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1. 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.

2. 发明申请

US20060040947A1 Amino-heterocycles as vr-1 antagonists for treating pain 失效
公开(公告)号：US20060040947A1
公开(公告)日：2006-02-23
申请号：US10534584
申请日：2003-11-14
申请人： Peter Blurton , Frank Burkamp , Sttephen Fletcher , Gregory Hollingworth , A. Brian Jones , edward McIver , Christopher Moyes , Lauren Rogers
发明人： Peter Blurton , Frank Burkamp , Sttephen Fletcher , Gregory Hollingworth , A. Brian Jones , edward McIver , Christopher Moyes , Lauren Rogers
IPC分类号： A61K31/513 , A61K31/497 , A61K31/4965 , C07D403/02
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04
摘要： the present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C—Ar2, with the proviso that when Y is N or CH then Z is C—Ar2, and with the further proviso that when Y is C—Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONR3R4, NR3SO2R6, SO2NR3R4, —(CH2)mcarboxy, esterified —(CH2)mcarboxy or —(CH2)mNR3R4; R2 represents hydrogen, halogen, hydroxy, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, haloC1-6alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; R3 and R4 are each independently hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or fluoroC1-6alkyl; or R3 and R4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C1-4alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O)2, or NR5; R5 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R6 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, C3-7cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.

3. 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。

4. 发明申请

US20070078156A1 Derivatives of n-(1h-indazolyl)-and n-(1h-indolyl)-urea as well as related compounds as modulators of the vanilloid-1 receptor (vr1) for treatment of pain 审中-公开
公开(公告)号：US20070078156A1
公开(公告)日：2007-04-05
申请号：US10571544
申请日：2004-09-16
申请人： Stephen Fletcher , Gregory Hollingworth , Brian Jones , Richard Moyes , Lauren Rogers
发明人： Stephen Fletcher , Gregory Hollingworth , Brian Jones , Richard Moyes , Lauren Rogers
IPC分类号： A61K31/4745 , C07D498/04 , C07D491/04 , C07D471/02
CPC分类号： C07D275/04 , C07C275/28 , C07D209/34 , C07D231/56 , C07D235/06 , C07D263/56 , C07D307/79 , C07D471/04
摘要： Compounds of formula (I): wherein A, B and D are each C, N, O or S; E is C or N; the dotted circle within the five-membered ring indicates that the ring may be unsaturated or partially saturated; R1 is halogen, hydroxy, C1-6 alkyl, haloC1-6 alkyl, hydroxyC1-6 alkyl, C1-6 alkoxy, halo C1-6 alkoxy, hydroxyC1-6 alkoxy, C3-7 cycloalkyl, C3-5 cycloalkylC1-4 alkyl, NR7R8, C1-6 alkyl substituted with NR7R8, C,1-6 alkoxy substituted with NR7R8, oxo, cyano, SO2NR7R8, CONR7R8, NHCOR9 or NHSO2R9; R2 is halogen, hydroxy, C1-6 alkyl, halo C1-6 alkyl, hydroxyC1-6 alkyl, C1-6 alkoxy, halo C1-6 alkoxy, hydroxyC1-6 alkoxy, C 3-7 cycloalkyl, C3-5 cycloalkylC1-4 alkyl, NR7R8, C1-6 alkyl substituted with NR7R8, C1-6, alkoxy substituted with NR7R8, cyano, SON2R7R8, CONR7R8, NHCOR9, or NHSO2R9; R3 and R4 are each independently hydrogen, C1-6, alkyl, phenyl or halophenyl; R5 and R6 are, at each occurrence, independently hydrogen, C1-6 alkyl, phenyl, halophenyl or carboxy; X is an oxygen or sulfur atom; Y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; n is either zero or an integer from 1 to 3; p is either zero or an integer from, 1 to 4; and q is either zero or an integer from 1 to 3; the other substituents are defined in claim 1; 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).

5. 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.

6. 发明申请

US20070135454A1 Bicyclic pyrimidin-4(3h)-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1-receptor(vr1) 审中-公开
标题翻译：调节香草醇-1-受体（vr1）功能的双环嘧啶-4（3h） - 酮及其类似物和衍生物
公开(公告)号：US20070135454A1
公开(公告)日：2007-06-14
申请号：US10578855
申请日：2004-11-12
申请人： Tracy Bayliss , Gregory Hollingworth , Rebecca Jarvis , Brian Jones , Timothy Sparey
发明人： Tracy Bayliss , Gregory Hollingworth , Rebecca Jarvis , Brian Jones , Timothy Sparey
IPC分类号： A61K31/519 , C07D498/02 , C07D491/02 , C07D487/02
CPC分类号： C07D473/22 , C07D471/04 , C07D473/18 , C07D473/24 , C07D495/04 , C07D513/04
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：式（I）化合物; 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。

7. 发明申请

US20140249139A1 Quinazoline Derivatives 审中-公开
标题翻译：喹唑啉衍生物
公开(公告)号：US20140249139A1
公开(公告)日：2014-09-04
申请号：US14352055
申请日：2012-10-19
申请人： Pascal Furet , Christina Hebach , Klemens Hogenauer , Gregory Hollingworth , Ian Lewis , Alexander Baxter Smith , Nicolas Solvermann , Frederic Stauffer , Romain Wolf , Frederic Zecri
发明人： Pascal Furet , Christina Hebach , Klemens Hogenauer , Gregory Hollingworth , Ian Lewis , Alexander Baxter Smith , Nicolas Solvermann , Frederic Stauffer , Romain Wolf , Frederic Zecri
IPC分类号： C07D401/04 , C07D413/14 , C07D401/14 , C07D487/08 , C07D403/04 , C07D239/74
CPC分类号： C07D401/04 , C07D239/74 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D487/08
摘要： The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译：本发明涉及式（I）的取代喹唑啉衍生物，其中A，X 1，X 2，X 3，X 4和R 5如说明书中所定义。这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。

8. 发明授权

US08653092B2 Tetrahydro-pyrido-pyrimidine derivatives 有权
标题翻译：四氢吡啶并嘧啶衍生物
公开(公告)号：US08653092B2
公开(公告)日：2014-02-18
申请号：US13175050
申请日：2011-07-01
申请人： Nigel Graham Cooke , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Christina Hebach , Klemens Högenauer , Gregory Hollingworth , Alexander Baxter Smith , Nicolas Soldermann , Frank Stowasser , Ross Strang , Nicola Tufilli , Anette Von Matt , Romain Wolf , Frédéric Zecri
发明人： Nigel Graham Cooke , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Christina Hebach , Klemens Högenauer , Gregory Hollingworth , Alexander Baxter Smith , Nicolas Soldermann , Frank Stowasser , Ross Strang , Nicola Tufilli , Anette Von Matt , Romain Wolf , Frédéric Zecri
IPC分类号： C07D471/04 , A61K31/519 , A61P37/08 , A61P25/28 , A61P35/00 , A61P37/06
CPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , C07B2200/05
摘要： The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译：本发明涉及式（I）的取代的四氢 - 吡啶并 - 嘧啶衍生物，其中Y，R 1，R 2和m如说明书中所定义。这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。

9. 发明申请

US20070213332A1 Prodrugs Of Substituted Amino Heterobicycles Which Modulate The Function Of The Vanilloid-1 Receptor (Vr1) 审中-公开
标题翻译：调节香草素-1受体（Vr1）功能的取代氨基异构体前体药物
公开(公告)号：US20070213332A1
公开(公告)日：2007-09-13
申请号：US10593766
申请日：2005-02-16
申请人： Frank Burkamp , Jose Luis Castro Pineiro , Gregory Hollingworth
发明人： Frank Burkamp , Jose Luis Castro Pineiro , Gregory Hollingworth
IPC分类号： A61K31/4985 , A61P29/00 , C07D471/04 , C07D487/04
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。

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