16513-67-0Relevant academic research and scientific papers
THIENODIAZEPINE DERIVATIVES AND APPLICATION THEREOF
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Paragraph 0232-0234, (2020/08/09)
The present invention relates to a class of thienodiazepine derivatives and an application thereof in the preparation of a drug for the treatment of diseases associated with bromodomain and extra-terminal (BET) Bromodomain inhibitors. Specifically, the present invention relates to compounds represented by formulas (I) and (II), as well as pharmaceutically acceptable salts thereof.
A kind of indan -5 - carboxamide ROR γ regulator and its use
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, (2019/03/15)
The invention relates to a structure of formula (I) compound of formula or a stereoisomer thereof, tautomers or its pharmaceutically acceptable salt or solvate or prodrug, its preparation method, a pharmaceutical composition containing these modulators and their use in the treatment ROR γ-mediated inflammatory, metabolic and autoimmune disorders.
Design, synthesis and evaluation of indene derivatives as retinoic acid receptor α agonists
Guan, Xianghong,Luo, Peihua,He, Qiaojun,Hu, Yongzhou,Ying, Huazhou
, (2017/01/24)
A series of novel indene-derived retinoic acid receptor α (RARα) agonists have been designed and synthesized. The use of receptor binding, cell proliferation and cell differentiation assays demonstrated that most of these compounds exhibited moderate RARα binding activity and potent antiproliferative activity. In particular, 4-((3-isopropoxy-2,3-dihydro-1H-inden-5-yl)-carbamoyl) benzoic acid (36d), which showed a moderate binding affinity, exhibited a great potential to induce the differentiation of NB4 cells (68.88% at 5 μM). Importantly, our work established indene as a promising skeleton for the development of novel RARα agonists.
Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ
Pujala, Brahmam,Agarwal, Anil K.,Middya, Sandip,Banerjee, Monali,Surya, Arjun,Nayak, Anjan K.,Gupta, Ashu,Khare, Sweta,Guguloth, Rambabu,Randive, Nitin A.,Shinde, Bharat U.,Thakur, Anamika,Patel, Dhananjay I.,Raja, Mohd.,Green, Michael J.,Alfaro, Jennifer,Avila, Patricio,Pérez de Arce, Felipe,Almirez, Ramona G.,Kanno, Stacy,Bernales, Sebastián,Hung, David T.,Chakravarty, Sarvajit,McCullagh, Emma,Quinn, Kevin P.,Rai, Roopa,Pham, Son M.
supporting information, p. 1161 - 1166 (2016/12/16)
The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3Kδ are kinases responsible for B-cell signal transduction, and inhibitors of these enzymes have demonstrated clinical benefit in certain types of lymphoma. Simultaneous inhibition of these pathways could result in more robust responses or overcome resistance as observed in single agent use. We report a series of novel compounds that have low nanomolar potency against both BTK and PI3Kδ as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Paragraph 0448, (2015/05/05)
The present application discloses compounds that are inhibitors of Btk, compounds that are inhibitors of ΡΒΚδ, and compounds that are dual inhibitors of both Btk and PI3Kδ. Also described are methods for synthesizing such inhibitors and methods for using such inhibitors for the treatment of diseases wherein inhibition of Btk and PI3Kδ provides a therapeutic benefit to a patient having the disease.
TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY
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Page/Page column 204-205, (2008/06/13)
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
Photoaddition of Water and Alcohols to 3-Nitrostyrenes. Structure-Reactivity and Solvent Effects
Wan, Peter,Davis, Michael J.,Teo, Mary-Anne
, p. 1354 - 1359 (2007/10/02)
The photoadditions of water and several alcohols to the triplet excited states of 3-nitrostyrenes 1, 3-5, and 8 to give the corresponding anti-Markovnikov addition products are reported.Both 3- and 4-nitrostilbenes (6 and 7, respectively) do not undergo photoaddition on direct or sensitized irradiation in aqeous or alcohol solutions; only trans to cis photoisomerisation is observed.It is proposed that for the nitrostilbenes, efficient twisting of the alkene in the triplet excited state competes favorably with photoaddition.The efficient photoaddition of the water and methanol observed for 5-nitroindene (8)-the alkene moiety of which cannot attain an orthogonal ("twisted") state-is taken as additional evidence that these photoadditions probably occur via the planar triplet state and that twisting results in only deactivation to the ground state.The use of cosolvents (CH3CN and HCONH2) on several photoadditions is also reported.For example, use of CH3CN cosolvent in aqueous solution decreases the efficiency of photohydration in the parent 3-nitrostyrene (1) but is observed to enhance the efficiency of reaction (until about 40-70 mol percent CH3CN, depending on the substrate) for 3, 4, and 8.Quantum yields for photohydration and photoaddition of alcohols are reported for several systems.
