PMID

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Article Title

Organization

N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.

Boehringer Ingelheim Pharmaceuticals

Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.

Peking Union Medical College And Chinese Academy Of Medical Sciences

Boronic acid-containing aminopyridine- and aminopyrimidinecarboxamide CXCR1/2 antagonists: Optimization of aqueous solubility and oral bioavailability.

Syntrix Biosystems

Boronic acid-containing CXCR1/2 antagonists: Optimization of metabolic stability, in vivo evaluation, and a proposed receptor binding model.

Syntrix Biosystems

Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists.

Astrazeneca

The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.

Novartis Institutes For Biomedical Research

2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.

Glaxosmithkline

Discovery of 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2.

Syntrix Biosystems

Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1).

Astrazeneca

Chemokine receptor antagonists.

National Heart And Lung Institute

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Evaluation of a series of bicyclic CXCR2 antagonists.

Astrazeneca R&D Charnwood

Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.

Johnson & Johnson Pharmaceutical Research And Development

Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.

Glaxosmithkline

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Schering-Plough Research Institute

Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.

Glaxosmithkline

Discovery, optimization, and pharmacological characterization of novel heteroaroylphenylureas antagonists of C-C chemokine ligand 2 function.

Telik

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

Università

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Genzyme

Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists.

Wuxi Pharmatech

Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.

Schering-Plough Research Institute

3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.

Schering-Plough Research Institute

Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.

Schering-Plough Research Institute

Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.

Pharmacopeia

Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.

Schering-Plough Research Institute

3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.

Schering-Plough Research Institute

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.

Glaxosmithkline

C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.

Schering-Plough Research Institute

N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.

Glaxosmithkline

Squaric acid analogues in medicinal chemistry.

Palacky University Olomouc

Synthesis and structure-activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists.

Pharmacopeia Drug Discovery

Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine.

Ku Leuven

Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists.

Pharmacopeia Drug Discovery

Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists.

Astrazeneca R&D Charnwood

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.

Pharmaceutical Research Institute

Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy.

Chinese Academy Of Medical Sciences And Peking Union Medical College

Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists.

Tsinghua University

BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.

Bristol Myers Squibb

Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.

Glaxosmithkline

Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists.

Astrazeneca R&D Charnwood

Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.

University Of Michigan

Discovery of 1,5-Dihydro-4

Zhejiang University

Nicotinanilides as inhibitors of neutrophil chemotaxis.

Celltech R&D

Nicotinamide N-oxides as CXCR2 antagonists.

Celltech R&D

Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead.

Hangzhou Institute Of Innovative Medicine

Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.

TBA

The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists.

Novartis Institutes For Biomedical Research

Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.

Glaxosmithkline

Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.

Phenex Pharmaceuticals

Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.

Gsk Pharmaceuticals R & D