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11.发明公开ALKYNYL CONTAINING HYDROXAMIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MATRIX METALLOPROTEINASE (MMP) INHIBITORS / TNF-ALPHA CONVERTING ENZYME (TACE) INHIBITORS 有权炔基异羟肟取代的衍生物，它们的制备和它们作为基质金属蛋白酶（MMP）抑制剂/ TNF-ALPHA转化酶（TACE）抑制剂
公开(公告)号：EP1147085A1
公开(公告)日：2001-10-24
申请号：EP00904569.1
申请日：2000-01-27
发明人： LEVIN, Jeremy, Ian , VENKATESAN, Aranapakam, Mudumbai , CHEN, James, Ming , ZASK, Arie , SANDANAYAKA, Vincent, Premarana , DU, Mila, Ti , BAKER, Jannie, Lea
IPC分类号： C07D211/66 , A61K31/445 , C07D309/08 , A61K31/35 , C07D401/06 , C07D409/06 , C07D401/12 , C07D413/04 , C07D407/06 , A61P19/00 , A61P19/02
CPC分类号： C07D309/08 , A61K31/351 , A61K31/435 , A61K31/445 , A61K31/496 , C07D211/60 , C07D211/62 , C07D211/66
摘要： Compounds of formula (I) wherein R1 is hydrogen, aryl, heteroaryl, alkyl of 1-8 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 3-6 carbon atoms, or -C4-C8-cycloheteroalkyl; R2 and R3 are hydrogen, alkyl of 1-6 carbon atoms, -CN, or CCH; R8, R9, R10 and R11 are hydrogen, aryl or heteroaryl, cycloalkyl of 3-6 carbon atoms, -C4-C8-cycloheteroalkyl, alkyl of 1-18 carbon atoms, alkenyl of 2-18 carbon atoms, alkynyl of 2-18 carbon atoms; with the proviso that one of the pairs R8 and R9, R9 and R10 or R10 and R11, together with the carbon atom or atoms to which they are attached, form a cycloalkyl ring of 3-6 carbon atoms, or a -C4-C8-cycloheteroalkyl ring; R12 is hydrogen, aryl or heteroaryl, cycloalkyl of 3-6 carbon atoms; -C4-C8-cycloheteroalkyl, or alkyl of 1-6 carbon atoms; A, X are O, S, SO, SO2, NR7, or CH2; Y is aryl or heteroaryl, with the proviso that A and X are not bonded to adjacent atoms of Y; and n is 0-2; or a pharmaceutically acceptable salt thereof; useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
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公开(公告)号：EP0805813A1
公开(公告)日：1997-11-12
申请号：EP96902143.0
申请日：1996-01-16
CPC分类号： C07D487/04
摘要： Tricyclic diazepines of Formula (I) wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
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公开(公告)号：EP0804438A1
公开(公告)日：1997-11-05
申请号：EP96903698.0
申请日：1996-01-16
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14
摘要： Tricyclic compound of general formula (I) as defined herein which exhibit antagonist activity at V1 and/or V2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.
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