专利号:US-2023357286-A1 优先权日:2020-07-24 标 题:Ketone synthesis and applications 发明人:KISHI YOSHITO; UMEHARA ATSUSHI 权利人:HARVARD COLLEGE 摘要:Provided are new nickel./zirconium-mediated coupling reactions useful in the synthesis of ketone-containing compounds, e.g., halichondrin natural products and related molecules. A feature of the present disclosure is the use of a nickel(I) catalyst in tandem with a nickel (II) catalyst in the Ni/Zr-mediated coupling reactions. Without wishing to be bound by any particular theory, the nickel (I) catalyst selectively activates the electrophilic coupling partner (i.e., the compound of Formula (A)), and the nickel(ll) catalyst selectively activates the nucleophilic coupling partner (i.e., a thioester of Formula (B)). This dual catalyst system leads to improved coupling efficiency and eliminates the need for a large excess of one of the coupling partners (i.e., a compound of Formula (A) or (B)).
专利号:US-8637434-B2 优先权日:1996-04-17 标题 :System for photolithographic synthesis of polymer arrays 发明人:GOLDBERG MARTIN J; DIGGELMAN MARTIN; HUBBELL EARL A; MCGALL GLENN H; NAM NGO; MORRIS MACDONALD S; YAMAMOTO MELVIN; TAN JENNIFER; RAVA RICHARD 权利人:AFFYMETRIX INC 摘要:The present invention provides novel processes for the large scale preparation of arrays of polymer sequences wherein each array includes a plurality of different, positionally distinct polymer sequences having known monomer sequences. The methods of the invention combine high throughput process steps with high resolution photolithographic techniques in the manufacture of polymer arrays.
专利号:US-2006183886-A1 优先权日:1995-11-22 标题:Ligands to enhance cellular uptake of biomolecules 发明人:TSO PAUL O; DUFF ROBERT; ZHOU YUANZHONG; DEAMOND SCOTT; ROBY CLINTON 权利人:CELL WORKS THERAPEUTICS INC A 摘要:The present invention relates to the design and synthesis of homogeneous A-L-P constructs, which contain a hepatic ligand to direct an oligomer or “payloadâ€? to a hepatocyte intracellularly via a receptor-mediated, ligand-directed pathway.
专利号:US-6989401-B2 优先权日:2000-07-19 标题:Sulfonic acid derivatives of hydroxamic acids and their use as medicinal products 发明人:MAEDA KAZUHIRO; SONDA SHUJI; TAKEMOTO TADAHIRO; GOTO TOMOKAZU; KOBAYASHI FUJIO; KAJII MASAHIKO; KOMORITA NARUYASU; HIRAYAMA FUMIHIRO 权利人:MITSUBISHI PHARMA CORP 摘要:The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.
专利号:WO-2011047481-A1 优先权日:2009-10-23 标题 :Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY 权利人:MERCK FROSST CANADA LTD; FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY 摘要:Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl- coenzyme. A delta-9 desaturase (SCDl) relative to other known stearoyl-coenzyme. A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).
专利号:US-2023135188-A1 优先权日:2017-07-06 标题:Fe/cu-mediated ketone synthesis 发明人:KISHI YOSHITO; YAHATA KENZO; KUMAR VEMULA PRAVEEN; VADDELA SUDHEER BABU 权利人:HARVARD COLLEGE 摘要:Provided herein are methods for preparing ketone-containing organic molecules. The methods are based on novel iron/copper-mediated (“Fe/Cu-mediatedâ€?) coupling reactions. The Fe/Cu-mediated coupling reaction can be used in the preparation of complex molecules, such as halichondrins and analogs thereof. In particular, the Fe/Cu-mediated ketolization reactions described herein are useful in the preparation of intermediates en route to halichondrins.