发明名称 4-aminoquinazolin-2-yl-1-pyrrazole-4-carboxylic acid compounds as prolyl hydroxylase inhibitors
摘要 Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.;
申请公布号 US8796263(B2) 申请公布日期 2014.08.05
申请号 US201113816747 申请日期 2011.08.12
申请人 Janssen Pharmaceutica NV 发明人 Rabinowitz Michael H.;Rosen Mark D.;Tarantino Kyle T.;Venkatesan Hariharan
分类号 A61K31/55;A61K31/517;A61K31/54;C07D401/00;C07D413/00;C07D243/08;C07D403/00 主分类号 A61K31/55
代理机构 代理人
主权项 1. A compound of the formula (I): wherein: n is 0-3 R1 is a member independently selected from the group consisting of halo, —O—Rc, —C1-4alkyl, cyclohexyl, phenyl optionally substituted with —C1-4alkyl, benzyl optionally substituted with —C1-4alkyl, and —NRaRb; Ra is H and Rb is benzyl optionally substituted with —C1-4alkyl, or Ra and Rb are taken together with the nitrogen to which they are attached to form a piperidine ring; Rc is cyclohexyl, phenyl optionally substituted with one or more Rd members; Rd is a member independently selected from the group consisting of —H, halo, and —C1-4alkyl; R2 is a member independently selected from the group consisting of —H, and —C1-4alkyl, R3 is a member independently selected from the group consisting of —H, —C1-4alkyl optionally substituted with —OCH3 or —N(C1-4alkyl)2, cyano, —SO2CH3, tetrahydropyran, —(CH2)mC3-8cycloalkyl, —(CH2)mphenyl optionally substituted with one or more halo, or —C1-4alkyl; m is 0-1; R2 and R3 can be taken together with the nitrogen to which they are attached to form a 4 to 7 membered heterocycloalkyl ring optionally containing O, N, S optionally substituted with —OH, cyano, halo, —N—C(O)C1-4alkyl, and —C1-4alkyl; and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof.
地址 Beerse BE