146396-03-4

Upstream product

• 124-63-0 methanesulfonyl chloride 
• 172734-75-7 [3-(3,4-Dichlorophenyl)-3-(3-hydroxy-propyl)-piperidin-1-yl]-phenyl-methanone 
• 182621-51-8 (+)-3-(3,4-dichlorophenyl)-3-(3-hydroxypropyl)-piperidine 
• 182621-49-4 4-Cyano-4-(3,4-dichloro-phenyl)-7-(tetrahydro-pyran-2-yloxy)-heptanoic acid 
• 182621-50-7 Acetic acid 3-[3-(3,4-dichloro-phenyl)-2,6-dioxo-piperidin-3-yl]-propyl ester 
• 146396-02-3 {3-(3,4-Dichloro-phenyl)-3-[3-(tetrahydro-pyran-2-yloxy)-propyl]-piperidin-1-yl}-phenyl-methanone 
• 146395-96-2 2-(3,4-dichloro-phenyl)-5-(tetrahydro-pyran-2-yl-oxy)-pentanenitrile 
• 146395-97-3 4-Cyano-4-(3,4-dichloro-phenyl)-7-(tetrahydro-pyran-2-yloxy)-heptanoic acid ethyl ester 
• 146395-98-4 5-tetrahydropyranyloxypropyl-5-(3,4-dichlorophenyl)piperidone 
• 146395-99-5 3-(3,4-Dichloro-phenyl)-3-[3-(tetrahydro-pyran-2-yloxy)-propyl]-piperidine 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 

Downstream Products

• 172734-92-8 (S)-(N)-(1-(3-(1-benzoyl-3(3,4-dichlorophenyl)piperidin-3-yl)propyl)-4-phenylpiperidin-4-yl)-N-methylacetamide 
• 172734-92-8 osanetant 
• 1071993-15-1 C₃₃H₃₈Cl₂N₄O₂ 
• 213180-01-9 C₃₄H₃₈Cl₂N₄O₂ 
• 182621-57-4 {3-(3,4-Dichloro-phenyl)-3-[3-(4-methylamino-4-phenyl-piperidin-1-yl)-propyl]-piperidin-1-yl}-phenyl-methanone 

Relevant academic research and scientific papers

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1

We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC50 = 8.30 and 9.00, respectively) and HIV-1 inhibitors (pIC50 = 7.80 and 7.84, respectively, in Ba-L-HOS assay). In addition, 64 and 68 were bioavailable in rodents, establishing them as lead molecules for further optimization toward CCR5 clinical candidates.

Human NK3 receptor-selective antagonist compounds, method for obtaining them and pharmaceutical compositions containing them

PCT No. PCT/FR96/01416 Sec. 371 Date Mar. 12, 1998 Sec. 102(e) Date Mar. 12, 1998 PCT Filed Sep. 13, 1996 PCT Pub. No. WO97/10211 PCT Pub. Date Mar. 20, 1997Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK3 receptor antagonists.

COMPOUNDS WHICH ARE SELECTIVE ANTAGONISTS OF THE HUMAN NK3 RECEPTOR AND THEIR USE AS MEDICINAL PRODUCTS AND DIAGNOSTIC TOOLS

A compound of formula: STR1 in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C 1-C 4)alkoxy;R 1 represents a methyl group;R 11 represents hydrogen; or R 1 and R 11 toge

High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template

High affinity, selective hNK2 or hNK3 ligands can be prepared from the common template 1 in a few simple chemical operations. The hNK3 ligands 3 antagonise the calcium mobilisation caused by activation of hNK3 receptors expressed in CHO cells as measured using fura-2 microspectrofluorimetry.

A reliable and efficient synthesis of SR 142801

A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1 -yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)-(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen.