专利号:US-7344863-B2 优先权日:1998-03-13 标题:Methods for producing polypeptides through enhanced synthesis of encoding nucleic acid molecules 发明人:LI WU-BO; JESSEE JOEL A; SCHUSTER DAVID; XIA JIULIN; GEBEYEHU GULILAT 权利人:INVITROGEN CORP 摘要:The present invention is directed to compositions and methods for enhancing synthesis of nucleic acid molecules, particularly GC-rich nucleic acid molecules. Specifically, the invention provides compositions comprising one or more nitrogen-containing organic compounds having a formula selected from the group consisting of formula I and formula II (or salts or derivatives thereof), preferably 4-methylmorpholine N-oxide or betaine (carboxymethyltrimethylammonium), and further comprising one or more compounds selected from the group consisting of proline and an N-alkylimidazole compound, and more preferably proline, 1-methylimidazole or 4-methylimidazole. The invention further relates to methods for enhanced, high-fidelity synthesis of nucleic acid molecules, including via amplification (particularly PCR), reverse transcription, and sequencing methods. The invention also relates to nucleic acid molecules synthesized by these methods, to fragments or derivatives thereof, and to vectors and host cells comprising such nucleic acid molecules, fragments, or derivatives. The invention also relates to kits for synthesizing, amplifying, reverse transcribing or sequencing nucleic acid molecules comprising one or more of the compositions of the invention.
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:WO-2014095657-A1 优先权日:2012-12-20 标题:Synthesis of a viral protease inhibitor intermediate 发明人:RIVA SERGIO; ALLEGRINI PIETRO; ATTOLINO EMANUELE; GRAZIOSI RENZO 权利人:DIPHARMA FRANCIS SRL 摘要:Synthesis of an intermediate useful in the synthesis of a viral protease inhibitor, and its use in the preparation of said inhibitor.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-9862745-B2 优先权日:2004-03-30 标题 :Synthesis of boronic ester and acid compounds 发明人:AMMOSCATO VINCE; BISHOP JOHN E; CHIU FANG-TING; GEISER ACHIM; GOMEZ JEAN-MARC; HETT ROBERT; KOELLNER CHRISTOPH; KULKARNI VITHALANAND R; LO YOUNG; MUNK STEPHEN; PICKERSGILL I FRASER 权利人:MILLENNIUM PHARM INC; MILLENNIUM PHARM INC 摘要:The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
参考文献:10.1107/s1600536811016473 摘要:Najafi E, Amini MM, Ng SW. Triethylammonium tetrachlorido(pyrazine-2-carboxylato-κ2N1,O)stannate(IV). Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m711. doi: 10.1107/s1600536811016473. 参考文献:10.1016/j.bmcl.2011.06.055 摘要:Sayahi H, Zimhony O, Jacobs WR, Shekhtman A, Welch JT. Pyrazinamide, but not pyrazinoic acid, is a competitive inhibitor of NADPH binding to Mycobacterium tuberculosis fatty acid synthase I. Bioorganic & Medicinal Chemistry Letters. 2011 Aug;21(16):4804–7. doi: 10.1016/j.bmcl.2011.06.055.