883969-09-3

Basic information

• Product Name: tert-butyl 4-(4-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)benzenesulfonylamino]tetrahydropyran-4-ylcarbonyl)piperazine-1-carboxylate
• Synonyms: tert-butyl 4-(4-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)benzenesulfonylamino]tetrahydropyran-4-ylcarbonyl)piperazine-1-carboxylate
• CAS NO: 883969-09-3
• Molecular Weight: 707.675
• Mol File: 883969-09-3.mol

Chemical Properties

• CAS DataBase Reference: tert-butyl 4-(4-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)benzenesulfonylamino]tetrahydropyran-4-ylcarbonyl)piperazine-1-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl 4-(4-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)benzenesulfonylamino]tetrahydropyran-4-ylcarbonyl)piperazine-1-carboxylate(883969-09-3)
• EPA Substance Registry System: tert-butyl 4-(4-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)benzenesulfonylamino]tetrahydropyran-4-ylcarbonyl)piperazine-1-carboxylate(883969-09-3)

Safety Data

• Hazardous Substances Data: 883969-09-3(Hazardous Substances Data)

Upstream product

• 883969-07-1 4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]-tetrahydropyran-4-carboxylic acid methyl ester 
• 883969-08-2 4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]-tetrahydropyran-4-carboxylic acid 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 

Downstream Products

• 1369389-91-2 (S)-5-amino-6-(4-(4-(2,4-dichloro-3-((2,4-dimethylquinolin-8-yloxy)methyl)phenylsulfonamido)tetrahydro-2H-pyran-4-carbonyl)piperazin-1-yl)-N,N,N-trimethyl-6-oxohexan-1-aminium trifluoroacetate salt 
• 1369389-70-7 [7-(4-(4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]-tetrahydro-pyran-4-carbonyl)-piperazin-1-yl)-7-oxo-heptyl]trimethylammonium trifluoroacetate salt 
• 1369389-66-1 [6-(4-(4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]-tetrahydro-pyran-4-carbonyl)-piperazin-1-yl)-6-oxo-hexyl]-trimethyl-ammonium trifluoroacetate salt 
• 1369389-59-2 [4-(4-(4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]tetrahydropyran-4-carbonyl)-piperazin-1-yl)-4-oxo-butyl]-trimethyl-ammonium trifluoroacetate salt 
• 1369389-54-7 [2-(4-(4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]tetrahydro-pyran-4-carbonyl)-piperazin-1-yl)-2-oxo-ethyl]-trimethylammonium trifluoroacetate salt 
• 883969-10-6 (4-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)benzenesulfonylamino]tetrahydropyran-4-yl)carbonylpiperazine hydrochloride 
• 884049-27-8 [4-tert-butoxycarbonylamino-5-(4-{4-[2,4-dichloro-3-(2,4-dimethyl-quinolin-8-yloxymethyl)-benzenesulfonylamino]-tetrahydro-pyran-4-carbonyl}-piperazin-1-yl)-5-oxo-pentyl]-trimethyl-ammonium 

Relevant articles and documents

Design and synthesis of novel sulfonamide-containing bradykinin hB 2 receptor antagonists. Synthesis and structure-relationships of α,α-tetrahydropyranylglycine

A series of α,α-cycloalkylglycine sulfonamide compounds of general formula 1 has previously been identified by our group as selective human B2(hB2) receptor antagonists. Here we report the in vitro and in vivo BK antagonist activity

Design and synthesis of novel sulfonamide-containing bradykinin hB 2 receptor antagonists. 2. Synthesis and structure-activity relationships of α,α-cycloalkylglycine sulfonamides

Recently we reported on the design and synthesis of a novel class of selective nonpeptide bradykinin (BK) B2 receptor antagonists (J. Med. Chem. 2006, 3602-3613). This work led to the discovery of MEN 15442, an antagonist with subnanomolar affinity for the human B2 receptor (hB2R), which also displayed significant and prolonged activity in vivo (for up to 210 min) against BK-induced bronchoconstriction in the guinea-pig at a dose of 300 nmol/kg (it), while demonstrating only a slight effect on BK-induced hypotension. Here we describe the further optimization of this series of compounds aimed at maximizing the effect on bronchoconstriction and minimizing the effect on hypotension, with a view to developing topically delivered drugs for airway diseases. The work led to the discovery of MEN 16132, a compound which, after intratracheal or aerosol administration, inhibited, in a dose-dependent manner, BK-induced bronchoconstricton in the airways, while showing minimal systemic activity. This compound was selected as a preclinical candidate for the topical treatment of airway diseases involving kinin B2 receptor stimulation.

NON-PEPTIDE BRADYKININ ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS THEREFROM

Non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an amino acid alpha substituted with a cyclic group and by a tetraalkylammonium group.