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.
专利号:US-8771639-B2 优先权日:2007-01-05 标 题 :Methods for preparing composites of substrate-molecular sieve 发明人:YOON KYUNG BYUNG; LEE JIN SEOK; KIM JAE HYUN; LEE YOUNG JU; JEONG NAK CHEON 权利人:YOON KYUNG BYUNG; LEE JIN SEOK; KIM JAE HYUN; LEE YOUNG JU; JEONG NAK CHEON; UNIV SOGANG IND UNIV COOP FOUN 摘要:The present invention relates to a method for preparing composites of substrate-molecular sieve, in particular, to a method for preparing a composite of substrate-molecular sieve, which comprises applying a physical pressure to molecular sieve crystals against a substrate to form a chemical bond between the molecular sieve crystal and the substrate. The present invention requiring no solvents, reactors and other equipments enables molecular sieve crystals to be stably attached to the surface of substrates through various chemical bonds, particularly ionic present invention ensures the synthesis of substrate-molecular sieve composites with enhanced attachment rate, degree of lateral close packing (DCP) and attachment strength in more time-saving and energy-saving manners. The present method works well for molecular sieve crystals with lager sizes (e.g., more than 3 μm) with no generation of parasitic crystals. Furthermore, the present invention shows excellent applicability to large substrates, enabling the mass production of substrate-molecular sieve composites.
专利号:US-11225655-B2 优先权日:2010-04-16 标题:Bi-functional complexes and methods for making and using such complexes 发明人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK 权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS 摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.
专利号:US-2003082830-A1 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
专利号:US-9994558-B2 优先权日:2013-09-20 标题 :Multicyclic compounds and methods of using same 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.