专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-9409945-B2 优先权日:1999-10-04 标 题 :Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery 发明人:DESLONGCHAMPS PIERRE; DORY YVES; BERTHIAUME GILLES; OUELLET LUC; LAN RUOXI 权利人:OCERA THERAPEUTICS INC 摘要:A library of macrocyclic compounds of the formula (I) n n n n n n n n n n n n where part (A) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; n where part (B) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; n where part (C) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) t — bivalent radical, or a covalent bond; and n where part (T) is a —Y-L-Z— radical wherein Y is CH 2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-8283502-B2 优先权日:2009-04-09 标题:Autocatalytic process for the synthesis of chiral propargylic alcohols 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:An autocatalytic process for the synthesis of chiral propargylic alcohols.
专利号:US-5969173-A 优先权日:1998-12-01 标 题:Method of making dialkali metal silanolates and siloxanolates 发明人:CLARKE STEPHEN ROSS; GRAIVER DANIEL; MATISONS JANIS GUNARS; OWEN MICHAEL JAMES 权利人:DOW CORNING 摘要:Dialkali metal organosilanolate and dialkali metal organosiloxanolate salts are manufactured from cyclic siloxanes or linear silicone polymers using a heterogeneous interfacial reaction process. A stoichiometric excess of an alkali metal hydroxide such as potassium hydroxide or an alkali metal oxide as a solid or dissolved or dispersed in a compatible solvent, is prepared and used as a first phase. The cyclic siloxane or linear silicone polymer is placed in a second phase either dissolved or dispersed in another solvent which is immiscible with the first phase. The resulting silanolate and siloxanolate salts can be used as monomers for solid-liquid phase and liquid-liquid phase interfacial polymerization or in a polycondensation process for the synthesis of alternating siloxane polymers. They can also be used as ring opening initiators for the base catalyzed polymerization of cyclic siloxanes.
专利号:US-10975096-B2 优先权日:2014-06-20 标题 :Synthesis of polycyclic-carbamoylpyridone compounds 发明人:CHIU ANNA; ENQUIST JR JOHN; GRIGGS NOLAN; HALE CHRISTOPHER; IKEMOTO NORIHIRO; KEATON KATIE ANN; KRAFT MATT; LAZERWITH SCOTT E; LEEMAN MICHEL; PENG ZHIHUI; SCHRIER KATE; TRINIDAD JONATHAN; VAN HERPT JOCHEM; WALTMAN ANDREW W 权利人:GILEAD SCIENCES INC 摘要:Methods of making compounds of Formula I are disclosed: