The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28174066 |
23 |
Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF |
Takeda Pharmaceutical |
27894044 |
37 |
An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold. |
University of Kwazulu-Natal |
26901666 |
26 |
Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists. |
Takeda Pharmaceutical |
26789203 |
100 |
Characterization of Multisubstituted Corticotropin Releasing Factor (CRF) Peptide Antagonists (Astressins). |
Salk Institute |
26456805 |
27 |
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 |
22381334 |
2 |
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 |
24675175 |
5 |
Synthesis of substituted pyrimidines as corticotropin releasing factor (CRF) receptor ligands. |
South Dakota State University |
23465610 |
16 |
Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones. |
Bristol-Myers Squibb Research and Development |
17629700 |
18 |
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists. |
Glaxosmithkline |
16134945 |
1 |
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. |
Neurocrine Biosciences |
22587443 |
55 |
Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor. |
Eisai |
21074436 |
17 |
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. |
Neurocrine Biosciences |
18975927 |
44 |
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 |
18989952 |
23 |
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. |
Glaxosmithkline |
22971011 |
26 |
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 |
23010264 |
14 |
[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 |
23062820 |
41 |
Synthesis and structure-activity relationships of 8-substituted-2-aryl-5-alkylaminoquinolines: Potent, orally active corticotropin-releasing factor-1 receptor antagonists. |
Eisai |
22871582 |
29 |
Design, synthesis, and structure-activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF1 receptor antagonists. |
Eisai |
22683343 |
27 |
Design, synthesis and structure-activity relationships of 5-alkylaminolquinolines as a novel series of CRF1 receptor antagonists. |
Eisai |
20408551 |
13 |
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular). |
Westfalische Wilhelms-Universitat |
19552436 |
43 |
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. |
Bristol-Myers Squibb |
18672365 |
33 |
2-Arylpyrimidines: novel CRF-1 receptor antagonists. |
Neurogen |
15743196 |
40 |
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists. |
Neurocrine Biosciences |
15943483 |
21 |
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core. |
Neurocrine Biosciences |
12361401 |
60 |
Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. |
Salk Institute |
10794681 |
43 |
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. |
Dupont Pharmaceuticals |
10669572 |
14 |
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 |
22196514 |
70 |
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 |
22104142 |
9 |
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8. |
Pfizer |
21889333 |
30 |
Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles. |
Pfizer |
21930387 |
60 |
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 |
21865047 |
48 |
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 |
21618986 |
65 |
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 |
21295475 |
21 |
Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists. |
Pfizer |
21414781 |
16 |
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 |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20471832 |
60 |
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 |
20185312 |
34 |
Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R). |
Bristol-Myers Squibb Research & Development |
19782566 |
30 |
Optimising metabolic stability in lipophilic chemical space: the identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist. |
Pfizer |
19954247 |
17 |
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 |
19552437 |
50 |
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists. |
Bristol-Myers Squibb |
18180159 |
32 |
The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists. |
Neurogen |
17888659 |
62 |
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists. |
Pfizer |
17258456 |
41 |
An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes. |
Pharmaceutical Research Institute |
16078829 |
26 |
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists. |
Neurocrine Biosciences |
15990298 |
43 |
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists. |
Pharmaceutical Research Institute |
15982881 |
44 |
Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists. |
Pharmaceutical Research Institute |
15603967 |
49 |
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 |
15509177 |
27 |
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 |
15341493 |
45 |
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 |
15225703 |
37 |
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists. |
Neurocrine Biosciences |
15225687 |
34 |
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor. |
Neurocrine Bioscience |
15203140 |
28 |
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility. |
Neurocrine Biosciences |
15115386 |
43 |
N-phenylphenylglycines as novel corticotropin releasing factor receptor antagonists. |
Bristol-Myers Squibb Pharma Research Laboratories |
15080983 |
20 |
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists. |
Neurocrine Biosciences |
14971886 |
21 |
New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor. |
Central Pharmaceutical Research Institute |
14592493 |
30 |
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12951129 |
30 |
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists. |
Neurocrine Biosciences |
12951128 |
51 |
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 |
12951127 |
32 |
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 |
12852951 |
21 |
2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists. |
Neurogen |
12127521 |
33 |
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists. |
Neurogen |
12014949 |
63 |
Arylamidrazones as novel corticotropin releasing factor receptor antagonists. |
TBA |
11720866 |
19 |
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 |
10395475 |
20 |
Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity. |
The University of Wollongong |
10328310 |
15 |
Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists. |
Dupont Pharmaceuticals |
10230641 |
14 |
Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists. |
Dupont Pharmaceuticals |
10230640 |
33 |
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists. |
Dupont Pharmaceuticals |
10230622 |
25 |
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists. |
Dupont Pharmaceuticals |
10072681 |
113 |
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines. |
Dupont Pharmaceuticals |
10072679 |
86 |
Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines. |
Dupont Pharmaceuticals |
9873487 |
14 |
Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. |
Warner-Lambert |
9171885 |
7 |
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
Pfizer |
8893829 |
13 |
Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. |
Neurocrine Biosciences |
8893828 |
28 |
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 |
22630076 |
38 |
Synthesis and anticholinesterase activities of novel 1,3,4-thiadiazole based compounds. |
University of Life Sciences |
26394156 |
11 |
Mechanism of MenE inhibition by acyl-adenylate analogues and discovery of novel antibacterial agents. |
Argonne National Laboratory |