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1. 发明申请

WO2014058747A1 5-PHENOXY-3H-PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译： 5-苯氧基-3H-吡啶二酮-4-酮衍生物及其作为HIV逆转录酶抑制剂的用途
公开(公告)号：WO2014058747A1
公开(公告)日：2014-04-17
申请号：PCT/US2013/063612
申请日：2013-10-07
申请人： MERCK SHARP & DOHME CORP. , ARRINGTON, Kenneth, L. , BURGEY, Christopher , GILFILLAN, Robert , HAN, Yongxin , PATEL, Mehul , LI, Chun Sing , LI, Yaozong , LUO, Yunfu , LEI, Zhiyu , XU, Jiayi
发明人： ARRINGTON, Kenneth, L. , BURGEY, Christopher , GILFILLAN, Robert , HAN, Yongxin , PATEL, Mehul , LI, Chun Sing , LI, Yaozong , LUO, Yunfu , XU, Jiayi
IPC分类号： C07D401/14 , C07D239/56 , C07D403/06 , C07D403/14 , C07D239/52 , C07D239/54 , C07D471/04 , A61K31/513 , A61P31/18
CPC分类号： C07D471/04 , A61K31/513 , A61K45/06 , C07D239/52 , C07D239/54 , C07D239/56 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14
摘要： Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R 1 , R 2 , R E , L, M and Z are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式（I）的化合物是HIV逆转录酶抑制剂，其中R1，R2，RE，L，M和Z在本文中定义。式（I）化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗HIV感染以及预防，延缓发作或进展以及治疗艾滋病。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

2. 发明申请

WO2008017650A1 AN AMINOISOQUINOLINE THROMBIN INHIBITOR WITH IMPROVED BIOAVAILABILITY 审中-公开
标题翻译：具有改善生物利用度的氨基磺酰胺抑制剂
公开(公告)号：WO2008017650A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/058111
申请日：2007-08-06
申请人： N.V. ORGANON , GILFILLAN, Robert , BENNETT, David, Jonathan
发明人： GILFILLAN, Robert , BENNETT, David, Jonathan
IPC分类号： C07D401/12 , A61K31/435 , A61P7/00
CPC分类号： C07D401/12 , A61K38/05 , C07K5/0202
摘要： The invention relates to the compound N-(2-oxo-2-propoxyethyl)-ß-phenyl-D-phenyl- alanyl-N-[(1-amino-6-isoquinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.
摘要翻译：本发明涉及化合物N-（2-氧代-2-丙氧基乙基）-β-苯基-D-苯基 - 丙氨酰-N - [（1-氨基-6-异喹啉基）甲基] -L-脯氨酰胺或其药学上可接受的其盐包含所述化合物的药物组合物，以及该化合物在制备用于治疗或预防凝血酶介导的疾病的药物中的用途。

3. 发明申请

WO2002102808A2 (PYRIDO/THIENO)-[f]-OXAZEPIN-5-ONE DERIVATIVES 审中-公开
标题翻译：（吡啶/噻吩） - [f] -OXAZEPIN-5-ONE衍生物
公开(公告)号：WO2002102808A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006364
申请日：2002-06-10
申请人： AKZO NOBEL N.V. , GROVE, Simon, James, Anthony , ADAM-WORRALL, Julia , ZHANG, Mingqiang , GILFILLAN, Robert
发明人： GROVE, Simon, James, Anthony , ADAM-WORRALL, Julia , ZHANG, Mingqiang , GILFILLAN, Robert
IPC分类号： C07D498/14
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R 1 , R 2 and R 3 are independently H or (C 1-4 )alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy(C 1-4 )alkyl, CF 3 , halogen, nitro, cyano, NR 4 R 5 , NR 4 COR 6 , and CONR 4 R 5 ; R 4 and R 5 are independently H or (C 1-4 )-alkyl; or R 4 and R 5 form together with the nitrogen atom to which they are bound a 5-or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR 6 ; R 6 is (C 1-4 )alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C 1-4 )alkyl, (C 1-4 )-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译：本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基，氰基，NR 4 R 5，NR 4 COR 6和CONR 4 R 5; R 4和R 5独立地为H或（C 1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外选自O，S或NR 6的杂原子; R 6是（C 1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素和氧代; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途）由AMPA受体介导的中枢神经系统。

4. 发明申请

WO2017178884A1 ANTI-BACTERIAL, SELF-CLEANING, WATER CONSERVING, ODOR REDUCING TOILET SYSTEM 审中-公开
标题翻译：抗细菌，自洁，保水，减少异味的厕所系统
公开(公告)号：WO2017178884A1
公开(公告)日：2017-10-19
申请号：PCT/IB2017/000479
申请日：2017-04-13
申请人： GILFILLAN, Robert
发明人： GILFILLAN, Robert
IPC分类号： E03D5/04 , E03D5/012 , A47K13/00
摘要： Described herein is an anti-bacterial, self-cleaning, odor reducing, and water conserving toilet system. The toilet system is generally operated though fluid communication with a closing and opening of a lid placed upon a toilet seat. The toilet seat includes a plurality of nozzles for directing fluid to an inner surface of the toilet bowl and wherein movement of the lid directs fluid out of the nozzles.
摘要翻译：这里描述的是一种抗菌，自清洁，减少气味和节水的马桶系统。通常通过与放置在马桶座上的盖的关闭和打开流体连通来操作马桶系统。马桶座包括多个喷嘴，用于将流体引导到马桶盆的内表面，并且盖的移动将流体引导出喷嘴。

5. 发明申请

WO2015161011A1 BENZAMIDE CGRP RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯扎林CGRP受体拮抗剂
公开(公告)号：WO2015161011A1
公开(公告)日：2015-10-22
申请号：PCT/US2015/026067
申请日：2015-04-16
申请人： MERCK SHARP & DOHME CORP. , CROWLEY, Brendan , FRALEY, Mark , POTTEIGER, Craig , GILFILLAN, Robert , PATEL, Mehul , ARRINGTON, Ken , MITCHELL, Helen , SCHIRRIPA, Kathy , MCWHERTER, Melody , BIFTU, Tesfaye , NAIR, Anilkumar , WANG, Cheng , YANG, De-Yi , ZHU, Cheng , KAR, Nam Fung , HUANG, Xianhai , CHEN, Lei , ZHOU, Wei , LIU, Qingsheng , CAI, Jiaqiang
发明人： CROWLEY, Brendan , FRALEY, Mark , POTTEIGER, Craig , GILFILLAN, Robert , PATEL, Mehul , ARRINGTON, Ken , MITCHELL, Helen , SCHIRRIPA, Kathy , MCWHERTER, Melody , BIFTU, Tesfaye , NAIR, Anilkumar , WANG, Cheng , YANG, De-Yi , ZHU, Cheng , KAR, Nam Fung , HUANG, Xianhai , CHEN, Lei , ZHOU, Wei , LIU, Qingsheng , CAI, Jiaqiang
IPC分类号： A61P25/06 , A61K31/165 , A61K31/445
CPC分类号： C07D498/04 , C07D207/273 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/04
摘要： The present invention is directed to benzamide compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译：本发明涉及作为CGRP受体的拮抗剂的苯甲酰胺化合物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。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和组合物在预防或治疗涉及CGRP的疾病中的用途。

6. 发明申请

WO02102808A3 (PYRIDO/THIENO)-[f]-OXAZEPIN-5-ONE DERIVATIVES AS POSITIVE MODULATORS OF THE AMPA RECEPTOR 审中-公开
标题翻译：（PYRIDO / THIENO） - [f] -OXAZEPIN-5-ONE衍生物作为AMPA受体的阳性调节剂
公开(公告)号：WO02102808A3
公开(公告)日：2003-03-20
申请号：PCT/EP0206364
申请日：2002-06-10
申请人： AKZO NOBEL NV , GROVE SIMON JAMES ANTHONY , ADAM-WORRALL JULIA , ZHANG MINGQIANG , GILFILLAN ROBERT
发明人： GROVE SIMON JAMES ANTHONY , ADAM-WORRALL JULIA , ZHANG MINGQIANG , GILFILLAN ROBERT
IPC分类号： A61K31/553 , A61P9/00 , A61P15/10 , A61P17/02 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P43/00 , C07D498/14
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) wherein R , R and R are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR R , NR COR , and CONR R ; R and R are independently H or (C1-4)-alkyl; or R and R form together with the nitrogen atom to which they are bound a 5-or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR ; R is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译：本发明涉及具有通式（I）的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C1- 4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基，氰基，NR 4 R 5，NR 4 COR 6和CONR 4 R 5; R 4和R 5独立地为H或（C 1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外选自O，S或NR 6的杂原子; R 6是（C 1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素和氧代; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途）由AMPA受体介导的中枢神经系统。

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