专利号:US-2008146656-A1 优先权日:2005-06-01 标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone 发明人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.
专利号:US-2024368075-A1 优先权日:2021-07-02 标题 :Synthesis of N,N-Dialkyl, -Dialkenyl, -Dialkynyl, and Related Cyclics, Sulfamoyl Fluoride Compounds Using Hydrogen Fluoride 发明人:SINGH RAJENDRA P; HU QICHAO 权利人:SES HOLDINGS PTE LTD 摘要:Methods of producing N,N-dimethyl sulfamoyl fluoride and related derivatives of the formula F—S(O)2—NR2 (I) by contacting a sulfamoyl nonfluorohalide compound of the formula X—S(O)2—NR2 (II) with anhydrous hydrogen fluoride under conditions sufficient to produce the N,N-dimethyl sulfamoyl fluoride or derivative thereof of Formula I, wherein R in each of Formulas I and II is, independently, a linear or branched alkyl, alkenyl, or alkynyl group containing 1 to 12 carbon atoms, the Rs can be joined to form a cyclic amine with the N, and X is any one of chlorine, bromine, and iodine.
专利号:US-2023322661-A1 优先权日:2020-08-21 标题 :Synthesis of N,N-Branched Sulfamoyl Fluoride Compounds Using Bismuth Trifluoride 发明人:SINGH RAJENDRA P; HU QICHAO; SHEIMAN JOHNATHAN 权利人:SES HOLDINGS PTE LTD 摘要:Methods of producing N,N-branched sulfamoyl fluoride compounds of the formula F-S(O) 2 -NR 2 by contacting bismuth trifluoride with an N,N-branched sulfamoyl nonfluorohalide compound of the formula X-SO 2 NR 2 , wherein X=chlorine (Cl), bromine (Br), or iodine (I), and each R is, independently, a linear or branched alkyl, fluoroalkyl, alkenyl, fluoroalkenyl, alkynyl, or fluoroalkynyl with 1 to 12 carbon atoms, to fluorinate the N,N-branched sulfamoyl nonfluorohalide compound. This is a non-aqueous method, the purity of product is very high, and the desired product can be isolated in quantitative yield. The N,N-branched sulfamoyl fluoride compounds so produced are useful in various applications including as electrolyte solvents and additives in electrochemical devices, such as lithium batteries and capacitors, and in biological fields, among others.
专利号:US-9873688-B2 优先权日:2013-11-08 标 题:Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor 发明人:TAO MING; FRIETZE WILLIAM; MELONI DAVID J; WENG LINGKAI; ZHOU JIACHENG; PAN YONGCHUN 权利人:INCYTE CORP; INCYTE HOLDINGS CORP 摘要:The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
专利号:US-2009247618-A1 优先权日:2008-03-26 标题 :Process for preparation of benzo-fused heteroaryl derivatives 发明人:BALLENTINE SCOTT A; REANY LAURA 权利人:BALLENTINE SCOTT A; REANY LAURA 摘要:The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
摘要:Gilchrist, T. L., Science of Synthesis, (2005) 18, 1031. 摘要:Chen, J.; Chiu, C. K.-F., Science of Synthesis, (2007) 31, 690. 摘要:Shcherbakova, I., Science of Synthesis, (2007) 31, 810.