173457-29-9

Upstream product

• 7226-23-5 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone 
• 106-95-6 allyl bromide 
• 6725-44-6 methyl 2-(3,4-dichlorophenyl)acetate 
• 67-56-1 methanol 
• 79333-48-5 2-(S)-(3,4-dichloro-phenyl)-4-pentenoic acid 
• 556-56-9 allyl iodid 
• 5807-30-7 3,4-dichlorophenyl acetic acid 

Downstream Products

• 1563182-47-7 (R)-2-(3,4-dichlorophenyl)-2-methylpent-4-enoic acid 
• 1563182-50-2 (S)-2-(3,4-dichlorophenyl)-2-methylpent-4-enoic acid 
• 1563182-54-6 (R)-2-(3,4-dichlorophenyl)-2-methylpent-4-enoic acid 2-trimethylsilanylethyl ester 
• 1563182-91-1 (R)-2-(3,4-dichlorophenyl)-4-(6-fluoro-1-methyl-2-oxo-1,2-dihydrospiro[benzo[d][1,3]oxazine-4,4'-piperidine]-1'-yl)-2-methylbutanoic acid 
• 1563182-55-7 (S)-2-(3,4-dichlorophenyl)-2-methylpent-4-enoic acid 2-trimethylsilanylethyl ester 
• 1563182-92-2 2-((S)-2-((R)-2-(3,4-dichlorophenyl)-4-(6-fluoro-1-methyl-2-oxo-1,2-dihydrospiro[benzo[d][1,3]oxazine-4,4'-piperidine]-1'-yl)-2-methylbutanamido)-2-phenylacetamido)ethyl carbamic acid tert-butyl ester 
• 1563182-93-3 (R)-2-(trimethylsilyl)ethyl 2-(3,4-dichlorophenyl)-2-methyl-4-(4-(N-propylmethylsulfonamido)piperidin-1-yl)butanoate 
• 1563182-94-4 (S)-2-(trimethylsilyl)ethyl 2-(3,4-dichlorophenyl)-2-methyl-4-(4-(N-propylmethylsulfonamido)piperidin-1-yl)butanoate 
• 1563182-95-5 2-((S)-2-((R)-2-(3,4-dichlorophenyl)-2-methyl-4-(4-(N-propylmethylsulfonamido)piperidin-1-yl)butanamido)-3-phenylpropanamido)ethyl carbamic acid benzyl ester 
• 1563182-96-6 2-((S)-2-((S)-2-(3,4-dichlorophenyl)-2-methyl-4-(4-(N-propylmethylsulfonamido)piperidin-1-yl)butanamido)-3-phenylpropanamido)ethyl carbamic acid benzyl ester 
• 1563182-97-7 (R)-2-(3,4-dichlorophenyl)-2-methyl-4-(1-methyl-2-oxospiro[indoline-3,4'-piperidine]-1'-yl)butanoic acid 
• 1563182-90-0 (R)-3-(3,4-dichlorophenyl)-5-hydroxy-3-methyldihydrofuran-2(3H)-one 
• 1563182-56-8 (R)-2-(trimethylsilyl)ethyl 2-(3,4-dichlorophenyl)-2-methyl-4-oxobutanoate 
• 1563182-99-9 (S)-2-(3,4-dichlorophenyl)-2-methyl-4-(1-methyl-2-oxospiro[indoline-3,4'-piperidine]-1'-yl)butanoic acid 

Relevant academic research and scientific papers

Design, synthesis, and optimization of balanced dual NK1/NK 3 receptor antagonists

In connection with a program directed at potent and balanced dual NK 1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pKi values of 8.6 and 8.1, respectively.

ARYL AND BIARYL COMPOUNDS HAVING MCH MODULATORY ACTIVITY

In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor. An illustrative inventive compound is shown below:

Synthesis and structure-antifungal activity relationships of 3-aryl-5-alkyl-2,5-dihydrofuran-2-ones and their carbanalogues: Further refinement of tentative pharmacophore group

Two series of 3-(substituted phenyl)-5-alkyl-2,5-dihydrofuran-2-ones related to a natural product, (-)incrustoporine, were synthesized and their in vitro antifungal activity evaluated. The compounds with halogen substituents on the phenyl ring exhibited selective antifungal activity against the filamentous strains of Absidia corymbifera and Aspergillus fumigatus. On the other hand, the influence of the lenghth of the alkyl chain at C(5) was marginal. The antifungal effect of the most active compound against the above strains was higher than that of ketoconazole, and close to that of amphotericin B. In order to verify the hypothesis about a possible relationship between the Michael-accepting ability of the compounds and their antifungal activity, a series of simple carbanalogues, 2-(substituted phenyl)cyclopent-2-enones, was prepared and subjected to antifungal activity assay as well.

3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: Synthesis and biological activity of a novel group of potential antifungal drugs

3-(Substituted phenyl)-5-acyloxymethyl-2H,5H-furan-2-ones related to the natural product (-)-incrustoporine were synthesized and their in vitro antifungal activity evaluated. The compounds with halogen substituents on the phenyl ring displayed much higher antifungal effect against Aspergillus fumigatus than selected representatives of azole antifungal drugs. In particular, the activity (1.34 μg/mL) of the most promising derivative, 3-(3,4-dichlorophenyl)-5-pivaloyloxymethyl-2H,5H-furan-2-one, was comparable to that of amphotericin B (0.5 μg/mL). Preliminary evaluation of the toxicity of the compound was carried out as well. Considering the size and properties of these molecules in comparison with those of amphotericin B, further development of this novel group of antifungals may lead to substances with better pharmacological profiles than that of the standard anti-Aspergillus drug.

3-Phenyl-5-methyl-2H,5H-furan-2-ones: Tuning antifungal activity by varying substituents on the phenyl ring

A series of racemic 3-phenyl-5-methyl-2H,5H-furan-2-ones related to a natural product, (-)incrustoporine, was synthesized, and their antifungal activity evaluated. The key structural feature, furanone ring, was closed via H2SO4-mediated cyclization of 2-phenylpent-4-enoic acids. The compounds displayed antifungal activity, especially against filamentous fungi. Expressed as the minimum inhibition concentration (MIC) in μmol/L, the activity of the most promising derivative against Absidia corymbifera matched that of ketoconazole (31.25 μmol/L). In terms of μg/mL, the substance was more active (7.6 μg/mL) than this standard antifungal drug (16.6 μg/mL). (C) 2000 Elsevier Science Ltd. All rights reserved.

Piperidine derivatives useful as neurokinin antagonists

Compounds of formula I STR1 wherein Q1, Q2, Q3, and Q4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.