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1. 发明授权

US06939891B2 Heterocyclic ureas, their preparation and their use as vanilloid receptor antagonists 失效
标题翻译：杂环脲，其制备及其作为香草素受体拮抗剂的用途
公开(公告)号：US06939891B2
公开(公告)日：2005-09-06
申请号：US10475937
申请日：2002-05-02
申请人： Harshad Kantilal Rami , Mervyn Thompson , Paul Adrian Wyman
发明人： Harshad Kantilal Rami , Mervyn Thompson , Paul Adrian Wyman
IPC分类号： A61K31/402 , A61P1/00 , A61P1/04 , A61P1/06 , A61P1/08 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/14 , A61P13/00 , A61P13/10 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/06 , A61P29/00 , A61P31/18 , A61P31/22 , A61P35/00 , A61P43/00 , C07D207/09 , C07D207/14 , A61K31/40
CPC分类号： C07D207/14 , C07D207/09
摘要： The invention relates to certain novel compounds having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
摘要翻译：本发明涉及某些具有香草素受体（VR1）拮抗剂活性的新化合物，其制备方法，含有它们的组合物及其在治疗各种疾病中的用途。

2. 发明申请

US20090163506A1 Urea-compounds active as vanilloid receptor antagonists for the treatment of pain 失效
标题翻译：用作治疗疼痛的香草素受体拮抗剂的尿素化合物
公开(公告)号：US20090163506A1
公开(公告)日：2009-06-25
申请号：US10489277
申请日：2002-09-13
申请人： Harshad Kantilal Rami , Mervyn Thompson , Paul Adrian Wyman
发明人： Harshad Kantilal Rami , Mervyn Thompson , Paul Adrian Wyman
IPC分类号： A61K31/501 , C07D401/04 , A61K31/4439 , C07D403/04
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14
摘要： Certain compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1, R2, P, P′, n, p, q, r and s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
摘要翻译：某些式（I）化合物或其药学上可接受的盐或其溶剂合物，其中R 1，R 2，P，P'，n，p，q，r和s如说明书中所定义，这样的化合物，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医药中的用途。

3. 发明授权

US06939871B2 Benzoxazinone derivatives, their preparation and use 失效
公开(公告)号：US06939871B2
公开(公告)日：2005-09-06
申请号：US10415119
申请日：2001-10-22
申请人： Christopher Norbert Johnson , Harshad Kantilal Rami , Geoffrey Stemp , Kevin Thewlis , Mervyn Thompson , Antonio Keuok Keong Vong
发明人： Christopher Norbert Johnson , Harshad Kantilal Rami , Geoffrey Stemp , Kevin Thewlis , Mervyn Thompson , Antonio Keuok Keong Vong
IPC分类号： A61K31/538 , A61P25/00 , A61P25/22 , A61P25/24 , C07D413/12 , C07D413/14 , C07D413/10 , A61P25/18
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is phenyl, naphthyl, a monocyclic heteroaromatic group or a bicyclic heteroaromatic group, said Ar group being optionally substituted by 1-4 substituents, which may be the same or different, and which are selected from the group consisting of: halogen, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-6alkyl, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-6alkoxy, arylC1-6alkoxy, C1-6alkylthio, C1-6alkoxyC1-6-alkyl, C3-7cycloalkylC1-6alkoxy, C1-6alkanoyl, C1-6alkoxycarbonyl, C1-6alkylsulfonyl, C1-6alkylsulfinyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, C1-6alkylsulfonamido, C1-6alkylamido, C1-6alkylsulfonamidoC1-6alkyl, C1-6alkylamidoC1-6alkyl, arylsulfonamido, arylcarboxamido, alkylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, arolC1-6alkyl, arylC1-6alkanoyl, a group R OCO(CH2)s, R CON(R )(CH2)s, R R NCO(CH2)s or R R NSO2(CH2) where each of R and R independently represents a hydrogen atom or C1-4alkyl or R and R form part of a C3-6azacyloalkane or C3-6(2-oxo)azacycloalkane ring and s represents zero or an integer from 1 to 4, and a group Ar Z, wherein Z represents a single bond, O, S or CH2 and Ar represents a phenyl or a monocyclic heteroaromatic group, said Ar group being optionally substituted by 1-3 substituents, which may be the same or different, and which are selected from the group consisting of a halogen, hydroxy, cyano, trifluoromethyl, C1-6alkyl, C1-6alkoxy or C1-6alkanoyl; when Ar is a phenyl or a monocyclic heteroaromatic group, substitutents positioned ortho to one another may be linked to form a 5- or 6-membered ring; R is hydrogen, C1-6alkyl, C3-6alkenyl, C3-6alkynyl or arylC1-6alkyl; R is halogen, C1-6alkyl, cyano, CF3, C1-6alkanoyl, C1-6alkoxy or hydroxy; X is CH or N; Y is a single bond, O, or C═O; p is 0, 1 or 2; r is 0, 1, 2 or 3; m is 2, 3 or 4; n and q are independently 1 or 2. Processes for preparing the compounds, pharmaceutical compositions containing them and their use as medicaments for various CNS disorders, including deression and/or anxiety, are also disclosed.

4. 发明授权

US07538121B2 Vanilloid receptor modulators 失效
标题翻译：香草素受体调节剂
公开(公告)号：US07538121B2
公开(公告)日：2009-05-26
申请号：US10503648
申请日：2003-02-13
申请人： Gregor James MacDonald , Darren Jason Mitchell , Harshad Kantilal Rami , Mervyn Thompson , Susan Marie Westaway
发明人： Gregor James MacDonald , Darren Jason Mitchell , Harshad Kantilal Rami , Mervyn Thompson , Susan Marie Westaway
IPC分类号： C07D403/02 , A61K31/47
CPC分类号： C07D401/12 , C07D215/38 , C07D409/12 , C07D409/14
摘要： Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, P, X, Y, q, r ans s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译：某些式（I）化合物或其药学上可接受的盐或溶剂合物，其中R 1，R 2，R 3，P，X，Y，q，r s s如本说明书中所定义，制备此类化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

5. 发明授权

US07528151B2 Heterocyclic urea derivatives for the treatment of pain 失效
标题翻译：用于治疗疼痛的杂环脲衍生物
公开(公告)号：US07528151B2
公开(公告)日：2009-05-05
申请号：US10548260
申请日：2004-03-05
申请人： Stephen Frederick Moss , Harshad Kantilal Rami , Mervyn Thompson , David Richard Witty
发明人： Stephen Frederick Moss , Harshad Kantilal Rami , Mervyn Thompson , David Richard Witty
IPC分类号： C07D401/14 , C07D401/12 , A61K31/4725
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14
摘要： Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein: P, P′, R1, R2, n, p, q, r, and s are as defined in the specification, processes for preparing such compounds, pharmaceutical compositions comprising such compounds and their use in therapy.
摘要翻译：式（I）化合物或其药学上可接受的盐或其溶剂合物，其中：P，P'，R 1，R 2，n，p，q，r和s如说明书中所定义，这些化合物，包含这些化合物的药物组合物及其在治疗中的用途。

6. 发明授权

US07390817B2 Combinations of a vanilloid antagonist and an NSAID for the treatment of pain 失效
标题翻译：用于治疗疼痛的香草素拮抗剂和NSAID的组合
公开(公告)号：US07390817B2
公开(公告)日：2008-06-24
申请号：US10540100
申请日：2003-12-17
申请人： Charanjit Bountra , John Beresford Davis , Harshad Kantilal Rami , Mervyn Thompson
发明人： Charanjit Bountra , John Beresford Davis , Harshad Kantilal Rami , Mervyn Thompson
IPC分类号： A61K31/44 , A01N43/42
CPC分类号： A61K45/06 , A61K31/365 , A61K31/4439 , A61K2300/00
摘要： A method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, a vanilloid VR-1 antagonist or a pharmaceutically acceptable derivative thereof and an NSAID or a pharmaceutically acceptable derivative thereof, wherein said VR-1 antagonist or said NSAID may optionally be administered as a sub-maximal amount.
摘要翻译：一种治疗与疼痛相关的症状并缓解与之相关的症状的方法，其包括对哺乳动物，包括人类，凡那酸VR-1拮抗剂或其药学上可接受的衍生物和NSAID或其药学上可接受的衍生物施用，其中所述VR- 1拮抗剂或所述NSAID可以任选地作为次最大量施用。

7. 发明授权

US08063078B2 Urea-compounds active as vanilloid receptor antagonists for the treatment of pain 失效
标题翻译：用作治疗疼痛的香草素受体拮抗剂的尿素化合物
公开(公告)号：US08063078B2
公开(公告)日：2011-11-22
申请号：US10489277
申请日：2002-09-13
申请人： Harshad Kantilal Rami , Mervyn Thompson
发明人： Harshad Kantilal Rami , Mervyn Thompson
IPC分类号： A61K31/4025 , A61K31/443 , C07D207/44 , C07D401/04
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14
摘要： Certain compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1, R2, P, P′, n, p, q, r and s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
摘要翻译：某些式（I）化合物或其药学上可接受的盐或其溶剂合物，其中R 1，R 2，P，P'，n，p，q，r和s如说明书中所定义，这样的化合物，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医药中的用途。

8. 发明申请

US20110059979A1 Piperidine/Cyclohexane Carboxamide Derivatives For Use as Vanilloid Receptor Modulators 审中-公开
标题翻译：哌啶/环己烷羧酰胺衍生物用作香草素受体调节剂
公开(公告)号：US20110059979A1
公开(公告)日：2011-03-10
申请号：US10568028
申请日：2004-08-12
申请人： Craig Jamieson , David Drysdale Miller , Harshad Kantilal Rami , Mervyn Thompson
发明人： Craig Jamieson , David Drysdale Miller , Harshad Kantilal Rami , Mervyn Thompson
IPC分类号： A61K31/506 , A61K31/501 , A61K31/4709 , A61K31/4545 , A61K31/454 , C07D403/02 , C07D401/02
CPC分类号： C04B35/632 , C07C311/46 , C07C317/40 , C07C2601/14 , C07D215/38 , C07D277/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, P, P′, X, m and n are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译：某些式（I）化合物或其药学上可接受的盐或溶剂合物，其中R 1，R 2，P，P'，X，m和n如说明书中所定义，制备该化合物的方法，这些化合物和这些化合物在医药中的应用。

9. 发明授权

US07531558B2 Carboxamide derivatives 有权
标题翻译：甲酰胺衍生物
公开(公告)号：US07531558B2
公开(公告)日：2009-05-12
申请号：US10545283
申请日：2004-02-12
申请人： Gregor James Macdonald , Darren Jason Mitchell , Harshad Kantilal Rami , Mervyn Thompson , Leontine Saskia Trouw , Susan Marie Westaway
发明人： Gregor James Macdonald , Darren Jason Mitchell , Harshad Kantilal Rami , Mervyn Thompson , Leontine Saskia Trouw , Susan Marie Westaway
IPC分类号： A61K31/4436 , C07D417/12
CPC分类号： C07D401/12 , C07D417/12
摘要： Compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein P, W, X, Y, R2, R3, r and s are as defined in the specification, processes for preparing such compounds, pharmaceutical compositions comprising such compounds and their use in therapy.
摘要翻译：式（I）化合物或其药学上可接受的盐或溶剂合物，其中P，W，X，Y，R 2，R 3，r和s如本说明书中所定义，制备此类化合物的方法，包含这些化合物的药物组合物及其在治疗中的应用。

10. 发明授权

US07528150B2 Urea derivatives having vanilloid receptor antagonist activity 失效
标题翻译：具有香草素受体拮抗剂活性的尿素衍生物
公开(公告)号：US07528150B2
公开(公告)日：2009-05-05
申请号：US10548133
申请日：2004-03-04
申请人： Gregor James MacDonald , Harshad Kantilal Rami , Mervyn Thompson
发明人： Gregor James MacDonald , Harshad Kantilal Rami , Mervyn Thompson
IPC分类号： C07D401/02 , A61K31/47
CPC分类号： C07D401/12 , C07D401/14
摘要： According to the invention there are provided compounds of formula (I) wherein R1, p, P, n, s, r, W, P′, t, R2 and q are as defined in the specification, processes for preparing them and their use in therapy.
摘要翻译：根据本发明，提供式（I）化合物，其中R 1，p，P，n，s，r，W，P'，t，R 2和q如说明书中所定义，其制备方法及其用途在治疗。

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