147269-67-8Relevant academic research and scientific papers
Identification of Imidazo[1,2- b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors
Liu, Chunjian,Lin, James,Moslin, Ryan,Tokarski, John S.,Muckelbauer, Jodi,Chang, ChiehYing,Tredup, Jeffrey,Xie, Dianlin,Park, Hyunsoo,Li, Peng,Wu, Dauh-Rurng,Strnad, Joann,Zupa-Fernandez, Adriana,Cheng, Lihong,Chaudhry, Charu,Chen, Jing,Chen, Cliff,Sun, Huadong,Elzinga, Paul,D'Arienzo, Celia,Gillooly, Kathleen,Taylor, Tracy L.,McIntyre, Kim W.,Salter-Cid, Luisa,Lombardo, Louis J.,Carter, Percy H.,Aranibar, Nelly,Burke, James R.,Weinstein, David S.
, p. 383 - 388 (2019)
In sharp contrast to a previously reported series of 6-anilino imidazopyridazine based Tyk2 JH2 ligands, 6-((2-oxo-N1-substituted-1,2-dihydropyridin-3-yl)amino)imidazo[1,2-b]pyridazine analogs were found to display dramatically improved metabolic stabilit
Optimization of peptide-based inhibitors targeting the HtrA serine protease in Chlamydia: Design, synthesis and biological evaluation of pyridone-based and N-Capping group-modified analogues
Hwang, Jimin,Strange, Natalie,Phillips, Matthew J.A.,Krause, Alexandra L.,Heywood, Astra,Gamble, Allan B.,Huston, Wilhelmina M.,Tyndall, Joel D.A.
, (2021/07/16)
The obligate intracellular bacterium Chlamydia trachomatis (C. trachomatis) is responsible for the most common bacterial sexually transmitted infection and is the leading cause of preventable blindness, representing a major global health burden. While C.
SYSTEMIC FORMULATION OF A PYRIDINONE DERIVATE FOR COELIAC DISEASE
-
Paragraph 0713; 0724-0726, (2021/11/04)
The present invention relates to a systemic formulation, in particular an oral formulation, for the prophylaxis and/or treatment of coeliac disease, i.e. for use in the prophylaxis and/or treatment of coeliac disease.
SYSTEMIC FORMULATION OF A PYRIDINONE DERIVATE FOR TG2-RELATED DISEASES
-
Paragraph 0666-0668, (2021/11/04)
The present invention relates to a formulation in particular an oral formulation for the prophylaxis and treatment of TG2-related disorders like fibrosis in particular diabetic nephropathy and/or diabetic associated non-alcoholic steatohepatitis (NASH) an
ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
-
Page/Page column 708, (2018/09/21)
Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
IMIDAZOPYRIDAZINE COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES
-
Page/Page column 83; 84, (2015/06/25)
Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
ARYLPYRIDINONE ITK INHIBITORS FOR TREATING INFLAMMATION AND CANCER
-
Paragraph 0176; 0215; 0216, (2015/08/04)
Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein Ar, R2, R4, R5, n and X are as defined in
Arylpyridinone ITK inhibitors for treating inflammation and cancer
-
Page/Page column 46, (2015/11/27)
Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein Ar, R2, R4, R5, n and X are as defined in
Development of Novel Peptidomimetics Containing a Vinyl Sulfone Moiety as Proteasome Inhibitors
Ettari, Roberta,Bonaccorso, Cinzia,Micale, Nicola,Heindl, Cornelia,Schirmeister, Tanja,Calabro, Maria Luisa,Grasso, Silvana,Zappala, Maria
experimental part, p. 1228 - 1237 (2012/04/18)
Proteasome inhibition is a topic of great interest in anticancer research. The proteolytic activity of this multicatalytic complex relies on three subunits, β1, β2 and β5, containing a caspase-like, a trypsin-like and a chymotrypsin-like active site, respectively. Several studies have demonstrated that, of the three activities, the chymotrypsin-like activity was the most necessary for cell viability and protein processing. Thus, most efforts towards the development of proteasome inhibitors have focused on the selective inhibition of the β5 subunit active site. Herein, we report the design and synthesis of a series of conformationally constrained tripeptidyl vinyl sulfones were determined to be good inhibitors of the chymotrypsin-like activity of proteasome, with KI values in the sub-micromolar to micromolar range. These compounds were also tested against bovine pancreatic α-chymotrypsin and human cathepsinB and L, revealing a good selectivity for the target enzyme over these related enzymes. Molecular straitjackets! Conformationally constrained tripeptidyl vinyl sulfones were identified as good inhibitors of proteasome chymotrypsin-like activity, with KI values in the sub-micromolar to micromolar range. Derivatives were also tested against bovine pancreatic α-chymotrypsin and human cathepsins B andL, revealing a good selectivity for the target enzyme.
3, 5-DISUBSTITUTED PYRID-2-ONES USEFUL AS INHIBITORS OF TEC FAMILY OF NON-RECEPTOR TYROSINE KINASES
-
Page/Page column 39-40, (2010/11/26)
The present invention relates to pyrid-2-one compounds of formula (I) useful as inhibitors of protein kinase of Tec family (e.g., Tec, Btk, Itk/Emt/Tsk, Bmx,Txk/Rlk) protein kinases. These compounds and pharmaceutically acceptable compositions thereof are
