873537-45-2Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0310, (2021/01/23)
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
REMODILINS TO PREVENT OR TREAT CANCER METASTASIS, GLAUCOMA, AND HYPOXIA
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Paragraph 0137; 0239, (2020/10/20)
Disclosed herein is a class of molecules termed remodilins that inhibit serum response factor (SRF). By inhibiting SRF, a number of downstream pathways can be targeted. The remodilins can be used to treat glaucoma, inhibit tumor cell growth, inhibit tumor metastasis, inhibit hypoxia-induced response, and/or reduce cellular metabolism.
REMODILINS FOR AIRWAY REMODELING AND ORGAN FIBROSIS
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Paragraph 0222, (2020/10/20)
Disclosed herein is a class of molecules termed remodilins that are effective in treating asthma, pulmonary fibrosis, and associated disorders. The molecules ameliorate asthma and pulmonary fibrosis symptoms by various mechanisms, including inhibiting air
Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors
Ferguson, Fleur M.,Ni, Jing,Zhang, Tinghu,Tesar, Bethany,Sim, Taebo,Kim, Nam Doo,Deng, Xianming,Brown, Jennifer R.,Zhao, Jean J.,Gray, Nathanael S.
supporting information, p. 908 - 912 (2016/10/22)
Dual inhibition of PI3K-δ and PI3K-γ is an established therapeutic strategy for treatment of hematological malignancies. Reported molecules targeting PI3K-δ/γ selectively are chemically similar and based upon isoquinolin-1(2H)-one or quinazolin-4(3H)-one scaffolds. Here we report a chemically distinct series of potent, selective PI3K-δ/γ inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold with comparable biochemical potency and cellular effects on PI3K signaling. We envisage these molecules will provide useful leads for development of next-generation PI3K-δ/γ targeting therapeutics.
Fluorinated pyrrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors
Le Darz, Alexandre,Mingot, Agnès,Bouazza, Fodil,Castelli, Ugo,Karam, Omar,Tanc, Muhammet,Supuran, Claudiu T.,Thibaudeau, Sébastien
, p. 737 - 745 (2015/09/15)
A series of substituted pyrrolidines and piperidines were synthesized using superacid HF/SbF5 chemistry. Investigated as inhibitors of several human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, i.e. the cytosolic hCA I and II as well as the t
Discovery of sulfonamidebenzamides as selective apoptotic CHOP pathway activators of the unfolded protein response
Flaherty, Daniel P.,Miller, Justin R.,Garshott, Danielle M.,Hedrick, Michael,Gosalia, Palak,Li, Yujie,Milewski, Monika,Sugarman, Eliot,Vasile, Stefan,Salaniwal, Sumeet,Su, Ying,Smith, Layton H.,Chung, Thomas D. Y.,Pinkerton, Anthony B.,Aub, Jeffrey,Callaghan, Michael U.,Golden, Jennifer E.,Fribley, Andrew M.,Kaufman, Randal J.
supporting information, p. 1278 - 1283 (2015/01/09)
Cellular proteins that fail to fold properly result in inactive or disfunctional proteins that can have toxic functions. The unfolded protein response (UPR) is a two-tiered cellular mechanism initiated by eukaryotic cells that have accumulated misfolded p
INHIBITORS OF PROTEIN KINASES
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Page/Page column 130, (2009/12/05)
The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex
Sun, Aiming,Yoon, Jeong-Joong,Yin, Yan,Prussia, Andrew,Yang, Yutao,Min, Jaeki,Plemper, Richard K.,Snyder, James P.
scheme or table, p. 3731 - 3741 (2009/04/10)
Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds could conceivably diminish these statistics and pr
