专利号:US-10918627-B2 优先权日:2016-05-11 标 题:Convergent and enantioselective total synthesis of Communesin analogs 发明人:MOVASSAGHI MOHAMMAD; LATHROP STEPHEN PAUL; POMPEO MATTHEW W; CHANG WEN-TAU TIMOTHY 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): n nor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 -R 8 and m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.
专利号:WO-2024104433-A9 优先权日:2022-11-16 标 题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament 发明人:ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING 权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING 摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-9394264-B2 优先权日:2009-11-13 标 题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA 权利人:RECEPTOS INC 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-9359327-B2 优先权日:2008-06-30 标题:Process for the preparation of substituted pyrimidine derivatives 发明人:CESCO-CANCIAN SERGIO; CHEN HONGFENG; GRIMM JEFFREY S; MANI NEELAKANDHA S; MAPES CHRISTOPHER M; PALMER DAVID C; PIPPEL DANIEL J; SORGI KIRK L; XIAO TONG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H 4 receptor modulators, and to intermediates in H4 modulator synthesis.
专利号:US-10640508-B2 优先权日:2017-10-13 标 题 :Diazene directed modular synthesis of compounds with quaternary carbon centers 发明人:MOVASSAGHI MOHAMMAD; LINDOVSKA PETRA 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II): n nwherein R 1 -R 5 and q are as defined independently for each occurrence herein. A wide variety of compounds can be accessed in this manner, including oligocyclotryptamines, where the stereochemistry of each subunit is beneficially secured before fragment coupling.
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