167837-49-2

Upstream product

• 167837-47-0 N-(3-((tert-butyldiphenylsilyloxy)methyl)-2,4-dichlorophenyl)-2-(1,3-dioxoisoindolin-2-yl)-N-methylacetamide 
• 167837-46-9 N-(3-((tert-butyldiphenylsilyloxy)methyl)-2,4-dichlorophenyl)-2-(1,3-dioxoisoindol-in-2-yl)-acetamide 
• 167837-44-7 tert-butyl(2,6-dichloro-3-nitrobenzyloxy)diphenylsilane 
• 167837-45-8 3-amino-1-(tert-butyldiphenylsilyloxymethyl)-2,6-dichlorobenzene 
• 160647-01-8 2,6-Dichloro-3-nitrobenzyl alcohol 
• 6780-38-7 N-phthaloylglycine chloride 
• 124-63-0 methanesulfonyl chloride 
• 167837-48-1 N-(2,4-dichloro-3-(hydroxymethyl)phenyl)-2-(1,3-dioxoisoindolin-2-yl)-N-methylacetamide 

Downstream Products

• 179626-17-6 2-amino-N-[2,4-dichloro-3-({[4-(dimethylamino)-2-methyl-8-quinolinyl]oxy}methyl)phenyl]-N-methylacetamide 
• 179626-19-8 2-amino-N-[2,4-dichloro-3-({[2-methyl-4-(4-morpholinyl)-8-quinolinyl]oxy}methyl)phenyl]-N-methylacetamide 
• 179626-18-7 2-amino-N-[2,4-dichloro-3-({[2-methyl-4-(1-piperidinyl)-8-quinolinyl]oxy}methyl)phenyl]-N-methylacetamide 
• 179624-67-0 5-[(1E)-3-({2-[2,4-dichloro-3-({[4-(dimethylamino)-2-methyl-8-quinolinyl]oxy}methyl)methylanilino]-2-oxoethyl}amino)-3-oxo-1-propenyl]-2-pyridinecarboxylic acid 
• 179624-71-6 5-[(1E)-3-({2-[2,4-dichloro-3-({[4-(dimethylamino)-2-methyl-8-quinolinyl]oxy}methyl)methylanilino]-2-oxoethyl}amino)-3-oxo-1-propenyl]-N-methyl-2-pyridinecarboxamide 
• 179624-26-1 ethyl 5-[(1E)-3-({2-[2,4-dichloro-3-({[4-(dimethylamino)-2-methyl-8-quinolinyl]oxy}methyl)methylanilino]-2-oxoethyl}amino)-3-oxo-1-propenyl]-2-pyridinecarboxylate 
• 179624-69-2 5-[(1E)-3-({2-[2,4-dichloro(methyl)-3-({[2-methyl-4-(4-morpholinyl)-8-quinolinyl]oxy}methyl)anilino]-2-oxoethyl}amino)-3-oxo-1-propenyl]-2-pyridinecarboxylic acid 
• 179624-53-4 ethyl 5-[(1E)-3-({2-[2,4-dichloro(methyl)-3-({[2-methyl-4-(4-morpholinyl)-8-quinolinyl]oxy}methyl)anilino]-2-oxoethyl}amino)-3-oxo-1-propenyl]-2-pyridinecarboxylate 

Relevant academic research and scientific papers

A New Series of Highly Potent Non-Peptide Bradykinin B2 Receptor Antagonists Incorporating the 4-Heteroarylquinoline Framework. Improvement of Aqueous Solubility and New Insights into Species Difference

Introduction of nitrogen-containing heteroaromatic groups at the 4-position of the quinoline moiety of our non-peptide B2 receptor antagonists resulted in enhancing binding affinities for the human B 2 receptor and reducing binding affinities for the guinea pig one, providing new structural insights into species difference. A CoMFA study focused on the diversity of the quinoline moiety afforded correlative and predictive QSAR models of binding for the human B2 receptor but not for the guinea pig one. A series of 4-(1-imidazolyl)quinoline derivatives could be dissolved in a 5% aqueous solution of citric acid up to a concentration of 10 mg/mL. A representative compound 48a inhibited the specific binding of [ 3H]BK to the cloned human B2 receptor expressed in Chinese hamster ovary cells with an IC50 value of 0.26 nM and significantly inhibited BK-induced bronchoconstriction in guinea pigs even at 1 μg/kg by intravenous administration.

A New Class of Nonpeptide Bradykinin B2 Receptor Ligand, Incorporating a 4-Aminoquinoline Framework. Identification of a Key Pharmacophore to Determine Species Difference and Agonist/Antagonist Profile

Introduction of various aliphatic amino groups at the 4-position of the quinoline moiety of our nonpeptide bradykinin (BK) B2 receptor antagonists afforded highly potent ligands for human B2 receptor with various affinities for guine

Benzimidazole compounds as bradykinin antagonists

PCT No. PCT/JP95/01478 Sec. 371 Date Feb. 3, 1997 Sec. 102(e) Date Feb. 3, 1997 PCT Filed Jul. 25, 1995 PCT Pub. No. WO96/04251 PCT Pub. Date Feb. 15, 1996This invention relates to a heterocyclic compound of the formula: wherein a group of the formula: is a group of the formula: etc., X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a]pyridine moiety

Recently we reported on overcoming the species difference of our first orally active non-peptide bradykinin (BK) B2 receptor antagonists, incorporating an 8-[[3-(N-acylglycyl-N-methylamino)-2,6-dichlorobenzyl]oxy]- 3-halo-2-methylimidazo[1,2-α]

BRADYKININ ANTAGONIST QUINOLINES

This invention relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof. More particularly, this invention relates to new heterocyclic compounds and salts thereof which display bradykinin antagonist activity, to processes for preparing these compounds, to a pharmaceutical composition comprising these compounds, and to methods of using same in the prevention and/or the treatment of bradykinin-or bradykinin analogue-mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, in human beings or in animals.