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11. 发明申请

WO2016033460A1 PROBES FOR IMAGING HUNTINGTIN PROTEIN 审中-公开
标题翻译：用于成像蛋白质的探针
公开(公告)号：WO2016033460A1
公开(公告)日：2016-03-03
申请号：PCT/US2015/047427
申请日：2015-08-28
申请人： CHDI FOUNDATION, INC. , DOMINGUEZ, Celia , WITYAK, John , BARD, Jonathan , BROWN, Christopher, John , PRIME, Michael, Edward , WEDDELL, Derek, Alexander , WALTER, Daryl, Simon , GILES, Paul, Richard , WIGGINTON, Ian, James , TAYLOR, Malcolm, George , GALAN, Sébastien, René, Gabriel , JOHNSON, Peter, David , KRÜLLE, Thomas, Martin , MORAO, Inaki , CLARK-FREW, Daniel , SCHAERTL, Sabine , HERRMANN, Frank , GRIMM, Steffen, Kaspar , KAHMANN, Jan, Dirk , SCHEICH, Christoph
发明人： DOMINGUEZ, Celia , WITYAK, John , BARD, Jonathan , BROWN, Christopher, John , PRIME, Michael, Edward , WEDDELL, Derek, Alexander , WALTER, Daryl, Simon , GILES, Paul, Richard , WIGGINTON, Ian, James , TAYLOR, Malcolm, George , GALAN, Sébastien, René, Gabriel , JOHNSON, Peter, David , KRÜLLE, Thomas, Martin , MORAO, Inaki , CLARK-FREW, Daniel , SCHAERTL, Sabine , HERRMANN, Frank , GRIMM, Steffen, Kaspar , KAHMANN, Jan, Dirk , SCHEICH, Christoph
IPC分类号： A01N43/42
CPC分类号： C12Q1/6823 , A61K51/0419 , A61K51/0453 , A61K51/0455 , C07D253/08 , C07D401/04 , C07D473/00
摘要： Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.
摘要翻译：提供了包含式（I）化合物或其药学上可接受的盐的成像剂及其使用方法。

12. 发明申请

WO2009077362A1 ISOTHIAZOLIDINE 1,1-DIOXIDE AND TETRAHYDRO-2H-1,2-THIAZINE 1,1-DIOXIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的异噻唑烷1,1-二氧化物和四氢-2H- 2H-1,2-噻唑烷-1,1-二氧化物衍生物
公开(公告)号：WO2009077362A1
公开(公告)日：2009-06-25
申请号：PCT/EP2008/066945
申请日：2008-12-05
申请人： GLAXO GROUP LIMITED , WALTER, Daryl Simon
发明人： WALTER, Daryl Simon
IPC分类号： C07D275/02 , C07D279/02 , A61K31/41 , A61K31/54
CPC分类号： C07D275/03 , C07D279/02
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof:(formula) wherein: R 1 represents optionally substituted C 1-4 alkyl; X represents -(CR 10 R 11 ) n - in which n represents 1 or 2; R 2 , R 3 and R 4 independently represent H, F or Me; and R 5 , R 6 ; R 7 ; R 8 and R 9 independently represent hydrogen, halogen, or cyano; or optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkyl, such that at least one of R 5 and R 9 represents a group other than hydrogen. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prevention of inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐：（式）其中：R 1表示任选取代的C 1-4烷基; X表示 - （CR10R11）n-，其中n表示1或2; R2，R3和R4独立地表示H，F或Me; 和R5，R6; R7; R8和R9独立地表示氢，卤素或氰基; 或任选取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或C 3-6环烷基，使得R 5和R 9中的至少一个表示除氢以外的基团。认为化合物或盐可以调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。本发明还提供了化合物或盐在治疗或预防炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎或骨关节炎中的用途。

13. 发明申请

WO2009074519A1 COMBINATIONS OF PYRAZOLYL OR ISOXAZOLYL P2X7 MODULATORS WITH FURTHER THERAPEUTIC AGENTS 审中-公开
标题翻译：吡唑啉或异辛唑P2X7调节剂与其他治疗剂的组合
公开(公告)号：WO2009074519A1
公开(公告)日：2009-06-18
申请号：PCT/EP2008/066891
申请日：2008-12-05
申请人： GLAXO GROUP LIMITED , MICHEL, Anton Duval , WALTER, Daryl Simon
发明人： MICHEL, Anton Duval , WALTER, Daryl Simon
IPC分类号： A61K31/415 , A61K31/42 , A61P29/00 , A61P25/28 , A61P11/00 , A61P9/00
CPC分类号： A61K31/415 , A61K31/42 , A61K31/635 , A61K2300/00
摘要： The present invention relates to combination comprising a compound of formula (I) or (IA) or a pharmaceutically acceptable salt thereof: together with a further therapeutic agent or agents. The pyrazolyl (I) and isoxazolyl (IA) compounds of formula (I) and (IA) are thought to be P2X7 receptor antagonists, i.e. to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The further therapeutic agent can e.g. be methotrexate, an NSAID, a TNFα inhibitor, sulfasalazine, a statin, or an anti-CD20 monoclonal antibody, e.g. for the treatment of rheumatoid arthritis; or can be e.g. paracetamol, an opioid, pregabalin, gabapentin, gabapentin enacarbil, or carbamazepine, e.g. for inflammatory or neuropathic pain.
摘要翻译：本发明涉及包含式（I）或（IA）化合物或其药学上可接受的盐的组合，以及另外的治疗剂或药剂。认为式（I）和（IA）的吡唑基（I）和异恶唑基（IA）化合物是P2X7受体拮抗剂，即调节P2X7受体功能并能够拮抗ATP在P2X7受体上的作用。另外的治疗剂可以例如甲氨蝶呤，NSAID，TNFa抑制剂，柳氮磺吡啶，他汀类或抗CD20单克隆抗体，例如，用于治疗类风湿关节炎; 或者可以是例如对乙酰氨基酚，阿片样物质，普瑞巴林，加巴喷丁，加巴喷丁恩卡巴尔或卡马西平，如卡马西平。用于炎性或神经性疼痛。

14. 发明申请

WO2007141267A1 N- (PHENYLMETHYL) -2- (1H-PYRAZ0L-4-YL) ACETAMIDE DERIVATIVES AS P2X7 ANTAGONISTS FOR THE TREATMENT OF PAIN, INFLAMMATION AND NEURODEGENERATION 审中-公开
标题翻译： N-（苯基甲基）-2-（1H-吡唑-4-基）乙酰胺衍生物作为治疗疼痛，炎症和神经细胞增生的P2X7拮抗剂
公开(公告)号：WO2007141267A1
公开(公告)日：2007-12-13
申请号：PCT/EP2007/055518
申请日：2007-06-05
申请人： GLAXO GROUP LIMITED , BESWICK, Paul, John , CHAMBERS, Laura, J. , DAVIES, David, John , DEAN, David, Kenneth , DEMONT, Emmanuel, Hubert , ROOMANS, Susan , WALTER, Daryl, Simon
发明人： BESWICK, Paul, John , CHAMBERS, Laura, J. , DAVIES, David, John , DEAN, David, Kenneth , DEMONT, Emmanuel, Hubert , ROOMANS, Susan , WALTER, Daryl, Simon
IPC分类号： A61K31/415 , A61P25/04 , A61P25/28
CPC分类号： C07D231/12
摘要： The present invention relates to novel pyrazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor, and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
摘要翻译：本发明涉及结合P2X7受体并能够干扰ATP在P2X7受体上的作用的式（I）的吡唑衍生物，以及这些化合物或其药物组合物在治疗疾病介导中的用途通过P2X7受体，例如疼痛，炎症和神经变性。

15. 发明申请

WO2006040151A8 SUBSITUTED HYDROXYETHYLAMINE COMPOUNDS FOR TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的羟基乙酰胺化合物
公开(公告)号：WO2006040151A8
公开(公告)日：2006-09-14
申请号：PCT/EP2005011004
申请日：2005-10-11
申请人： GLAXO GROUP LTD , DEMONT EMMANUEL HUBERT , REDSHAW SALLY , WALTER DARYL SIMON
发明人： DEMONT EMMANUEL HUBERT , REDSHAW SALLY , WALTER DARYL SIMON
IPC分类号： C07D513/06 , A61K31/554 , A61P25/28
CPC分类号： C07D513/06
摘要： The present invention relates to novel hydroxyethylamine compounds of formula (1) wherein, inter alia, A-B represents -NR 5 -SO 2 -;-W-represents -(CH 2 ) 3 - or -C(H)=C(H)-CH 2 -; X-Y-Z represents -C=CR 8 -NR 9 -, having Asp2 (ß-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ß- amyloid levels or ß-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及式（1）的新型羟乙胺化合物，其中特别地，AB表示-NR 5 -SO 2 - ; -W-表示 - （CH 3） 3 - 或 - C（H）= C（H）-CH 2 - ; XYZ表示具有Asp2（ß-分泌酶，BACE1或Memapsin-2）抑制活性的药物，其制备方法，含有它们用于治疗以β-淀粉样蛋白水平升高或β-淀粉样蛋白沉积物为特征的疾病，特别是阿尔茨海默氏病。

16. 发明申请

WO2006040149A1 HETEROCYCLIC KETOE COMPOUNDS FOR TREATING ALZHEIMER’S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的杂环酮类化合物
公开(公告)号：WO2006040149A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/011002
申请日：2005-10-11
申请人： GLAXO GROUP LIMITED , DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
发明人： DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
IPC分类号： C07D513/06 , A61P25/28 , A61K31/554
CPC分类号： C07D513/06
摘要： The present invention relates to novel ketone compounds' of formula (I) wherein, inter alla, A-B represents -NR 5 p ' SO 2 -; -W- represents -CH 2 -, -(CH 2 ) 2 -, -(CH 2 ) 3 - or -C(H)=C(H)-; X-Y-Z represents -C=CR 8 -NR 9 -, having Asp2 (ß-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to -compositions containing them and to their use in the treatment of diseases characterised by elevated ß- amyloid levels or ß-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及式（I）的新型酮化合物，其中，全部A-B表示-NR

17. 发明申请

WO2010125103A1 DIKETOPIPERAZINE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译： DIKETOPIPERAZINE衍生物作为P2X7调节剂
公开(公告)号：WO2010125103A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055716
申请日：2010-04-28
申请人： GLAXO GROUP LIMITED , CHAMBERS, Laura Jane , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
发明人： CHAMBERS, Laura Jane , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
IPC分类号： C07D241/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D413/04 , A61K31/4965 , A61K31/497 , A61P25/28 , A61P25/08 , A61P29/00
CPC分类号： C07D241/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D413/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein: A represents an aryl, heteroaryl or heterocyclyl group; and any ring or ring system of said aryl or heteroaryl is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C 1-6 alkyl, -CF 3 , - OCF 3 , cyano, C 1-6 alkoxy, -NR 10 R 11 , -X-aryl, -X-heteroaryl and -X-heterocyclyl; R 1 , R 2 , R 3 , R 4 and R 5 independently represent hydrogen, fluorine, chlorine, -CF 3 , cyano or C 1-6 alkyl, such that at least one of R 1 , R 2 , R 3 , R 4 and R 5 is other than hydrogen; R 6 , R 7 , R 8 , R 9 , R 10 and R 11 independently represent hydrogen or C 1-6 alkyl; X represents a linker selected from a bond, -(CH 2 ) n - and -O-(CH 2 ) n -; and n represents an integer from 1 to 3. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor ("P2X7 receptor antagonists").
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐：（I）其中：A表示芳基，杂芳基或杂环基; 并且所述芳基或杂芳基的任何环或环系统任选地被1至3个可以相同或不同的取代基取代，所述取代基可以选自卤素，C 1-6烷基，-CF 3，-OCF 3，氰基，C 1 -6-烷氧基，-NR10R11，-X-芳基，-X-杂芳基和-X-杂环基; R 1，R 2，R 3，R 4和R 5独立地表示氢，氟，氯，-CF 3，氰基或C 1-6烷基，使得R 1，R 2，R 3，R 4和R 5中的至少一个不是氢; R6，R7，R8，R9，R10和R11独立地表示氢或C1-6烷基; X表示选自键， - （CH 2）n - 和-O-（CH 2）n - 的连接体; 并且n表示1至3的整数。化合物或盐调节P2X7受体功能并且能够拮抗ATP在P2X7受体（“P2X7受体拮抗剂”）的作用。

18. 发明申请

WO2009077559A2 5-OXO-3-PYRROLIDINECARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的5-氧代-3-吡咯烷酮甲酰胺衍生物
公开(公告)号：WO2009077559A2
公开(公告)日：2009-06-25
申请号：PCT/EP2008/067733
申请日：2008-12-17
申请人： GLAXO GROUP LIMITED , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
发明人： STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
IPC分类号： A61K31/4015 , A61P25/00 , A61P29/00
CPC分类号： A61K31/4015
摘要： The present invention provides a compound of formula (IA) or a pharmaceutically acceptable salt thereof: wherein: R 1 represents C 1-4 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 3-6 cycloalkylmethyl-, phenyl-X- or heteroaryl, any of which may be optionally substituted; X represents -(CR 12 R 13 ) n -; n represents 0 to 2; and R 7 , R 8 , R 9 , R 10 and R 11 independently represent H, halogen, or cyano; or optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkyl; such that at least two of R 7 , R 8 , R 9 , R 10 and R 11 represent a group other than H and at least one of R 7 and R 11 represents a group other than H; and wherein the compound is other than N -[(2,4-dichlorophenyl)methyl]-5-oxo-1-(phenylmethyl)-3-pyrrolidinecarboxamide. The compounds and salts are thought to modulate P2X7 receptor function and be capable of antagonizing the effects of ATP at the P2X7 receptor.
摘要翻译：本发明提供式（IA）化合物或其药学上可接受的盐：其中：R 1表示C 1-4烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，C 3-6环烷基甲基 - ，苯基 - X-或杂芳基，其中任何一个可以任选被取代; X表示 - （CR12R13）n-; n表示0〜2; 且R 7，R 8，R 9，R 10和R 11独立地表示H，卤素或氰基; 或任选取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或C 3-6环烷基; 使得R 7，R 8，R 9，R 10和R 11中的至少两个表示除H以外的基团，并且R 7和R 11中的至少一个表示除H以外的基团; 并且其中所述化合物不是N - [（2,4-二氯苯基）甲基] -5-氧代-1-（苯甲基）-3-吡咯烷甲酰胺。化合物和盐被认为调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。

19. 发明申请

WO2008119825A2 IMIDAZOLIDINE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：咪唑啉酰胺衍生物作为P2X7调节剂
公开(公告)号：WO2008119825A2
公开(公告)日：2008-10-09
申请号：PCT/EP2008053962
申请日：2008-04-02
申请人： GLAXO GROUP LTD , BESWICK PAUL JOHN , DEAN DAVID KENNETH , GLEAVE ROBERT JAMES , MOSES ANDREW PETER , WALTER DARYL SIMON
发明人： BESWICK PAUL JOHN , DEAN DAVID KENNETH , GLEAVE ROBERT JAMES , MOSES ANDREW PETER , WALTER DARYL SIMON
IPC分类号： C07D233/36 , A61K31/4166 , A61P29/00 , C07D401/04 , C07D401/06 , C07D403/04
CPC分类号： C07D233/36 , C07D401/04 , C07D401/06 , C07D403/04
摘要： The present invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders / diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：该化合物或盐调节P2X7受体功能并且能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症/疾病中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛，神经性疼痛或内脏痛。

20. 发明申请

WO2008119685A3 OXAZOLIDINE AND MORPHOLINE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
公开(公告)号：WO2008119685A3
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053431
申请日：2008-03-20
申请人： GLAXO GROUP LIMITED , BESWICK, Paul, John , WALTER, Daryl, Simon
发明人： BESWICK, Paul, John , WALTER, Daryl, Simon
IPC分类号： C07D263/24 , C07D265/32 , A61P29/00
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

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