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:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
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-4072677-A 优先权日:1975-12-13 标题 :Penicillin synthesis 发明人:CALLANDER SIDNEY EDWARD 权利人:BEECHAM GROUP LTD 摘要:Process of preparing phthalidyl ampicillin or other orally absorbable penicillin ester by esterification of the parent penicillin in a two-phase system using a phase transfer catalyst which increases the solubility of a salt form of the penicillin in the water-immiscible solvent used in the process. The phase transfer catalysts are quaternary ammonium salts or tertiary amines of non-low molecular weight, or crown ethers.
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.
1: Smellie JM, Grüneberg RN, Bantock HM, Katz G. Talampicillin in the treatment and prophylaxis of urinary tract infection in children. Chemotherapy. 1982;28(3):218-23.
合成参考文献
摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956