MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
发明人:
CHRISTOS DR. TSAKLAKIDIS,MARKUS DR. KLEIN
申请号：
ARP130102620
公开号：
AR091875A1
申请日:
2013.07.24
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
In particular hidroxistatina derivatives and Medicines containing at least one of these derivatives for use in the Prevention and / or treatment of Physiological and / or pathophysiological States, which is involved in triggering the cathepsin D, in particular for use in the treatment and Or the Prevention of traumatic injury of Cartilage, Osteoarthritis, arthritis, Pain,Allodynia or hyperalgesia. It also provides a procedure for its preparation.Claim 1: compounds of formula (1) or, where i u00b9, i u00b3, i u2074, i u2075 are independently between themselves, or CR； t is a phenyl, naphthyl substituted biphenyl or not or mono -, di -, Tri - or tetrasustituido with R or a saturated or mono Aromatic Heterocycles, unsaturated - or bicyclic with 1 to 4 Or n ATOMS, and / or s, which can be mono -, di - or trisustituido with R = S = U = nr and / or； r u00b9 is Ethyl, n-propyl,ISO - propyl, butyl, ciclopropilo, ISO - butyl, sec butyl, ciclobutilo, ter butyl, phenyl, Benzyl, oxetanilo 2 -, 3 - oxetanilo, tetrahydrofuran-3-yl tetrahydrofuran-2-ylmethyl 2 - ILO, ILO, Cyclopentyl, Pentyl, metilsulfanilmetilo, etilsulfanilmetilo, 1 - or 2 - metilsulfaniletilo, metilsulfaniletilo； R u00b2 is Ethyl, N - ISO - propyl, butyl, propyl, ciclopropilo, ISO - butyl, sec butyl, ciclobutilo, ter butyl, phenylOxetanilo Benzyl 2 -, 3 -, oxetanilo, tetrahydrofuran-3-yl tetrahydrofuran-2-ylmethyl 2 - ILO, ILO, Cyclopentyl, Pentyl, metilsulfanilmetilo, etilsulfanilmetilo metilsulfaniletilo 1 -, 2 - or metilsulfaniletilo； a u00b9 is a simple link or 1 to 3 amino acid residues linked peptides as, co, and OCO. - NRCO -- or - - - SO u2082 a-squared nrso u2082； is a simple link or 1 to 3 amino acid residues linked as l u00b9 peptides； is a simple Link, a linear or branched alkyl Linker with c u2081 u208b u2081 u2080, where 1 - 5 ch u2082 groups, independent of each other, can be replaced by o, S, whoa, whoa u2082, NR - (c = o) - - - - - CRR, OCO, nrconr NRCO - - - - - nrso u2082r - Coo -, - wit
