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    • 1. 发明申请
      WO2004046133A1 AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 审中-公开
    • AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN
    • AMINO-HETEROCYCLES作为VR-1拮抗剂治疗疼痛
    • WO2004046133A1
    • 2004-06-03
    • PCT/GB2003/004969
    • 2003-11-14
    • MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
    • BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
    • C07D401/12
    • C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04
    • the present invention provides a compound of formula (I): wherein V represents NR 5 , O, S, SO or S(O) 2 ; W and X each independently represent CH or N; Y represents N, CH or C-Ar 2 , with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar 2 , with the proviso that when Y is N or CH then Z is C-Ar 2 , and with the further proviso that when Y is C-Ar 2 then Z is CH; Ar 1 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; Ar 2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R 1 represents halogen, hydroxy, oxo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkoxy, C 3-5 cycloalkylC 1-4 alkyl, cyano, nitro, SR 6 , SOR 6 , SO 2 R 6 , COR 6 , NR 3 COR 6 , CONR 3 R 4 , NR 3 SO 2 R 6 , SO 2 NR 3 R 4 , -(CH 2 ) m carboxy, esterified -(CH 2 ) m carboxy or -(CH 2 ) m NR 3 R 4 ; R 2 represents hydrogen, halogen, hydroxy, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; R 3 and R 4 are each independently hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl or fluoroC 1-6 alkyl; or R 3 and R 4 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 C 1-4 alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O) 2 , or NR 5 ; R 5 represents hydrogen, C 1-4 alkyl, hydroxyC 1-4 alkyl or C 1-4 alkoxyC 1-4 alkyl; R 6 represents hydrogen, C 1-6 alkyl, fluoroC 1-6 alkyl, C 3-7 cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; 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.
    • 本发明提供式（I）化合物：其中V表示NR 5，O，S，SO或S（O）2; W和X各自独立地表示CH或N; Y表示N，CH或C-Ar2，条件是W，X和Y中至少一个，但不超过两个为N; Z表示CH或C-Ar2，条件是当Y为N或CH时，则Z为C-Ar2，进一步条件是当Y为C-Ar 2时，Z为CH; Ar 1表示含有选自氮，氧和硫的一个，两个，三个或四个杂原子的稠合的9或10元杂双环体系，其中所述环系中的至少一个环是芳族的; Ar2表示任选稠合和取代的选自苯基，吡啶基，嘧啶基和哒嗪基的芳环; R 1表示卤素，羟基，氧代，C 1-6烷基，C 2-6烯基，C 2-6炔基，卤代C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，羟基C 1-6烷氧基，C 3-7环烷基，C 3-7环烷氧基 ，C 3-8环烷基C 1-4烷基，氰基，硝基，SR 6，SOR 6，SO 2 R 6，COR 6，NR 3 COR 6，CONR 3 R 4，NR SO 2 R 6，SO 2 NR 3 R 4， - （CH 2）m羧基，酯化 - （CH 2）m羧基或 - （CH 2）m NR 3 R 4; R 2表示氢，卤素，羟基，C 1-6烷基，卤代C 1-6烷基，C 3-7环烷基，C 1-6烷氧基，卤代C 1-6烷氧基，未取代的苯基或被一个或两个选自卤素，C 1-6烷基，卤代C C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R 3和R 4各自独立地为氢，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基或氟C 1-6烷基; 或R 3和R 4并且它们所连接的氮原子一起形成4至7个环原子的杂脂肪族环，任选地被一个或两个选自羟基或C 1-4烷氧基的基团取代，该环可任选地被 含有所述环原子之一为氧或硫原子，S（O），S（O）2或NR 5; R 5表示氢，C 1-4烷基，羟基C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 6表示氢，C 1-6烷基，氟C 1-6烷基，C 3-7环烷基，未取代的苯基或被一个或两个选自卤素，C 1-6烷基，卤代C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或C 1-6烷基的基团取代的苯基 haloC1-6alkoxy; m为零或1至4的整数; n为0或1至3的整数; 或其药学上可接受的盐，N-氧化物或其前药; 包含它的药物组合物; 其用于治疗方法; 使用它来制造用于治疗VR-1相关病症的药物，例如其中疼痛和/或炎症占优势的病症; 和治疗方法
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明申请
      WO2005047279A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
    • SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN
    • 用作治疗疼痛的VANILLOID-1受体拮抗剂的含有NITRUTED的含六聚氨基甲酰胺的氨基酸
    • WO2005047279A1
    • 2005-05-26
    • PCT/GB2004/004719
    • 2004-11-09
    • MERCK SHARP & DOHME LIMITED , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
    • HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
    • C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
    • C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
    • The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, hydroxyC 1- 4 alkyl, cyano, hydroxy, C 1-4 cycloalkoxy, C 1-4 alkylthio, haloC 1-4 alkoxy, nitro, Q, (CH 2 ) p Q, NR 2 R 3 , -(CH 2 ) p NR 2 R 3 and -O(CH 2 ) p NR 2 R 3 ; 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, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, 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 C 1-4 alkyl; each R 2 and R 3 is chosen from H and C 1-4 alkyl, or R 2 and R 3 , 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 C 1-4 alkyl 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.
    • 本发明提供式（I）化合物：YJ-NH-Z其中：Y是喹啉或异喹啉，其任选地被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基 卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，C 3-5烃基，C 1-4烷氧基，羟基C 1-4烷基，氰基，羟基，C 1 （CH 2）pQ，NR 2 R 3， - （CH 2）p NRR R 3和-O（CH 2）p NRR 2，其中R 1，R 2， > - [R <3>; 其中J在NH和Y彼此间位置取代; Z是任选被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基的取代基取代的苯基或吡啶基; Q是苯基，含有一个，两个，三个或四个选自O，N和S，至多一个杂原子是O或S的杂原子的五元杂环，或含有一个，两个或三个氮的六元杂环 任选被C 1-4烷基取代的原子; 每个R 2和R 3选自H和C 1-4烷基，或R 2和R 3与它们所连接的氮原子一起可以形成任选含有 氧原子或另外的氮原子，该环任选被C 1-4烷基或Q取代; p为1,2或3; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗方法; 使用它制造药物; 以及使用它来治疗需要施用VR1拮抗剂例如疼痛，咳嗽，GERD和抑郁症的疾病的方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      WO2006038041A1 BESYLATE SALTS OF SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
    • BESYLATE SALTS OF SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN
    • 作为VANILLOID-1受体拮抗剂治疗疼痛的六成分氨基酸杂合物的乙酸盐
    • WO2006038041A1
    • 2006-04-13
    • PCT/GB2005/050172
    • 2005-10-04
    • Merck Sharp & Dohme Limited , Merck & Co., Inc. , CAI, Dongwei , JONES, A., Brian
    • CAI, Dongwei , JONES, A., Brian
    • C07D401/04 , C07D401/14 , C07D471/04 , C07D403/04 , A61K31/4725 , A61P43/00
    • C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04
    • The present invention provides a compound of formula I: Y-J-NH-Z (I) 10 wherein: Y is a quinoline or isoquinoline optionally substituted wit h one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two 15 substituents in dependently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, hydroxyC 1-4 alkyl, cyano, hydroxy, C 1-4 cycloalkoxy, C 1-4 alkylthio, haloC 1-4 alkoxy, nitro, Q, (CH 2 ) p Q, -NR 2 R 3 , -(CH 2 ) p NR 2 R 3 and -O(CH 2 ) p NR 2 R 3 ; 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 20 from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, 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 C 1-4 alky l; each R 2 and R 3 is chosen from H and C 1-4 alkyl, or R 2 and R 3 , together with the nitrogen atom to 25 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 C 1-4 alkyl or Q; p is 1, 2 or 3; as the besylate salt; 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 30 a VR1 antagonist such as pain, cough, GERD and depression.
    • 本发明提供式I的化合物：YJ-NH-Z（I）10其中：Y是喹啉或异喹啉，任选地被一个或两个独立地选自羟基，卤素，卤代C 1-4的取代基取代， 烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选地被一个或两个15个取代基取代，所述取代基依赖性地选自羟基，卤素，卤代C 1-4 - 烷基，C 1-4 烷基，C 3-5环烷基，C 1-4烷氧基，羟基C 1-4烷基，氰基，羟基，C 1 -C 4烷基， 1-4个环烷氧基，C 1-4烷硫基，卤代C 1-4烷氧基，硝基，Q，（CH 2 2） Q 2，-NR 2 R 3， - （CH 2）n， NR 2 R 3和-O（CH 2 CH 2）n NR 2 R 2 3 ; 其中J在NH和Y彼此间位置取代; 并且Z是任选地被一个或两个独立地选自20的取代基取代的苯基或吡啶基，所述取代基独立地选自20，卤素，C 1-4烷基，C 1-4烷基，C 1 -4个烷氧基，卤代C 1-4烷氧基，硝基和氨基; Q是苯基，含有一个，两个，三个或四个选自O，N和S，至多一个杂原子是O或S的杂原子的五元杂环，或含有一个，两个或三个氮的六元杂环 任选被C 1-4烷基取代的原子; 每个R 2和R 3选自H和C 1-4烷基，或R 2和R 2 它们连接的氮原子与它们所连接的氮原子一起可以形成任选地含有氧原子或另外的氮原子的六元环，该环任选被C 1 -4个烷基或Q; p为1,2或3; 作为苯磺酸盐; 包含它的药物组合物; 其用于治疗方法; 使用它制造药物; 以及使用它来治疗需要给予VR1拮抗剂30例如疼痛，咳嗽，GERD和抑郁症的疾病的方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO2005051390A1 E-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN 审中-公开
    • E-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN
    • E-FLOROR-4-（PYRIDIN-2-YL） - 哌啶-1-羧酰胺衍生物及其相关化合物，其调节VANILLOID-1受体（VR1）用于治疗疼痛的功能
    • WO2005051390A1
    • 2005-06-09
    • PCT/GB2004/004538
    • 2004-10-27
    • MERCK SHARP & DOHME LIMITED , BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
    • BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
    • A61K31/4545
    • C07D451/04 , C07D401/04
    • Compounds of formula (I): wherein: A 1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A 2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from 0, N and S, at most one heteroatom being O or S; L is a bond or C 1-6 alkylene; R 1 and R 2 independently chosen from hydrogen and C 1-6 alkyl or R l and R 2 may, together, form a methylene or ethylene bridge; W is halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; X is O, S or NR 3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A 2 ; Y is a bond, C 1-4 alkylene, NH or NH(CH 2 ) 1-3 ; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1; 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).
    • 式（I）的化合物：其中：A 1是苯基，含有一个，两个或三个氮原子的六元芳族杂环，或含有至多四个选自O，N和S的杂原子的五元芳族杂环 至多一个杂原子是O或S; A 2是苯基，含有一个，两个或三个氮原子的六元芳族杂环，或含有至多四个选自0，N和S的杂原子的五元芳族杂环，最多一个杂原子是O或S ; L是键或C1-6亚烷基; R 1和R 2独立地选自氢和C 1-6烷基或R 1和R 2可以一起形成亚甲基或亚乙基桥; W是卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; X是O，S或NR 3或X，连同其所连接的原子，Y与A 2一起形成不饱和五元环; Y是键，C1-4亚烷基，NH或NH（CH2）1-3; 或其药学上可接受的盐; 其它取代基如权利要求1中所定义; 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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