专利号:US-6172205-B1 优先权日:1997-12-11 标题 :Synthetic process toward total synthesis of eleutherobin and its analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; CHEN XIAO-TAO; GUTTERIDGE CLARE E; BHATTACHARYA SAMIT K; ZHOU BISHAN 权利人:TRUSTEES OF COLUMBIA IN THE CI 摘要:This invention provides a process for the preparation of a Eleutherobin derivative of the formula: n wherein R 1 is a hydrogen, ester, nitrile or C 2 H 4 —R wherein R 4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R 2 is a linear or branched alkyl moiety, R 3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R 4 is a hydrogen or CH 2 ,position C 2 and C 3 is cis or trans,position C 8 is α or β and a compound is produced having the structures: n Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.
专利号:US-6194568-B1 优先权日:1998-07-13 标题:Process for synthesizing carbapenem intermediates 发明人:JENSEN MARK S; XIAO YI; YANG CHUNHUA; WELLS KENNETH M; YASUDA NOBUYOSHI 权利人:MERCK & CO INC 摘要:The invention describes an improved process for synthesizing 1-beta-methyl-2-hydroxymethyl substituted carbapenems as key intermediates for the synthesis of anti-MRSA carbapenem antibiotics. The synthesis eliminates the use of BU3SnCH2OH and HMPA, which are toxic substances and not amenable to industrial scale production. The novel intermediates are also within the scope of this invention.The invention relates to the synthesis of a compound of formula 3:wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents H or methyl; and R5 represents a carboxy protecting group as well as the compounds made therein.
专利号:EP-1015452-B1 优先权日:1997-08-26 标题:Optionally protected 3-hydroxymethyl carbapenems and synthesis 发明人:CHUNG JOHN Y; LEAZER JOHNNIE L JR; YASUDA NOBUYOSHI; JENSEN MARK S; WELLS KENNETH M; YANG CHUNHUA 权利人:MERCK & CO INC 摘要:Novel crystalline carbapenem intermediate compounds of formula (I) wherein R1 represents CH3 or H; and P and P' independently represent H or a protecting group; and efficient process for synthesis thereof.
专利号:CN-114957258-A 优先权日:2021-02-25 标题 :Synthesis of a broad-spectrum serine β-lactamase inhibitor based on carbapenem structure and its application in the inhibition of drug-resistant bacteria
专利号:US-6346617-B1 优先权日:1997-08-26 标 题 :Crystalline 2-hydroxymethyl carbapenem intermediate compounds and process for synthesis thereof 发明人:CHUNG JOHN Y; YASUDA NOBUYOSHI; LEAZER JR JOHNNIE L; JENSEN MARK S; WELLS KENNETH M; YANG CHUNHUA 权利人:MERCK & CO INC 摘要:A process for preparation of a compound of formula I:wherein:R1 represents CH3 or H; and P represents a protecting group;comprising reacting a compound of formula IV: wherein R1 and P and are defined above and R4 represents triflate or SO2F;in the presence of a catalyst and (R3)3SnCH2OP'', wherein each R3 represents C1-4 lower alkyl, and P'' represents H or a protecting group, to yield the compound of formula I.
专利号:EP-1935869-A1 优先权日:2000-10-02 标题:Retinoids for the treatment of emphysema 发明人:LAPIERRE JEAN MARC; ROTSTEIN MARC; SJOGREN ERIC BRIAN 权利人:HOFFMANN LA ROCHE 摘要:The current invention provides novel retinoid compounds and methods for their synthesis, the use of such compounds for the preparation of medicaments for treating or preventing emphysema, cancer and dermatological disorders, methods for such deseases and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.