136 articles for JE Macor
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Bristol-Myers Squibb
Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
Bristol-Myers Squibb
Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] asa7 Nicotinic Receptor Agonists.
Bristol-Myers Squibb Research and Development
Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Bristol-Myers Squibb
Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.
Bristol-Myers Squibb
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.
Bristol-Myers Squibb Research & Development
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents.
Bristol-Myers Squibb
Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based¿-secretase modulators.
Bristol-Myers Squibb
Design and optimization of tricyclic gamma-secretase modulators.
Bristol-Myers Squibb Research and Development
Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines.
Bristol-Myers Squibb Discovery
Macrocyclic prolinyl acyl guanidines as inhibitors ofß-secretase (BACE).
Bristol-Myers Squibb
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.
Bristol-Myers Squibb
Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Bristol-Myers Squibb Research and Development
The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Lexicon Pharmaceuticals
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Bristol-Myers Squibb
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Amri
Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.
Bristol-Myers Squibb
Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.
Bristol-Myers Squibb
Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.
Bristol-Myers Squibb
Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.
Bristol-Myers Squibb R & D
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Bristol-Myers Squibb
Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones.
Bristol-Myers Squibb Research and Development
Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Bristol-Myers Squibb Research & Development
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.
Bristol-Myers Squibb Research and Development
Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.
Bristol-Myers Squibb Research & Development
Acyl guanidine inhibitors ofß-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.
Bristol-Myers Squibb Research
[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
Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.
TBA
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 and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor.
Bristol-Myers Squibb R & D
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.
Bristol-Myers Squibb Research & Development
Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.
Bristol-Myers Squibb Research & Development
Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates.
Bristol-Myers Squibb Research & Development
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
Astrazeneca
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Monosubstituted¿-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors ofß-secretase (BACE).
Bristol-Myers Squibb
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Bristol-Myers Squibb Research and Development
Small molecule receptor protein tyrosine phosphatase¿ (RPTP¿) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.
Bristol-Myers Squibb Research and Development
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
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb
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
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
Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.
Bristol-Myers Squibb Research and Development
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist
TBA
Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability.
Bristol-Myers Squibb Research and Development
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and effic
Bristol-Myers Squibb Research & Development
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bristol-Myers Squibb
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Biocon-Bristol Myers Squibb Research and Development Center
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Bristol-Myers Squibb Research & Development
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-
Biocon-Bristol Myers Squibb Research and Development Center
Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.
Bristol-Myers Squibb
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Bristol-Myers Squibb
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
Bristol Myers Squibb
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).
Biocon Bristol Myers Squibb Research Center (Bbrc)
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead.
Bristol-Myers Squibb
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Bristol Myers Squibb
beta-alanine dipeptides as MC4R agonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Bristol-Myers Squibb Research & Development
Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders.
Sanofi R&D
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Bristol-Myers Squibb
Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Bristol-Myers Squibb
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.
Bristol Myers Squibb
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.
Bristol-Myers Squibb
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Bristol Myers Squibb
The discovery of novel, potent and selective PDE5 inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu
Vanderbilt University
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Bristol Myers Squibb
Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Bristol-Myers Squibb Research and Development
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.
Bristol-Myers Squibb Research & Development
Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine β-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.
Bristol-Myers Squibb
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.
Bristol-Myers Squibb Research & Development
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.
Bristol-Myers Squibb
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
Pfizer
Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.
Bristol-Myers Squibb Research and Development
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors.
Bristol-Myers Squibb R&D
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu
Vanderbilt University
Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor.
Bristol-Myers Squibb Pharmaceutical Research Institute
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Bristol-Myers Squibb Research and Development
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
Pfizer
Development of spiroguanidine-derivedα7 neuronal nicotinic receptor partial agonists.
Bristol-Myers Squibb Research and Development
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.
Pfizer
1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors.
Pfizer
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Bristol-Myers Squibb
COMPOSITION FOR PREVENTING OR TREATING GRAVES' DISEASE COMPRISING COMPOUND CONTAINING AN IMIDAZOPYRIDINE STRUCTURE AS ACTIVE INGREDIENT
Esgelbio
NAMPT ACTIVATORS FOR TREATING METABOLIC AND NEUROLOGICAL DISORDERS
University of Illinois
Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
Revolution Medicines
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer
The Institute of Cancer Research: Royal Cancer Hospital
Diaminopyrimidine benzenesulfone derivatives and uses thereof
Dana-Farber Cancer Institute
Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors
Merck Sharp & Dohme
Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
Jenrin Discovery
Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
Forma Therapeutics
Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators
Beigene
Effects of some drugs on human cord blood erythrocyte carbonic anhydrases I and II: an in vitro study.
Erzincan University
In vitro effects of some drugs on human erythrocyte glutathione reductase.
Ataturk University
Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer's disease.
Sichuan University
Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
Acetylon Pharmaceuticals
Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.
Tehran University of Medical Sciences
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
Birla Institute of Technology
Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding.
Academia Sinica