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    • 7. 发明申请
    • PIPERAZINE MELANOCORTIN-SPECIFIC COMPOUNDS
    • 哌嗪吗啉特异性化合物
    • WO2005102340A1
    • 2005-11-03
    • PCT/US2004/001462
    • 2004-01-21
    • PALATIN TECHNOLOGIES, INC.SHARMA, Shubh, D.SHI, Yi-QunWU, ZhijunRAJPUROHIT, Ramesh
    • SHARMA, Shubh, D.SHI, Yi-QunWU, ZhijunRAJPUROHIT, Ramesh
    • A61K31/495
    • C07D403/12C07D241/08C07D403/06
    • Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or C=O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
    • 具有结构(I)的黑皮质素受体特异性哌嗪或酮哌嗪化合物; 其中X为CH 2或C = O,R 1,R 2和R 3如说明书中所述,优选其中R 3为具有至少一个取代或未取代的苯基或萘基芳基的D-氨基酸 并且其中R 3任选地还包括胺封端基团,第二氨基酸残基或具有胺封端基团的第二氨基酸残基,所述化合物是一种或多种黑皮质素受体的激动剂,拮抗剂或混合激动剂和拮抗剂,并且具有 用于治疗黑皮质素受体相关疾病和病症。 还公开了结构(I)化合物的合成方法,含有结构(I)化合物的药物组合物及其使用方法。