236406-14-7Relevant academic research and scientific papers
2,3-DIHYDRO-1H-PYRROLIZINE-7-FORMAMIDE DERIVATIVE AND APPLICATION THEREOF
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, (2021/04/16)
The present application relates to a 2,3-dihydro-1H-pyrrolizine-7-formamide derivative as a nucleoprotein inhibitor and a use in preparation of a drug for treating HBV related diseases. The present application specifically relates to a compound represented by formula (II), and isomers or pharmaceutically acceptable salts thereof.
Methods for treating neisseria gonorrhoeae infection with substituted 1,2-dihydro-2A,5,8A-triazaacenaphthylene-3,8-diones
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Page/Page column 90, (2020/07/21)
The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.
SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Paragraph 0149, (2018/04/20)
The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for suppressing tumor cell growth, ameliorating the pathogenesis of systemic lupus erythematosus, and the treatment of various other disorders, including Noonan syndrome, diabetes, neutropenia, neuroblastoma, melanoma, juvenile leukemia, juvenile myelomonocytic leukemia, chronic myelomonocytic leukemia, acute myeloid leukemia, and other cancers associated with SHP2 deregulation with the compounds and compositions of the invention, alone or in combination with other treatments. Other cancers associated with SHP2 deregulation include HER2-positive breast cancer, triple-negative breast cancer, ductal carcinoma of the breast, invasive ductal carcinoma of the breast, non-small cell lung cancer, esophageal cancer, gastric cancer, squamous-cell carcinoma of the head and neck (SCCHN), and colon cancer.
BROMODOMAIN INHIBITORS AND USES THEREOF
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Page/Page column 147, (2016/06/06)
The present invention relates to compounds of formula (I): [INSERT FORMULA (1)] and to salts thereof, wherein R1, R2, Rc, and Rd have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.
COMPOUNDS AND METHODS
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, (2013/03/26)
The present invention relates to novel retinoid-related orphan receptor gamma (RORy) modulators and their use in the treatment of diseases mediated by RORy.
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors
Kulagowski, Janusz J.,Blair, Wade,Bull, Richard J.,Chang, Christine,Deshmukh, Gauri,Dyke, Hazel J.,Eigenbrot, Charles,Ghilardi, Nico,Gibbons, Paul,Harrison, Trevor K.,Hewitt, Peter R.,Liimatta, Marya,Hurley, Christopher A.,Johnson, Adam,Johnson, Tony,Kenny, Jane R.,Bir Kohli, Pawan,Maxey, Robert J.,Mendonca, Rohan,Mortara, Kyle,Murray, Jeremy,Narukulla, Raman,Shia, Steven,Steffek, Micah,Ubhayakar, Savita,Ultsch, Mark,Van Abbema, Anne,Ward, Stuart I.,Waszkowycz, Bohdan,Zak, Mark
experimental part, p. 5901 - 5921 (2012/08/27)
A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as rheumatoid arthritis (RA), by specific targeting of the JAK1 pathway. Examination of the preferred binding conformation of clinically effective, pan-JAK inhibitor 1 led to identification of a novel, tricyclic hinge binding scaffold 3. Exploration of SAR through a series of cycloamino and cycloalkylamino analogues demonstrated this template to be highly tolerant of substitution, with a predisposition to moderate selectivity for the JAK1 isoform over JAK2. This study culminated in the identification of subnanomolar JAK1 inhibitors such as 22 and 49, having excellent cell potency, good rat pharmacokinetic characteristics, and excellent kinase selectivity. Determination of the binding modes of the series in JAK1 and JAK2 by X-ray crystallography supported the design of analogues to enhance affinity and selectivity.
IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
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, (2008/12/04)
Compounds of Formula (I) in which A, B, R1, R1a, R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1
TRICYCLIC NITROGEN CONTAINING COMPOUNDS AS ANTIBACTERIAL AGENTS
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Page/Page column 74-75, (2008/12/08)
Tricyclic nitrogen containing compounds and their use as antibacterials. Z1and Z2 are independently selected from CH and N.
HETEROCYCLIC-SUBSTITUTED PIPERDINE COMPOUNDS AND THE USES THEREOF
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Page/Page column 234, (2008/12/07)
The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl] amino-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): A very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes
Madar, David J.,Kopecka, Hana,Pireh, Daisy,Yong, Hong,Pei, Zhonghua,Li, Xiaofeng,Wiedeman, Paul E.,Djuric, Stevan W.,Von Geldern, Thomas W.,Fickes, Michael G.,Bhagavatula, Lakshmi,McDermott, Todd,Wittenberger, Steven,Richards, Steven J.,Longenecker, Kenton L.,Stewart, Kent D.,Lubben, Thomas H.,Ballaron, Stephen J.,Stashko, Michael A.,Long, Michelle A.,Wells, Heidi,Zinker, Bradley A.,Mika, Amanda K.,Beno, David W. A.,Kempf-Grote, Anita J.,Polakowski, James,Segreti, Jason,Reinhart, Glenn A.,Fryer, Ryan M.,Sham, Hing L.,Trevillyan, James M.
, p. 6416 - 6420 (2008/04/18)
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are poised to be the next major drug class for the treatment of type 2 diabetes. Structure-activity studies of substitutions at the C5 position of the 2-cyanopyrrolidide warhead led to the discovery of potent inhibitors of DPP-IV that lack activity against DPP8 and DPP9. Further modification led to an extremely potent (KiDPP-IV = 1.0 nM) and selective (KiDPP8 > 30 μM; KiDPP9 > 30 μM) clinical candidate, ABT-279, that is orally available, efficacious, and remarkably safe in preclinical safety studies.
