3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic and / or immunostimulatory activity
LEBLOND, Bertrand,BEAUSOLEIL, Eric,TAVERNE, Thierry,DONELLO, John E.
申请号：
ES06719422
公开号：
ES2565236T3
申请日:
2006.01.25
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound represented by the following Formula 1 or a pharmaceutically acceptable salt thereof: ** Formula ** wherein: R1 and R2 form a saturated or unsaturated 5 or 6-membered ring together with the nitrogen atom, optionally including ring one or two additional heteroatoms independently selected from N, O and S, the ring being optionally substituted with one or two groups / atoms COOH, CH2OH, OH, B (OH) 2, halogen, cyano or C1-6 alkyl, or one being attached or two carbon atoms of the ring to an oxygen atom to form a keto group, and the ring being optionally condensed with a 5 or 6-membered aromatic or non-aromatic ring that optionally includes one or two heteroatoms selected from N, O and S ； each R3 is H, or one R3 is H and the other R3 is benzyl, benzyl substituted with monohalogen, dihalogen, methyl or methoxy, cyclohexyl, C1-7 alkyl, COR7 or COOR7； R7 is C1-15 alkyl, benzyloxy, phenyl, methoxyphenyl, phenyl substituted with monohalogen or dihalogen, 2-hydroxy-1- phenylethyl, or C1-20 alkyl substituted with NH2, NHCO-C1-15 alkyl or NHCOO-C1-15 alkyl ； R4 is H or COR8； R8 is C1-6 alkyl； wavy lines represent bonds connected to carbons that have an R or S configuration； the dotted lines represent an optional bond, with the proviso that the ring containing the dotted lines is aromatic； m, n and q are whole numbers independently selected from 0, 1, 2 and 3, with the proviso that the sum of m, n and q is 2 or 3； W, X and Y each independently represent CH, CR5, CR6 or a heteroatom selected from N, O and S, with the proviso that when the sum of m, n and q is 2, one or two of W, X and Y is a heteroatom, and when the sum of m, n and q is 3, none or one of W, X and Y is a heteroatom； s is 0, except when X is N, in which case s is 0 or 1； R5 and R6 are independently selected from H, halogen, C1-6 alkyl, halogen substituted C1-6 alkyl, C1-6 alkoxy, C1-3 thioxy and phenyl, or R5 and R6, together with the atoms to which they are attached , form a carbocyclic or heterocyclic r
