823226-18-2

Upstream product

• 75322-09-7 3-cyclohexyloxypropyl alcohol 
• 124-63-0 methanesulfonyl chloride 
• 27912-81-8 3-(cyclohexyloxy)propionic acid 
• 121-44-8 triethylamine 
• 7170-38-9 3-phenoxypropanoic acid 

Downstream Products

• 16728-63-5 3-(cyclohexyloxy)propan-1-amine 
• 200400-23-3 2-amino-N-(3-cyclohexyloxy-propyl)-3-hydroxy-propionamide 
• 200400-56-2 N-<3-(cyclohexyloxy)propyl>-2-<4-(3-pyridylcarbonyl)phenyl>-4-oxazolecarboxamide 
• 200400-48-2 (S)-2-[4-(Pyridine-3-carbonyl)-phenyl]-4,5-dihydro-oxazole-4-carboxylic acid (3-cyclohexyloxy-propyl)-amide 
• 200400-40-4 N-[1-(3-cyclohexyloxy-propylcarbamoyl)-2-hydroxy-ethyl]-4-(pyridine-3-carbonyl)-benzamide 
• 1027371-03-4 5-Cyclohexyloxy-2-[2-(2-methoxy-ethoxymethoxy)-benzoyl]-pentanoic acid ethyl ester 
• 161053-78-7 (3-iodopropoxy)cyclohexane 

Relevant academic research and scientific papers

4-(AMINOMETHYL)-PIPERIDINE BENZAMIDES AS 5HT4-ANTAGONISTS

The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds

Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted ω-phenyl-ω-(3-pyridyl)alkenoic acid derivatives and related compounds

A novel series of oxazolecarboxamide-substituted ω-phenyl-ω-(3- pyridyl)alkenoic acid derivatives was discovered as potent dual-acting agents to block the TXA2 receptor and to inhibit the thromboxane synthase (TRA/TSI). Synthesis, structure-activity relationship (SAR), and in vitro and in vivo pharmacology of this series of compounds are described. Modification of the series revolved around the oxazole moiety to increase the hydrophilicity of the compounds and to correlate the biological activity with lipophilicity of the compounds. The most potent in the series was (E)-7-[4- [4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept- 6-enoic acid (14) with K(d) = 9.9 ± 0.4 nM for the thromboxane receptor antagonism and IC50 = 55.0 ± 17.9 nM for thromboxane synthase inhibition. The compound 14 was a selective TRA/TSI which exhibited desirable characteristics for oral activity, 'shunt' effect to elevate PGI2 level, and absence of agonist activity.

σ Ligands with subnanomolar affinity and preference for the σ2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines

Spiro[isobenzofuran-1(3H),4'-piperidines] and the corresponding benzofuran and benzopyran derivatives have been synthesized and evaluated as σ ligands. The compounds are related to Lu 28-179 (1'[4-[1(4fluorophenyl)-1H-indol-3- yl]-1-butyl]spiro[isobenzofu

A novel nonpeptide HIV-1 protease inhibitor: Elucidation of the binding mode and its application in the design of related analogs

HIV-1 protease has been identified as a significant target enzyme in AIDS research. While numerous peptide-derived inhibitors have been described, the identification of a nonpeptide inhibitor remains an important goal. Using an HIV-1 protease mass screening technique, 4-hydroxy-3-(3-phenoxypropyl)-2H-1- benzopyran-2-one (1) was identified as a nonpeptide competitive inhibitor of the enzyme. Employing a Monte Carlo-based docking procedure, the coumarin was docked in the active site of the enzyme, revealing a binding mode that was later confirmed by the X-ray crystal analysis. Several analogs were prepared to test the binding interactions and improve the overall binding affinity. The most active compound in the study was 4,7-dihydroxy-3-[4-(2- methoxyphenyl)butyl]-2H-1-benzopyran-2-one (31).

N-(4-piperodinyl)(dihydrobenzofuran or dihydro-2H-benzopyran) carboxamide derivatives

Piperidine derivatives of formula STR1 wherein A is a radical of formula STR2 wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C1-6 alkyl radical; R1 is hydrogen or halo; R2 is hydrogen, amino, mono or di(C1-6 alkyl)amino or C1-6 alkylcarbonylamino; R3 is hydrogen or C1-6 alkyl; L is C3-6 cycloalkyl, C5-6 cycloalkanone, C3-6 alkenyl optionally substituted with aryl, or L is a radical of formula STR3 the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.