| 摘要 |
The present invention describes novel thiazolo[4,5-d]pyrimidines of formula (I), or a pharmaceutically acceptable salt thereof, wherein X is CR<4> or N; Y is selected from the group: S, O and NR<5>; R<1> is selected from the group: H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, Cl, F, Br, I, -CN, C1-5 haloalkyl, -NR<6>R<7>, -NR<6>COR<7>, -OR<8>, -SH, and -S(O)nR<9>; R<2> is selected from the group: -CR<10>R<11>R<12>, -NR<10a>R<11a>, -NHCR<10>R<11>R<12>, -OCR<10>R<11>R<12>, and phenyl, wherein the phenyl is substituted with 0-4 R<a>; R<3> is selected from the group: phenyl, pyridyl, pyrimidyl, napthyl, triazinyl, furanyl, quinolinyl, isoquinolinyl, thienyl, thiazolyl, pyrrolyl, oxazolyl, benzofuranyl, benzothienyl, benzothiazolyl, isoxazolyl, and pyrazolyl, and is substituted with 1 to 4 R<b> groups; R<4> is selected from the group: H, C1-4 alkyl, and C1-4 haloalkyl, halogen, NH2, NH(C1-4 alkyl), NH(C1-4 alkyl)2, CN, OR<8>; and R<5> is -CO(C1-4 alkyl) or -CO2(C1-4 alkyl), which are useful as CRF antagonists.
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