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1. 发明专利

IL180680D0 PIPERAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS 未知
公开(公告)号：IL180680D0
公开(公告)日：2007-06-03
申请号：IL18068007
申请日：2007-01-11
申请人： GLAXO GROUP LTD , GAIBA ALESSANDRA , KING NIGEL PAUL , TAKLE ANDREW KENNETH , WITHERINGTON JASON , DEAN DAVID KENNETH
IPC分类号： C07D20100101
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.

2. 发明申请

WO2010125102A1 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译： 5,6,7,8-四氢[1,2,4]三唑[4,3-a]吡嗪衍生物作为P2X7调节剂
公开(公告)号：WO2010125102A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055715
申请日：2010-04-28
申请人： GLAXO GROUP LIMITED , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALTER, Daryl Simon
发明人： DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALTER, Daryl Simon
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein A is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 1-3 alkoxy, C 1-3 alkoxy C 1-4 alkyl, C 1-2 fluoroalkyl, halogen, NR 6 R 7 , optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined in the description. 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 prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
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A为氢，C 1-4烷基，C 3-6环烷基，C 1-3烷氧基，C 1-3烷氧基C 1-4烷基，C 1-10 - 烷基，卤素，NR 6 R 7，任选取代的杂芳基（Het）或任选取代的苯基，并且R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。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例如炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎，骨关节炎或神经变性疾病中的用途。

3. 发明申请

WO2010125101A1 5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的5,6,7,8-四氢吡啶并[1,2-A]吡嗪衍生物
公开(公告)号：WO2010125101A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055714
申请日：2010-04-28
申请人： GLAXO GROUP LIMITED , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALL, Ian David , WALTER, Daryl Simon
发明人： DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALL, Ian David , WALTER, Daryl Simon
IPC分类号： C07D487/04 , A61P29/00 , A61K31/4985
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 1-3 alkoxy, C 1-3 alkoxy C 1-4 alkyl, C 1-2 fluoroalkyl, halogen, NR 6 R 7 optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined in the description. 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 prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.
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A为氢，C 1-4烷基，C 3-6环烷基，C 1-3烷氧基，C 1-3烷氧基C 1-4烷基，C 1-2 - 氟烷基，卤素，NR 6 R 7 取代的杂芳基（Het）或任选取代的苯基，并且R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。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例如炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎或骨关节炎或神经变性疾病中的用途。

4. 发明申请

WO2008125600A3 PYRAZOLE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的吡唑衍生物
公开(公告)号：WO2008125600A3
公开(公告)日：2009-01-22
申请号：PCT/EP2008054382
申请日：2008-04-10
申请人： GLAXO GROUP LTD , BESWICK PAUL JOHN , DEAN DAVID KENNETH , WALTER DARYL SIMON
发明人： BESWICK PAUL JOHN , DEAN DAVID KENNETH , WALTER DARYL SIMON
IPC分类号： C07D231/12 , A61K31/415 , A61P25/00 , A61P29/00 , C07D231/16
CPC分类号： C07D231/16 , C07D231/12
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 represents C1-6 alkyl or C3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 halogen atoms; and R2 represents hydrogen, halogen, C1-6 alkyl or C3-6 cycloalkyl; and either of said C1-6 alkyl or C3-6 cycloalkyl is optionally substituted with 1, 2 or 3 halogen atoms. The pyrazole compounds of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to 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.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：（I）其中R 1表示C 1-6烷基或C 3-6环烷基，其任一个任选被1,2或3个卤素原子取代; 并且R 2表示氢，卤素，C 1-6烷基或C 3-6环烷基; 并且所述C 1-6烷基或C 3-6环烷基中的任一个任选被1,2或3个卤素原子取代。式（I）的吡唑化合物或其盐调节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。本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

5. 发明申请

WO2008125600A2 PYRAZOLE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的吡唑衍生物
公开(公告)号：WO2008125600A2
公开(公告)日：2008-10-23
申请号：PCT/EP2008/054382
申请日：2008-04-10
申请人： GLAXO GROUP LIMITED , BESWICK, Paul, John , DEAN, David, Kenneth , WALTER, Daryl, Simon
发明人： BESWICK, Paul, John , DEAN, David, Kenneth , WALTER, Daryl, Simon
IPC分类号： C07D231/12 , C07D231/16 , A61K31/415 , A61P25/00 , A61P29/00
CPC分类号： C07D231/16 , C07D231/12
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R 1 represents C 1-6 alkyl or C 3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 halogen atoms; and R 2 represents hydrogen, halogen, C 1-6 alkyl or C 3-6 cycloalkyl; and either of said C 1-6 alkyl or C 3-6 cycloalkyl is optionally substituted with 1, 2 or 3 halogen atoms. The pyrazole compounds of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to 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.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：（I）其中R 1表示C 1-6烷基或C 1 -C 6烷基， 3-6个环烷基，其任一个任选被1,2或3个卤素原子取代; R 2表示氢，卤素，C 1-6烷基或C 3-6环烷基; 并且所述C 1-6烷基或C 3-6环烷基中的任一个任选被1,2或3个卤素原子取代。式（I）的吡唑化合物或其盐调节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。本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

6. 发明申请

WO2008119825A3 IMIDAZOLIDINE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
公开(公告)号：WO2008119825A3
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053962
申请日：2008-04-02
申请人： GLAXO GROUP LIMITED , 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 , C07D401/04 , C07D401/06 , C07D403/04 , A61K31/4166 , 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 (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.

7. 发明申请

WO2006125665A1 SUBSTITUTED PIPERIDINE ANTAGONIST OF HI RECEPTOR TO BE USED FOR THE TREATMENT OF RHINITIS 审中-公开
标题翻译：用于治疗RHINITI的HI受体的替代哌啶拮抗剂
公开(公告)号：WO2006125665A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/005053
申请日：2006-05-23
申请人： GLAXO GROUP LIMITED , BAMFORD, Mark, James , DEAN, David, Kenneth , HANCOCK, Ashley, Paul , WILSON, David, Matthew
发明人： BAMFORD, Mark, James , DEAN, David, Kenneth , HANCOCK, Ashley, Paul , WILSON, David, Matthew
IPC分类号： C07D401/14 , A61K31/435 , A61P37/00 , A61P29/00
CPC分类号： C07D211/46 , C07D401/14
摘要： The present invention relates to the compound, (I) and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various disorders, such as allergic rhinitis.
摘要翻译：本发明涉及化合物（I）及其盐，其制备方法，含有它的组合物及其在治疗各种疾病如过敏性鼻炎中的用途。

8. 发明申请

WO2003022840A1 PYRIDINE DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：吡啶衍生物作为RAF激酶抑制剂
公开(公告)号：WO2003022840A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009946
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM PLC , BAMFORD, Mark, James , DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： BAMFORD, Mark, James , DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D405/14
CPC分类号： C07D405/04 , C07D405/14
摘要： Compounds (I) and their use as pharmaceuticals particularly as Raf Kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要翻译：化合物（I）及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。

9. 发明申请

WO2003022832A1 PYRIDYLFURANS AND PYRROLES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：吡咯烷酮和吡咯烷酮作为RAF激酶抑制剂
公开(公告)号：WO2003022832A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009943
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM p.l.c. , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , A61K31/44 , A61K31/505 , C07D405/04
摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要翻译：化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。

10. 发明申请

WO2002094808A1 IMIDAZOLE-2-CARBOXAMIDE DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：咪唑-2-羧酰胺衍生物作为RAF激酶抑制剂
公开(公告)号：WO2002094808A1
公开(公告)日：2002-11-28
申请号：PCT/GB2002/002353
申请日：2002-05-20
申请人： SMITHKLINE BEECHAM P.L.C. , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of formula (I): wherein X is O, CH 2 , S or NH, or the moiety X-R 1 is hydrogen; Y 1 and Y 2 independently represent CH or N; R 1 is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, arylC 1-6 alkyl, heterocyclyl, heterocyclylC 1-6 alkyl, heteroaryl, or heteroarylC 1-6 alkyl, any of which except hydrogen may be optionally substituted; R 2 and R 3 independently represent hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, arylC 1-6 alkyl, heteroaryl, heteroarylC 1-6 alkyl, heterocyclyl, or heterocyclylC 1-6 alkyl, or R 2 and R 3 together with the nitrogen atom to which they are attached form a 4- to 10-membered monocyclic or bicyclic ring; Ar is a group of the formula a) or b), wherein A represents a fused 5- to 7-membered ring optionally containing up to two heteroatoms selected from O, S and NR 5 , wherein R 5 is hydrogen or C 1-6 alkyl, which ring is optionally substituted by up to 2 substituents selected from halogen, C 1-6 alkyl, hydroxy, C 1-6 alkoxy or keto ; R a and R 4 are independently selected from hydrogen, halogen, C 1-6 alkyl, aryl, arylC 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, haloC 1-6 alkyl, arylC 1-6 alkoxy, hydroxy, nitro, cyano, azido, amino, mono- and di- N -)C 1-6 alkylamino, acylamino, arylcarbonylamino, acyloxy, carboxy, carboxy salts, carboxy esters, carbamoyl, mono- and di- N -C 1-6 alkylcarbamoyl, C 1-6 alkoxycarbonyl,aryloxycarbonyl, ureido, guanidino, C 1-6 alkylguanidino, amidino, C 1-6 alkylamidino, sulphonylamino, aminosulphonyl, C 1-6 alkylthio, C 1-6 alkyl sulphinyl or C 1-6 alkylsulphonyl; and one of X 1 and X 2 is N and the other is NR 6 , wherein R 6 is hydrogen, C 1-6 alkyl, or arylC 1-6 alkyl; or pharmaceutically acceptable salts thereof.
摘要翻译：式（I）化合物：其中X是O，CH 2，S或NH，或X-R 1部分是氢; Y1和Y2独立地表示CH或N; R 1是氢，C 1-6烷基，C 3-7环烷基，芳基，芳基C 1-6烷基，杂环基，杂环基C 1-6烷基，杂芳基或杂芳基C 1-6烷基，除氢之外的任何一个可以是任选取代的; R 2和R 3独立地表示氢，C 1-6烷基，C 3-7环烷基，芳基，芳基C 1-6烷基，杂芳基，杂芳基C 1-6烷基，杂环基或杂环基C 1-6烷基，或R 2和R 3 与它们所连接的氮原子一起形成4-至10-元单环或双环; Ar是式a）或b）的基团，其中A表示稠合的5-至7-元环，任选地含有至多两个选自O，S和NR 5的杂原子，其中R 5是氢或 C 1-6烷基，该环任选被至多2个选自卤素，C 1-6烷基，羟基，C 1-6烷氧基或酮的取代基取代; R a和R 4独立地选自氢，卤素，C 1-6烷基，芳基，芳基C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，卤代C 1-6烷基，芳基C 1-6烷氧基，羟基，硝基，氰基，叠氮基，氨基，单 - 和二 - N - C 1-6烷基氨基，酰氨基，芳基羰基氨基，酰氧基，羧基，羧基盐，羧基酯，氨基甲酰基，单 - 和二 - C 1-6烷基氨基甲酰基，C 1-6烷氧基羰基，芳氧基羰基，脲基，胍基，C 1-6烷基胍基，脒基，C 1-6烷基脒基，磺酰基氨基，氨基磺酰基，C 1-6烷硫基，C 1-6烷基亚磺酰基或C 1-6烷基磺酰基; X 1和X 2之一是N，另一个是NR 6，其中R 6是氢，C 1-6烷基或芳基C 1-6烷基; 或其药学上可接受的盐。

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