Conformationally constrained, fully synthetic macrocyclic compounds

US9695191B2 · kind B2 · utility

Assignee

• POLYPHOR AG · CH

Inventors

• Daniel Obrecht · Amriswil, CH
• Philipp Ermert · Allschwil, CH
• Said Oumouch · Mulhouse, FR
• Franck Lach · Châlons-en-Champagne, FR
• Anatol Luther · Binzen, DE
• Karsten Marx · Basel, CH
• Kerstin Möhle · Wettswil, CH

Key dates

• Filing date: Aug 5, 2009
• Grant date: Jul 4, 2017
• Expiry date: Jun 22, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D498/18
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.