专利号:US-4876323-A 优先权日:1984-02-27 标题:α-substituted acrylic acid esters, their polymers and method of synthesizing same 发明人:ENGEL JAMES F; BYERLEY THOMAS J; CHRISTIE HOWARD W 权利人:MIDWEST RESEARCH INST 摘要:α-Substituted acrylic acid esters, their polymers and adhesives therefrom, and methods of synthesizing these compounds. The compounds of the invention are useful as intermediates in the synthesis of isocyanato esters and can be polymerized to form an effective, non-toxic adhesive. The method of the invention encompasses utilizing the adhesive composition in biomedical applications, such as joining live animal tissue. Other adhesive applications are contemplated for living tissue and inanimate objects. The compounds are also used as monomers which can be polymerized, used in conjunction with other monomers as adhesive compositions, cross-linking agents, dye acceptor additives to vinylic polymers and useful chemical intermediates. The method of the invention encompasses synthesizing the aforementioned monomers and intermediates. Methyl α-(ethoxycarbonamido)acrylate is synthesized from either DL-serine or methyl pyruvate. For use as an intermediate, silyl substitution of the compound is accomplished by reacting the ester with trimethylchlorosilane. This α-substituted silated ester is used as an intermediate in the preparation of methyl α-isocyanatoacrylate, which can be polymerized with N-vinyl-2-pyrrolidone to produce a desirable adhesive. Analagous procedures, starting with L-ethyl serine and L-benzyl serine, respectively, are followed to arrive at the corresponding ethyl and benzyl esters.
专利号:US-6593347-B2 优先权日:1998-10-30 标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
专利号:US-6552166-B1 优先权日:1999-10-19 标 题:Process for the preparation of conjugates useful in the treatment of prostate cancer 发明人:LYNCH JOSEPH E; ROBBINS MICHAEL A; SHI YAO-JUN; LIEBERMAN DAVID R 权利人:MERCK & CO INC 摘要:The present invention is directed to the improved synthesis of compounds of formula I:which may be useful in the treatment of prostate cancer. Such compounds are synthesized in the presence of a carboxyl activating agent, an additive and a base for the preparation of a PSA conjugate which comprises an anthracycline antibiotic and an oligopeptide.
专利号:US-2013253061-A1 优先权日:2012-03-20 标 题:Method of droxidopa synthesis 发明人:PIMPLASKAR HARISH K; KADAM SHASHIKANT VITHAL; MALLESH VOORADI; KAWALE PRAMOD MANGALDAS 权利人:CHELSEA THERAPEUTICS INC 摘要:The present application relates to a novel method of preparing L-threo-dihydroxyphenylserine (droxidopa). Specifically, the application is directed to a method of preparing droxidopa via a deprotection step that is an alternative to deprotection steps that have been previously disclosed. The new deprotection strategy is advantageous in that it avoids the need to use hydrogenolysis or hydrazine.
专利号:US-4704466-A 优先权日:1984-02-27 标题:α-substituted acrylic acid esters 发明人:ENGEL JAMES F; BYERLEY THOMAS J; CHRISTIE HOWARD W 权利人:MIDWEST RESEARCH INST 摘要:α-Substituted acrylic acid esters, their polymers and adhesives therefrom, and methods of synthesizing these compounds. The compounds of the invention are useful as intermediates in the synthesis of isocyanato esters and can be polymerized to form an effective, non-toxic adhesive. The method of the invention encompasses utilizing the adhesive composition in biomedical applications, such as joining live animal tissue. Other adhesive applications are contemplated for living tissue and inanimate objects. The compounds are also used as monomers which can be polymerized, used in conjunction with other monomers as adhesive compositions, cross-linking agents, dye acceptor additives to vinylic polymers and useful chemical intermediates. The method of the invention encompasses synthesizing the aformentioned monomers and intermediates. Methyl α-(ethoxycarbonamido)acrylate is synthesized from either DL-serine or methyl pyruvate. For use as an intermediate, silyl substitution of the compound is accomplished by reacting the ester with trimethylchlorosilane. This α-substituted silated ester is used as an intermediate in the preparation of methyl α-isocyanatoacrylate, which can be polymerized with N-vinyl-2-pyrrolidone to produce a desirable adhesive. Analagous procedures, starting with L-ethyl serine and L-benzyl serine, respectively, are followed to arrive at the corresponding ethyl and benzyl esters.
专利号:MX-2008012847-A 优先权日:2006-04-06 标题:TOTAL SYNTHESIS OF SALINOSPORAMIDA A AND ANALOGS OF THE SAME.
参考文献:10.1007/bf01978790 摘要:Baumanis EA, Kalnina IE, Kaminka ME, Mashkovsky MD, Gorkin VZ. Modification of the activity of mitochondrial monoamine oxidases in vitro and in vivo. Agents Actions. 1981 Dec;11(6-7):685–92. doi: 10.1007/bf01978790.