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    • 1. 发明申请
    • 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS
    • 作为VR1拮抗剂的2,3-取代的氟吡啶-4(3H) - 酮
    • WO2006100520A1
    • 2006-09-28
    • PCT/GB2006/050060
    • 2006-03-21
    • MERCK SHARP & DOHME LIMITEDBAYLISS, TracyBROWN, Rebecca ElizabethHOLLINGWORTH, Gregory JohnJONES, A. BrianMOYES, Christopher RichardROGERS, Lauren
    • BAYLISS, TracyBROWN, Rebecca ElizabethHOLLINGWORTH, Gregory JohnJONES, A. BrianMOYES, Christopher RichardROGERS, Lauren
    • C07D473/32C07D471/04C07D495/04C07D513/04A61K31/522A61P29/00
    • C07D473/18C07D471/04C07D495/04
    • 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 CH 2 ; when n is two or three, V is CH 2 , O or NR 5 ; 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 R 1 groups; and R 7 and R 8 are independently hydrogen, hydroxy, halogen or C 1-4 alkyl; 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, NR 2 R 3 or S(O) r NR 2 R 3 where NR 2 R 3 is as defined above, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, haloC 1-6 alkylthio,C 3-7 cycloalkyl, hydroxyC 1-6 alkyl, a five-membered heteroaromatic ring containing 1, 2or 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 VRl antagonists, including conditions such as depression, GERD, itch and urinary incontinence.
    • 式(I)的化合物,其中W为式(1); A是苯环,含有1,2或3个独立地选自O,N和S的杂原子的f元环杂芳环,条件是不存在不超过一个O或S原子,或含有1个或6个杂芳环 2或3个N原子; n为零,一,二或三; 当n为0或1时,V为CH 2 2; 当n为2或3时,V为CH 2,O或NR 5; 当V为CH 2时,由V形成的键和相邻碳环原子任选地与苯环稠合,含有1,2或3个独立地选自O,N和S的杂原子的五元杂芳环,条件是不再有 存在一个O或S,或含有1,2或3个N原子的六元杂芳环; 该环任选地被一个或多个R 1基团取代; R 7和R 8独立地是氢,羟基,卤素或C 1-4烷基; Z是苯环,含有一个,两个,三个或四个独立地选自O,N或S,至多一个杂原子是O或S的杂原子的五元杂芳环或含有一个,二个 或三个N原子,任选地被一个或多个选自卤素,羟基,氰基,硝基,NR 2 R 3或S(O) 其中NR 2 R 3如上所定义,C 1和R 2如上定义,其中R 1,R 2,R 3, C 1-6烷基,C 2-6链烯基,C 2-6亚炔基,卤代C 1-6烷基,C <亚 > 1-6个烷氧基,卤代C 1-6烷氧基,C 1-6烷硫基,卤代C 1-6烷硫基,C 3-7环烷基,羟基C 1-6烷基,含有独立选自O,N和S的1,2或3个杂原子的五元杂芳环,条件是不再有 存在一个O或S原子,或含有1,2或3个N原子的6元杂芳环; 或其药学上可接受的盐或N-氧化物; 包含它们的药物组合物; 用于治疗方法的化合物; 以及用于制备用于治疗作为VR1拮抗剂的疼痛的药物的化合物的使用,包括诸如抑郁症,GERD,瘙痒和尿失禁的病症。
    • 3. 发明申请
    • 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 LIMITEDBAYLISS, TracyBROWN, Rebecca, ElizabethBURKAMP, FrankJONES, A., BrianNEDUVELIL, Joseph, George
    • BAYLISS, TracyBROWN, Rebecca, ElizabethBURKAMP, FrankJONES, A., BrianNEDUVELIL, Joseph, George
    • A61K31/4545
    • C07D451/04C07D401/04
    • 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。