1264243-48-2

Upstream product

• 107-97-1 sarcosine 
• 104-15-4 toluene-4-sulfonic acid 
• 107-18-6 allyl alcohol 

Downstream Products

• 1264241-81-7 C₄₀H₅₁FN₄O₁₁ 

Relevant academic research and scientific papers

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, SYNTHETIC MACROCYCLIC COMPOUNDS

PROBLEM TO BE SOLVED: To provide a novel macrocyclic compound showing agonistic or antagonistic activity on a motilin receptor, a serotonin receptor and a prostaglandin F2A receptor. SOLUTION: This invention provides a macrocyclic compound incorporating building blocks A, B and C, represented by formula (I). The compound is useful for the treatment of motility disorders of the gastrointestinal tract, CNS-related disease and ocular hypertension. COPYRIGHT: (C)2015,JPO&INPIT

CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS

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.