Modified aminoacids, pharmaceuticals containing these compounds and method for their production

• Main Authors: HALLERMAYER, GERHARD, EBERLEIN, WOLFGANG, RUDOLF, KLAUS, PIEPER, HELMUT, DOODS, HENRI, WIENEN, WOLFGANG, ENGEL, WOLARD, ENTZEROTH, MICHAEL
• Format: Patent
• Language: English; French; German
• Published: 23.07.2008
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TESTING

Modified aminoacids of formula RC(=O)ZC(R11)((C=O)m(CH2)nR2)C(=X)ANR3R4 (I), their tautomers, diastereomers, enantiomers, mixtures and salts are new. R = 1-7C n-alkyl (optionally ~w-substituted), 1-6C n-alkylamino (optionally N-substituted) etc.; X = O or H; Z = CH2 or NR1; R1 = H, alkyl or phenylalkyl; R11 = H, 1-3C alkyl, 2-4C alkoxycarbonyl or benzyl; n = 1 or 2, or may be 0 if m = 1; m = 0 or 1; R2 = Ph, 1- or 2- naphthyl, 1,2,3,4-tetrahydro-1-naphthyl, 1H-indol-3-yl, 1-(methyl, formyl or t-butoxycarbonyl)-1H-indol-3-yl, 4-imidazolyl etc. (all optionally C-substituted); A = a direct bond or NR8CHR9CO; R8+R9 = (CH2)3; or R8 = H, alkyl or phenylalkyl; R9 = H or 1-5C alkyl, optionally ~w substituted if unbranched; R3 = H, 1-7C alkyl (optionally ~w-substituted) or phenyl or pyridinyl (optionally C-substituted); R4 = H or 1-3C alkyl (optionally substituted by Ph or pyridinyl).