719 results on '"Macor, John E."'
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2. What I Did on My Summer Vacation and Molecules That Broke My Heart: Insights from a 35-Year Adventure In Drug Discovery
3. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors
4. Design, Structure–Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors
5. Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia
6. Site-Selective C–H Functionalization of N-Aryl and N-Heteroaryl Piperidines, Morpholines, and Piperazines Controlled by a Chiral Dirhodium Tetracarboxylate Catalyst
7. 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
8. Structure-Activity Relationship (SAR) Studies on Substituted 2-(Pyridin-2-ylamino)-N-(pyridin-3-yl)isonicotinamide as Highly Potent, Selective and Brain Penetrant Glycogen Synthase Kinase-3 (GSK-3) Inhibitors
9. Structure–activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4′ and C6 variations
10. Identification and characterization of a MAPT-targeting locked nucleic acid antisense oligonucleotide therapeutic for tauopathies
11. Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8)
12. 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
13. Discovery of (S)-1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain
14. Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists–serotonin reuptake transporter inhibitors for the treatment of depression
15. B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor
16. Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors
17. Development of a Rapid Scale-Up Synthesis of (S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide, a Potent Adaptor-Associated Kinase 1 Inhibitor
18. Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead
19. 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
20. Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists
21. Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite
22. In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10)
23. NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the Gerbil forced swim test
24. Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2
25. Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches
26. Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach
27. Pharmacological and behavioral characterization of the novel CRF1 antagonist BMS-763534
28. Preface
29. Development of a Rapid Scale-Up Synthesis of (S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide, a Potent Adaptor-Associated Kinase 1 Inhibitor.
30. Preface
31. Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders
32. Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist
33. Preface
34. Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt—Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy
35. Characterization of the in vitro atropisomeric interconversion rates of an endothelin A antagonist by enantioselective liquid chromatography
36. Heteroarylsulfonamido Biphenyls as Potent Dual Antagonists Blocking Angiotensin and Endothelin Receptors and Useful as Novel Anti-hypertensives
37. Chapter 7. Advances in the understanding and treatment of congestive heart failure (HF)
38. Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability
39. 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
40. Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
41. 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)
42. Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481
43. The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate
44. Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson’s Disease
45. Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability
46. Design and synthesis of a novel series of 4-heteroarylamino-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR
47. Development of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists
48. Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential
49. Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors
50. Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box
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