PMID

Data

Article Title

Organization

Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.

Goethe-University Frankfurt

New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.

Ono Pharmaceutical

Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.

TBA

Synthesis and structure-activity relationship studies of a series of 5-aryl-4,6-dithianonanedioic acids and related compounds: a novel class of leukotriene antagonists.

TBA

Development of new chromanol antagonists of leukotriene D4.

Pfizer

Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.

Eli Lilly

Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.

Shanghai Institute Of Materia Medica

Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.

Glenmark Research Centre

Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.

Setsunan University

Discovery of a potent, orally available dual CysLT1 and CysLT2 antagonist with dicarboxylic acid.

Ono Pharmaceutical

Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.

Ono Pharmaceutical

Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl)oxy]methyl]acetophenone derivatives.

TBA

Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela

Pfizer

Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.

Zhejiang University

Modulators of leukotriene biosynthesis and receptor activation.

Abbott Laboratories

Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic

Merck Frosst Centre For Therapeutic Research

The Role of Receptor Binding in Drug Discovery

TBA

 

Discovery of L-740,515, a potent thienopyridine cysLT₁ receptor (LTD₄ receptor) antagonist

TBA

A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

Merck Frosst Center For Therapeutic Research

Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.

Novartis Pharma

Synthesis and structure-activity relationships of carboxylated chalcones: a novel series of CysLT1 (LTD4) receptor antagonists.

Vrije Universiteit

High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.

TBA

3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.

Roche Research Center

Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles.

Ici Pharmaceuticals Group

Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist.

Merck Frosst Centre For Therapeutic Research

The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.

Rorer Central Research

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.

Rorer Central Research

Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents.

Warner-Lambert