发明名称 SUBSTITUTED PYRIMIDINES
摘要 The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
申请公布号 US2014349972(A1) 申请公布日期 2014.11.27
申请号 US201214346513 申请日期 2012.09.19
申请人 MERCK SHARP & DOHME CORP 发明人 Dang Qun;Zhou Changyou;Zou Wuxin;Hua Yuxia
分类号 C07F9/6558 主分类号 C07F9/6558
代理机构 代理人
主权项 1. A compound of formula I or pharmaceutically acceptable salts thereof: R1 is a heteroaryl selected from isoxazolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, pyridinyl, pyradizinyl, and pyrimidinyl; R2 and R3 are each independently chosen from hydrogen, hydroxy, —OR, —OCOR, —OCOOR, —OCONHR, and C1-6alkyl; X is selected from —(C0-3alkyl)PO(R′)OR, —(C0-3 alkyl)PO(OR)2, —(C0-3alkyl)PO(NRR)2, —SO3R, —(C0-3 alkyl)PO(C1-10alkyl)OR, —(C0-3 alkyl)PO(C3-10cycloalkyl)OR,(C0-3alkyl)PO(H)OR, —(C0-3alkyl)PO(NHCR′R″COOR)2 and —COOR; R is independently selected from hydrogen, C1-10 alkyl, —C1-5 alkylaryl, —CR′R′—OCO—C1-10 alkyl, and —CR′R′—OCO—O—C1-10 alkyl; R′ and R″ are independently selected from hydrogen and C1-10 alkyl; L is chosen from a bond, —CONR4—, —NR4CO—, aryl, and heteroaryl; D is chosen from a bond, aryl, and heteroaryl, provided that when L is a bond then D is aryl or heteroaryl; R4, R6, and R7 are each independently selected from hydrogen,halogen,carboxyl C0-10 alkyl,C1-10 alkyl,C2-10 alkenyl,C2-10 alkynyl,C1-10 alkenylamino,C1-10 alkyl(oxy)0-1 carbonylC1-10 alkyl,aryl C0-10 alkyl(oxy)0-1 carbonylC1-10 alkyl,C3-8 cycloalkyl C0-10 alkyl(oxy)0-1carbonyl C1-10 alkyl,(C3-8)heterocyclyl C0-10 alkyl(oxy)0-1 carbonyl C1-10 alkyl,(C3-8)heterocycloalkyl C0-10 alkyl(oxy)0-1 carbonyl C1-10 alkyl,aryl(oxy)0-1C0-10 alkyl,C3-8 cycloalkyl(oxy)0-1 C0-10 alkyl,C3-8 heterocyclyl(oxy)0-1 C0-10 alkyl,C3-8 heterocycloalkyl (oxy)0-1C0-10 alkyl,C1-10 alkoxyl,arylC1-10 alkoxyl, andhydroxyC0-10alkyl; wherein R1, R2, R3, R4, R6, R7, and D are optionally substituted with 1, 2, or 3 substituent R5 chosen from: halogen,(carbonyl)0-1C1-10 alkyl,(carbonyl)0-1C2-10 alkenyl,(carbonyl)0-1 C2-10 alkynyl,C1-10 alkylcarbonyl,C2-10 alkenylcarbonyl,C2-10 alkynylcarbonyl,aryl C0-10 alkyl,(C3-8)heterocyclyl C0-10 alkyl,C3-8 cycloalkyl C0-10 alkyl,(C3-8)heterocycloalkyl C0-10 alkyl,C1-4acylamino C0-10 alkyl,C0-10 alkylamino C0-10 alkyl,arylC0-10 alkylamino C0-10 alkyl,C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,C3-8 heterocycloalkyl C0-10 alkylamino C0-10 alkyl,C1-10alkyloxy C0-10alkyl,(C1-10 alkyl)2aminocarbonyloxy,hydroxy C0-10alkyl,C1-10 alkylsulfonyl,C1-10 alkylsulfonylamino,aryl C1-10 alkylsulfonylamino,C3-8 heterocyclyl C1-10 alkylsulfonylamino,C3-8 heterocycloalkyl C1-10 alkylsulfonylamino,C3-8 cycloalkyl C1-10 alkylsulfonylamino,cyano,nitro,perfluoroC1-6alkyl, andperfluoroC1-6alkoxy; wherein R5 is optionally substituted with 1, 2, or 3 substituents chosen from hydrogen, hydroxy, (C1-6)alkoxyl, halogen, CO2H, CN, O(C═O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, —O(0-1)(C1-10)perfluoroalkyl, and NH2; and provided that when X is —COOR then L is isoxazoldiyl and D is phenyl.
地址 RAHWAY NJ US