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1. 发明授权

US07189741B2 Indolylpiperidine derivatives as antihistaminic and antiallergic agents 失效
标题翻译：吲哚基哌啶衍生物作为抗组胺和抗过敏剂
公开(公告)号：US07189741B2
公开(公告)日：2007-03-13
申请号：US10415693
申请日：2001-10-26
申请人： Silvia Fonquerna Pou , Lluis Pages Santacana , Carles Puig Duran , Lidia Soca Pueyo
发明人： Silvia Fonquerna Pou , Lluis Pages Santacana , Carles Puig Duran , Lidia Soca Pueyo
IPC分类号： A61K31/445 , C07D401/14
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.
摘要翻译：本发明涉及式（I）的吲哚基哌啶基衍生物，其中：A 1表示亚烷基，亚烷基氧基，亚烷基硫代，亚烷基或羟基亚烷基; 代表亚烷基，亚烷基氧基，亚烷硫基，亚烷基亚烷基或亚烷基氧亚烷基; W 1表示未被取代或被一个或多个卤素原子，烷氧基和/或烷基取代的亚苯基，呋喃基或亚吡啶基; W 2表示含有1至3个杂原子的3-10元单环或双环，所述基团未被取代或被一个或多个卤素原子，烷基，烷氧基和/或氧代基取代; R 1表示氢或卤素原子或烷基，烷氧基或甲基氨基; R 2表示羧基; 及其药学上可接受的盐; 进行准备; 含有它们的药物组合物; 以及作为抗组胺药和抗过敏剂的医疗用途。

2. 发明授权

US06518303B2 2-phenylpyran-4-one derivatives 失效
标题翻译： 2-苯基吡喃-4-酮衍生物
公开(公告)号：US06518303B2
公开(公告)日：2003-02-11
申请号：US09809645
申请日：2001-03-16
申请人： Maria Isabel Crespo Crespo , Juan Miguel Jimenez Mayorga , Carles Puig Duran , Lidia Soca Pueyo
发明人： Maria Isabel Crespo Crespo , Juan Miguel Jimenez Mayorga , Carles Puig Duran , Lidia Soca Pueyo
IPC分类号： A61K3135
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 R4 and R5 each independently represents a hydrogen atom or an alkyl group; R2 represents an alkyl, C3-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, hydroxalkyl or hydroxycarbonyl groups; R3 represents a methyl, hydroxymethyl, alkoxymethyl, C3-C7 cycloalkoxymethyl, benzyloxymethyl, hydroxycarbonyl, nitrile, trifluoromethyl or difluoromethyl group or a CH2—R6 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：R1表示烷基或-NR4R5基团，其中R4和R5各自独立地表示氢原子或烷基; R2表示烷基，C3-C7环烷基，三氟甲基，羟基，烷氧基，甲硫基，氨基，一烷基氨基或二烷基氨基，羟烷基或羟基羰基可被取代或被一个或多个卤原子取代或被一个或多个卤原子取代的苯基; R3表示甲基，羟甲基，烷氧基甲基，C3-C7环烷氧基甲基，苄氧基甲基，羟基羰基，腈，三氟甲基或二氟甲基或CH2-R6基团，其中R6表示烷基; 和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，其制备方法和用于所述方法的合成中间体，含有它们的药物组合物及其在医疗中的用途。

3. 发明授权

US06683096B2 Indolylpiperidine derivatives as antihistaminic and antiallergic agents 失效
标题翻译：吲哚基哌啶衍生物作为抗组胺和抗过敏剂
公开(公告)号：US06683096B2
公开(公告)日：2004-01-27
申请号：US10006416
申请日：2001-12-04
申请人： Lluis Pages Santacana , Silvia Fonquerna Pou , Carles Puig Duran , Maria Dolors Fernandez Forner
发明人： Lluis Pages Santacana , Silvia Fonquerna Pou , Carles Puig Duran , Maria Dolors Fernandez Forner
IPC分类号： A61K31445
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： Indolylpiperidine compounds of formula (I) wherein: A1 represents an alkylene, alkyleneoxy, alkylenethio, alkanoyl or hydroxyalkylene group; A2 represents a single bond, an alkylene or alkenylene group; W represents a single bond or a phenylene or furanylene group which is unsubstituted or substituted by one or more halogen atoms, alkoxy groups and/or alkyl groups; R2 represents a hydrogen or halogen atom or an alkyl or alkoxy group; and R3 represents a carboxyl group or a tetrazolyl group. The present invention provides novel indolylpiperidine compounds having imporved antihistamine and antiallergic activity.
摘要翻译：式（I）的吲哚基哌啶化合物，其中：A 1表示亚烷基，亚烷基氧基，亚烷基硫代，烷酰基或羟基亚烷基; A 2表示单键，亚烷基或亚烯基; W表示单键或亚苯基或未被取代或被一个或多个卤素原子，烷氧基和/或烷基取代的呋喃基; R 2表示氢或卤原子或烷基或烷氧基; R 3表示羧基或四唑基。本发明提供具有抗组胺和抗过敏活性的新的吲哚基哌啶化合物。

4. 发明授权

US06869968B1 2-(3H)-oxazolone derivatives and their use as COX-2 inhibitors 失效
标题翻译： 2-（3H） - 恶唑酮衍生物及其作为COX-2抑制剂的用途
公开(公告)号：US06869968B1
公开(公告)日：2005-03-22
申请号：US09158966
申请日：1998-09-21
申请人： Carles Puig Duran , Ferran Pujol Noguera , Dolors Fernandez Forner
发明人： Carles Puig Duran , Ferran Pujol Noguera , Dolors Fernandez Forner
IPC分类号： A61K31/00 , A61K31/42 , A61K31/421 , A61P11/00 , A61P11/06 , A61P29/00 , C07D263/38 , C07D263/04
CPC分类号： C07D263/38
摘要： The invention relates to 2-(3H)-oxazolone derivatives. They may be used as COX-2 inhibitors. The compounds may be used in the treatment of colorectal cancer.
摘要翻译：本发明涉及2-（3H） - 恶唑酮衍生物。它们可以用作COX-2抑制剂。该化合物可用于治疗结肠直肠癌。

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