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公开(公告)号:US06642390B2
公开(公告)日:2003-11-04
申请号:US10193591
申请日:2002-07-11
申请人: Hartmuth C. Kolb , Cullen Cavallaro , Zhi-Cai Shi , Alexander Gontcharov , Zhi-Min Wang , Paul F. Richardson , Ramanaiah C. Kanamarlapudi
发明人: Hartmuth C. Kolb , Cullen Cavallaro , Zhi-Cai Shi , Alexander Gontcharov , Zhi-Min Wang , Paul F. Richardson , Ramanaiah C. Kanamarlapudi
IPC分类号: C07D24904
CPC分类号: C07D249/04
摘要: Disclosed is a one step method for preparing a 1,2,3-triazole carboxylic acid by treating an azide with a &bgr;-ketoester in the presence of a base.
摘要翻译: 公开了通过在碱存在下用β-酮酯处理叠氮化物来制备1,2,3-三唑羧酸的一步法。
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公开(公告)号:US20050282805A1
公开(公告)日:2005-12-22
申请号:US11151667
申请日:2005-06-13
申请人: Jon Hangeland , Mimi Quan , Joanne Smallheer , Gregory Bisacchi , James Corte , Todd Friends , Zhong Sun , Karen Rossi , Cullen Cavallaro
发明人: Jon Hangeland , Mimi Quan , Joanne Smallheer , Gregory Bisacchi , James Corte , Todd Friends , Zhong Sun , Karen Rossi , Cullen Cavallaro
IPC分类号: A61K31/00 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/538 , C07D231/12 , C07D233/54 , C07D233/68 , C07D233/90 , C07D235/10 , C07D235/14 , C07D249/08 , C07D249/12 , C07D263/32 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D413/02 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06 , C07D43/02
CPC分类号: C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
摘要: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要翻译: 本发明提供了治疗有需要的患者治疗有效量的至少一种式(I)或式(V)化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法: 其形式,其中变量A,L,Z,R 3,R 4,R 6,R 11, >,X 1,X 2和X 3如本文所定义。 式(I)的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶,因子Xa,因子XIa,因子IXa,因子VIIa和/或血浆激肽释放酶。 特别地,它涉及作为选择性因子XIa抑制剂的化合物。 本发明还提供了式I范围内的化合物,涉及包含这些化合物的药物组合物。
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3.
公开(公告)号:US06713514B1
公开(公告)日:2004-03-30
申请号:US09552477
申请日:2000-04-18
IPC分类号: A61K31195
CPC分类号: C07C323/42 , C07C237/30 , C07C237/38 , C07C2601/08 , C07C2601/14
摘要: N-(substituted)carbamoylaryl- and heteroaryl substituted aminopropanoic and butanoic acid compounds which are highly selective agonists for the PPAR-&ggr; receptor or prodrugs of agonists for the PPAR-&ggr; receptor, and are useful in the treatment of Type II diabetes (NIDDM). Specifically disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: Z is aryl or heteroaryl; n and m are 0, 1 or 2; A is a carboxylic acid or ester; or A is where D, F and G are hydrogen, (un)substituted amino, (un)substituted alkoxy, methylene or an (un)substituted sulfide; R4 is oxo, hydrogen, hydroxy, lower alkyl, lower alkoxy, cycloalkyl, keto, acyl, or sulfonyl; Y is hydrogen, (un)substituted amino, (un)substituted alkoxy, methylene, an (un)substituted sulfide, (un)substituted sulfonyl or an (un)substituted sulfoxide; and R5, R6 and R8 are hydrogen, lower alkyl, lower alkoxy, cycloalkyl, keto, acyl, or sulfonyl; or R5 and R6 together form a ring.
摘要翻译: 作为PPAR-γ受体的高选择性激动剂或PPAR-γ受体激动剂前药的N-(取代的)氨基甲酰基芳基和杂芳基取代的氨基丙酸和丁酸化合物,可用于治疗II型糖尿病(NIDDM) 。 具体公开的是下式的化合物或其药学上可接受的无毒盐,其中:Z是芳基或杂芳基; n和m是0,1或2; A是羧酸或酯; 或A是其中D,F和G是氢,(未)取代的氨基,(未)取代的烷氧基,亚甲基或(取代的)取代的硫醚; R 4是氧代,氢,羟基,低级烷基,低级烷氧基,环烷基,酮基,酰基, 或磺酰基; Y是氢,(未)取代的氨基,(未)取代的烷氧基,亚甲基,(未)取代的硫醚,(未)取代的磺酰基或(取代的)取代的亚砜; R 5,R 6和R 8是氢,低级烷基,低级烷氧基,环烷基,酮基,酰基或磺酰基; 或R 5和R 6一起形成环。
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