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1. 发明申请

US20050107388A1 Heteroaromatic urea derivatives as vr-1receptor modulators for treating pain 失效
标题翻译：异恶唑脲衍生物作为治疗疼痛的vr-1受体调节剂
公开(公告)号：US20050107388A1
公开(公告)日：2005-05-19
申请号：US10505358
申请日：2003-03-21
申请人： Rebecca Brown , Victoria Doughty , Gregory Hollingworth , A. Jones , Matthew Lindon , Christopher Moyes , Lauren Rogers
发明人： Rebecca Brown , Victoria Doughty , Gregory Hollingworth , A. Jones , Matthew Lindon , Christopher Moyes , Lauren Rogers
IPC分类号： C07D237/28 , A61K31/427 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/502 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P11/00 , A61P11/06 , A61P13/10 , A61P19/02 , A61P19/06 , A61P25/02 , A61P25/04 , A61P25/06 , A61P29/00 , A61P37/02 , C07D215/38 , C07D217/02 , C07D217/08 , C07D217/14 , C07D217/16 , C07D217/22 , C07D217/24 , C07D217/26 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/541 , A61K31/496 , A61K31/498 , A61K31/517
CPC分类号： C07D401/12 , C07D215/38 , C07D217/02 , C07D217/08 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds of formula (I); pharmaceutically acceptable salts and N-oxides thereof in which A, B, D and E are C or N with the proviso that one or more are N, R1, R2, R3, R4, R5 and R6 are simple substituents, n is 0-3 and y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; as VR-1 antagonists for treating conditions or diseases in which pain and/or inflammation predominates; the use of the same for manufacturing medicaments, pharmaceutical compositions comprising them and methods of treatment utilising them.
摘要翻译：本发明提供式（I）化合物; 其中A，B，D和E为C或N的药学上可接受的盐和N-氧化物，条件是一个或多个为N，R 1，R 2， R 3，R 4，R 5和R 6是简单的取代基，n是0-3和 y是芳基，杂芳基，碳环基或稠合碳环基; 作为用于治疗其中疼痛和/或炎症占优势的病症或疾病的VR-1拮抗剂; 使用它们制造药物，包含它们的药物组合物和使用它们的治疗方法。

2. 发明申请

US20050197342A1 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain 审中-公开
公开(公告)号：US20050197342A1
公开(公告)日：2005-09-08
申请号：US10984336
申请日：2004-11-09
申请人： Gregory Hollingworth , A. Jones , Edward McIver , Christopher Moyes , Lauren Rogers
发明人： Gregory Hollingworth , A. Jones , Edward McIver , Christopher Moyes , Lauren Rogers
IPC分类号： A61K31/497 , A61K31/501 , A61K31/506 , C07D43/02
CPC分类号： C07D401/04
摘要： The present invention provides a compound of formula I: Y-J-NH-Z (I)wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1-4alkyl, cyano, hydroxy, C1-4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)pQ, —NR2R3, —(CH2)pNR2R3 and —O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected from halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alkyl; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3, together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.

3. 发明申请

US20060154930A1 Substituted amino heterocycles as vr-1 antagonists for treating pain 审中-公开
公开(公告)号：US20060154930A1
公开(公告)日：2006-07-13
申请号：US10545877
申请日：2004-02-20
申请人： Rebecca Brown , Frank Burkamp , Victoria Doughty , Stephen Fischer , Gregory Hollingworth , A. Jones , Timothy Sparey
发明人： Rebecca Brown , Frank Burkamp , Victoria Doughty , Stephen Fischer , Gregory Hollingworth , A. Jones , Timothy Sparey
IPC分类号： C07D487/04 , A61K31/503
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula I: in which: one of T1 and T4 is N and the other is C; T2 and T3 are independently N or C(CH2)nR2; X, Y and Z are independently N or C(CH2)nR3; R1 is Ar1 or R1 is C1-6alkyl 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, CF3, OCF3, C1-6-alkyl, C2-6alkenyl, C2-6alkynyl, nitro, cyano, isonitrile, hydroxy, C1-6alkoxy, C1-6alkylthio, —NR6R7, —CONR6R7, —COH, CO2H, C1-6alkoxycarbonyl, haloC1-4alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, C1-4alkylcarbonyl 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 C1-6alkyl, 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.

4. 发明申请

US20060122242A1 2-Aryloxy-2-arylalkanoic acids for diabetes and lipid disorders 失效
标题翻译： 2-芳氧基-2-芳基链烷酸用于糖尿病和脂质疾病
公开(公告)号：US20060122242A1
公开(公告)日：2006-06-08
申请号：US11334152
申请日：2006-01-18
申请人： Alan Adams , A. Jones , Joel Berger , James Dropinski , Alexander Elbrecht , Kun Liu , Karen MacNaul , Guo-Qiang Shi , Derek Von Langen , Gaochao Zhou
发明人： Alan Adams , A. Jones , Joel Berger , James Dropinski , Alexander Elbrecht , Kun Liu , Karen MacNaul , Guo-Qiang Shi , Derek Von Langen , Gaochao Zhou
IPC分类号： A61K31/428 , A61K31/423 , A61K31/425 , A61K31/42
CPC分类号： C07D257/04 , C07C59/90 , C07D213/55 , C07D261/20 , C07D263/32 , C07D263/58 , C07D413/12 , C07D417/12
摘要： A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
摘要翻译：一类2-芳氧基-2-芳基链烷酸包括作为PPARα和/或γ的有效激动剂的化合物，因此可用于治疗，控制或预防非胰岛素依赖型糖尿病（NIDDM），高血糖症，血脂异常高脂血症，高胆固醇血症，高甘油三酯血症，动脉粥样硬化，肥胖症，血管再狭窄，炎症和其他PPARα和/或γ介导的疾病，病症和病症。

5. 发明申请

US20050239769A1 Therapeutic compounds for treating dyslipidemic conditions 失效
标题翻译：用于治疗血脂异常的治疗化合物
公开(公告)号：US20050239769A1
公开(公告)日：2005-10-27
申请号：US10522114
申请日：2003-07-21
申请人： A. Jones , Alan Adams , Ahren Green , Shaei Huang , Bruno Tse , Clare Gutteridge , Yuan Cheng
发明人： A. Jones , Alan Adams , Ahren Green , Shaei Huang , Bruno Tse , Clare Gutteridge , Yuan Cheng
IPC分类号： A61K31/454 , A61K31/496 , A61K31/513 , A61K31/53 , A61K31/5377 , A61K31/551 , C07D261/20 , C07D413/02 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D413/12 , C07D261/20 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
摘要翻译：本发明涉及式I的新型LXR配体及其药学上可接受的盐，酯和互变异构体，其可用于治疗血脂异常状况，特别是降低的HDL胆固醇水平。

6. 发明申请

US20050003592A1 All-around MOSFET gate and methods of manufacture thereof 审中-公开
标题翻译：全面MOSFET栅极及其制造方法
公开(公告)号：US20050003592A1
公开(公告)日：2005-01-06
申请号：US10465087
申请日：2003-06-18
申请人： A. Jones
发明人： A. Jones
IPC分类号： H01L21/336 , H01L29/423 , H01L29/786 , H01L21/00 , H01L21/84 , H01L29/04 , H01L29/76 , H01L31/036
CPC分类号： H01L29/785 , H01L29/42384 , H01L29/42392 , H01L29/66795
摘要： Metal oxide field effect transistor having a channel and a gate that surrounds the channel on four sides. Method of manufacture of the transistor includes processing the back of a silicon wafer to form a buried gate that is electrically connected to the gate of a conventional field effect transistor to form an all-around structure.
摘要翻译：金属氧化物场效应晶体管具有通道和围绕四边的通道的栅极。晶体管的制造方法包括处理硅晶片的背面以形成与常规场效应晶体管的栅极电连接以形成全能结构的掩埋栅极。

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