552331-15-4Relevant academic research and scientific papers
TREATMENT OF FIBROSIS WITH IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00199, (2020/11/30)
Provided herein are methods of using IRE1 small molecule inhibitors in combination therapies for treating fibrosis in a subject. The IRE1 small molecule inhibitors described herein may be used in combination therapies for treating fibrosis
IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00151, (2020/07/06)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a
COMBINATION THERAPIES WITH IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00223, (2020/12/01)
Provided herein are methods of using IRE1 small molecule inhibitors in combination therapies for treating cancer in a subject. The IRE1 small molecule inhibitors described herein may be used in combination therapies for treating solid and hematologic cancers.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 0960-0962, (2019/04/25)
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00259, (2019/05/30)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00260, (2018/06/22)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a
IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00175, (2019/01/05)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer
Zhu, Wei,Chen, Hui,Wang, Yulan,Wang, Jiang,Peng, Xia,Chen, Xianjie,Gao, Yinglei,Li, Chunpu,He, Yulong,Ai, Jing,Geng, Meiyu,Zheng, Mingyue,Liu, Hong
, p. 6018 - 6035 (2017/08/02)
A novel series of pyridin-3-amine derivatives were designed, synthesized, and evaluated as multitargeted protein kinase inhibitors for the treatment of non-small cell lung cancer (NSCLC). Hit 1 was first disclosed by in silico screening against fibroblast
FUSED AMINODIHYDROPYRIMIDINE DERIVATIVE
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Paragraph 0200; 0201, (2013/08/28)
The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2═X3 is CR5—CR6═CRs
Maximizing lipophilic efficiency: The use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase
Freeman-Cook, Kevin D.,Amor, Paul,Bader, Scott,Buzon, Leanne M.,Coffey, Steven B.,Corbett, Jeffrey W.,Dirico, Kenneth J.,Doran, Shawn D.,Elliott, Richard L.,Esler, William,Guzman-Perez, Angel,Henegar, Kevin E.,Houser, Janet A.,Jones, Christopher S.,Limberakis, Chris,Loomis, Katherine,McPherson, Kirk,Murdande, Sharad,Nelson, Kendra L.,Phillion, Dennis,Pierce, Betsy S.,Song, Wei,Sugarman, Eliot,Tapley, Susan,Tu, Meihua,Zhao, Zhengrong
supporting information; experimental part, p. 935 - 942 (2012/03/11)
This paper describes the design and synthesis of a novel series of dual inhibitors of acetyl-CoA carboxylase 1 and 2 (ACC1 and ACC2). Key findings include the discovery of an initial lead that was modestly potent and subsequent medicinal chemistry optimization with a focus on lipophilic efficiency (LipE) to balance overall druglike properties. Free-Wilson methodology provided a clear breakdown of the contributions of specific structural elements to the overall LipE, a rationale for prioritization of virtual compounds for synthesis, and a highly successful prediction of the LipE of the resulting analogues. Further preclinical assays, including in vivo malonyl-CoA reduction in both rat liver (ACC1) and rat muscle (ACC2), identified an advanced analogue that progressed to regulatory toxicity studies.
