专利号:US-2007203079-A1 优先权日:2005-11-21 标题:Methods of using small molecule compounds for neuroprotection 发明人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG 权利人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG 摘要:Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.
专利号:US-2025002508-A1 优先权日:2020-05-05 标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof 发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS 权利人:QPEX BIOPHARMA INC 摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
专利号:US-4439363-A 优先权日:1979-06-20 标题:Acetylmethyl ester of hetacyllin and/or salts of this ester 发明人:GRUSZECKI WOJCIECH A; BUSKO-OSZCZOPOWICZ IRENA M; GDULEWICZ-GRUSZECKA MARIA; CIESLAK JERZY J; BOROWSKI EDWARD; GUMIEZNA TERESA 权利人:POLITECHNIKA GDANSKA; INST PRZEMYSLU FARMACEUTYOZNEG 摘要:The acetylmethyl ester of hetacyllin and/or its salts of an organic or inorganic acid are described and methods for their synthesis wherein a tertiary amine and chloroacetone are introduced to hetacyllin in an organic solvent or chloroacetone is introduced to hetacyllin in the form of a salt with an alkali metal in an organic solvent, and then from the reaction mixture, the acetylmethyl ester of hetacyllin is isolated in free form and, if desired, a salt of the ester is obtained by reaction with an organic or inorganic acid in an organic solvent. n As tertiary amines, trialkylamine, N-methylpiperidine, N-ethylpiperidine or N-methylmorpholine are used; as organic solvents in obtaining the ester, dimethylformamide, dimethylacetamide or dimethylsulfoxide are used. In obtaining salts of the ester the organic solvents used are aliphatic alcohols of a chain length C 2 -C 5 ; ketones, preferably acetone; ethers, such as diethyl, dipropyl, diisopropyl, dibutyl ethers, or their mixtures. n The obtained compounds show an antibacterial action like ampicillin but after administration per os they show a considerably higher level of the antibiotic than that after administration of free ampicillin or its esters.
专利号:US-4452796-A 优先权日:1982-06-14 标题:6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors 发明人:BARTH WAYNE E 权利人:PFIZER 摘要:Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, used in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.
专利号:US-8933207-B2 优先权日:2010-07-28 标 题 :Drug-ligand conjugates, synthesis thereof, and intermediates thereto 发明人:CHEN ZHIYU; LANCASTER THOMAS M; ZION TODD C 权利人:CHEN ZHIYU; LANCASTER THOMAS M; ZION TODD C; SMARTCELLS INC 摘要:The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: I wherein each of X, Alk 1 , Alk 2 , and W are as defined and described herein.
专利号:US-4503040-A 优先权日:1984-02-27 标题:6-(Aminoacyloxymethyl)penicillanic acid 1,1-dioxides as beta-lactamase inhibitors 发明人:BARTH WAYNE E 权利人:PFIZER 摘要:Beta-lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.
1: Winther L, Baptiste KE, Friis C. Pharmacokinetics in pulmonary epithelial lining fluid and plasma of ampicillin and pivampicillin administered to horses. Res Vet Sci. 2012 Feb;92(1):111-5. doi: 10.1016/j.rvsc.2010.11.001. Epub 2010 Dec 7. 5: Ensink JM, Moi A, Vulto AG, Tukker JJ. Bioavailability of pivampicillin and ampicillin trihydrate administered as an oral paste in horses. Vet Q. 1996;18 Suppl 2:S117-20.
合成参考文献
参考文献:10.1007/bf01677396 摘要:Kvile G, Langeland P, Norling B. Treatment of salpingitis with pivampicillin. A comparison of twice-daily and thrice-daily dosages. Infection. 1980;8(1):32–6. doi: 10.1007/bf01677396. 参考文献:10.2147/clep.s17747 摘要:Bjørn AM, Nørgaard M, Hundborg HH, Nohr EA, Ehrenstein V. Use of prescribed drugs among primiparous women: an 11-year population-based study in Denmark. Clin Epidemiol. 2011;3():149–56. 参考文献:10.1136/pgmj.68.805.932 摘要:Rose SJ, Stokes TC, Patel S, Cooper MB, Betteridge DJ, Payne JE. Carnitine deficiency associated with long-term pivampicillin treatment: the effect of a replacement therapy regime. Postgrad Med J. 1992 Nov;68(805):932–4. 参考文献:10.3109/00365519209088371 摘要:Holme E, Jodal U, Linstedt S, Nordin I. Effects of pivalic acid-containing prodrugs on carnitine homeostasis and on response to fasting in children. Scandinavian Journal of Clinical and Laboratory Investigation. 1992 Jan;52(5):361–72. doi: 10.3109/00365519209088371. 参考文献:10.1093/jac/16.6.808 摘要:Piot P, van Dyck E. In-vitro susceptibility of beta-lactamase-producing Haemophilus influenzae to the combinations ampicillin with mecillinam and ampicillin and VD2085. J Antimicrob Chemother. 1985 Dec;16(6):808–9. doi: 10.1093/jac/16.6.808.