862282-35-7

Upstream product

• 923948-65-6 (3S,4R)-4-(2,4-difluorophenyl)pyrrolidine-3-carboxylic acid methyl ester 
• 455957-73-0 methyl (3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)-pyrrolidine-3-carboxylate 
• 455957-94-5 (3S,4R)-N-tert-butyl-4-(2,4-difluoro-phenyl)-pyrrolidine-3-carboxylic acid 
• 852305-06-7 (4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonitrile 
• 1002728-74-6 (4R)-4-(2,4-difluorophenyl)pyrrolidin-3-carbonitrile 
• 862284-13-7 1-tert-butyl 3-methyl (3S,4R)-4-(2,4-difluorophenyl)pyrrolidine-1,3-dicarboxylate 
• 1002728-75-7 (4R)-1-tert-butoxycarbonyl-4-(2,4-difluorophenyl)pyrrolidin-3-carbonitrile 

Downstream Products

• 1221822-07-6 tert-butyl (3R,4S)-3-(2,4-difluorophenyl)-4-{[(1R)-1-phenylethyl]carbamoyl}pyrrolidine-1-carboxylate 
• 862283-13-4 tert-butyl (3R,4S)-3-(2,4-difluorophenyl)-4-{[(3R,4R,5S)-4-(3,4-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl]carbonyl}pyrrolidine-1-carboxylate 
• 862284-16-0 tert-butyl (3R,4S)-3-(2,4-difluorophenyl)-4-{[(3R,4R,5S)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl]carbonyl}pyrrolidine-1-carboxylate 
• 1352246-53-7 tert-butyl (3S,4R)-3-({4-[1-(3-chloro-4-fluorophenyl)-3-methyl-1H-pyrazol-5-yl]piperidin-1-yl}carbonyl)-4-(2,4-difluorophenyl)pyrrolidine-1-carboxylate 
• 1244781-15-4 C₃₃H₃₈ClF₂N₃O₄ 

Relevant academic research and scientific papers

Pharmaceutical compositions (by machine translation)

[Problem] imidazole compound or its pharmacologically acceptable salt in the melanocortin receptor activity that operates as an active ingredient of a pharmaceutical composition comprising. "I" general formula [a]" Formula, the aryl group may be substituted A ring represents a; R1 Represents a hydrogen atom, or an alkyl group which may be substituted represented; R2 Represents a hydrogen atom, a halogen atom or represents a; R3 The alkyl group may be substituted " represented by the imidazole compound, its pharmacologically acceptable salt as an active ingredient in a pharmaceutical composition. [Drawing] no (by machine translation)

INDOLEAMIDE COMPOUNDS AS AN IHNIBITOR OF CELLULAR NECROSIS

The present invention relates to a an indoleamide compound of chemical formula 1, pharmaceutically allowable salt thereof, or an isomer, to a composition for preventing or treating cellular necrosis and related diseases containing the same as an active in

Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans

The relevance of the melanocortin system to sexual activity is well established, and nonselective peptide agonists of the melanocortin receptors have shown evidence of efficacy in human sexual dysfunction. The role of the MC4 receptor subtype has received particular scrutiny, but the sufficiency of its selective activation in potentiating sexual response has remained uncertain owing to conflicting data from studies in preclinical species. We describe here the discovery of a novel series of small-molecule MC4 receptor agonists derived from library hit 2. The addition of methyl substituents at C3 and C5 of the 4-phenylpiperidin-4-ol ring was found to be markedly potency-enhancing, enabling the combination of low nanomolar potencies with full rule-of-five compliance. In general, the series shows only micromolar activity at other melanocortin receptors. Our preferred compound 40a provided significant systemic exposure in humans on both sublingual and oral administration and was safe and well tolerated up to the maximum tested dose. In a pilot clinical study of male erectile dysfunction, the highest dose of 40a tested (200 mg) provided a similar level of efficacy to sildenafil.

MELANOCORTIN RECEPTOR AGONISTS

The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.

MELANOCORTIN RECEPTOR AGONISTS

The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.

Use of Mc4 Receptor Agonist Compounds

This invention relates to the use of an MC4 receptor agonist compound for the manufacture of a medicament for the treatment of lower urinary tract dysfunction.

MELANOCORTIN RECEPTOR AGONISTS

The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

PIPERIDINOYL-PYRROLIDINE AND PIPERIDINOYL-PIPERIDINE COMPOUNDS

The present invention relates to a class of compounds of general formula (I) and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R6, R7 and R10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.

Pharmaceutically active compounds

The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to