专利号:US-2005186197-A1 优先权日:2002-08-29 标 题:Peptide inhibitors of beta lactamases 发明人:PALZKILL TIMOTHY; HUANG WANZHI 摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.
专利号:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
专利号:US-5202454-A 优先权日:1986-07-11 标 题 :Process for the manufacture of 1-bromoalkyl hydrocarbyl carbonates 发明人:WOODEN GARY; SENNYEY GERARD; SENET JEAN-PIERRE 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to a new process for the preparation of 1-bromoalkyl hydrocarbyl carbonates. The carbonates according to the invention are prepared by reacting an alpha-chlorinated carbonate of formula with an anhydrous brominated compound of formula ZBr in which Z represents hydrogen, the group (CH3)3-Si-, the group or bromine if R2 is other than an aromatic radical, in the presence of a catalyst chosen from the group consisting of heteroaromatic amines, quaternary ammonium or phosphonium halides, hexasubstituted guanidinium halides, alkaline earth metal halides or alkali metal halides in combination with a complexing agent for their cation. The carbonates according to the invention find their preferential applications as blocking agents for some antibiotics or as agents for the synthesis of phosphorus-containing carbonates which can be used as insecticides.
专利号:WO-2012149093-A1 优先权日:2011-04-26 标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof 发明人:LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
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-10385068-B2 优先权日:2016-03-08 标 题:Synthesis process of precursors of derivatives of beta-lactam nuclei and precursors and derivatives thereof 发明人:BONOMI PAOLO 权利人:BONOMI PAOLO 摘要:A synthesis process of precursors of derivatives of beta-lactam compounds, said beta-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, comprising the following steps: a) protection of the amine group of the beta-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, through the formation of a carbamate by reaction with a dicarbonate; b) esterification of the carboxyl group in position 2 of the beta-lactam compound obtained in step a) by reaction with propargyl alcohol.
参考文献:10.11150/kansenshogakuzasshi1970.59.708 摘要:Kobayashi H, Takamura K, Kono K, Nihei T, Saito A, Nakayama I, Ujiie A, Yajima O, Tango M, Tomizawa M. [Comparative study on sultamicillin and bacampicillin in the treatment of respiratory tract infections]. Kansenshogaku Zasshi. 1985 Jul;59(7):708–48. doi: 10.11150/kansenshogakuzasshi1970.59.708. 摘要:Sefton AM, Jepson AP, Sun ZM, Williams JD. A comparative pharmacokinetic study between lenampicillin, bacampicillin and amoxycillin. J Chemother. 1989 Jul;1(4 Suppl):494–5. 摘要:Ottaviani A, Sambataro G, Cantarella G, Scaramellini G. Comparison of two bacampicillin therapeutic regimens in infections of middle ear, pharynx and paranasal sinuses. J Chemother. 1989 Jul;1(4 Suppl):750–1.