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構象受限的完全合成的大環化合物
专利权人:
POLYPHOR AG
发明人:
OBRECHT, DANIEL D,ERMERT, PHILIPP P,OUMOUCH, SAID S,LACH, FRANCK F,LUTHER, ANATOL A,MARX, KARSTEN K,MOEHLE, KERSTIN K,.奧伯萊希特,.厄爾瑪特,.烏姆士,.拉什,.盧瑟爾,.馬克斯,.默勒
申请号:
HK16103994.2
公开号:
HK1216172A
申请日:
2012.10.30
申请国别(地区):
HK
年份:
2016
代理人:
摘要:
Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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