111 articles for thisTarget
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Article Title
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Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF
Takeda Pharmaceutical
An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
University of Kwazulu-Natal
Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists.
Takeda Pharmaceutical
Characterization of Multisubstituted Corticotropin Releasing Factor (CRF) Peptide Antagonists (Astressins).
Salk Institute
Synthesis, binding affinity, radiolabeling, and microPET evaluation of 4-(2-substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as ligands for brain corticotropin-releasing factor type-1 (CRF1) receptors.
Emory University
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Bristol-Myers Squibb
Synthesis of substituted pyrimidines as corticotropin releasing factor (CRF) receptor ligands.
South Dakota State University
Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones.
Bristol-Myers Squibb Research and Development
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.
Glaxosmithkline
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
Neurocrine Biosciences
Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.
Eisai
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
Neurocrine Biosciences
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.
Glaxosmithkline
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.
Glaxosmithkline
Design, synthesis, and structure-activity relationships of novel pyrazolo[5,1-b]thiazole derivatives as potent and orally active corticotropin-releasing factor 1 receptor antagonists.
Eisai
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Bristol-Myers Squibb
Synthesis and structure-activity relationships of 8-substituted-2-aryl-5-alkylaminoquinolines: Potent, orally active corticotropin-releasing factor-1 receptor antagonists.
Eisai
Design, synthesis, and structure-activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF1 receptor antagonists.
Eisai
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Bristol-Myers Squibb
Design, synthesis and structure-activity relationships of 5-alkylaminolquinolines as a novel series of CRF1 receptor antagonists.
Eisai
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).
Westfalische Wilhelms-Universitat
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
Neurocrine Biosciences
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
Neurocrine Biosciences
Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2.
National Institutes of Health
Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists.
Salk Institute
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.
Dupont Pharmaceuticals
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.
Dupont Pharmaceuticals
Corticotropin-releasing hormone receptor antagonists: framework design and synthesis guided by ligand conformational studies.
Dupont Pharmaceuticals
Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF¿?) receptor antagonists.
Minase Research Institute
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
Pfizer
Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles.
Pfizer
Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF¿?) receptor antagonists.
Minase Research Institute
6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.
Minase Research Institute
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
Neurogen
Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists.
Pfizer
Discovery of pyrrolo[2,3-d]pyrimidin-4-ones as corticotropin-releasing factor 1 receptor antagonists with a carbonyl-based hydrogen bonding acceptor.
Takeda Pharmaceutical
Potential CRF1R PET imaging agents: N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines.
Bristol-Myers Squibb Research and Development
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
Bristol-Myers Squibb Research and Development
Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R).
Bristol-Myers Squibb Research & Development
Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
Optimising metabolic stability in lipophilic chemical space: the identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist.
Pfizer
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Bristol-Myers Squibb
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists.
Neurogen
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.
Pfizer
An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes.
Pharmaceutical Research Institute
Pyrazolotriazines: Biological activities, synthetic strategies and recent developments.
Mazandaran University of Medical Sciences
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.
Universite de Tours
Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor1 receptor ligands.
Pharmaceutical Research Institute
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
Neurocrine Biosciences
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.
Pharmaceutical Research Institute
Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists.
Pharmaceutical Research Institute
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Discovery of corticotropin releasing factor 2 receptor selective sauvagine analogues for treatment of skeletal muscle atrophy.
Procter & Gamble Pharmaceuticals
Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
Neurocrine Biosciences
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.
Pharmaceutical Research Institute
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.
Neurocrine Biosciences
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
Neurocrine Bioscience
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.
Neurocrine Biosciences
N-phenylphenylglycines as novel corticotropin releasing factor receptor antagonists.
Bristol-Myers Squibb Pharma Research Laboratories
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
Neurocrine Biosciences
New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor.
Central Pharmaceutical Research Institute
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.
Neurocrine Biosciences
Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists.
Neurocrine Biosciences
Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists.
Neurocrine Biosciences
2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists.
Neurogen
1-Alkyl-3-amino-5-aryl-1H-[1,2,4]triazoles: novel synthesis via cyclization of N-acyl-S-methylisothioureas with alkylhydrazines and their potent corticotropin-releasing factor-1 (CRF(1)) receptor antagonist activities.
Neurocrine Biosciences
The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type.
Niddk
Discovery of a 7-arylaminobenzimidazole series as novel CRF1 receptor antagonists.
Takeda Pharmaceutical
Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor.
Niddk
Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity.
The University of Wollongong
Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Dupont Pharmaceuticals
Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.
Dupont Pharmaceuticals
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.
Dupont Pharmaceuticals
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Dupont Pharmaceuticals
Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.
Agouron Pharmaceuticals
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.
Dupont Pharmaceuticals
Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines.
Dupont Pharmaceuticals
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.
Pfizer
Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists.
Neurocrine Biosciences
Rapid microscale synthesis, a new method for lead optimization using robotics and solution phase chemistry: application to the synthesis and optimization of corticotropin-releasing factor1 receptor antagonists.
Neurocrine Biosciences
Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.
Bristol-Myers Squibb
Discovery of 1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazoles as novel class of corticotropin releasing factor 1 receptor antagonists.
Takeda Pharmaceutical
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.
University of Kwazulu-Natal
Synthesis of 2-imino and 2-hydrazono thiazolo[4,5-d]pyrimidines as corticotropin releasing factor (CRF) antagonists.
South Dakota State University
PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
Mitobridge
Peripheral-type benzodiazepine receptors in human cerebral cortex, kidney, and colon.
Technion-Israel Institute of Technology
Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.
University of California San Francisco
Complexation of ferrocene derivatives by the cucurbit[7]uril host: a comparative study of the cucurbituril and cyclodextrin host families.
University of Miami
Complexation and chiral recognition thermodynamics of 6-amino-6-deoxy-beta-cyclodextrin with anionic, cationic, and neutral chiral guests: counterbalance between van der Waals and coulombic interactions.
Japan Science and Technology Agency
Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.
Wyeth Research
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University