- NEUROPROTECTIVE PDI MODULATING SMALL MOLECULES AND METHODS OF USE THEREOF
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The present disclosure provides, inter alia, compounds and compositions having the formula (I) as defined herein. Methods of using and making such compounds and compositions are also provided. The present disclosure further provides screening methods, including detectable probes as well as diagnostic methods and methods for monitoring the progress of a disease, such as a neurodegenerative disease.
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- Isothiazolinone compound and corresponding application
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The invention provides an isothiazolinone compound with an IDO inhibitory activity, and a preparing method and pharmaceutical application thereof. The invention particularly relates to a compound shown in a formula I, pharmaceutically acceptable salts thereof, isomers and prodrugs, wherein definitions of all groups are shown in the description. The invention further relates to compound drug preparations, drug compositions and the application of the compound drug preparations and the drug compositions in treating, relieving and/or preventing various relevant diseases caused by immunosuppressionsuch as tumors, virus infection or autoimmune diseases. The isothiazolinone compound has the excellent IDO inhibitory activity.
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Paragraph 0077-0083
(2019/07/08)
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- CRBN LIGANDS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
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Paragraph 00485-00487
(2019/08/20)
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- Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors
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We present a combination of database screening, synthesis and in vitro testing to identify novel histone acetyltransferase (HAT) inhibitors. The National Cancer Institute compound collection (NCI) and several commercial databases were filtered by similarity-based virtual screening to find new HAT inhibitors. Employing the recombinant HAT p300/CBP-associated factor (PCAF) and two different histone substrates for screening, pyridoisothiazolones were identified as inhibitors of human PCAF. Due to the limited solubility of the initial hits, we synthesized and tested them on PCAF. The compounds inhibit the proliferation of cancer cells. In summary, valuable chemical tools and potential lead candidates for new anticancer agents directed against HATs as new targets have been identified.
- Furdas, Silviya D.,Shekfeh, Suhaib,Bissinger, Elisabeth-Maria,Wagner, Julia M.,Schlimme, Sonja,Valkov, Vassil,Hendzel, Michael,Jung, Manfred,Sippl, Wolfgang
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experimental part
p. 3678 - 3689
(2011/08/03)
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- Pyridinethiones. IX Preparation of Ricinidine, Thioricinidine and Other 2(1H)-Pyridones and -thiones Related to Nicotinic acid
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1(1H)-Pyridones and -thiones related to 1-substituted nicotinic acid derivatives have been prepared via the corresponding 1-substituted-3-formyl-2(1H)-pyridones and -thiones.A number of synthetic procedures for the interconversion of functional groups in these nicotinic acid derivatives are given i.e. preparation of the aldoximes, nitriles, carboxamides and carboxylic acids as well as the 3-hydroxyalkyl derivatives.The course of the basic peroxide oxidation of the 1-substituted-3-formyl-2(1H)-pyridinethiones is found to be very dependent upon the electronegativity ofthe 1-substituent.A preparation of ricinidine is also described.
- Becher, Jan,Johansen, Tea,Michael, Maged Aziz
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