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1. 发明申请

WO2007113202A1 PIPERAZINE DERIVATIVES AS GROWTH HORMONE SECRETAGOGUE (GHS) RECEPTOR AGONISTS 审中-公开
标题翻译：哌嗪衍生物作为生长激素释放因子（GHS）受体激动剂
公开(公告)号：WO2007113202A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053018
申请日：2007-03-29
申请人： GLAXO GROUP LIMITED , BLANEY, Emma, Louise , KING, Nigel, Paul , WITHERINGTON, Jason
发明人： BLANEY, Emma, Louise , KING, Nigel, Paul , WITHERINGTON, Jason
IPC分类号： C07D213/76 , C07D405/12 , C07D409/12 , A61K31/496 , A61K31/506 , A61P1/00
CPC分类号： C07D405/12 , C07D213/76 , C07D409/12
摘要： The present invention relates to compounds of formula (I), processes for their preparation, pharmaceutical compositions containing the same and to their use in the treatment of gastrointestinal and other disorders.
摘要翻译：本发明涉及式（I）化合物，其制备方法，含有该化合物的药物组合物及其在治疗胃肠道和其它疾病中的用途。

2. 发明申请

WO2007118852A1 ARYL AND HETEROARYL SULPHONAMIDES AS GROWTH HORMONE SECRETAGOGUE RECEPTOR AGONISTS 审中-公开
标题翻译： ARYL和HETEROARYL SULPHONAMIDES作为生长激素秘密吸收激素
公开(公告)号：WO2007118852A1
公开(公告)日：2007-10-25
申请号：PCT/EP2007/053619
申请日：2007-04-13
申请人： GLAXO GROUP LIMITED , WITHERINGTON, Jason , BLANEY, Emma, Louise , DEAN, David, Kenneth , GAIBA, Alessandra , KING, Nigel, Paul
发明人： BLANEY, Emma, Louise , DEAN, David, Kenneth , GAIBA, Alessandra , KING, Nigel, Paul
IPC分类号： C07C311/29 , C07D307/38 , C07D333/18 , C07D405/12 , A61K31/18 , A61P19/10
CPC分类号： C07C311/29 , C07D307/38 , C07D333/18 , C07D405/12
摘要： The present invention therefore provides compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) processes for their preparation, pharmaceutical compositions containing the same and to their use in the treatment of gastrointestinal and other disorders.
摘要翻译：因此，本发明提供式（I）化合物或其药学上可接受的盐：（I）其制备方法，含有该化合物的药物组合物及其在治疗胃肠道和其它疾病中的用途。

3. 发明申请

WO2006010629A1 PIPERAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：用于治疗胃肠疾病的哌哌啶衍生物
公开(公告)号：WO2006010629A1
公开(公告)日：2006-02-02
申请号：PCT/EP2005/008263
申请日：2005-07-26
申请人： GLAXO GROUP LIMITED , GAIBA, Alessandra , KING, Nigel, Paul , TAKLE, Andrew, Kenneth , WITHERINGTON, Jason
发明人： GAIBA, Alessandra , KING, Nigel, Paul , TAKLE, Andrew, Kenneth , WITHERINGTON, Jason
IPC分类号： C07D409/04
CPC分类号： C07D295/135 , C07D207/27 , C07D215/36 , C07D231/12 , C07D261/10 , C07D263/32 , C07D265/28 , C07D271/12 , C07D307/10 , C07D333/08 , C07D333/62 , C07D409/04 , C07D409/14 , C07D413/04 , C07D495/04
摘要： The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R a , R b , R c , R d , R e , R f and Y are as defined in the specification. The compounds are partial or full agonists at the growth hormone secretagogue (GHS) receptors . Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R

4. 发明申请

WO2003053925A1 PYRROLIDINE-2-ONES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：吡咯烷-2-酮作为因子XA抑制剂
公开(公告)号：WO2003053925A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014826
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , CHAN, Chuen , KELLY, Henry, Anderson , KING, Nigel, Paul , KLEANTHOUS, Savvas , MASON, Andrew, McMurtrie , PINTO, Ivan, Leo , POLLARD, Derek, Roland , SENGER, Stefan , SHAH, Gita, Punjabhai , WATSON, Nigel, Stephen , YOUNG, Robert, John
发明人： BORTHWICK, Alan, David , CHAN, Chuen , KELLY, Henry, Anderson , KING, Nigel, Paul , KLEANTHOUS, Savvas , MASON, Andrew, McMurtrie , PINTO, Ivan, Leo , POLLARD, Derek, Roland , SENGER, Stefan , SHAH, Gita, Punjabhai , WATSON, Nigel, Stephen , YOUNG, Robert, John
IPC分类号： C07D207/273
CPC分类号： C07D207/273 , C07D401/12 , C07D403/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D417/04
摘要： The invention relates to compounds of formula (I): , and pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（I）化合物：及其药学上可接受的衍生物。本发明还涉及制备式（I）化合物的方法，包含式（I）化合物的药物组合物和式（I）化合物在医药中的用途，特别是在改善临床病症方面指示因子Xa抑制剂。

5. 发明申请

WO2003043981A1 2-(3-SULFONYLAMINO-2-OXOPYRROLIDIN-1-YL)PROPANAMIDES AS FACTOR XA INHIBITORS 审中-公开
标题翻译： 2-（3-磺酰氨基-2-氧代吡咯烷-1-基）丙酰胺作为因子XA抑制剂
公开(公告)号：WO2003043981A1
公开(公告)日：2003-05-30
申请号：PCT/GB2002/005134
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , CAMPBELL, Matthew , CHAN, Chuen , KELLY, Henry, Anderson , KING, Nigel, Paul , KLEANTHOUS, Savvas , MASON, Andrew, McMurtrie , SENGER, Stefan , SMITH, Paul, William , WATSON, Nigel, Stephen , YOUNG, Robert, John
发明人： BORTHWICK, Alan, David , CAMPBELL, Matthew , CHAN, Chuen , KELLY, Henry, Anderson , KING, Nigel, Paul , KLEANTHOUS, Savvas , MASON, Andrew, McMurtrie , SENGER, Stefan , SMITH, Paul, William , WATSON, Nigel, Stephen , YOUNG, Robert, John
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The invention relates to compounds of formula (I), wherein: R 1 represents hydrogen or -C 1-3 alkylCONR a R b ; One of R 2 and R 3 represents -C 1-3 alkyl and the other represents hydrogen; R 4 represents hydrogen, -C 1-4 alkyl, -C 3-4 alkenyl, -C 2-4 alkylOH, -C 2-4 alkylOC 1-4 alkyl, -C 1-4 alkylCN or -C 0-4 alkylC 3-6 cycloalkyl; R 5 represents -C 2-4 alkylOH, -C 1-4 alkyl, -C 2-4 alkylOC 1-4 alkyl, -C 1-4 alkylCN, -C 1-4 alkylCONR c R d , -C 2-4 alkylNR a R b , -C 2-4 alkylNHCOC 1-3 alkyl, -C 2-4 alkylNHCONR a R b , -C2-4alkylNHSO 2 R e , -C 2-4 alkylSO 2 NR a R b , -C 2-4 alkylNHCO 2 C 1-4 alkyl, -C 2-4 alkylNHC(NH 2 )=NR f , or a group X-Y; X represents -C 1-4 alkylene- optionally substitued by -OH, or a direct link, with the proviso that when X is substituted by -OH, X represents C 2-4 alkylene and the -OH group is not alpha with respect to the amide N atom to which the group X is attached; Y represents -C 3-6 cycloalkyl, phenyl, or an aromatic or non-aromatic 5-, 6- or 7-membered heterocyclic group containing at least one heteroatom selected from O, N or S and optionally substituted at C and/or N atoms by -C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylOH, halogen, -CN, -CF 3 , -NH 2 , -CO 2 H and -OH; R a and R b independently represent hydrogen or -C 1-4 alkyl; R c and R d independently represent hydrogen or -C 1-4 alkyl or together with the N atom to which they are attached form a non-aromatic 5-, 6- or 7- membered heterocyclic group optionally substituted by a heteroatom selected from O, N or S; R e represents -C 1-4 alkyl or -CF 3 ; R f represents NO 2 or CN; R 6 represents a group selected from: (i), (ii), (iii), (iv), (v), Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents a heteroatom selected from S or N; and pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（I）化合物，其中：R 1表示氢或-C 1-3烷基CONR a R b; R 2和R 3中的一个表示-C 1-3烷基，另一个表示氢; R 4表示氢，-C 1-4烷基，-C 3-4链烯基，-C 2-4烷基，C 2-4烷基，C 1-4烷基，-C 1-4烷基，或C 0-4烷基。 R 5表示-C 2-4芳烷基，C 1-4烷基，-C 2-4烷基，C 1-4烷基，-C 1-4烷基，C 1-4烷基，C R 6，-C 2-4烷基，NR a R b，，-C2-4烷基NHCOC1-3烷基，-C2-4烷基NHCORRαR2，-C2-4烷基NHSO2R5，-C2-4烷基，SO2NR，R2，-C2-4烷基，NHCO2C1-4烷基， 4烷基NH（NH 2）= NR或基团XY; X代表-C 1-4亚烷基 - 任选被-OH取代或直接连接，条件是当X被-OH取代时，X代表C2-4亚烷基，-OH基团相对于酰胺N原子不是α 组X连接到其上; Y代表-C3-6环烷基，苯基或含有至少一个选自O，N或S的杂原子的芳族或非芳族的5元，6元或7元杂环基，并且任选地在C和/或N原子被C -C 1-3烷基，C 1-3烷氧基，C 1-3烷基OH，卤素，-CN，-CF 3，-NH 2，-CO 2 H和-OH; R a和R b独立地表示氢或-C 1-4烷基; R c和R d独立地表示氢或-C 1-4烷基或与它们所连接的N原子一起形成任选被被选定的杂原子取代的非芳香族5-，6-或7-元杂环基来自O，N或S; R e表示-C 1-4烷基或-CF 3; R表示NO2或CN; R 6表示选自以下的基团：（i），（ii），（iii），（iv），（v），Z表示任选的取代基卤素，alk表示亚烷基或亚烯基，T表示选自S 或N; 及其药学上可接受的衍生物。本发明还涉及制备式（I）化合物的方法，包含式（I）化合物的药物组合物和式（I）化合物在医药中的用途，特别是在改善临床病症方面指示因子Xa抑制剂。

6. 发明申请

WO2009071576A1 5-ARYL-1,3,4-OXADIAZOLE-2-AMINES AS NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS 审中-公开
标题翻译： 5-ARYL-1,3,4-OXADIAZOLE-2-AMINES作为NICOTINIC乙酰胆碱受体激动剂
公开(公告)号：WO2009071576A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066698
申请日：2008-12-03
申请人： GLAXO GROUP LIMITED , HURST, David, Nigel , KING, Nigel, Paul , MAEDA, Yutaka , SCOCCITTI, Tiziana , SKIDMORE, John
发明人： HURST, David, Nigel , KING, Nigel, Paul , MAEDA, Yutaka , SCOCCITTI, Tiziana , SKIDMORE, John
IPC分类号： C07D413/10 , A61P25/00 , A61K31/4245 , C07D413/04
CPC分类号： C07D413/10 , C07D413/04
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders. wherein R 1 and R 2 independently represent hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl; or R 1 and R 2 together with the nitrogen atom to which they are attached form a nitroge containing heterocyclyl group which is unsubstituted or substituted with 1, 2, or 3 substituents selected from methyl or fluoro; Q represents -(CH 2 ) n- wherein n represents 3 or 4; A represents a phenyl ring and B represents a 5 or 6 membered heteroaryl ring or B represents a phenyl ring and A represents a 5 or 6 membered heteroaryl ring; R 3 and R 4 independently represent C 1-6 alkyl, C 1-6 alkoxy and halo; t and m independently represent an integer from 0 to 3. Compounds of formula (I) and their pharmaceutically acceptable salts may have affinity for and be agonists at the nicotinic α7 receptor and are believed to be of potential use in the treatment of neurological diseases including Alzheimer's disease.
摘要翻译：本发明涉及具有药理活性的新型恶二唑衍生物，其制备方法，含有它们的组合物及其在治疗神经，精神病和胃肠道疾病中的用途。其中R1和R2独立地表示氢，C1-6烷基或C3-6环烷基; 或R 1和R 2与它们所连接的氮原子一起形成含有未取代或被1,2或3个选自甲基或氟取代的取代基的杂环基的硝基; Q表示 - （CH2）n-，其中n表示3或4; A表示苯环，B表示5或6元杂芳基环或B表示苯基环，A表示5或6元杂芳基环; R3和R4独立地表示C1-6烷基，C1-6烷氧基和卤素; 式（I）化合物及其药学上可接受的盐可以在尼古丁a7受体上具有亲和力并且是激动剂，并被认为可用于治疗神经疾病，包括阿尔茨海默氏病。

7. 发明申请

WO2009071577A1 OXADIAZOLE DERIVATIVES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS 审中-公开
标题翻译：奥沙利多衍生物及其作为非线性乙酰胆碱受体调节剂
公开(公告)号：WO2009071577A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066699
申请日：2008-12-03
申请人： GLAXO GROUP LIMITED , HURST, David, Nigel , KING, Nigel, Paul , MAK, Sing, Yeung , SCOCCITTI, Tiziana , SKIDMORE, John
发明人： HURST, David, Nigel , KING, Nigel, Paul , MAK, Sing, Yeung , SCOCCITTI, Tiziana , SKIDMORE, John
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/4245 , A61P25/00 , C07D413/04 , C07D417/04 , C07D271/113
CPC分类号： C07D271/113 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Oxadiazole derivatives of formula (I) where ring A is a bicyclic or tricyclic system. Claimed compounds are active on nicotinic acetylcholine receptors (nAChRs), and are useful to treat neurological, psychiatric, and gastrointestinal disorders, as well as sepsis and obesity.
摘要翻译：式（I）的恶二唑衍生物，其中环A是双环或三环体系。声称的化合物对烟碱乙酰胆碱受体（nAChR）有活性，可用于治疗神经系统疾病，精神病学和胃肠道疾病以及败血症和肥胖症。

8. 发明申请

WO2002100830A1 PYRROLIDINE DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为因子XA抑制剂
公开(公告)号：WO2002100830A1
公开(公告)日：2002-12-19
申请号：PCT/GB2002/002721
申请日：2002-06-06
申请人： GLAXO GROUP LIMITED , CHAN, Chuen , HAMBLIN, Julie, Nicole , KELLY, Henry, Anderson , KING, Nigel, Paul , MASON, Andrew, McMurtrie , PATEL, Vipulkumar, Kantibhai , SENGER, Stefan , SHAH, Gita, Punjabhai , WATSON, Nigel, Stephen , WESTON, Helen, Elisabeth , WHITWORTH, Caroline , YOUNG, Robert, John
发明人： CHAN, Chuen , HAMBLIN, Julie, Nicole , KELLY, Henry, Anderson , KING, Nigel, Paul , MASON, Andrew, McMurtrie , PATEL, Vipulkumar, Kantibhai , SENGER, Stefan , SHAH, Gita, Punjabhai , WATSON, Nigel, Stephen , WESTON, Helen, Elisabeth , WHITWORTH, Caroline , YOUNG, Robert, John
IPC分类号： C07D207/26
CPC分类号： C07D413/14 , A61K31/5377 , C07D207/12 , C07D413/06 , C07D417/14 , C07D495/04
摘要： The invention relates to compounds of formula (I) which processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及其制备方法的式（I）化合物，含有它们的药物组合物及其在医药中的用途，特别是用于改善指示因子Xa抑制剂的临床病症。

9. 发明申请

WO2012170752A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2012170752A1
公开(公告)日：2012-12-13
申请号：PCT/US2012/041442
申请日：2012-06-08
申请人： GLAXO WELLCOME MANUFACTURING PTE LTD , CHEN, Deborah, W. , DUNCAN, Sarah , KING, Nigel, Paul , LEE, Kiew, Ching , MAK, Sing, Yeung , RIVERS, Dean, Andrews
发明人： CHEN, Deborah, W. , DUNCAN, Sarah , KING, Nigel, Paul , LEE, Kiew, Ching , MAK, Sing, Yeung , RIVERS, Dean, Andrews
IPC分类号： A01N43/42 , C07D401/00
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
摘要翻译：本发明涉及新型NADPH氧化酶II抑制剂及其在治疗由NADPH氧化酶介导的疾病中的应用。

10. 发明申请

WO2004000315A1 PHENYLALKANOIC ACID AND PHENYLOXYALKANOIC ACID DERIVATIVES AS HPPAR ACTIVATORS 审中-公开
标题翻译：作为HPPAR激活剂的苯甲酸和苯甲酸衍生物
公开(公告)号：WO2004000315A1
公开(公告)日：2003-12-31
申请号：PCT/EP2003/006415
申请日：2003-06-18
申请人： SMITHKLINE BEECHAM CORPORATION , HAMLETT, Christopher, Charles, Frederick , BELL, Richard , BESWICK, Paul, John , GOSMINI, Romain, Luc, Marie , KING, Nigel, Paul , PATEL, Vipulkumar, Kantibhai
发明人： HAMLETT, Christopher, Charles, Frederick , BELL, Richard , BESWICK, Paul, John , GOSMINI, Romain, Luc, Marie , KING, Nigel, Paul , PATEL, Vipulkumar, Kantibhai
IPC分类号： A61K31/44
CPC分类号： C07D213/30 , C07C59/64 , C07C59/68 , C07C323/20 , C07D213/32 , C07D213/34
摘要： The present invention provides a compound of formula (I):wherein:R1 and R2 are independently H or C1-3 alkyl;X represents a O or (CH2)n where n is 0, 1 or 2;R3and R4 independently represent H, C1-3 alkyl, -OCH3, -CF3, allyl, or halogen;X1 represents O, S, SO2, SO, or CH2;R5 and R6 independently represent hydrogen, C1-6 alkyl (including branched alkyl and optionally substituted by one or more halogens or C1-6alkoxy), or together with the carbon atom to which they are bonded form a 3-6 membered cycloalkyl ring;R7 represents a phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 nitrogen atoms wherein the phenyl or heteroaryl group is substituted by 1, 2 or 3 moieties selected from the group consisting of halogen, C1-6 alkoxy, C1-6 alkyl, CF3, hydroxy, or phenyl (which may be optionally substituted by one or more C1-3 alkyl, -OC1-3 alkyl, CN, acetyl, hydroxy, halogen or CF3).
摘要翻译：本发明提供式（I）化合物：其中：R1和R2独立地为H或C1-3烷基; X表示O或（CH2）n，其中n为0,1或2; R3和R4独立地表示H， C 1-3烷基，-OCH 3，-CF 3，烯丙基或卤素; X 1表示O，S，SO 2，SO或CH 2; R 5和R 6独立地表示氢，C 1-6烷基（包括支链烷基，更多的卤素或C 1-6烷氧基），或与它们所键合的碳原子一起形成3-6元环烷基环; R7代表含有1,2或3个氮原子的苯基或6元杂芳基，其中苯基或杂芳基被1,2或3个选自卤素，C 1-6烷氧基，C 1-6烷基，CF 3，羟基或苯基（可以任选被一个或多个C 1-3烷基， -OC1-3烷基，CN，乙酰基，羟基，卤素或CF 3）。

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