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1. 发明申请

WO1995001170A2 USE OF PHENETHANOLAMINE DERIVATIVES IN THE TREATMENT OF GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：苯乙醇胺衍生物在治疗胃肠疾病中的应用
公开(公告)号：WO1995001170A2
公开(公告)日：1995-01-12
申请号：PCT/EP1994002106
申请日：1994-06-29
申请人： GLAXO GROUP LIMITED , STORER, Richard , FOXTON, Michael, Walter , HARTLEY, Charles, David , GREEN, Richard, Howard , TRAVERS, Stuart
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/165
CPC分类号： A61K31/195 , A61K31/135
摘要： The use of compounds of formula (I) in which: R is hydrogen, methyl or hydroxymethyl; R is substituted alkyl; R and R are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl group, or substituted alkyl; X is oxygen or sulphur; and Ar is optionally substituted phenyl or naphtyl; and pharmaceutically acceptable salts thereof in the treatment of gastrointestinal disorders is described.
摘要翻译：式（I）化合物的用途，其中：R 0是氢，甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自为氢，卤素，羟基，烷氧基，羧基，烷氧基羰基，烷基，硝基，卤代烷基或取代的烷基; X是氧或硫; 和Ar是任选取代的苯基或萘基; 和其药学上可接受的盐在治疗胃肠道疾病中的用途。

2. 发明申请

WO1997021665A1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS 审中-公开
标题翻译：芳香胺衍生物及其作为原子反应的激动剂使用
公开(公告)号：WO1997021665A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005469
申请日：1996-12-06
申请人： GLAXO GROUP LIMITED , GREEN, Richard, Howard , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07C229/42
CPC分类号： C07D209/08 , C07C217/84 , C07C229/42 , C07D215/04
摘要： The present invention relates to phenethanolamine derivatives of formula (I) wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the ring is substituted by one to four further substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; or R represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents ZCH2CO2H wherein Z represents a bond, or O; Y represents (CH2)n where n is 1-3; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基的取代基取代的芳基; R 2表示氢或C 1-6烷基; R 3表示其中环被1-4个其它取代基取代的基团（A），所述取代基选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基; 或R 3表示其中芳环任选被至多三个选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的其它取代基取代的基团（B）; R 4表示氢或C 1-6烷基; R 5表示ZCH 2 CO 2 H，其中Z表示键或O; Y表示（CH2）n，其中n为1-3; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

3. 发明申请

WO1997021666A1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS 审中-公开
标题翻译：芳香胺衍生物及其作为原子反应的激动剂使用
公开(公告)号：WO1997021666A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005470
申请日：1996-12-06
申请人： GLAXO GROUP LIMITED , HARTLEY, Charles, David , CARTER, Malcolm, Clive , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07C229/42
CPC分类号： C07D257/04 , C07C229/42 , C07C229/46 , C07C237/20 , C07C275/40 , C07C309/24 , C07C311/35 , C07C2601/08 , C07F9/3882
摘要： The present invention relates to phenethanolamine derivatives of formula (I), wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the aromatic ring may be optionally substituted by up to four substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents CO2R , C1-6alkylCO2R , CONR R , NHCONR R , SO2NHR , P(O)(OR )2, SO3H, C1-6alkylSO3H, NHSO2R , NHCOR or tetrazol-5-yl; R and R independently represent hydrogen, C1-6alkyl, trifluoromethyl, CN, OH, CO2R , CH2CO2R , or R and R form a 5-6 membered cycloalkyl ring; R represents hydrogen, or C1-6alkyl; R represents hydrogen, C1-6alkyl, or C1-6alkylOR ; R , R , R , R -R , and R -R each independently represent hydrogen, or C1-6alkyl; R represents C1-6alkyl or trifluoromethyl; R represents C1-6alkyl or trifluoromethyl; with the proviso that when R and R are both hydrogen, R is other than hydrogen; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基的取代基取代的芳基 ; R 2表示氢或C 1-6烷基; R 3表示芳基可以任选被至多四个选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的取代基取代的基团（A）; R 4表示氢或C 1-6烷基; R 5表示CO 2 R 8，C 1-6烷基CO 2 R 16，CONR 9 R 10，NHCONR 11 R 12，SO 2 NHR 13，P（O）（OR 14） 2，SO 3 H，C 1-6烷基SO 3 H，NHSO 2 R 15，NHCOR 17或四唑-5-基; R 6和R 7独立地表示氢，C 1-6烷基，三氟甲基，CN，OH，CO 2 R 18，CH 2 CO 2 R 19或R 6和R 7形成5-6元环烷基环; R 8表示氢或C 1-6烷基; R 9表示氢，C 1-6烷基或C 1-6烷基OR 20; R 10，R 11，R 12，R 14 -R 16和R 18 -R 20各自独立地表示氢或C 1-6烷基; R 13表示C 1-6烷基或三氟甲基; R 17表示C 1-6烷基或三氟甲基; 条件是当R 6和R 7都是氢时，R 8不是氢; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

4. 发明申请

WO1993025548A1 5-(1,2,4-TRIAZOL-1-YLMETHYL)-3H-ISOBENZOFURAN-1-ONE DERIVATIVES, THEIR PREPARATION AND USE AS AROMATASE INHIBITORS 审中-公开
标题翻译： 5-（1,2,4-TRIAZOL-1-YLMETHYL）-3H-ISOBENZOFURAN-1-ONE衍生物，其制备和用作芳香酶抑制剂
公开(公告)号：WO1993025548A1
公开(公告)日：1993-12-23
申请号：PCT/EP1993001520
申请日：1993-06-14
申请人： GLAXO GROUP LIMITED , CHERRY, Peter, Clive , FOXTON, Michael, Walter , MERRITT, Andrew, Thomas
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D405/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention relates to heterocyclic compounds which are inhibitors of the enzyme aromatase, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Particular compounds of the invention are compounds of formula (I) wherein R represents a cyano or nitro group; R represents hydrogen or one or more halogen atoms; R represents a C1-6alkyl group and R represents hydrogen or a C1-6alkyl group or R and R together represent a C3-6cycloalkyl group; and R represents hydrogen or one or more halogen atoms or C1-6alkoxy groups and pharmaceutically acceptable salts and solvates thereof.
摘要翻译：本发明涉及作为芳香酶的抑制剂，其制备方法的杂环化合物，含有它们的药物组合物及其在医药中的用途。本发明的具体化合物是式（I）的化合物，其中R 1表示氰基或硝基; R 2表示氢或一个或多个卤素原子; R 3表示C 1-6烷基，R 4表示氢或C 1-6烷基，或者R 3和R 4一起表示C 3-6环烷基; R 5表示氢或一个或多个卤素原子或C 1-6烷氧基及其药学上可接受的盐和溶剂化物。

5. 发明申请

WO9501170A3 USE OF PHENETHANOLAMINE DERIVATIVES IN THE TREATMENT OF GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：苯乙醇胺衍生物在治疗胃肠疾病中的应用
公开(公告)号：WO9501170A3
公开(公告)日：2002-02-14
申请号：PCT/EP9402106
申请日：1994-06-29
申请人： GLAXO GROUP LTD , STORER RICHARD , FOXTON MICHAEL WALTER , HARTLEY CHARLES DAVID , GREEN RICHARD HOWARD , TRAVERS STUART
发明人： STORER RICHARD , FOXTON MICHAEL WALTER , HARTLEY CHARLES DAVID , GREEN RICHARD HOWARD , TRAVERS STUART
IPC分类号： A61K45/06 , A61K31/135 , A61K31/195 , A61P1/00 , A61P1/04 , A61P29/00 , A61K31/165
CPC分类号： A61K31/195 , A61K31/135
摘要： The use of compounds of formula (I) in which: R is hydrogen, methyl or hydroxymethyl; R is substituted alkyl; R and R are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl group, or substituted alkyl; X is oxygen or sulphur; and Ar is optionally substituted phenyl or naphtyl; and pharmaceutically acceptable salts thereof in the treatment of gastrointestinal disorders is described.
摘要翻译：式（I）化合物的用途，其中：R 0是氢，甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自为氢，卤素，羟基，烷氧基，羧基，烷氧基羰基，烷基，硝基，卤代烷基或取代的烷基; X是氧或硫; 和Ar是任选取代的苯基或萘基; 和其药学上可接受的盐在治疗胃肠道疾病中的用途。

6. 发明申请

WO1995033724A1 PHENETHANOLAMINE DERIVATIVES AND THEIR USE AS ATYPICAL BETA-ADRENOCEPTOR AGONISTS 审中-公开
标题翻译：苯乙醇胺衍生物及其作为原位β-受体激动剂的用途
公开(公告)号：WO1995033724A1
公开(公告)日：1995-12-14
申请号：PCT/EP1995002133
申请日：1995-06-06
申请人： GLAXO GROUP LIMITED , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07C229/42 , C07C2601/02 , C07D231/38 , C07D277/42 , C07D317/68
摘要： The present invention relates to phenethanolamine derivatives of formula (I), wherein: R represents an aryl group optionally substituted by one or more substituents selected from halo, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents H or C1-6alkyl; R represents a phenyl or heteroaryl group substituted by R and R ; R and R each independently represent H or C1-6alkyl or, R and R together form a C3-6cycloalkyl group; R represents ZCH2CO2H and R represents H or ZCH2CO2H, or R and R together represent a group (a), wherein each Z may be the same or different and is selected from a bond, CH2, O, S or NR , R is H or CO2H and R is H or C1-6alkyl; X represents(CH2)n where n is 1 or 2; and pharmaceutically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中：R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基; R 2表示H或C 1-6烷基; R 3表示被R 6和R 7取代的苯基或杂芳基; R 4和R 5各自独立地表示H或C 1-6烷基，或者R 4和R 5一起形成C 3-6环烷基; R 6表示ZCH 2 CO 2 H，R 7表示H或ZCH 2 CO 2 H，或R 6和R 7一起表示基团（a），其中每个Z可以相同或不同，并且选自键， CH 2，O，S或NR 9，R 8是H或CO 2 H，R 9是H或C 1-6烷基; X表示（CH 2）n，其中n为1或2; 及其药学上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

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