Patent ID: 7115592

Claim:
A compound of the formula (I): wherein * designates a chiral carbon atom; R 1 is H, amino, or methylsulfanyl; R 2 is H, methyl, halo, —N(R 5 ) 2 , hydroxy, or protected hydroxy; R 3 is independently methyl, hydroxymethyl, halomethyl, or protected hydroxymethyl; R 4 is selected from: (i) C 1 to C 10 alkyl, (ii) C 2 to C 10 alkenyl, or, (iii) C 2 to C 10 alkynyl, (iv) C 3 –C 8 cycloalkyl, (v) aryl, (vi) heteroaryl, (vii) C 7 –C 14 arylalkyl, (viii) heteroarylalkyl, (ix) —CH 2 OH, (x) —CH 2 OR 5 (xi) —CH 2 C(O)R 5 , (xii) —CH 2 R 6 , (xiii) —CH 2 OC(O)R 5 (xiv) —CH 2 OC(O)CH(R 7 )(NHR 8 ), (xv) —CH 2 NR 9 R 10 , (xvi) —CH 2 CN, (xvii) —CO 2 R 5 (xviii) —CH 2 CH 2 OH, (xix) —CH 2 CH 2 OR 5 (xx) —CH 2 CH 2 OC(O)R 5 (xxi) —CH 2 CH 2 OC(O)CH(R 7 )(NHR 8 ), (xxii) —CH 2 SH, (xxiii) —C(O)H, (xxiv) —CH 2 CO 2 R 9 , (xxv) —CH 2 SO 3 H, (xxvi) —CH 2 CH 2 SO 3 H, (xxvii) —CH 2 CH 2 PO 3 H 2 , (xxviii) —CH 2 CH 2 OCH 2 PO 3 H 2 , (xxix) —CH 2 OPO 3 H 2 , (xxx) —OCH 2 PO 3 H 2 , (xxxi) —OH, (xxxii) —OR 10 (xxxiii) —NH 2 , (xxxiv) —NR 11 R 12 , (xxxv) —SH, (xxxvi) —SR 5 , (xxxvii) —SCN, (xxxviii) —N 3 , (xxxix) —CN, (xl) —CONR 11 R 12 (xli) —CH 2 CONR 11 R 12 (xlii) —NHOH, (xliii) —NHOR 5 , (xliv) —NO, (xlv) —NO 2 , (xlvi) —NHNR 11 R 12 (xlvii) 2-halovinyl, (xlviii) 3,3,3-trifluoropropenyl, (xlix) C 1 –C 10 2-(alkoxycarbonyl)ethenyl, (1) 2-carboxyethenyl, (li) 2-cyanoethenyl, (lii) difluoromethyl, (liii) trifluoromethyl, (liv) 2,2,2-trifluoroethyl, (lv) 2-haloethyl; and (lvi) —CH 2 N 3 ; X independently is oxygen, sulfur, or a bond; Z independently is hydroxy, an ester or amide; R 5 is independently H, C 1 –C 10 alkyl or a protecting group; R 6 is F, Cl, Br or I; R 7 is the side chain of any of the unprotected or N-protected α-amino acids; R 8 is H or —C(O)CH(R 7 )(NH 2 ); R 9 and R 10 are independently selected from H, C 1 –C 10 alkyl, carboxyalkyl, aminoalkyl, and C 2 –C 10 alkenyl, or both together form a cycle with or without participation of heteroatom; and R 11 and R 12 are independently selected from H, C 1 to C 10 alkyl, C 3 –C 8 cycloalkyl, heteroaryl and C 7 –C 12 arylalkyl, or both together form a cycle with or without participation of heteroatom; and salts and solvates thereof.