发明名称 PURIN DERIVATIVES FOR USE IN THE TREATMENT OF FAB-RELATED DISEASES
摘要 The invention is directed to the use of selected purine derivatives for the treatment of hyperproliferative diseases.
申请公布号 US2016136180(A1) 申请公布日期 2016.05.19
申请号 US201615001301 申请日期 2016.01.20
申请人 Boehringer Ingelheim International GmbH 发明人 Himmelsbach Frank;Mark Michael;Tadayyon Mohammad;Thomas Leo
分类号 A61K31/553;A61K31/551;A61K31/5513;A61K31/522;A61K31/55 主分类号 A61K31/553
代理机构 代理人
主权项 1. A method for treatment of a disease that responds to the inhibition of FAP comprising administering to a patient in need thereof a compound of formula (I), (II), (III), or (IV): wherein R1 denotes pyridinylmethyl, pyrimidinylmethyl, quinolinylmethyl, (2-oxo-1,2-dihydro-quinolinyl)methyl, isoquinolinylmethyl, quinazolinylmethyl, (4-oxo-3,4-dihydro-quinazolinyl)methyl, quinoxalinylmethyl, [1,5]naphthyridinylmethyl, (1H-perimidinyl)methyl, phenanthridinylmethyl, (11H-dibenzo[b,e]azepinyl)methyl, (dibenzo[b,f][1,4]oxazepinyl)methyl, (5H-dibenzo[b,e][1,4]diazepinyl)methyl or (imidazo[1,2-a]quinolinyl)methyl and the heterocyclic groups of the above-mentioned groups may be mono- or disubstituted by Ra, while the substituents may be identical or different and Ra denotes fluorine, chlorine, bromine, cyano, methyl, ethyl, propyl, isopropyl, cyclopropyl, phenyl, methoxy, ethyloxy, amino, methylamino, dimethylamino, pyrrolidino, piperidino, morpholino, piperazino or N-methylpiperazino, R2 denotes methyl, ethyl, propyl, isopropyl, cyclopropyl or phenyl and the methyl, ethyl, propyl and isopropyl group may be substituted by carboxy, methoxycarbonyl, ethyloxycarbonyl, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, pyrrolidinocarbonyl, piperidinocarbonyl, morpholinocarbonyl, piperazinocarbonyl or N-methylpiperazinocarbonyl, R3 denotes 2-buten-1-yl, 3-methyl-2-buten-1-yl, 2-butyn-1-yl, benzyl, fluorobenzyl, chlorobenzyl, bromobenzyl or cyanobenzyl and R4 denotes piperazino, homopiperazino, 3-(R)-amino-piperidin-1-yl, 3-(S)-amino-piperidin-1-yl, (2-amino-ethyl)-methylamino, (2-amino-2-methyl-propyl)-methylamino, ((R)-2-amino-propyl)-methylamino or ((S)-2-amino-propyl)-methylamino, or a tautomer, enantiomer or salt thereof, or a mixture thereof, wherein said disorder that responds to the inhibition of FAP is a wound healing disorder or acne.
地址 Ingelheim am Rhein DE