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1. 发明授权

US07790728B2 Pyrazine derivatives useful as adenosine receptor antagonists 失效
标题翻译：用作腺苷受体拮抗剂的吡嗪衍生物
公开(公告)号：US07790728B2
公开(公告)日：2010-09-07
申请号：US11997048
申请日：2006-07-25
申请人： Bernat Vidal Juan , Christina Esteve Trias , Lidia Soca Pueyo , Paul Robert Eastwood
发明人： Bernat Vidal Juan , Christina Esteve Trias , Lidia Soca Pueyo , Paul Robert Eastwood
IPC分类号： A61K31/4965
CPC分类号： C07D487/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 are chosen from a hydrogen atom and specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moiety of formulae (IIa) and (IIb): or a pharmaceutically acceptable salt thereof, or a N-oxide thereof. The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.
摘要翻译：本发明涉及式（I）化合物，其中：A为任选取代的单环或多环芳基或杂芳基; B是任选取代的单环含氮杂芳基; 和a）R 1和R 2选自氢原子和特定取代基，或b）R 2，R 1和R 1连接的-NH-基团，形成选自式（IIa）和（IIb）部分的部分）：或其药学上可接受的盐或其N-氧化物。本公开还涉及用于治疗受到A2B腺苷受体拮抗作用而易于改善的病理状况或疾病的受试者的治疗方法。

2. 发明申请

US20090042891A1 Pyrazine Derivatives Useful as Adenosine Receptor Antagonists 失效
标题翻译：用作腺苷受体拮抗剂的吡嗪衍生物
公开(公告)号：US20090042891A1
公开(公告)日：2009-02-12
申请号：US11997048
申请日：2006-07-25
申请人： Bernat Vidal Juan , Cristina Esteve Trias , Lidia Soca Pueyo , Paul Robert Eastwood
发明人： Bernat Vidal Juan , Cristina Esteve Trias , Lidia Soca Pueyo , Paul Robert Eastwood
IPC分类号： A61K31/495 , C07D401/06 , C07D471/04 , A61P11/06 , A61K31/4965
CPC分类号： C07D487/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 are chosen from a hydrogen atom and specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moiety of formulae (IIa) and (IIb): or a pharmaceutically acceptable salt thereof, or a N-oxide thereof. The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.
摘要翻译：本发明涉及式（I）化合物，其中：A为任选取代的单环或多环芳基或杂芳基; B是任选取代的单环含氮杂芳基; 和a）R 1和R 2选自氢原子和特定取代基，或b）R 2，R 1和R 1连接的-NH-基团，形成选自式（IIa）和（IIb）部分的部分）：或其药学上可接受的盐或其N-氧化物。本公开还涉及用于治疗受到A2B腺苷受体拮抗作用而易于改善的病理状况或疾病的受试者的治疗方法。

3. 发明申请

US20100273757A1 PYRAZINE DERIVATIVES USEFUL AS ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：有用的亚氨基衍生物作为腺苷受体拮抗剂
公开(公告)号：US20100273757A1
公开(公告)日：2010-10-28
申请号：US12794059
申请日：2010-06-04
申请人： Bernat Vidal Juan , Cristina Esteve Trias , Lidia Soca Pueyo , Paul Robert Eastwood
发明人： Bernat Vidal Juan , Cristina Esteve Trias , Lidia Soca Pueyo , Paul Robert Eastwood
IPC分类号： A61K31/56 , C07D401/04 , C07D417/04 , C07D405/14 , C07D401/14 , C07D471/04 , C07D413/14 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61P11/06 , A61P37/08 , A61P9/12 , A61P9/10 , A61P29/00 , A61P1/00 , A61P3/10 , A61P37/00 , A61P43/00 , A61P11/08
CPC分类号： C07D487/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.
摘要翻译：本发明提供式（I）化合物，其中：A表示任选取代的单环或多环芳基或杂芳基B表示任选取代的单环含氮杂芳基; 和a）R 1和R 2表示氢或特定取代基，或b）R 2，R 1和R 1连接的-NH-基团，形成选自式（IIa）和（IIb）部分的部分：（IIa ）这些化合物可用作A2B受体的拮抗剂，例如用于治疗哮喘。

4. 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。

5. 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。

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