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标题翻译：因子XA与亚氨基和衍生物的抑制剂及其衍生物

公开(公告)号：KR1020020070385A

公开(公告)日：2002-09-06

申请号：KR1020027009662

申请日：2001-01-04

申请人： 주식회사 엘지생명과학

发明人： 강명균 , 박두희 , 권오환 , 김유니스은경 , 황광연 , 허용석 , 박태교 , 이태희 , 문광율 , 박종우 , 장혜경 , 이상구 , 이선화 , 박수경 , 이승학 , 박희동

IPC分类号： C07D213/04

CPC分类号： C07D207/27 , C07B2200/09 , C07C257/18 , C07C259/18 , C07C271/22 , C07C271/64 , C07C275/24 , C07C275/42 , C07C311/06 , C07C311/13 , C07C311/16 , C07C311/29 , C07C311/46 , C07C311/48 , C07C317/40 , C07C317/44 , C07C2601/02 , C07C2601/10 , C07D207/333 , C07D207/34 , C07D213/40 , C07D213/75 , C07D213/78 , C07D213/82 , C07D213/84 , C07D217/22 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08 , C07D249/12 , C07D263/22 , C07D265/10 , C07D275/02 , C07D277/56 , C07D333/34 , C07D333/38 , C07D401/10 , C07D401/12 , C07D403/10 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06

摘要： PURPOSE: Provided are a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amidinoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). Also, provided are a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for the treatment and the prevention of thrombosis disorders. CONSTITUTION: The novel compound of the formula(1) has a good FXa inhibition activity and consequently an excellent selectivity against trypsin and thrombin. In the formula(1), Ar is selected from the groups consisting of benzene, pyridine, thiophene, naphthalene and isoquinoline; G is selected from the groups consisting of R, F, Cl, Br, I, CN, OR, OCOR, CO2R and CONR2, where R represents H or a linear, branched, cyclic or branched cyclic alkyl group having 1 to 10 of carbon atoms; A is selected from the groups consisting of Al, A2, A3 and A4; D represents-NH2, or-CH2NH2; L is a simple linker and represents -(CH2)m-(m = 0, 1); P is selected from the groups consisting of phenyl, pyridine, pyrrole, furan, thiophene, oxazole, isoxazole, imidazole, 1, 2-diazole, thiazole, isothiazole, pyridazine(1, 2-diazine), pyrimidine, pyrazine(1, 4-diazine), naphthalene, quinoline, isoquinoline, benzofuran, benzothiophene, and indole; X is selected from the groups consisting of R, F, Cl, Br, I, CN, OR, COA COR, CONR2, NR2, NR((C=O) R), CF3, OCF3, SO2NR2, SONR2, SO2R, SOR, N ((C=O) R)2, imidazole, 1, 2-diazole, thiazole, isothiazole, pyridazine(= 1, 2-diazine), pyrimidine, pyrazine(= 1, 4-diazine), 1, 2, 3-triazole, 1, 2, 4-triazole, tetrazole, 1, 3, 5-triazine, (1, 2)-imidazoline-2-yl, N-methyl- (1, 2)-imidazoline-2-yl, and NHC (=NR) R; n represents a number of 0, 1 or 2; Q represents hydrogen or is selected from the groups consisting of phenyl, pyridine,pyrrole, furan, thiophene, oxazole, isoxazole, imidazole, 1, 2-diazole, thiazole, isothiazole, pyridazine(= 1, 2-diazine), pyrimidine, and pyrazine(= 1, 4-diazine), provided that when Q represents hydrogen, the substituents Y and Z are meant to be directly connected to P; and Y and Z are independently selected from the group consisting of R, F, Cl, Br, I, CN, OR, COA COR, CONR2, NR2, NR((C=O) R), N((C=O) R)2, CF3, OCF3, SO2NR2, SONR2, SOA SOR, imidazole, 1, 2-diazole, thiazole, isothiazole, pyridazine (=1, 2-diazine), pyrimidine, pyrazine (= 1, 4-diazine), 1, 2, 3-triazole, 1, 2, 4-triazole, tetrazole and 1, 3, 5-triazine.

摘要翻译：目的：提供与式（1）表示的芳基脒，特别是脒基芳基 - 环丙烷，脒基芳基甲基吡咯，脒基芳基 - 苯，脒基芳基 - 吡啶或脒基芳基 - 丙氨酸的化合物，其药学上可接受的盐，前药，水合物，其溶剂化物或异构体，其是凝血酶抑制剂，因子Xa（FXa）。此外，提供含有该化合物的药物组合物及其用作抗凝血剂的方法用于治疗和预防血栓形成障碍。构成：式（1）的新化合物具有良好的FXa抑制活性，因此对胰蛋白酶和凝血酶具有优异的选择性。在式（1）中，Ar选自苯，吡啶，噻吩，萘和异喹啉; G选自由R，F，Cl，Br，I，CN，OR，OCOR，CO 2 R和CONR 2组成的组，其中R表示H或具有1至10个碳的直链，支链，环状或支链的环状烷基原子; A选自由Al，A2，A3和A4组成的组; D表示-NH 2或-CH 2 NH 2; L是简单的接头，代表 - （CH 2）m - （m = 0,1）; P选自苯基，吡啶，吡咯，呋喃，噻吩，恶唑，异恶唑，咪唑，1,2-二唑，噻唑，异噻唑，哒嗪（1,2-diazine），嘧啶，吡嗪（1,4 二嗪），萘，喹啉，异喹啉，苯并呋喃，苯并噻吩和吲哚; X选自由R，F，Cl，Br，I，CN，OR，COA COR，CONR2，NR2，NR（（C = O）R），CF3，OCF3，SO2NR2，SONR2，SO2R，SOR组成的组，N（（C = O）R）2，咪唑，1,2-二噻唑，噻唑，异噻唑，哒嗪（= 1,2-二嗪），嘧啶，吡嗪（= 1,4-二嗪）（1,2） - 咪唑啉-2-基，N-甲基 - （1,2） - 咪唑啉-2-基，和NHC（= NR）R; n表示0,1或2的数; Q代表氢或选自苯基，吡啶，吡咯，呋喃，噻吩，恶唑，异恶唑，咪唑，1,2-二噻唑，噻唑，异噻唑，哒嗪（= 1,2-二嗪），嘧啶和吡嗪（= 1,4-二嗪），条件是当Q表示氢时，取代基Y和Z意在直接与P连接; 并且Y和Z独立地选自由R，F，Cl，Br，I，CN，OR，COA COR，CONR2，NR2，NR（（C = O）R），N（（C = O） R 2，CF 3，OCF 3，SO 2 NR 2，SONR 2，SOA SOR，咪唑，1,2-二噻唑，噻唑，异噻唑，哒嗪（= 1,2-二嗪），嘧啶，吡嗪（= 1,4-二嗪），2,3,3-三唑，1,2,4-三唑，四唑和1,3,5-三嗪。

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