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2-Alkylamino-7,8-dihydropteridin-6(5H)-one and 2-alkylamino-8,9-dihydro-5H-pyrimido[4,5-b][1,4]diazepin-6(7H)-one derivatives
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
CHARRIER, JEAN-DAMIEN,DURRANT, STEVEN
申请号:
NZ59029709
公开号:
NZ590297A
申请日:
2009.06.23
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are 2-alkylamino-7,8-dihydropteridin-6(5H)-one and 2-alkylamino-8,9-dihydro-5H-pyrimido[4,5-b][1,4]diazepin-6(7H)-one derivatives as represented by the general formula (I) or a pharmaceutically acceptable salt thereof, wherein: Y is O or NR9 R1 is optionally substituted cycloalkyl or optionally substituted heterocycloalkyl R2 is H, alkyl, or cycloalkyl each of R3 and R4 is independently H, alkyl, cycloalkyl, aryl, or heteroaryl or R3 and R4 together with the carbon atom to which they are attached, form a cycloalkyl each of R5 and R6 is independently H, alkyl, cycloalkyl, aryl, or heteroaryl R7 is H or alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl, any of which is optionally substituted or R8 is optionally substituted alkyl R9 is H or alkyl or R2 and R9 together with the atoms to which they are attached, optionally form a 5- to 8-membered monocyclic ring containing additional 0 to 2 hetero atoms each independently selected from O, N, and S, wherein said monocyclic ring is optionally substituted with 0 to 4 groups each independently being alkyl, halo, alkoxy, or hydroxy and q is 0 or 1. Representative compounds include 9-cyclopentyl-5,7,7-trimethyl-2-(1-(1-methylpiperidin-4-yl)ethylamino)-8,9-dihydro-5H-pyrimido[4,5-b][1,4]diazepin-6(7H)-one, 2-(1-cyclohexylethylamino)-8-cyclopentyl-7-ethyl-5-methyl-7,8-dihydropteridin-6(5H)-one, 2-(4-(1-(8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)ethyl)piperidin-1-yl)acetonitrile. Further disclosed is a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier, adjuvant, or vehicle, for treating a proliferative disorder, a neurodegenerative disorder, an autoimmune disorder, an inflammatory disorder, or an immunologically mediated disorder in a patient, and particularly for treating melanoma, leukemia, lymphoma or cancer.
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