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Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP

Novartis Institutes For Biomedical Research

Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists.

RhôNe-Poulenc Rorer

A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.

Amgen

Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: the role of a hydrogen-bond acceptor in long receptor residence times.

RhôNe-Poulenc Rorer

Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: lead optimization.

RhôNe-Poulenc Rorer

Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I.

RhôNe-Poulenc Rorer

Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists.

RhôNe-Poulenc Rorer

Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.

Amgen

Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.

Pfizer

Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.

Merck Research Laboratories

2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists.

RhôNe-Poulenc Rorer

Isoquinoline derivatives as potent CRTH2 antagonists: design, synthesis and SAR.

Taisho Pharmaceutical

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.

Novartis Institutes For Biomedical Research

Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold.

Actelion Pharmaceuticals

Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist.

Actelion Pharmaceuticals

2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.

RhôNe-Poulenc Rorer

Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.

University Of Southern Denmark

Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.

Pfizer

Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.

Oxagen

Novel 2-(2-(benzylthio)-1H-benzo[d]imidazol-1-yl)acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype.

Actelion Pharmaceuticals

Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists.

TBA

Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.

TBA

Use of libraries to access new chemical space: applications to CRTH2.

Pfizer

Isoquinoline derivatives as potent CRTH2 receptor antagonists: synthesis and SAR.

Taisho Pharmaceutical

Benzodiazepinone Derivatives as CRTH2 Antagonists.

TBA

Discovery and optimization of CRTH2 and DP dual antagonists.

Amgen

Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.

Merck Frosst Canada

Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.

Amgen

Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.

TBA

Discovery of novel and potent CRTH2 antagonists.

Astellas Pharma

Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.

Amgen

Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.

Amira Pharmaceuticals

Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981.

Astrazeneca R&D Charnwood

Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.

Merck Serono

Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.

Astrazeneca R&D Charnwood

New indole amide derivatives as potent CRTH2 receptor antagonists.

Merck Frosst

Zwitterionic CRTh2 antagonists.

Astrazeneca R&D Charnwood

Thienopyrrole acetic acids as antagonists of the CRTH2 receptor.

Abbott Laboratories

Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.

Amira Pharmaceuticals

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.

Merck Frosst Centre For Therapeutic Research

The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.

Merck Frosst Centre For Therapeutic Research

Azaindoles as potent CRTH2 receptor antagonists.

Merck Frosst Centre For Therapeutic Research

Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.

Merck Frosst Canada

3-Indolyl sultams as selective CRTh2 antagonists.

Athersys

Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.

7Tm Pharma

Tetrahydroquinoline derivatives as CRTH2 antagonists.

Amgen

Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.

7Tm Pharma

Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.

7Tm Pharma

The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.

Merck Frosst Centre For Therapeutic Research

Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.

Amira Pharmaceuticals

7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.

Novartis Institutes Of Biomedical Research

Discovery of potent and selective DP1 receptor antagonists in the azaindole series.

Merck Frosst Centre For Therapeutic Research

2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.

Novartis Institutes Of Biomedical Research

Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

Merck Frosst Canada

Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.

7Tm Pharma

Discovery of potent CRTh2 (DP2) receptor antagonists.

Astrazeneca R&D Charnwood

Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.

Oxagen

Synthesis of 15R-PGD2: a potential DP2 receptor agonist.

Florida Institute Of Technology

Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.

Athersys

Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.

7Tm Pharma

Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.

Merck Research Laboratory

The synthesis of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as potent CRTh

Merck

Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes.

Dumlupinar University

4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.

Wyeth-Ayerst Research