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1. 发明申请

US20170267678A1 Tetrahydro-Pyrido-Pyrimidine Derivatives 审中-公开
公开(公告)号：US20170267678A1
公开(公告)日：2017-09-21
申请号：US15613560
申请日：2017-06-05
申请人： Nigel Graham COOKE , Paulo Fernandes Gomes Dos Santos , Nadege GRAVELEAU , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Alexander Baxter SMITH , Nicolas SOLDERMANN , Frank STOWASSER , Ross Sinclair STRANG , Nicola TUFILLI , Anette von MATT , Romain WOLF , Frederic ZECRI
发明人： Nigel Graham COOKE , Paulo Fernandes Gomes Dos Santos , Nadege GRAVELEAU , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Alexander Baxter SMITH , Nicolas SOLDERMANN , Frank STOWASSER , Ross Sinclair STRANG , Nicola TUFILLI , Anette von MATT , Romain WOLF , Frederic ZECRI
IPC分类号： C07D471/04 , A61K31/519 , A61K31/5377
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.

2. 发明申请

US20110152242A1 2,3-Substituted Fused Pyrimidin -4 (3H)-Ones as VR1 Antagonists 审中-公开
公开(公告)号：US20110152242A1
公开(公告)日：2011-06-23
申请号：US11886812
申请日：2006-03-21
申请人： Tracy Bayliss , Rebecca Elizabeth Brown , Gregory John Hollingworth , Brian A. Jones , Christopher Richard Moyes , Lauren Rogers
发明人： Tracy Bayliss , Rebecca Elizabeth Brown , Gregory John Hollingworth , Brian A. Jones , Christopher Richard Moyes , Lauren Rogers
IPC分类号： A61K31/522 , C07D473/18 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/5377 , A61K31/519 , A61P29/00 , A61P25/06 , A61P25/00 , A61P27/16 , A61P27/02 , A61P9/00 , A61P21/00 , A61P17/04 , A61P25/02 , A61P1/00 , A61P13/00 , A61P11/00 , A61P11/08 , A61P11/06 , A61P11/02 , A61P37/02 , A61P25/24 , A61P1/04
CPC分类号： C07D473/18 , C07D471/04 , C07D495/04
摘要： A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, at most one heteroatom being O or S, or a six-membered heteroaromatic ring containing one, two or three N atoms, optionally substituted by one or more groups chosen from halogen, hydroxy, cyano, nitro, NR2R3 or S(O)rNR2R3 where NR2R3 is as defined above, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, haloC1-6alkylthio, C3-7cycloalkyl, hydroxyC1-6alkyl, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; or a pharmaceutically acceptable salt or N-oxide thereof; pharmaceutical compositions comprising them; the compounds for use in methods of treatment; and use of the compounds for manufacturing medicaments for treating pain as VR1 antagonists, including conditions such as depression, GERD, itch and urinary incontinence.

3. 发明授权

US07442701B2 Amino-heterocycles as VR-1 antagonists for treating pain 失效
公开(公告)号：US07442701B2
公开(公告)日：2008-10-28
申请号：US10534584
申请日：2003-11-14
申请人： Peter Blurton , Frank Burkamp , Stephen Robert Fletcher , Gregory John Hollingworth , A. Brian Jones , Edward Giles McIver , Christopher Richard Moyes , Lauren Rogers
发明人： Peter Blurton , Frank Burkamp , Stephen Robert Fletcher , Gregory John Hollingworth , A. Brian Jones , Edward Giles McIver , Christopher Richard Moyes , Lauren Rogers
IPC分类号： A61K31/44 , A61K31/497 , 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.

4. 发明授权

US07253205B2 Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents 失效
标题翻译：双 - 二取代的环己烷衍生物及其作为治疗剂的用途
公开(公告)号：US07253205B2
公开(公告)日：2007-08-07
申请号：US10481477
申请日：2002-06-10
申请人： Jose Luis Castro Pineiro , Kevin Dinnell , Jason Matthew Elliott , Gregory John Hollingworth , Duncan Edward Shaw , Christopher John Swain
发明人： Jose Luis Castro Pineiro , Kevin Dinnell , Jason Matthew Elliott , Gregory John Hollingworth , Duncan Edward Shaw , Christopher John Swain
IPC分类号： A61K31/4545 , C07D401/02
CPC分类号： C07D207/26 , C07D211/76 , C07D241/08 , C07D405/04 , C07D491/10
摘要： The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a variety of substituents, ring A is a phenyl or pyridyl ring; d is zero, 1 or 2; and pharmaceutically acceptable salts and N-oxides thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia
摘要翻译：本发明涉及式（I）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 7，R 8，R 9， SUP>和R 10代表各种取代基，环A是苯基或吡啶环; d为零，1或2; 及其药学上可接受的盐和N-氧化物。该化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，偏头痛，呕吐或带状疱疹后神经痛

5. 发明授权

US6096729A Use of NK-1 receptor antagonists for treating amnestic disorders 失效
标题翻译：使用NK-1受体拮抗剂治疗遗忘性疾病
公开(公告)号：US6096729A
公开(公告)日：2000-08-01
申请号：US980928
申请日：1997-12-01
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： C07D491/107 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/4525 , A61K31/5375 , A61K31/5377 , A61K31/675 , A61K45/00 , A61P9/10 , A61P25/28 , C07D211/56 , C07D265/32 , C07D413/06 , C07D491/10 , A61K31/44 , A61K31/535
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides methods for the treatment or prevention of amnestic disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist.
摘要翻译：本发明提供了治疗或预防遗忘性疾病的方法，其包括口服活性的长效中枢神经系统（CNS）渗透的NK-1受体拮抗剂的口服给药。

6. 发明授权

US10004732B2 Amino pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors 有权
公开(公告)号：US10004732B2
公开(公告)日：2018-06-26
申请号：US15303868
申请日：2014-04-24
申请人： Benjamin Richard Bellenie , Graham Charles Bloomfield , Ian Bruce , Andrew James Culshaw , Edward Charles Hall , Gregory John Hollingworth , James Neef , Matthew Spendiff , Simon James Watson
发明人： Benjamin Richard Bellenie , Graham Charles Bloomfield , Ian Bruce , Andrew James Culshaw , Edward Charles Hall , Gregory John Hollingworth , James Neef , Matthew Spendiff , Simon James Watson
IPC分类号： C07D401/04 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , A61K31/497 , A61K31/5377 , C07D403/04
CPC分类号： A61K31/497 , A61K31/5377 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.

7. 发明申请

US20170037032A1 AMINO PYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译：氨基吡啶衍生物作为磷脂酰肌醇三激酶抑制剂
公开(公告)号：US20170037032A1
公开(公告)日：2017-02-09
申请号：US15303879
申请日：2014-04-24
申请人： Benjamin Richard BELLENIE , Graham Charles BLOOMFIELD , Ian BRUCE , Andrew James CULSHAW , Edward Charles HALL , Gregory John HOLLINGWORTH , James NEEF , Matthew SPENDIFF , Simon James WATSON
发明人： Benjamin Richard BELLENIE , Graham Charles BLOOMFIELD , Ian BRUCE , Andrew James CULSHAW , Edward Charles HALL , Gregory John HOLLINGWORTH , James NEEF , Matthew SPENDIFF , Simon James WATSON
IPC分类号： C07D401/14 , C07D401/04 , A61K31/4439 , C07D417/04 , C07D413/04 , C07D417/14 , C07D491/107 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/55 , A61K31/444 , C07D413/14
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D213/73 , C07D401/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/107
摘要： The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.
摘要翻译：本发明提供抑制PI 3激酶γ同种型活性的式（I）化合物，其可用于治疗由PI3激酶γ同种型激活介导的疾病。

8. 发明申请

US20140128370A1 Tetrahydro-Pyrido-Pyrimidine Derivatives 审中-公开
标题翻译：四氢吡啶并嘧啶衍生物
公开(公告)号：US20140128370A1
公开(公告)日：2014-05-08
申请号：US14151796
申请日：2014-01-09
申请人： Nigel Graham COOKE , Frédéric ZECRI , Nicolas SOLDERMANN , Romain WOLF , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Anette VON MATT , Ross Sinclair STRANG , Alexander Baxter SMITH , Paulo FERNANDES GOMES DOS SANTOS , Nadege GRAVELEAU , Frank STOWASSER , Nicola TUFILLI
发明人： Nigel Graham COOKE , Frédéric ZECRI , Nicolas SOLDERMANN , Romain WOLF , Christina HEBACH , Klemens HOEGENAUER , Gregory John HOLLINGWORTH , Anette VON MATT , Ross Sinclair STRANG , Alexander Baxter SMITH , Paulo FERNANDES GOMES DOS SANTOS , Nadege GRAVELEAU , Frank STOWASSER , Nicola TUFILLI
IPC分类号： C07D471/04
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

US20090233947A1 2,3-Substituted fused bicyclic pyrimidin-4(3H)-ones which modulating 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2,3-取代的稠合双环嘧啶-4（3H） - 酮
公开(公告)号：US20090233947A1
公开(公告)日：2009-09-17
申请号：US11920065
申请日：2006-05-10
申请人： Tracy Bayliss , Rebecca Elizabeth Brown , Gregory John HollingWorth , A. Brian Jones
发明人： Tracy Bayliss , Rebecca Elizabeth Brown , Gregory John HollingWorth , A. Brian Jones
IPC分类号： A61K31/522 , C07D473/30 , A61P25/00
CPC分类号： C07D473/04
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, also known as TRPV1).
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，也称为TRPV1）的功能而改善的疼痛和其它病症。

10. 发明授权

US06476045B2 Azaindole derivatives and their use as therapeutic agents 失效
标题翻译： Azaindole衍生物及其作为治疗剂的用途
公开(公告)号：US06476045B2
公开(公告)日：2002-11-05
申请号：US09903108
申请日：2001-07-11
申请人： Kevin Dinnell , Jason Matthew Elliott , Gregory John Hollingworth , Duncan Edward Shaw
发明人： Kevin Dinnell , Jason Matthew Elliott , Gregory John Hollingworth , Duncan Edward Shaw
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D209/14 , C07D235/14 , C07D471/04
摘要： The present invention relates to compounds of the formula (I): wherein: Het represents a heterocyclic residue selected from: where the dotted line in (b) represents an optional double bond; A completes a fused pyridine ring; and B completes a fused benzene or pyridine ring. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
摘要翻译：本发明涉及式（I）的化合物：其中：Het表示选自：其中（b）中的虚线表示任选的双键的杂环残基; A完成稠合吡啶环; 和B完成稠合的苯或吡啶环。该化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，迁移物，呕吐或带状疱疹后神经痛。

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