ROGER TARROUX,MARIE CHARVERON,SYLVIE DAUNES MARION
申请号：
FR0753864
公开号：
FR2913685B1
申请日:
2007.03.15
申请国别(地区):
FR
年份:
2012
代理人:
摘要：
Unsaturated fatty amino acid derivatives (I) and their acid addition salts, as drugs, are new. Unsaturated fatty amino acid derivatives of formula (R a)(R b)N-CH 2-(CH(R n)) n-CH=C(R 1)-C(O)-OR (I) and their acid addition salts, as drugs, are new. X : O or NH； R nH or 1-6C alkyl (optionally substituted by halo), preferably H； R 1H, F, Cl or Br, CF 3, CHF 2 or 1-6C alkyl, 1-6C alkenyl or 1-6C alkynyl (optionally substituted by halo), preferably H or F； R : H, 1-6C alkyl or 3-6C cycloalkyl (optionally substituted by halo), preferably H； R a, R bH, 1-6C alkyl or 1-6C acyl, preferably H, or 4-6C hydrocarbon ring； and n : 2-14, preferably 3. Provided that as a new compound (I) is excluded from 6-amino-hex-2-enoic acid, its hydrochloride and trifluoroacetate, 8-amino-oct-2-enoic acid trifluoroacetate, 8-(dimethylamino)-oct-2-enoic acid, 12-(dimethylamino)-dodec-2-enoic acid, 6-(isopropylamino)-2-methyl-hex-2-enoate, ethyl-6-(tert-butylamino)-2-methyl-hex-2-enoate, 6-amino-2-methyl-hex-2-enoate, 7-amino-hept-2-enoate, 7-amino-2-methyl-hept-2-enoate and 7-amino-4-methyl-hept-2-enoate. Independent claims are included for: (1) the preparation of (I)； and (2) an ester compound of formula PG-N(R d)-CH 2-(CHR 1)-C(O)-OR c (VIII). R cH or 1-6C alkyl； R 1H, F, Cl, Br, -CF 3 or -CHF 2, or 1-6C alkyl, alkenyl or alkynyl (optionally substituted by halo, preferably F)； PG : a protecting group forming a carbamate group, preferably tert. butyl carbamate or benzyl carbamate, and R dH or PG, provided that (VIII) is excluded from tert-butyl-(E)-6-(N,N-di-tert-butoxycarbonylamino)-hex-2-tert-enoate, ethyl (E)-6-(N-tert-butoxy-carbonylamino)-hex-2-enoate, methyl-(E)-7-(E-tert-butoxy-carbonylamino)-hept-2-enoate and (E)-7-(E-tert-butoxy-carbonylamino)-hept-2-enoic acid. ACTIVITY : Dermatological； Antiinflammatory； Antipruritic； Vulnerary. MECHANISM OF ACTION : Melanogenesis modulator.
