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11. 发明申请

WO2011033265A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2011033265A1
公开(公告)日：2011-03-24
申请号：PCT/GB2010/001746
申请日：2010-09-17
申请人： ALMAC DISCOVERY LIMITED , BELL, Mark Peter , O'DOWD, Colin Roderick , ZHANG, Lixin , TEVITT, Graham Peter , HARRISON, Timothy , BATTACHARYYA, Sumita , ROUNTREE, James Samuel Shane , BURKAMP, Frank , PRICE, Stephen , MACLEOD, Calum , ELLIOTT, Richard Leonard , SMITH, Phillip , BLENCH, Toby Jonathan , DYKE, Hazel Joan
发明人： BELL, Mark Peter , O'DOWD, Colin Roderick , ZHANG, Lixin , TEVITT, Graham Peter , HARRISON, Timothy , BATTACHARYYA, Sumita , ROUNTREE, James Samuel Shane , BURKAMP, Frank , PRICE, Stephen , MACLEOD, Calum , ELLIOTT, Richard Leonard , SMITH, Phillip , BLENCH, Toby Jonathan , DYKE, Hazel Joan
IPC分类号： C07D311/26 , C07D407/04 , C07D491/04 , A61K31/353 , A61K31/4155 , A61K31/4162 , A61K31/436 , A61P35/00
CPC分类号： C07D311/26 , C07D407/04 , C07D491/04
摘要： The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
摘要翻译：本发明涉及具有特定活性的一系列化合物作为丝氨酸 - 苏氨酸激酶AKT的抑制剂。还提供了包含其的药物组合物以及治疗癌症的方法。

12. 发明申请

WO2005080391A1 PRODRUGS OF SUBSTITUTED AMINO HETEROBICYCLES WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：调节VANILLOID-1受体（VR1）功能的替代氨基杂环化合物的产物
公开(公告)号：WO2005080391A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000548
申请日：2005-02-16
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
发明人： BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of formula (I) which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
摘要翻译：可用作治疗化合物的式（I）化合物，特别是用于治疗通过调节香草素-1受体（VR1）的功能而改善的疼痛和其它病症。

13. 发明申请

WO2004074290A1 SUBSTITUTED AMINO HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：作为VR-1拮抗剂治疗疼痛的替代氨基酸异种
公开(公告)号：WO2004074290A1
公开(公告)日：2004-09-02
申请号：PCT/GB2004/000702
申请日：2004-02-20
申请人： MERCK SHARP & DOHME LIMITED , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , DOUGHTY, Victoria, Alexandra , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, Brian, A. , SPAREY, Timothy, Jason
发明人： BROWN, Rebecca, Elizabeth , BURKAMP, Frank , DOUGHTY, Victoria, Alexandra , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, Brian, A. , SPAREY, Timothy, Jason
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula I: in which: one of T 1 and T 4 is N and the other is C; T 2 and T 3 are independently N or C(CH 2 ) n R 2 ; X, Y and Z are independently N or C(CH 2 ) n R 3 ; R 1 is Ar 1 or R 1 is C 1-6 alkyl optionally substituted with one or two groups Ar1; Ar1 is an optionally substituted cyclohexyl, piperidinyl, piperazinyl, morpholinyl, adamantyl, phenyl, naphthyl, a six - membered heteroaromatic ring containing one, two or three nitrogen atoms, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one O or S atom being present, or a nine - or ten - membered bicyclic heteroaromatic ring in which phenyl or a six - membered heteroaromatic ring as defined above is fused to a six - or five - membered heteroaromatic ring as defined above; Ar is an optionally substituted phenyl, a six - membered heteroaromatic ring containing one, two or three nitrogen atoms or a five - membered heteroaromatic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, Ar being optionally substituted by one, two or three groups chosen from halogen, CF 3 , OCF 3 , C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, nitro, cyano, isonitrile, hydroxy, C 1-6 alkoxy, C 1-6 alkylthio, -NR 6 R 7 , -CONR 6 R 7 , -COH, CO 2 H, C 1-6 alkoxycarbonyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkylcarbonyl and a five - membered heteroaromatic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, optionally substituted by C 1-6 alkyl, halogen, amino, hydroxy or cyano; or a pharmaceutically acceptable salt thereof as a VR-1 ligand; pharmaceutical compositions comprising it; its use in therapy; use of it in the manufacture of a medicament to treat pain; and methods of treating subjects suffering from pain.
摘要翻译：本发明提供了式I化合物：其中：T 1和T 4中的一个是N，另一个是C; T 2和T 3独立地是N或C（CH 2）n R 2; X，Y和Z独立地为N或C（CH 2）n R 3; R 1是Ar 1或R 1是任选被一个或两个Ar 1基团取代的C 1-6烷基; Ar1是任选取代的环己基，哌啶基，哌嗪基，吗啉基，金刚烷基，苯基，萘基，含有一个，两个或三个氮原子的六元杂芳环，含有一个，两个，三个或四个的五元杂芳环选自O，N和S，至多存在一个O或S原子的杂原子，或其中如上所定义的苯基或六元杂芳环的九个或十元二环杂芳环是与如上定义的六个或五元杂芳族杂环稠合; Ar是任选取代的苯基，含有一个，两个或三个氮原子的六元杂芳族环或含有一个，两个，三个或四个选自O，N和S的杂原子的五元杂芳环，在大多数一个杂原子是O或S，Ar任选被一个，两个或三个选自卤素，CF 3，OCF 3，C 1-6烷基，C 2-6烯基，C 2-6炔基，硝基，氰基，异氰酸酯，羟基，C 1-6烷氧基，C 1-6烷硫基，-NR 6 R 7，-CONR 6 R 7，-COH，CO 2 H，C 1-6烷氧基羰基，卤代C 1-6烷基，羟基C 1-6烷基，氨基C 1-6烷基，C 1-6烷基羰基和含有一个，两个，三个或四个选自O，N和S的杂原子的五元杂芳环，最多一个杂原子是O或S，任选被C 1-6烷基，卤素，氨基，羟基或氰基取代; 或其药学上可接受的盐作为VR-1配体; 包含它的药物组合物; 其用于治疗; 在制造治疗疼痛的药物中的用途; 以及治疗痛苦患者的方法。

14. 发明申请

WO2004014865A1 PHENYLPYRIDAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：作为GABA受体配体的苯基吡啶衍生物
公开(公告)号：WO2004014865A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003376
申请日：2003-08-04
申请人： MERCK SHARP & DOHME LIMITED , BLACKABY, Wesley, Peter , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JENNINGS, Andrew , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STREET, Leslie, Joseph , THOMAS, Steve , VAN NIEL, Monique, Bodil , WILSON, Kevin
发明人： BLACKABY, Wesley, Peter , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JENNINGS, Andrew , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STREET, Leslie, Joseph , THOMAS, Steve , VAN NIEL, Monique, Bodil , WILSON, Kevin
IPC分类号： C07D237/24
CPC分类号： C07D231/12 , C07D233/56 , C07D237/08 , C07D237/14 , C07D237/20 , C07D237/24 , C07D249/08 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D417/14
摘要： A class of 4-phenylpyridazine derivatives of Formula (I), being selective ligands for GABA A receptors, in particular having high affinity for the α2 and/or α3 and or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类式（I）的4-苯基哒嗪衍生物，作为GABA A受体的选择性配体，特别是对α2和/或其α3和α5亚基具有高亲和力，因此在治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

15. 发明申请

WO2012069852A1 PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF SPHINGOSINE KINASE 审中-公开
标题翻译：作为SPHINGOSINE激酶的抑制剂的药物化合物
公开(公告)号：WO2012069852A1
公开(公告)日：2012-05-31
申请号：PCT/GB2011/052334
申请日：2011-11-25
申请人： ALMAC DISCOVERY LIMITED , HARRISON, Timothy , BURKAMP, Frank , JORDAN, Linda , BELL, Mark , JANSSEN, Dominic , MIEL, Hugues , MCFARLAND, Mary
发明人： HARRISON, Timothy , BURKAMP, Frank , JORDAN, Linda , BELL, Mark , JANSSEN, Dominic , MIEL, Hugues , MCFARLAND, Mary
IPC分类号： C07D241/04 , C07D213/76 , C07D403/04 , C07D401/04 , C07D239/26 , C07D471/04 , C07D471/10 , C07D239/34 , C07D487/04 , C07D213/24 , C07D239/42 , A61K31/4418 , C07D213/30 , C07D401/14 , A61K31/4427
CPC分类号： C07D241/04 , C07D213/24 , C07D213/30 , C07D213/76 , C07D239/26 , C07D239/34 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04 , C07D471/10 , C07D487/04
摘要： The present invention relates to compounds that are useful as inhibitors of the activity of one or more isoforms of sphingosine kinase. Particularly, although not exclusively, the present invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment and/or prevention of cancers, hyperproliferative, inflammatory, angiogenic, immune and viral infectious diseases.
摘要翻译：本发明涉及可用作一种或多种鞘氨醇激酶同种型的活性抑制剂的化合物。特别地，尽管不是唯一地，本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗和/或预防癌症，过度增殖，炎性，血管生成，免疫和病毒感染性疾病中的用途。

16. 发明申请

WO2007054739A1 TETRAHYDROINDOLE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的四氢吡啶衍生物
公开(公告)号：WO2007054739A1
公开(公告)日：2007-05-18
申请号：PCT/GB2006/050368
申请日：2006-11-03
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
发明人： BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
IPC分类号： C07D209/30 , C07D209/42 , C07D209/08 , C07D405/04 , C07D231/56 , C07D209/86 , C07D401/04 , A61K31/403 , A61K31/404 , A61K31/416 , A61P25/28
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默病。

17. 发明申请

WO2005051390A1 E-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN 审中-公开
标题翻译： E-FLOROR-4-（PYRIDIN-2-YL） - 哌啶-1-羧酰胺衍生物及其相关化合物，其调节VANILLOID-1受体（VR1）用于治疗疼痛的功能
公开(公告)号：WO2005051390A1
公开(公告)日：2005-06-09
申请号：PCT/GB2004/004538
申请日：2004-10-27
申请人： MERCK SHARP & DOHME LIMITED , BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
发明人： BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
IPC分类号： A61K31/4545
CPC分类号： C07D451/04 , C07D401/04
摘要： Compounds of formula (I): wherein: A 1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A 2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from 0, N and S, at most one heteroatom being O or S; L is a bond or C 1-6 alkylene; R 1 and R 2 independently chosen from hydrogen and C 1-6 alkyl or R l and R 2 may, together, form a methylene or ethylene bridge; W is halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; X is O, S or NR 3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A 2 ; Y is a bond, C 1-4 alkylene, NH or NH(CH 2 ) 1-3 ; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1; which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
摘要翻译：式（I）的化合物：其中：A 1是苯基，含有一个，两个或三个氮原子的六元芳族杂环，或含有至多四个选自O，N和S的杂原子的五元芳族杂环至多一个杂原子是O或S; A 2是苯基，含有一个，两个或三个氮原子的六元芳族杂环，或含有至多四个选自0，N和S的杂原子的五元芳族杂环，最多一个杂原子是O或S ; L是键或C1-6亚烷基; R 1和R 2独立地选自氢和C 1-6烷基或R 1和R 2可以一起形成亚甲基或亚乙基桥; W是卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; X是O，S或NR 3或X，连同其所连接的原子，Y与A 2一起形成不饱和五元环; Y是键，C1-4亚烷基，NH或NH（CH2）1-3; 或其药学上可接受的盐; 其它取代基如权利要求1中所定义; 其可用作治疗化合物，特别是用于治疗通过调节香草素-1受体（VR1）的功能而改善的疼痛和其它病症。

18. 发明申请

WO2005049601A1 INDAZOL-3-ONES AND ANALOGUES AND DERIVATIVES THEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：调节VANILLOID-1受体（VR1）功能的INDAZOL-3-ONES及其衍生物及其衍生物
公开(公告)号：WO2005049601A1
公开(公告)日：2005-06-02
申请号：PCT/GB2004/004809
申请日：2004-11-12
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , FLETCHER, Stephen, Robert
发明人： BURKAMP, Frank , FLETCHER, Stephen, Robert
IPC分类号： C07D401/04
CPC分类号： C07D231/56 , C07D401/04 , C07D471/04
摘要： Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
摘要翻译：可用作治疗化合物的式（I）化合物，特别是用于治疗通过调节香草素-1受体（VR1）的功能而改善的疼痛和其它病症。

19. 发明申请

WO2003086406A1 IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO2003086406A1
公开(公告)日：2003-10-23
申请号：PCT/GB2003/001465
申请日：2003-04-03
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , STREET, Leslie, Joseph
发明人： BURKAMP, Frank , STREET, Leslie, Joseph
IPC分类号： A61K31/505
CPC分类号： C07D471/04 , A61K31/505
摘要： A class of imidazo[4,5- b ]pyridine derivatives, substituted at the 1-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABA A receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在1位被取代的咪唑并[4,5-b]吡啶衍生物，是GABA A受体的选择性配体，尤其对α2和因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，抽搐和认知障碍）方面是有益的。

20. 发明申请

WO2011077098A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2011077098A1
公开(公告)日：2011-06-30
申请号：PCT/GB2010/002329
申请日：2010-12-23
申请人： ALMAC DISCOVERY LIMITED , ZHANG, Lixin , TREVITT, Graham, Peter , MIEL, Hughes , BURKAMP, Frank , HARRISON, Timothy , WILKINSON, Andrew, John , FABRITIUS, Charles-Henry
发明人： ZHANG, Lixin , TREVITT, Graham, Peter , MIEL, Hughes , BURKAMP, Frank , HARRISON, Timothy , WILKINSON, Andrew, John , FABRITIUS, Charles-Henry
IPC分类号： C07D471/04 , C07D498/04 , C07D498/14 , A61K31/4741 , A61P35/00
CPC分类号： C07D498/04 , C07D471/04 , C07D498/14
摘要： The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
摘要翻译：本发明涉及作为丝氨酸 - 苏氨酸激酶AKT抑制剂的特定活性的一系列化合物。还提供了包含其的药物组合物以及用于治疗癌症的方法。

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