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-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
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-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-2006078560-A1 优先权日:2003-06-23 标 题 :Method of inducing apoptosis and inhibiting cardiolipin synthesis 发明人:JAMIL HARIS; AHMAD MOGHIS U; AHMAD IMRAN 权利人:NEOPHARM INC 摘要:The present invention provides a method for inducing apoptosis within a cell by exposing the cell to an inhibitor of cardiolipin synthesis under conditions sufficient to induce apoptosis within the cell. The method can be used to investigate or treat disorders such as cancer, obesity, and cardiovascular disorders. The invention also provides a pharmaceutical composition including an inhibitor of cardiolipin synthesis and a liposomal carrier.
专利号:US-2008286351-A1 优先权日:2004-06-29 标 题:Pegylated Cardiolipin Analogs, Methods of Synthesis, and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.
1: Kim E, Kang W. Simultaneous determination of N(1)-acetyl sulfisoxazole and its metabolites, and relative bioavailability compare to sulfisoxazole in rats. J Pharm Biomed Anal. 2016 Sep 10;129:117-120. doi: 10.1016/j.jpba.2016.06.055. Epub 2016 Jul 1. doi: 10.1016/j.jpba.2016.07.029. Epub 2016 Jul 18. 7: Oie S, Gambertoglio JG, Fleckenstein L. Comparison of the disposition of total and unbound sulfisoxazole after single and multiple dosing. J Pharmacokinet Biopharm. 1982 Apr;10(2):157-72. French. Review. French.