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公开(公告)号：EP3551638A2
公开(公告)日：2019-10-16
申请号：EP17818009.7
申请日：2017-12-06
发明人： DESROSIERS, Jean-Nicolas , FANDRICK, Daniel Robert , HADDAD, Nizar , LI, Guisheng , PATEL, Nitinchandra D. , QU, Bo , RODRIGUEZ, Sonia , SENANAYAKE, Chris Hugh , SIEBER, Joshua Daniel , TAN, Zhulin , WANG, Xiao-Jun , YEE, Nathan K. , ZHANG, Li , ZHANG, Yongda
IPC分类号： C07F9/6568 , C07B53/00 , C07F15/00
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2.发明公开PROCESS FOR ASYMETRIC METHYLALLYLATION IN THE PRESENCE OF A 2, 2 ' - SUBSTITUTED 1, 1 ' -BI - 2 -NAPHTHOL CATALYST 审中-公开用于非对称METHYLALLYLIERUNG PROCEDURE在存在2,2-取代的1,1'-联-2-萘酚CATALYST
公开(公告)号：EP2683678A1
公开(公告)日：2014-01-15
申请号：EP12709230.2
申请日：2012-03-06
CPC分类号： C07C39/14 , C07B2200/07 , C07C29/143 , C07C29/38 , C07C37/055 , C07C37/62 , C07C39/38 , C07C41/48 , C07C43/313 , C07C33/483
摘要： Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X
1 , X
2 , R
3 and R
4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-β- hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors including 1, 3-disubstituted oxazinan-2-ones.-
公开(公告)号：EP4308580A1
公开(公告)日：2024-01-24
申请号：EP22715594.2
申请日：2022-03-16
发明人： ZHANG, Yongda , WU, Linglin
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公开(公告)号：EP2655349B1
公开(公告)日：2014-10-15
申请号：EP11810721.8
申请日：2011-12-15
发明人： FANDRICK, Daniel Robert , LU, Zhi-Hui , REEVES, Diane Crimhilda , REEVES, Jonathan Timothy , SENANAYAKE, Chris Hugh , SONG, Jinhua J. , ZHANG, Yongda
IPC分类号： C07D265/10 , C07C271/16
CPC分类号： C07D413/10 , C07C271/48 , C07D213/64 , C07D265/10
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公开(公告)号：EP2655349A1
公开(公告)日：2013-10-30
申请号：EP11810721.8
申请日：2011-12-15
发明人： FANDRICK, Daniel Robert , LU, Zhi-Hui , REEVES, Diane Crimhilda , REEVES, Jonathan Timothy , SENANAYAKE, Chris Hugh , SONG, Jinhua J. , ZHANG, Yongda
IPC分类号： C07D265/10 , C07C271/16
CPC分类号： C07D413/10 , C07C271/48 , C07D213/64 , C07D265/10
摘要： Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R
1 to R
4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11- β-hydroxysteroid hydrogenase type 1 (11- β-HSD1) inhibitors.-
公开(公告)号：EP3551639A1
公开(公告)日：2019-10-16
申请号：EP17817612.9
申请日：2017-12-05
发明人： BISWAS, Soumik , DESROSIERS, Jean-Nicolas , LAO, Kendricks , MANGUNURU, Hari P.R. , QU, Bo , RODRIGUEZ, Sonia , SENANAYAKE, Chris Hugh , SIEBER, Joshua Daniel , WANG, Xiao-Jun , YEE, Nathan K. , ZHANG, Yongda
IPC分类号： C07F9/6581 , C07B53/00 , C07F15/00
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7.发明公开
公开(公告)号：EP2323994A1
公开(公告)日：2011-05-25
申请号：EP09780984.2
申请日：2009-07-23
发明人： FANDRICK, Keith R. , GAO, Ju , LI, Wenjie , LU, Bruce , ZHANG, Yongda
IPC分类号： C07D265/10 , C07D413/06
CPC分类号： C07D265/10 , C07D413/06 , C07D413/10
摘要： Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
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公开(公告)号：EP1853589A1
公开(公告)日：2007-11-14
申请号：EP06734761.7
申请日：2006-02-10
IPC分类号： C07D403/04 , C07D409/04 , C07D401/04 , C07D209/08 , C07D209/12 , C07D209/10
CPC分类号： C07D209/10 , C07D209/08 , C07D209/12 , C07D401/04 , C07D403/04 , C07D409/04
摘要： Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.
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