专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
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-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:EP-0024372-A1 优先权日:1979-08-03 标题:Derivatives of clavulanic acid, their preparation and pharmaceutical compositions containing them 发明人:DENERLEY PAUL MILLINGTON; EGLINGTON ALFRED JOHN; HARBRIDGE JOHN BARRY 权利人:BEECHAM GROUP PLC 摘要:The compounds of the formula (II):n and salts and esters thereof wherein the hydroxyl group occupies position 2 or 4 R 1 and R 2 may be the same or different and represent hydrogen, halogen, hydroxy, lower alkyl, cyclopentyl, cyclohexyl, lower alkoxy or R, and R 2 when an adjacent carbon atoms may together represent a 1,4-buta-1,3-dienylene group or a polymethylene group containing from 3 to 5 carbon atoms; have been found to be β-lactam antibiotics and synergists with penicillins and cephalosporins. Their preparation and use is described. The synthesis of intermediates useful in their preparation is also described.
专利号:WO-9925385-A1 优先权日:1997-11-17 标 题:A method of increasing nucleic acid synthesis with ultrasound 发明人:UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID 权利人:IMARX PHARMACEUTICAL CORP 摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.
专利号:US-2005010262-A1 优先权日:2002-02-01 标题 :Modulation of the pain circuitry to affect chronic pain 发明人:REZAI ALI; SHARAN ASHWINI 摘要:The present invention relates to methods of affecting chronic pain by electrically and/or chemically stimulating target sites of the pain circuitry associated with chronic pain. Such target sites include cerebral target sites, including limbic structures, associated with the emotional and suffering components of chronic pain, as well as deep brain target sites associated with the affective and sensory components of chronic pain. Also provided is a method of affecting chronic pain by stimulating a target site of the pain circuitry associated with chronic pain to stimulate the synthesis or release of endogenous opioids.
1: Scheld WM, Sydnor A Jr, Farr B, Gratz JC, Gwaltney JM Jr. Comparison of cyclacillin and amoxicillin for therapy for acute maxillary sinusitis. Antimicrob Agents Chemother. 1986 Sep;30(3):350-3. 2: Hooton TM, Running K, Stamm WE. Single-dose therapy for cystitis in women. A comparison of trimethoprim-sulfamethoxazole, amoxicillin, and cyclacillin. JAMA. 1985 Jan 18;253(3):387-90. 6: McLinn SE, Serlin S. Cyclacillin versus amoxicillin as treatment for acute otitis media. Pediatrics. 1983 Feb;71(2):196-9.
合成参考文献
摘要:Chemotherapy, 22(154), 1976 [] 摘要:Tested as SID 103770339 in AID 781325: 参考文献:10.1007/s192-002-8352-0 摘要:Ribeiro RM, Rossi P, Pacetta AM, Haddad JM, Pinotti JA. Therapy of uncomplicated urinary tract infections. Int Urogynecol J Pelvic Floor Dysfunct. 2002;13(3):190–4. doi: 10.1007/s192-002-8352-0.