| 摘要 |
Amino acid amide compounds (I), are new. Amino acid amide compounds of formula (I), their optical isomers and acid addition salts are new. R1 = aryl, heteroaryl, 1-6C alkyl (optionally substituted by at least one aryl or heteroaryl), or (CO)-CR6R7-NR8R9; R2 = H or 1-6C alkyl; R3, R4 = 1-6C alkyl, or CR3R4 = 3-18 membered mono-, bi- or tri-cyclic ring containing at least one O, N or S heteroatom (optionally substituted by at least one halo, 1-6C alkyl or 1-6C alkoxy), OH, 1-6C trihaloalkyl, amino, alkylamino, dialkylamino or carboxy; n = 0, 1 or 2; Ar = aryl or heteroaryl; R5 = amino, guanidino or amidino optionally substituted by OH or 1-6C alkoxycarbonyl; R6 = aryl, heteroaryl, heterocycloalkyl, 3-8C cycloalkyl, or 1-6C alkyl (optionally substituted by at least one aryl, heteroaryl, heterocycloalkyl, cycloalkyl or carboxy); R7 = H or 1-6C alkyl, or R6 + R7 = 3-8C cycloalkyl; R8 = H or 1-6C alkyl; R9 = H or R9a; R9a = 1-6C alkyl (optionally substituted by aryl, carboxy, alkoxycarbonyl or carbamoyl), aryl, heteroaryl or sulfonyl substituted by cycloalkyl, heterocycloalkyl, aryl (optionally substituted by aryloxy or heteroaryloxy), or alkyl optionally substituted by aryl, heteroaryl, cycloalkyl, or heterocycloalkyl; heterocycloalkyl = 3-8 membered saturated monocyclic group containing 1-3 O, N or S heteroatoms (optionally substituted by at least one halo, 1-6C alkyl, 1-6C alkoxy, oxo, OH, 1-6C trihaloalkyl, or amino (optionally substituted by at least one 1-6C alkyl)); aryl = phenyl, biphenylyl or naphthyl (all optionally substituted by at least one halo, 1-6C alkyl, 1-6C alkoxy, oxo, OH, 1-6C trihaloalkyl, or amino (optionally substituted by at least one 1-6C alkyl)), and heteroaryl = 5-12 membered aromatic mono- or bi-cyclic group containing 1-3 O, N or S heteroatoms (optionally substituted by at least one halo, 1-6C alkyl, 1-6C alkoxy, oxo, OH, 1-6C trihaloalkyl, or amino (optionally substituted by at least one 1-6C alkyl)). An Independent claim is also claimed for the preparation of (I). |
