Tripeptide derivatives for the treatment of postlesional diseases of the nervous system
申请人:Rapin Jean
公开号:US20050101539A1
公开(公告)日:2005-05-12
The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy formula (I), wherein X represents OH, (C
1-5
)alkoxy, NH
2
, NH—C
1-5
-alkyl, N(C
1-5
alkyl)
2
; R
1
is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C
1-5
) alkoxy group, a (C
1-5
) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R
2
is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R
3
and R
4
independently represent H, OH, (C
1
-C
5
) alkyl, or (C
1-5
)alkoxy, provided that R
3
and R
4
are not both OH or (C
1-5
)alkoxy; R
5
represents H, OH, (C
1-5
)alkyl or (C
1-5
)alkoxy; and wherein R
0
preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.
本发明涉及使用特定的三肽治疗缺血性、创伤性或中毒性后遗症。三肽衍生物符合式 (I),其中 X 代表 OH、(C
1-5
烷氧基、NH
2
、NH-C
1-5
-烷基、N(C
1-5
烷基)
2
; R
1
是衍生自 Phe、Tyr、Trp、Pro 中任何一种氨基酸的残基,其中每种氨基酸均可任选被(C
1-5
烷氧基、(C
1-5
)烷基或卤原子取代,以及 Ala、Val、Leu 或 Ile 取代;R
2
是衍生自 Gly、Ala、Ile、Val、Ser、Thr、His、Arg、Lys、Pro、Glu、Gln、pGlu、Asp、Leu 和 Asn 中任何一种氨基酸的残基;R
3
和 R
4
分别代表 H、OH、(C
1
-C
5
烷基,或 (C
1-5
烷氧基,条件是 R
3
和 R
4
既不是 OH 也不是 (C
1-5
烷氧基;R
5
代表 H、OH、(C
1-5
)烷基或 (C
1-5
烷氧基;其中 R
0
最好代表肉桂酰残基;或其药学上可接受的盐类。