异丁硫醇置于磺酰氯,Potassium Nitrate,碳酸氢钠体系中,用 乙腈,水 用作溶剂,化学反应 3.0H,以95%的收率获得2-甲基丙烷磺酰氯 参考文献: Cyclohexyl Sulphones As Gamma-Secretase Inhibitors[fr] Sulfones Cyclohexyliques Tels Que Des Inhibiteurs De Gamma-Secretase 标题: Cyclohexyl Sulphones As Gamma-Secretase Inhibitors[fr] Sulfones Cyclohexyliques Tels Que Des Inhibiteurs De Gamma-Secretase 摘要:式(I)的化合物抑制γ-分泌酶对app的加工,因此对治疗或预防阿尔茨海默病有用.
专利信息
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-6479668-B1 优先权日:1998-09-08 标 题 :Method of producing pyrrolidine derivatives 发明人:MURAOKA HIDEO; SATO HARUYO 权利人:TORAY INDUSTRIES 摘要:A method for producing pyrrolidine derivatives such as 3,4-epoxypyrrolodines, 3-pyrrolidols and the like, by oxidizing 3-pyrrolines with at least one peroxide in the presence of at least one acid is disclosed. The 3-pyrrolines are produced by deriving cis-2-butene compounds from cis-2-butene-1,4-diols and performing a cyclization between the cis-2-butene derivatives and at least one primary amine. The method may be performed as a one-pot synthesis and may be performed as a continuous reaction.
专利号:US-2025188083-A1 优先权日:2021-06-25 标 题:Modulators of Histone Acetyltransferase 1 and Methods of Treatment Thereof 发明人:GRUBER JOSHUA JAMES; LIPCHIK ANDREW; SNYDER MICHAEL P; SCHOW STEVEN R 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Small molecules compounds and methods of their synthesis are provided. Small molecules identified can inhibit histone acetyltransferase 1 activity. Formulations and medicaments are also provided that are directed to the treatment of human disorders and conditions, such as, for example, neoplasms, cancers, viral, fungal, and parasitic infections, and aging. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
专利号:US-9771356-B2 优先权日:2012-09-21 标题 :Inhibitors of beta-hydroxylase for treatment of cancer 发明人:WANDS JACK R; DE LA MONTE SUZANNE; AIHARA ARIHIRO; OLSEN MARK JON; THOMAS JOHN-MICHAEL 权利人:RHODE ISLAND HOSPITAL; UNIV MIDWESTERN 摘要:The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydroxylase (e.g., Asparatyl (asparaginyl) β-hydroxylase (ASPH)), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
专利号:US-7491727-B2 优先权日:2003-01-31 标题:Arylpiperazinyl compounds 发明人:DHANOA DALE S; CHEN DONGLI; BECKER OREN; NOIMAN SILVIA; CHERUKU SRINIVASA R; MARANTZ YAEL; SHARADENDU ANURAG; SHACHAM SHARON; HEIFETZ ALEXANDER; MOHANTY PRADYUMNA; INBAL BOAZ; FICHMAN MERAV; NUDELMAN RAPHAEL; BAR-HAIM SHAY 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:ES-2501640-T3 优先权日:2009-06-30 标题:Benzenesulfonamide compounds, their method of synthesis and their use in medicine