| 摘要 |
There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0):and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl as defined herein; where said alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 0 to 3 R<9>; or is a member selected from the group consisiting of the following radicals: A<1>-NHC(=O)NH-A<2>-, A<1>-NHC(=O)O-A<2>-, A<1>-OC(=O)NH-A<2>-, A<1>-NHSO2NH-A<2>-, A<1>-NHC(=O)-A<2>-, A<1>-C(=O)NH-A<2>-, A<1>-NHSO2-A<2>-, A<1>-SO2NH-A<2>-, A<1>-(CH2)rO-A<2>-, A<1>-O(CH2)r-A<2>-, A<1>-(CH2)r-A<2>-, where A<1 >is aryl and A<2 >is aryl or pyridyl; where said aryl or pyridyl group is substituted with 0 to 3 R<9>; -B is oxazolinyl or isoxazolinyl; wherein said oxazolinyl and said isoxazolinyl may be optionally substituted with R<9>; R<2 >is hydrogen or methyl; R<3 >is taken together with R<4 >and the carbon and nitrogen atoms to which it is attached to form a pyrrolidinyl group substituted with 0 to 3 R<13>;and the remaining variables are as defined in the specification.
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