CAS: 762287-57-0; (4-Chloro-2-Methoxyphenyl)Boronic Acid

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CAS号174913-09-8 2-溴-5-氯苯甲醚 | CAS号1377503-12-2 2-羟基-4-氯苯硼酸频哪醇酯

2-溴-5-氯苯甲醚置于正丁基锂,Triisopropyl Borate,盐酸体系中,用 四氢呋喃,正己烷,水,乙酸乙酯 作为反应溶剂,化学反应 1.0H,反应生成 4-氯-2-甲氧基苯硼酸
参考文献:New 5-Aryl-1H-Imidazoles Display In Vitro Antitumor Activity Against Apoptosis-Resistant Cancer Models,Including Melanomas,Through Mitochondrial Targeting
标题:New 5-Aryl-1H-Imidazoles Display In Vitro Antitumor Activity Against Apoptosis-Resistant Cancer Models,Including Melanomas,Through Mitochondrial Targeting
摘要:We Designed And Synthesized 48 Aryl-1H-Imidazole Derivatives And Investigated Their In Vitro Growth Inhibitory Activity In Cancer Cell Lines Known To Present Various Levels Of Resistance To Proapoptotic Stimuli. The Ic50 In Vitro Growth Inhibitory Concentration Of These Compounds Ranged From >100 Mu M To Single Digit Mu M. Among The Most Active Compounds,2I Displayed Similar In Vitro Growth Inhibition In Cancer Cells Independent Of The Cells' Levels Of Resistance To Proapoptotic Stimuli And Was Found To Be Cytostatic In Melanoma Cell Lines. Compound 2I Was Then Tested By The National Cancer Institute Human Tumor Cell Line Anti-Cancer Drug Screen,And The Nci Compare Algorithm Did Not Reveal Any Correlation Between Its Growth Inhibition Profiles With The Nci Database Compound Profiles. The Use Of Transcriptomically Characterized Melanoma Models Then Enabled Us To Highlight Mitochondrial Targeting By 2I. This Hypothesis Was Further Confirmed By Reactive Oxygen Production Measurement And Oxygen Consumption Analysis.
DOI:10.1021/jm400287V

专利信息

专利号:US-7968752-B2
优先权日:2003-06-16
标 题:Hydrolytically-resistant boron-containing therapeutics and methods of use
发明人：LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A
权利人:ANACOR PHARMACEUTICALS INC
摘要:Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.

专利号:US-7645754-B2
优先权日:2001-12-20
标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

专利号:US-2025026766-A1
优先权日:2022-01-12
标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors
发明人：LI JING; XU WENQING; WANG ZHIWEI
权利人:BEIGENE LTD
摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.

专利号:US-9951062-B2
优先权日:2012-12-14
标 题 :Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
发明人：VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANIPISETTY VENU BABU; TALLURI SURESHKUMAR; APPALANENI RAJENDRA P
权利人:ARRIEN PHARMACEUTICALS LLC
摘要:Compounds according to Formulas I, IA or IB: n nto pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.