1264263-56-0

Upstream product

• 1145-80-8 N-(benzyloxycarbonyl)-L-serine 
• 1264243-55-1 5-acetoxynicotinoyl chloride 
• 1264239-65-7 (S)-allyl 2-(benzyloxycarbonylamino)-3-(methylamino)propanoate hydrochloride 
• 27828-71-3 5-hydroxynicotinic acid 

Downstream Products

• 1264263-57-1 (S)-allyl 2-(benzyloxycarbonylamino)-3-(5-hydroxy-N-methylnicotinamido)propanoate 
• 1264242-87-6 C₃₈H₅₀N₆O₁₁ 

Relevant academic research and scientific papers

CONFORMATION-LOCKED, SYNTHETIC MACROCYCLIC COMPOUND

PROBLEM TO BE SOLVED: To provide a compound effective for treating: diabetic gastroparesis, and impairment of hypomotility in the gastrointestinal tract such as constipation type irritable bowel syndrome; CNS related disorders such as migraine, schizophre

Conformation-constrained entirely-synthetic macrocyclic compounds

The invention relates to conformation-constrained entirely-synthetic macrocyclic compounds. A conformation-constrained, space-defined 12-30-member macrocyclic system (I) which is as shown in the description comprises three different constitution units: an aromatic template a, a confor1ation regulator b and a spaced part c, which are illustrated in the description and the claims. The macrocyclic compounds (I) can be easily prepared according to a parallel synthesis method or a combinatorial chemistry method, and are designed for realizing interaction with a specific biological target. Particularly, the compounds show agonistic or antagonistic activity to the following matters: a motilin receptor (MR), a 5-hydroxytryptamine receptor (5-HT2B receptor) of a subtype 5-HT2B, and a prostaglandin F2alpha receptor (FP receptor). Thus, the compounds are effectively used for treating gastrointestinal tract hypomotility disorder such as diabetic gastroparesis and constipation-predominant irritable bowel syndrome, CNS-related diseases such as migraine, schizophrenia, psychosis and depression, ocular hypertension such as glaucoma-related ocular hypertension, and premature delivery.

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 P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the β-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.