专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 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-HT 2B (5-HT 2B 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.
参考文献:10.1007/s00044-015-1352-6 摘要:Markad SD, Kaur P, Kishore Reddy BK, Chinnapattu M, Raichurkar A, Nandishaiah R, Panda M, Iyer PS. Novel lead generation of an anti-tuberculosis agent active against non-replicating mycobacteria: exploring hybridization of pyrazinamide with multiple fragments. Medicinal Chemistry Research. 2015 Mar 08;24(7):2986–92. doi: 10.1007/s00044-015-1352-6.