环吡司胺置于盐酸体系中,用 水,乙酸乙酯 用作溶剂,以84%的收率获得环吡酮 参考文献: Methods Of Bladder Cancer Treatment With Ciclopirox,Ciclopirox Olamine,Or A Ciclopirox Prodrug[fr] Procédés De Traitement Du Cancer De La Vessie Avec Le Ciclopirox,Le Ciclopirox Olamine Ou Un Promédicament à Base De Ciclopirox 标题: Methods Of Bladder Cancer Treatment With Ciclopirox,Ciclopirox Olamine,Or A Ciclopirox Prodrug[fr] Procédés De Traitement Du Cancer De La Vessie Avec Le Ciclopirox,Le Ciclopirox Olamine Ou Un Promédicament à Base De Ciclopirox 摘要:提供了一种治疗膀胱癌的方法.治疗膀胱癌的方法可以包括:提供含有环丙沙星或环丙沙星醇胺或具有本文提供的任一式的结构或其衍生物或立体异构体或其药用可接受盐的环丙沙星-Pom前药的药物组合物;并将该药物组合物给予患有膀胱癌的受试者.环丙沙星或环丙沙星醇胺或环丙沙星-Pom前药可以以治疗有效量进行给予.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-10933051-B2 优先权日:2017-06-09 标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections 发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN 权利人:FOB SYNTHESIS INC 摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
专利号:US-8106031-B2 优先权日:2006-05-02 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: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; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-9382288-B2 优先权日:2010-10-06 标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action 发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO 权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG 摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
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合成参考文献
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