专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-8106031-B2 优先权日:2006-05-02 标题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:WO-2007141253-A1 优先权日:2006-06-07 标 题 :Process for the production of intermediates for the preparation of tricyclic imidazopyridines 发明人:PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 摘要:The invention relates to a process for the synthesis of compounds of the formula (1-a) and compounds of the formula (1-b). The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Arom have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-2007275962-A1 优先权日:2003-09-10 标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents 发明人:KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES 权利人:GPC BIOTECH AG 摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
专利号:US-10000487-B2 优先权日:2015-11-20 标 题 :Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers 发明人:SPRENGELER PAUL A; REICH SEIGFRIED H; WEBBER STEPHEN E; ERNST JUSTIN T 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. n nFor Formula IA and Formula IB compounds A 1 , A 2 , A 3 , A 4 , W 1 , W 2 , Y, X, R 1 , R 2 , R 3 , R 4a , R 4b , R 5a , R 5b , R 6 , R 7 , R 8 , R 9 , R 9a , R 9b , R 10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:US-8338451-B2 优先权日:2008-03-21 标 题 :Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof 发明人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO 权利人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO; SANOFI SA 摘要:Compounds of formula (I): n nwherein R, R 1 , R 2 , R 3 , R 4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 77. 摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 97. 摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 78. 摘要:Stewart, S. G., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 511. 摘要:Makida, Y.; Kuwano, R., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 276.