The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties-Reference-Cited by-同舟云学术

The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties

Published:2017-12-04 Issue:23 Volume:60 Page:9676-9690
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Siu Tony¹²^ORCID,Brubaker Jason¹²,Fuller Peter¹²,Torres Luis¹²,Zeng Hongbo¹²,Close Joshua¹²,Mampreian Dawn M.¹²,Shi Feng¹²,Liu Duan¹²,Fradera Xavier¹²,Johnson Kevin¹²,Bays Nathan¹²,Kadic Elma¹²,He Fang¹²,Goldenblatt Peter¹²,Shaffer Lynsey¹²,Patel Sangita B.¹²,Lesburg Charles A.¹²,Alpert Carla¹²,Dorosh Lauren¹²,Deshmukh Sujal V.¹²,Yu Hongshi¹²,Klappenbach Joel¹²,Elwood Fiona¹²,Dinsmore Christopher J.¹²,Fernandez Rafael¹²,Moy Lily¹²,Young Jonathan R.¹²

Affiliation:

1. Department of Medicinal Chemistry, ‡Department of Discovery Process Chemistry, §Department of Modeling & Informatics, ∥Department of In Vitro Pharmacology, ⊥Department of Structural Chemistry, #Department of Pharmacokinetics Pharmacodynamics and Drug Metabolism, ∇Department of Discovery Pharmaceutical Sciences, ○Department of Molecular Biomarkers, ¶Department of In Vivo Pharmacology, $Department of Respiratory and Immunology, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United...

2. Department of Chemistry and ◇Department of Biology, Pharmaron Beijing Co. Ltd, 6 Taihe Road BDA, Beijing 100176, P.R. China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.7b01135

Reference51 articles.

1. Regulation of JAK–STAT signalling in the immune system

2. Therapeutic targeting of Janus kinases

3. The JAK-STAT Pathway: Impact on Human Disease and Therapeutic Intervention

4. Advances in the treatment of inflammatory arthritis

5. The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo

Cited by 14 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Revisiting Structure-activity Relationships: Unleashing the potential of selective Janus kinase 1 inhibitors;Bioorganic Chemistry;2024-08

2. Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity;European Journal of Medicinal Chemistry;2024-03

3. Insight into Janus kinases specificity: From molecular architecture to cancer therapeutics;MedComm – Oncology;2024-03

4. Discovery of C-5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1;Journal of Medicinal Chemistry;2023-05-10

5. Pharmacophore-Based Virtual Screening and Experimental Validation of Pyrazolone-Derived Inhibitors toward Janus Kinases;ACS Omega;2022-09-06