Patent ID: 6534650
Filing Date: 2003-03-18
Classification: A61K,C07C,C07D,C07K

Abstract:
An amine of Formula VHâ€”Yâ€”Gâ€”R â€ƒâ€ƒV wherein â€”Yâ€”Gâ€” is in whichr is 0, 1 or 2; Rg is (C1-C6)alkyl, (C3-C8)cycloalkyl, or â€”(CH2)pâ€”Lâ€”(CH2)qâ€”Tâ€²; Rp is (C1-C6)alkyl, (C3-C8)cycloalkyl, or â€”(CH2)pâ€”Lâ€”(CH2)qâ€”Tâ€²; where p is 0, 1, 2, 3, or 4; L is a bond, â€”Oâ€”, â€”Sâ€”, or â€”NHâ€”; q is 0, 1, 2 or 3; and Tâ€² is (C1-C4)alkyl, (C3-C8)cycloalkyl, â€”COOH, â€”CONH2, or Ar, where Ar is unsubstituted or substituted aryl, where aryl is phenyl, naphthyl, a 5- or 6-membered unsubstituted or substituted aromatic heterocyclic ring, having one or two heteroatoms which are the same or different and which are selected from sulfur, oxygen and nitrogen, or a 9- or 10-membered unsubstituted or substituted fused bicyclic aromatic heterocyclic group having one or more heteroatoms which are the same or different and which are selected from sulfur, oxygen and nitrogen; Ry is â€”CH2 â€”, â€”Oâ€”, â€”Sâ€”, or â€”NHâ€”; and Rz is a bond or, when taken with Ry and the three adjoining carbon atoms, forms a saturated carbocyclic ring of 5-8 atoms, one atom of which may be â€”Oâ€”, â€”Sâ€”, or â€”NHâ€”; â€”Gâ€”R is â€”C(O)â€”NHâ€”(CH2)sâ€”R, â€”CH2â€”NHâ€”(CH2)sâ€”R, â€”CH2â€”NHâ€”C(O)â€”R or â€”(CH2)tâ€”Oâ€”R in which s is 1 or 2 and t is 1, 2 or 3; and R is a 4-amidino-3-hydroxyphenyl group bearing 0, 1, 2 or 3 fluoro substituents.