上下游产品
3-Aminomethylpyridine (1-{[1-Phenyl-meth-(E)-ylidene]-amino}-2-pyridin-3-yl-ethyl)-phosphonic acid diethyl ester 3-pyridinecarboxaldehyde 2-[isobutyl-(4-methoxy-benzenesulfonyl)-amino]-4-(pyridin-3-ylmethylsulfanyl)-butyric acid methyl ester (+)-(R,R,R)-1,3,5-tris[1-methoxy-2-(3-pyridyl)ethyl]benzene 3-甲基吡啶置于溴,Silica Gel体系中,用 四氯化碳 作为反应溶剂,化学反应 24.0H,反应生成 3-溴甲基吡啶
参考文献:Increasing The Selectivity Of Bromination Of Aromatic Compounds Using Br2/sio2
标题:Increasing The Selectivity Of Bromination Of Aromatic Compounds Using Br2/sio2
摘要:在硅胶存在下,几种芳香烃如甲苯,邻-,间-,对-二甲苯,蒽和酚在温和条件下被br2溴化;例如,Br2/sio2在25oc下能迅速溴化萘反应生成1-溴萘.为了比较,我们还在没有硅胶的情况下用溴对所有底物进行了溴化.
DOI:10.1246/bcsj.74.1151
专利信息
专利号:US-2022265691-A1
优先权日:2019-07-12
标 题 :Methods for use of gene expression as an indicator of e-selectin inhibitor efficacy and clinical outcome for multiple tumor types
发明人:MAGNANI JOHN L; FOGLER WILLIAM E; THACKRAY HELEN M; FELDMAN ERIC J; STEWART DAVID
权利人:GLYCOMIMETICS INC
摘要:Cancer patients that express high levels of the E-selectin ligand (sialyl Lea/x) on their tumors have a poorer outcome. Interestingly, relapsed/refractory acute myeloid leukemia (AML) patients expressing high levels of sialyl Lex on their blasts show the greatest therapeutic response when treated with the E-selection inhibitor compound of Formula I. Transcriptome profiling of E-selectin ligand-forming glycosylation genes showed that ST3GAL4 and FUT7 were consistently expressed in the majority of cancers evaluated. Poor survival outcomes of FLT3-mutated AML patients that express high levels of ST3GAL4 and FUT7 implicated E-selectin in this disease state. These genes may be predictive biomarkers in AML patients. Methods of treatment of cancer comprising screening AML patients for expression of genes that contribute to the synthesis of the E-selectin ligand sialyl Lex, then treating those patients with an E-selection inhibitor, are disclosed.
专利号:US-6281245-B1
优先权日:1996-10-28
标 题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof
发明人:PATEL DINESH V; NGU KHEHYONG
权利人:VERSICOR INC
摘要:A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteinases).
专利号:US-6541276-B2
优先权日:1996-10-28
标题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives and combinatorial libraries thereof
发明人:PATEL DINESH V; NGU KHEHYONG
权利人:VERSICOR INC
摘要:A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteases).
专利号:US-2023192718-A1
优先权日:2018-03-30
标 题 :Bicyclic enone carboxylates as modulators of transporters and uses thereof
发明人:SANDANAYAKA VINCENT
权利人:NIROGY THERAPEUTICS INC
摘要:The invention generally relates to the field of monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate enone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.
专利号:US-8476313-B2
优先权日:2004-08-26
标 题:Heteroaryl-containing isoflavones as aromatase inhibitors
发明人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C
权利人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C; UNIV OHIO STATE RES FOUND
摘要:Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: n nwherein X is selected from O, N, S, SO, SO 2 , and S(CH 2 ) n , wherein n=1-10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
专利号:WO-2010096722-A1
优先权日:2009-02-20
标 题 :3-oxo-2, 3-dihydro- [1,2, 4] triazolo [4, 3-a]pyridines as soluble epoxide hydrolase (seh) inhibitors
发明人:FENG JUN; KEUNG WALTER; NOTZ WOLFGANG REINHARD LUDWIG
权利人:TAKEDA PHARMACEUTICAL; FENG JUN; KEUNG WALTER; NOTZ WOLFGANG REINHARD LUDWIG
摘要:Claimed are intermediates in the synthesis of N-Arylmethyl-3-Oxo-2,3-dihydro- [1,2,4]triazolo[4,3-a]pyridine-6-carboxamides as well as a process (A) to arrive at 3-Oxo-2, 3-dihydro-[1,2,4]triazolo[4,3-a]pyridine-6-carboxylic acid. The triazolo[4,3-a]pyridine-6-carboxamides of formula (I) are used as soluble epoxide hydrolase inhibitors (sEH) having therapeutic effect in pathologic conditions such as hypertension, stroke, inflammatory processes, diabetes and a variety of cardiovascular diseases.