多取代卤素，CF 3，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，氰基，氨基，单 - 或二 - （C 1 -C 4）烷基氨基，（C 1 -C 4）酰氨基，羧基，（C 1 -C 4）氨基羰基，单 - 或二 - （C 1 -C 4）烷基氨基羰基，氨基（C 1 -C 4）烷基，羟基（C 1 -C 4）烷基或卤代（C 1 -C 4）烷基。本发明还涉及制备它们的方法和含有它们的药物组合物。这些化合物具有神经营养和神经保护活性。

3. 发明申请

WO1998033502A1 USE OF 1-[4-(3-TRIFLUOROMETHYLPHENYL)-1,2,3,6-TETRAHYDROPYRID-1YL]-2-(6,7-DIMETHOXYNAPHT-2-YL) ETHANE FOR PREPARING MEDICINES FOR THE TREATMENT OF CEREBRAL AND NEURONAL DISORDERS 审中-公开
标题翻译： 1- [4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶-1-基] -2-（6,7-二甲基亚氨基-2-基）乙烯的制备用于治疗谷胱甘肽和神经元的药物的用途病症
公开(公告)号：WO1998033502A1
公开(公告)日：1998-08-06
申请号：PCT/FR1997000202
申请日：1997-02-03
申请人： SANOFI , CROCI, Tiziano , FOURNIER, Jacqueline , GUZZI, Umberto , PALMIERI, Costantino
发明人： SANOFI
IPC分类号： A61K31/44
CPC分类号： A61K31/44
摘要： The invention concerns the use of 1-[4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyrid-1yl]-2-(6,7-dimethoxynapht-2-yl) ethane (I) for preparing medicines for the treatment and/or prevention of cerebral and neuronal disorders
摘要翻译：本发明涉及1- [4-（3-三氟甲基苯基）-1,2,3,6-四氢吡咯-1-基] -2-（6,7-二甲氧基萘-2-基）乙烷（I）用于制备药物用于治疗和/或预防脑和神经元疾病

4. 发明申请

WO1997001536A1 4-ARYL-1-PHENYLALKYL-1,2,3,6-TETRAHYDROPYRIDINES HAVING NEUROTROPHIC AND NEUROPROTECTIVE ACTIVITY 审中-公开
标题翻译：具有神经营养因子和神经保护活性的4-芳基-1-苯甲基-1,2,3,6-四氢吡啶
公开(公告)号：WO1997001536A1
公开(公告)日：1997-01-16
申请号：PCT/FR1996000995
申请日：1996-06-26
申请人： SANOFI , BADONE, Domenico , BARONI, Marco , CARDAMONE, Rosanna , FOURNIER, Jacqueline , GUZZI, Umberto , IELMINI, Alessandra
发明人： SANOFI
IPC分类号： C07D211/70
CPC分类号： C07D401/04 , C07D211/52 , C07D211/70
摘要： Compounds of formula (I), wherein Y is -CH- or -N-; R1 is hydrogen, halogen, a CF3 group, (C3-4) alkyl or (C1-4) alkoxyl; R2 is hydrogen, halogen, hydroxyl, a CF3 group, (C3-4) alkyl or (C1-4) alkoxyl; each of R3 and R4 is hydrogen or (C1-3) alkyl; X is (a) (C3-6) alkyl, (C3-6) alkoxyl, (C3-7) carboxyalkyl, (C1-4)alkoxycarbonyl(C3-6)alkyl, (C3-7) carboxyalkoxyl or (C1-4)alkoxycarbonyl(C3-6)alkoxyl; (b) a radical selected from (C3-7) cycloalkyl, (C3-7) cycloalkyloxy, (C3-7) cycloalkylmethyl, (C3-7) cycloalkylamino and cyclohexenyl, said radical being optionally substituted by halogen, hydroxy, (C1-4) alkoxy, carboxy, (C1-4) alkoxycarbonyl, amino, mono- or di-(C1-4)alkylamino; or (c) a group selected from phenyl, phenoxy, phenylamino, N-(C1-3) alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulphonyl, phenylsulphinyl or styryl, said group being optionally mono- or polysubstituted on the phenyl group by halogen, CF3, (C1-4)alkyl, (C1-4)alkoxy, cyano, amino, mono- or di-(C1-4)alkylamino, (C1-4)acylamino, carboxy, (C1-4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-4)alkylaminocarbonyl, amino(C1-4)alkyl, hydroxy(C1-4)alkyl or halo(C1-4)alkyl; and salts, solvates and quaternary ammonium salts thereof; a method for preparing said compounds; and pharmaceutical compositions containing same, are disclosed. Said compounds have neurotrophic and neuroprotective activity.
摘要翻译：式（I）化合物，其中Y为-CH-或-N-; R1是氢，卤素，CF3基，（C3-4）烷基或（C1-4）烷氧基; R2是氢，卤素，羟基，CF3基，（C3-4）烷基或（C1-4）烷氧基; R 3和R 4各自为氢或（C 1-3）烷基; X为（a）（C3-6）烷基，（C3-6）烷氧基，（C3-7）羧基烷基，（C1-4）烷氧基羰基（C3-6）烷基，（C3-7）羧烷基氧基或（C1-4 ）烷氧基羰基（C 3-6）烷氧基; （c）选自（C3-7）环烷基，（C3-7）环烷基氧基，（C3-7）环烷基甲基，（C3-7）环烷基氨基和环己烯基的基团，所述基团任选被卤素，羟基，（C1- 4）烷氧基，羧基，（C 1-4）烷氧基羰基，氨基，单 - 或二 - （C 1-4）烷基氨基; 或（c）选自苯基，苯氧基，苯基氨基，N-（C 1-3）烷基 - 苯基氨基，苯基甲基，苯乙基，苯基羰基，苯硫基，苯基磺酰基，苯基亚磺酰基或苯乙烯基中的基团，所述基团任选地在苯基氰基，氨基，单 - 或二 - （C1-4）烷基氨基，（C1-4）酰基氨基，羧基，（C1-4）烷基，（C1-C4）烷氧基，烷氧基羰基，氨基羰基，单 - 或二 - （C 1-4）烷基氨基羰基，氨基（C 1-4）烷基，羟基（C 1-4）烷基或卤代（C 1-4）烷基; 及其盐，溶剂化物和季铵盐; 制备所述化合物的方法; 和含有它们的药物组合物。所述化合物具有神经营养和神经保护活性。

5. 发明申请

WO1995031449A1 NOVEL 3,5-DIMETHYLPIPERIDIN-1-YLALKYL ESTERS 审中-公开
标题翻译：新的3,5-二甲基哌啶-1-基乙酸酯
公开(公告)号：WO1995031449A1
公开(公告)日：1995-11-23
申请号：PCT/FR1995000632
申请日：1995-05-16
申请人： SANOFI , MIDY S.P.A. , LANGLOIS, Michel , GUZZI, Umberto , CECCHI, Roberto , CROCI, Tiziano
发明人： SANOFI , MIDY S.P.A.
IPC分类号： C07D295/08
CPC分类号： C07D295/088
摘要： Novel 3,5-dimethylpiperidin-1-ylalkyl esters and, in particular, the use of a 3,5-dimethylpiperidin-1-ylalkyl radical as a carboxylic group ester in compounds having an affinity for the 5-HT4 receptor. The present invention mainly concerns 3,5-dimethylpiperidinoalkyl esters of formula (I) in which Alk is an alkylene group having 2-4 carbon atoms; n is 0 or 1; and X is an aromatic monocyclic or polycyclic group such as an aromatic monocyclic or bicyclic group or a heteroaromatic monocyclic, bicyclic or tricyclic group. The invention also concerns the salts, solvates and quaternary ammonium salts of said esters only when X is an aromatic monocyclic or bicyclic group.
摘要翻译：新的3,5-二甲基哌啶-1-基烷基酯，特别是在对5-HT 4受体具有亲和力的化合物中使用3,5-二甲基哌啶-1-基烷基作为羧基酯。本发明主要涉及式（I）的3,5-二甲基哌啶子基烷基酯，其中Alk是具有2-4个碳原子的亚烷基; n为0或1; 并且X是芳族单环或多环基团，例如芳族单环或双环基团或杂芳族单环，双环或三环基团。只有当X是芳族单环或双环基团时，本发明还涉及所述酯的盐，溶剂合物和季铵盐。

6. 发明申请

WO1998028274A1 USE OF BENZOYLALKYL-1,2,3,6-TETRAHYDROPYRIDINS 审中-公开
标题翻译：苯甲酰基-1,2,3,6-四氢吡啶的使用
公开(公告)号：WO1998028274A1
公开(公告)日：1998-07-02
申请号：PCT/FR1997002424
申请日：1997-12-24
申请人： SANOFI , BARONI, Marco , CARDAMONE, Rosanna , FOURNIER, Jacqueline , GUZZI, Umberto , IELMINI, Alessandra
发明人： SANOFI
IPC分类号： C07D211/70
CPC分类号： C07D211/70 , A61K31/4418
摘要： The invention concerns the use of compounds of formula (I) for preparing medicines for the treatment of neuronal and cerebral disorders. The invention also concerns the compounds of formula (I') their method of preparation and the pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物用于制备用于治疗神经元和脑障碍的药物的用途。本发明还涉及式（I'）化合物及其制备方法和含有它们的药物组合物。

7. 发明申请

WO1998025904A1 DIPHENYL ALKYL-TETRAHYDROPYRIDINES, PROCESS FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：二苯甲基四氢吡啶类，其制备方法和含有它们的药物组合物
公开(公告)号：WO1998025904A1
公开(公告)日：1998-06-18
申请号：PCT/FR1997002289
申请日：1997-12-12
申请人： SANOFI , BARONI, Marco , CARDAMONE, Rosanna , FOURNIER, Jacqueline , GUZZI, Umberto
发明人： SANOFI
IPC分类号： C07D211/70
CPC分类号： C07D401/04 , C07D211/70
摘要： The invention relates to the compounds of formula: (I) wherein Y represents -CH- or -N-; R1 represents a halogen, a CF3 group, (C1-C4) alkyl or (C1-C4) oxyalkylate; R2 and R3 each represent hydrogen or a (C1-C3) alkyl; n represents 0 or 1 Ph1 and Ph2 each independently represent a non-substituted, monosubstituted, or polysubstituted phenyl group. The invention further concerns a process for the preparation of the compounds as well as the pharmaceutical compositions which contain them. These compounds have neurotrophic and neuro-protective properties.
摘要翻译：本发明涉及式（I）的化合物，其中Y代表-CH-或-N-; R1表示卤素，CF3基，（C1-C4）烷基或（C1-C4）烷氧基化物; R2和R3各自表示氢或（C1-C3）烷基; n表示0或1，Ph1和Ph2各自独立地表示未取代的单取代或多取代的苯基。本发明还涉及制备化合物的方法以及含有它们的药物组合物。这些化合物具有神经营养和神经保护性质。

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