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 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 146395-99-5 3-(3,4-Dichloro-phenyl)-3-[3-(tetrahydro-pyran-2-yloxy)-propyl]-piperidine 
• 146395-98-4 5-tetrahydropyranyloxypropyl-5-(3,4-dichlorophenyl)piperidone 
• 146395-97-3 4-Cyano-4-(3,4-dichloro-phenyl)-7-(tetrahydro-pyran-2-yloxy)-heptanoic acid ethyl ester 
• 146395-96-2 2-(3,4-dichloro-phenyl)-5-(tetrahydro-pyran-2-yl-oxy)-pentanenitrile 
• 146396-02-3 {3-(3,4-Dichloro-phenyl)-3-[3-(tetrahydro-pyran-2-yloxy)-propyl]-piperidin-1-yl}-phenyl-methanone 
• 182621-50-7 Acetic acid 3-[3-(3,4-dichloro-phenyl)-2,6-dioxo-piperidin-3-yl]-propyl ester 
• 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 

Downstream Products

• 1071993-15-1 C₃₃H₃₈Cl₂N₄O₂ 
• 213180-01-9 C₃₄H₃₈Cl₂N₄O₂ 
• 172734-92-8 osanetant 
• 172734-92-8 (S)-(N)-(1-(3-(1-benzoyl-3(3,4-dichlorophenyl)piperidin-3-yl)propyl)-4-phenylpiperidin-4-yl)-N-methylacetamide 
• 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.

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.

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

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.