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1. 发明公开

EP1330453A1 INDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS 有权
标题翻译： INDOLYLPIPERIDINDERIVATE ALS抗组胺药和抗过敏药
公开(公告)号：EP1330453A1
公开(公告)日：2003-07-30
申请号：EP01992709.4
申请日：2001-10-26
申请人： Almirall Prodesfarma, S.A.
发明人： FONQUERNA POU, Silvia , PAGES SANTACANA, Lluis , PUIG DURAN, Carles , SOCA PUEYO, Lidia
IPC分类号： C07D405/14 , A61K31/445 , A61P43/00 , C07D401/14 , C07D409/14 , C07D413/14
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention relates to indolyl piperidinyl derivatives of formula (I) wherein: A1 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or hydroxyalkylene group; A2 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or an alkyleneoxyalkylene group; W1 represents a phenylene, furanylene or pyridinylene group which is unsubstituted or substituted by one or more halogen atoms, alkoxy groups and/or alkyl groups; W2 represents a 3-10 membered monocyclic or bicyclic group containing from 1 to 3 heteroatoms said group being unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups and/or oxo groups; R1 represents a hydrogen or halogen atom or an alkyl, alkoxy or methylamino group; and R2 represents a carboxyl group; and pharmaceutically acceptable salts thereof; to processes for their preparation; to pharmaceutical compositions containing them; and to their medical use as antihistaminic and antiallergic agents.

2. 发明授权

EP1330453B1 INDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS 有权
标题翻译： INDOLYLPIPERIDINDERIVATE ALS抗组胺药和抗过敏药
公开(公告)号：EP1330453B1
公开(公告)日：2006-03-29
申请号：EP01992709.4
申请日：2001-10-26
申请人： Almirall Prodesfarma, S.A.
发明人： FONQUERNA POU, Silvia , PAGES SANTACANA, Lluis , PUIG DURAN, Carles , SOCA PUEYO, Lidia
IPC分类号： C07D405/14 , A61K31/445 , A61P43/00 , C07D401/14 , C07D409/14 , C07D413/14
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention relates to indolyl piperidinyl derivatives of formula (I) wherein: A1 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or hydroxyalkylene group; A2 represents an alkylene, alkyleneoxy, alkylenethio, alkanoylene or an alkyleneoxyalkylene group; W1 represents a phenylene, furanylene or pyridinylene group which is unsubstituted or substituted by one or more halogen atoms, alkoxy groups and/or alkyl groups; W2 represents a 3-10 membered monocyclic or bicyclic group containing from 1 to 3 heteroatoms said group being unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups and/or oxo groups; R1 represents a hydrogen or halogen atom or an alkyl, alkoxy or methylamino group; and R2 represents a carboxyl group; and pharmaceutically acceptable salts thereof; to processes for their preparation; to pharmaceutical compositions containing them; and to their medical use as antihistaminic and antiallergic agents.

3. 发明公开

EP1115716A1 2-PHENYLPYRAN-4-ONE DERIVATIVES 有权
标题翻译： 2-苯基吡喃-4-酮衍生物
公开(公告)号：EP1115716A1
公开(公告)日：2001-07-18
申请号：EP99947372.1
申请日：1999-09-16
申请人： Almirall Prodesfarma, S.A.
发明人： CRESPO CRESPO, M Isabel , JIMENEZ MAYORGA, Juan Miguel , PUIG DURAN, Carles , SOCA PUEYO, Lidia
IPC分类号： C07D309/38 , C07D309/40 , C07D405/04 , C07D409/04 , A61K31/35 , C07C317/24 , C07C311/29
CPC分类号： C07D405/04 , C07C311/29 , C07C317/24 , C07D309/38 , C07D309/40 , C07D409/04
摘要： 2-Phenylpyran-4-one derivatives of formula (I), wherein R1 represents an alkyl or -NR4R5 group, wherein R?4 and R5¿ each independently represents a hydrogen atom or an alkyl group; R2 represents an alkyl, C¿3?-C7 cycloalkyl, pyridyl, thienyl, naphthyl, tetrahydronaphthyl or indanyl group, or a phenyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, trifluoromethyl, hydroxy, alkoxy, methylthio, amino, mono- or dialkylamino, hydroxyalkyl or hydroxycarbonyl groups; R?3¿ represents a methyl, hydroxymethyl, alkoxymethyl, C¿3?-C7 cycloalkoxymethyl, benzyloxymethyl, hydroxycarbonyl, nitrile, trifluoromethyl or difluoromethyl group or a CH2-R?6¿ group wherein R6 represents an alkyl group; and X represents a single bond, an oxygen atom, a sulfur atom or a methylene group; or pharmaceutically acceptable salts thereof, processes for their production and synthetic intermediates used in said processes, pharmaceutical compositions containing them and their use in medical treatment.
摘要翻译：式（I）的2-苯基吡喃-4-酮衍生物，其中R 1代表烷基或-NR 4 R 5基团，其中R 14和R 5各自独立地代表氢原子或烷基; R 2代表烷基，C 3 -C 7环烷基，吡啶基，噻吩基，萘基，四氢萘基或2,3-二氢化茚基，或可以未被取代或被一个或多个卤素原子或烷基，三氟甲基，羟基，烷氧基，甲硫基，氨基，单或二烷基氨基，羟烷基或羟基羰基; R 3代表甲基，羟甲基，烷氧基甲基，C 3 -C 7环烷氧基甲基，苄氧基甲基，羟基羰基，腈基，三氟甲基或二氟甲基或CH 2 -R 6基，其中R 6代表烷基; X表示单键，氧原子，硫原子或亚甲基; 或其药学上可接受的盐，其制备方法和所述方法中使用的合成中间体，含有它们的药物组合物以及它们在医学治疗中的用途。

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