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    • 68. 发明公开
    • METHODS FOR MAKING 4-TETRAZOLYL-4-PHENYLPIPERIDINE COMPOUNDS
    • 制备4-四唑-4-基苯基哌啶化合物的方法
    • EP1709029A2
    • 2006-10-11
    • EP05712568.4
    • 2005-01-31
    • EURO-CELTIQUE S.A.
    • BROWN, KevinDOYLE, Timothy, J.WHITEHEAD, John, W.,F.
    • C07D401/04C07D211/64C07D257/04C07D307/22C07C237/20
    • C07D211/64C07D257/04C07D307/22C07D401/04
    • Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula (I), where Ar1 is -C3-C8 cycloalkyl, phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Ar2 is phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Z1 and Z2 are each independently a -(C1-C4 alkyl) group; R1 is -(CH2)nC(O)N(R3)(R4) where R3 and R4 are each independently H or -(C1-C4 alkyl); R2 is halogen, -C1-C3 alkyl, -O-(C1-C3 alkyl), -NH(C1-C3 alkyl) or -N(C1-C3 alkyl)2; n is an integer ranging from 1 to 4; m is an integer ranging from 0 to 4; and, in certain embodiments, the phenyl moiety attached to the 4-position of the piperidine ring of a compound according to Formula (I) can be optionally substituted with one or mor R2 groups.
    • 公开了用于制备式(I)的4-四唑基-4-苯基哌啶化合物的方法,组合物和中间体,其中Ar1是-C3-C8环烷基,苯基,萘基,蒽基,菲基或 - (5-7 - 元)杂芳基,各自未被取代或被一个或多个R 2基团取代; Ar 2是苯基,萘基,蒽基,菲基或 - (5-7元)杂芳基,各自未被取代或被一个或多个R 2基团取代; Z 1和Z 2各自独立地为 - (C 1 -C 4烷基)基团; R 1是 - (CH 2)n C(O)N(R 3)(R 4),其中R 3和R 4各自独立地为H或 - (C 1 -C 4烷基)。 R2为卤素,-C1-C3烷基,-O-(C1-C3烷基), - NH(C1-C3烷基)或-N(C1-C3烷基)2; n是1至4的整数; m是0至4的整数; 并且在某些实施方案中,连接到式(I)化合物的哌啶环的4-位的苯基部分可以任选地被一个或多个R 2基团取代。
    • 70. 发明公开
    • THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
    • 治疗疼痛的治疗药物
    • EP1648880A1
    • 2006-04-26
    • EP04779721.2
    • 2004-07-30
    • Euro-Celtique S.A.
    • KYLE, Donald, J.SUN, Qun
    • C07D401/04A61K31/495A61P1/04A61P13/02
    • C07D401/04C07D213/74C07D213/85
    • Compounds of formulae (I) and (II) where X is S or O and Ar2, R1, R2, R3, R8, n, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a '3-substituted Pyridyl Compound'), compositions comprising an effective amount of a 3-substituted Pyridyl Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndrome, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a 3-substituted Pyridyl Compound are disclosed herein.
    • 其中X是S或O和Ar 2,R 1,R 2,R 3,R 8,n,m和t的式(I)和(II)化合物或其药学上可接受的盐('3-取代的吡啶基 化合物'),包含有效量的3-取代的吡啶基化合物的组合物,以及用于治疗或预防疼痛,尿失禁,溃疡,炎性肠病,肠易激综合征,成瘾症,帕金森病,帕金森病, 焦虑症,癫痫症,中风,惊厥,瘙痒症状,精神病,认知障碍,记忆缺陷,脑功能受限,亨廷顿舞蹈症,肌萎缩侧索硬化症,痴呆,视网膜病,肌肉痉挛,偏头痛,呕吐,运动障碍或抑郁症 在动物中给予有需要的动物有效量的本发明公开的3-取代的吡啶基化合物。