95656-86-3Relevant academic research and scientific papers
Multi-arm polymeric prodrug conjugates of pemetrexed-based compounds
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Page/Page column 43; 44; 45, (2020/08/30)
Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of pemetrexed-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved.
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells
Che, Jinxin,Chen, Binhui,Dong, Xiaowu,Gao, Anhui,Gao, Jian,Hu, Xiaobei,Hu, Yongzhou,Huang, Feng,Li, Jia,Qu, Bingxue,Xu, Gaoya,Ying, Huazhou,Zhang, Jianjun,Zhang, Mengmeng,Zhou, Yubo
, (2020/07/15)
The enzymes involved in the metabolic pathways in cancer cells have been demonstrated as important therapeutic targets such as the isocitrate dehydrogenase 2 (IDH2). A series of macrocyclic derivatives was designed based on the marketed IDH2 inhibitor AG-221 by using the conformational restriction strategy. The resulted compounds showed moderate to good inhibitory potential against different IDH2-mutant enzymes. Amongst, compound C6 exhibited better IDH2R140Q inhibitory potency than AG-221, and showed excellent activity of 2-hydroxyglutarate (2-HG) suppression in vitro and its mesylate displayed good pharmacokinetic profiles. Moreover, C6 performed strong binding mode to IDH2R140Q after computational docking and dynamic simulation, which may serve as a good starting point for further development.
QUINOLINE AND QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 00453-00454, (2020/10/09)
Compounds and methods for their preparation and use as therapeutic or prophylactic agents, fo example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase- 1 (ENPP1).
NON-FUSED TRICYCLIC COMPOUNDS
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Paragraph 00671, (2018/11/26)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
POLYFLUORINATED COMPOUNDS ACTING AS BRUTON TYROSINE KINASE INHIBITORS
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Paragraph 0779; 0780, (2016/08/17)
Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
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Paragraph 0768; 0769, (2016/12/22)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
ANTHRACYCLINE DISULFIDE INTERMEDIATES, ANTIBODY-DRUG CONJUGATES AND METHODS
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Paragraph 0324-0326; 0330, (2016/04/09)
The invention provides antibody-drug conjugates comprising an antibody conjugated to an anthracycline drug moiety via a disulfide linker, anthracycline disulfide intermediates, and methods of using the antibody-drug conjugates.
NOVEL CONDENSED PYRAZOLE DERIVATIVE AND MEDICAL USES THEREOF
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Paragraph 0270; 0271, (2016/10/10)
PROBLEM TO BE SOLVED: To provide a preventive or therapeutic agent for mood disorder, anxiety disorder, schizophrenia, dementia, drug dependence or the like related to subtypes of metabolism type glutamate receptor (mGlu) 2 and 3. SOLUTION: There are prov
CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
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Page/Page column 27; 28; 29, (2016/07/05)
The present invention relates to a chemical blowing agent comprising at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can for example be incorporated into thermally expandable baffle and/or reinforcement elements which are used in automotive manufacturing and building insulation.
