专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-8273403-B2 优先权日:2002-05-10 标题 :Generation of surface coating diversity 发明人:BARDEN MICHAEL C; KAMBOURIS PETER A 权利人:BARDEN MICHAEL C; KAMBOURIS PETER A; BIO LAYER PTY LTD 摘要:This invention relates to a surface discovery system and high-throughput combinatorial synthesis methods for generating large numbers of diverse surface coatings on solid substrates. The system is built upon a synthon which comprises at least three elements: a chemical backbone coating on the solid substrate that comprises a copolymer (B) of at least one passive constituent (P) and at least one active constituent (A); a spacer unit (S) separating the backbone from a functional group; and a functional group (F). The methods comprise the following steps: 1) selecting a plurality of synthons so that each synthon has at least two points of diversity selected from P, A, S and F; 2) applying copolymer B onto a substrate; and 3) attaching a combination of S and F to constituent A of copolymer B. Steps 2) and 3) are performed such that different synthons are generated on localized regions of the substrate.
专利号:US-5064953-A 优先权日:1983-12-29 标 题:Intermediates cephalosporin derivatives 发明人:OHNISHI HARUO; KOSUZUME HIROSHI; MIZOTA MASAHIRO; SUZUKI YASUO; MOCHIDA EI 权利人:MOCHIDA PHARM CO LTD 摘要:The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof. The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton. The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
专利号:US-4778805-A 优先权日:1987-06-18 标题:4,7-benzofurandione derivatives useful as inhibitors of leukotriene synthesis 发明人:ADAMS JULIAN; GUINDON YVAN; BELANGER PATRICE C; BELLEY MICHEL L; ROKACH JOSHUA 权利人:MERCK FROSST CANADA 摘要:4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention. ##STR1##
专利号:US-2015038591-A1 优先权日:2002-05-31 标 题:Compounds, compositions and methods for the treatment of tauopathies 发明人:SNOW ALAN D; CAM JUDY A; CASTILLO GERARDO; HU QUBAI; LAKE THOMAS 权利人:PROTEOTECH INC 摘要:Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of tauopathies, such as Alzheimer's disease and Parkinson's disease, and the manufacture of medicaments for such treatment.