Polyphor Ag

Karsten Marx

Daniel Obrecht

Anatol Luther

Philipp Ermert

Kerstin Möhle

Said Oumouch

Franck Lach

Kerstin Mohle

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(5-HTreceptor), and on the prostaglandin F2&#x2022;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. 

Conformationally constrained, fully synthetic macrocyclic compounds

Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y, as modulators of the serotonin receptor of subtype 5-HT, as blockers of the voltage-gated potassium channel K1.3 and as inhibitors of the &#x3b2;-catenin-dependent 'canonical' Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases. 

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Basel, Switzerland

Karsten Marx