专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-10472663-B2 优先权日:2015-01-21 标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis 发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A 权利人:ABM TECH LLC 摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.
专利号:US-9968710-B2 优先权日:2007-07-23 标 题:Pharmaceutical composition, substrate comprising a pharmaceutical composition, and use of a pharmaceutical composition 发明人:DUEWELHENKE NICOLE 权利人:BIOMET DEUTSCHLAND GMBH 摘要:Use of a pharmaceutical composition for the local treatment or prevention of a tissue infection at an infection site, the pharmaceutical composition comprising at least two different antibiotics of group A or pharmaceutically acceptable derivatives thereof, or an antibiotic of group A and at least one antibiotic of group B or pharmaceutically acceptable derivatives thereof. Group A comprises primarily intracellular active antibiotics working as inhibitor of bacterial RNA polymerase; as inhibitor of gyrase; or as inhibitor of bacterial protein synthesis. Group B comprises primarily extracellular active antibiotics working as inhibitor of bacterial cell wall synthesis; or inhibitor of bacterial protein synthesis; or by direct destabilization or rupture of the bacterial cell wall.
专利号:WO-2009094569-A2 优先权日:2008-01-25 标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
专利号:US-2005222431-A1 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
1: Hwang JH, Lee JH, Kim JS, Hwang JH, Lee CS. Arbekacin as an Alternative Drug to Teicoplanin for the Treatment of MRSA Infection. Yonsei Med J. 2016 Jul;57(4):1047-8. doi: 10.3349/ymj.2016.57.4.1047. 2: Lee JH, Lee CS. Clinical Usefulness of Arbekacin. Infect Chemother. 2016 Mar;48(1):1-11. doi: 10.3947/ic.2016.48.1.1. Epub 2016 Mar 31. Review. 3: Miura K, Nakagawa M, Takahashi H, Uchino Y, Kodaira H, Iriyama N, Sakagami M, Ohtake S, Kobayashi S, Hojo A, Kurita D, Kobayashi Y, Kusuda M, Hirabayashi Y, Hatta Y, Takei M. Clinical efficacy and safety of arbekacin for high-risk infections in patients with hematological malignancies. Int J Hematol. 2016 Mar;103(3):334-40. doi: 10.1007/s12185-015-1926-6. Epub 2015 Dec 29. doi: 10.3346/jkms.2015.30.6.688. Epub 2015 May 13.
合成参考文献
摘要:Kumamoto Y, Tsukamoto T, Ogihara M, Ishibashi K, Hirose T, Matsukawa M, Takahashi S, Kunishima Y, Shigeta S, Yoshida H, Imafuku Y, Ooe H, Nishikawa M, Murai M, Watanabe K, Kobayashi Y, Oka T, Kitamura M, Uchida H, Takano Y, Matsuoka Y, Matsuda S, Sato S, Furuhama T, Fujime M, Fujita K, Kumon H, Monden K, Igari J, Oguri T, Kohno S, Miyazaki Y, Yamaguchi T, Matsumoto K, Izumikawa K, Yamaguchi T, Kashitani F, Mochida C. [Comparative studies on activities of antimicrobial agents against causative organisms isolated from patients with urinary tract infections (1999). III. Secular changes in susceptibility]. Jpn J Antibiot. 2001 Jun;54(6):231–322. 参考文献:10.1097/00001432-200406000-00011 摘要:Weisman LE. Coagulase-negative staphylococcal disease: emerging therapies for the neonatal and pediatric patient. Current Opinion in Infectious Diseases. 2004 Jun;17(3):237–41. doi: 10.1097/00001432-200406000-00011. 参考文献:10.2147/tcrm.2006.2.2.169 摘要:Shoemaker DM, Simou J, Roland WE. A review of daptomycin for injection (Cubicin) in the treatment of complicated skin and skin structure infections. Therapeutics and Clinical Risk Management. 2006 Apr;2(2):169–74. doi: 10.2147/tcrm.2006.2.2.169.