专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
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-2009143426-A1 优先权日:2007-12-04 标 题:Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments 发明人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 权利人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 摘要:The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR 2 ′″ where R′″ is alkyl or cycloalkyl, and R″ is H or alkyl. The composition of the invented compounds as methods of antagonizing the action of endothelin-1 to treat cardiovascular, pulmonary diseases and obstetric disorders and preterm labor and preeclampsia in mammals is disclosed.
专利号:US-2005176941-A1 优先权日:2002-02-13 标 题:Nucleoside analogues whose sugar moieties are bound in s-form and oligonucleotide derivatives comprising nucleotide analogues thereof 发明人:IMANISHI TAKESHI; OBIKA SATOSHI 摘要:Compounds of the following general formula (1) and salts thereof: n n nwhere A represents an alkylene group having 1 to 2 carbon atoms, etc.; B represents an aromatic heterocyclic group which may have a substituent, etc.; R 1 and R 2 each represent a hydrogen atom, a protective group for a hydroxyl group for synthesis of nucleic acid, a phosphate group, or —P(R 4 )R 5 [where R 4 and R 5 are the same or different, and each represent a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, a mercapto group, a mercapto group protected with a protective group for synthesis of nucleic acid, etc.]; and R 3 represents a hydrogen atom, a halogen atom, a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, etc. nThese compounds are useful for producing oligonucleotide analogues useful for the antisense method, antigene method, etc., and for producing their intermediates.
专利号:US-2023295613-A1 优先权日:2020-02-14 标 题:Long chain carbon and cyclic amino acids substrates for genetic code reprogramming 发明人:JEWETT MICHAEL C; LEE JOONGOO; MOORE JEFFREY S; SCHWARZ KEVIN J 权利人:UNIV NORTHWESTERN; UNIV ILLINOIS 摘要:Abstract: Disclosed are methods, systems, components, and compositions for synthesis of sequence defined polymers. The methods, systems, components, and compositions may be utilized for incorporating novel substrates that include non-standard amino acid monomers and non-amino acid monomers into sequence defined polymers. As disclosed herein, the novel substrates may be utilized for acylation of tRNA via flexizyme catalyzed reactions. The tRNAs thus acylated with the novel substrates may be utilized in synthesis platforms for incorporating the novel substrates into a sequence defined polymer.
专利号:US-10189822-B2 优先权日:2015-03-19 标 题:Heterocyclic modulators of lipid synthesis 发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; HEUER TIMOTHY SEAN; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
参考标题:A Facile Microwave And Sncl2 Synthesis Of 2,3-Dihydroquinazolin-4(1H)-Ones 作者:Nicholas S. O'Brien,Adam Mccluskey 摘要:An Elegantly Simple, Facile, And Robust Approach To A Scaffold Of Biological Importance, 2,3-Dihydroquinazolin-4(1H)-Ones, Is Reported. A Catalytic 1 % Sncl2/microwave-Mediated Approach Afforded Access To Pure Material, Collected By Cooling And Filtration After 20-Min Microwave Irradiation At 120°C. A Total Of 41 Analogues Were Prepared In Isolated Yields Of 17-99 %. This Process Was Highly Tolerant
合成参考文献
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