专利号:US-9951088-B2 优先权日:2012-05-09 标题 :D2 receptor modulators and methods of use thereof in the treatment of diseases and disorders 发明人:JONES PHILIP G; LEW ROBERT; SPEAR KERRY L; XIE LINGHONG 权利人:SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
专利号:WO-2011050245-A1 优先权日:2009-10-23 标 题:Bicyclic heteroaryls as kinase inhibitors 发明人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS 权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS 摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.
专利号:US-8633204-B2 优先权日:2006-09-15 标 题 :4-methylpyridopyrimidinone compounds 发明人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN 权利人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN; PFIZER 摘要:The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), n nand to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).
专利号:US-9533996-B2 优先权日:2012-06-18 标 题 :Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6h)-ones 发明人:BRANSTETTER BRYAN; BREITENBUCHER JAMES; DYCK BRIAN; GOMEZ LAURENT; HUDSON ANDREW RICHARD; MARRONE TAMI JO; PETERS MARCO; VICKERS TROY; WEINHOUSE MICHAEL 权利人:DART NEUROSCIENCE (CAYMAN) LTD 摘要:Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
专利号:WO-2010001220-A1 优先权日:2008-07-01 标 题 :New 1,2,4-triazine derivatives and biological applications thereof 发明人:DESROY NICOLAS; DENIS ALEXIS; GERUSZ VINCENT; OLIVEIRA CHRYSTELLE; VONGSOUTHI VANIDA; MOREAU FRANCOISE; ESCAICH SONIA 权利人:MUTABILIS SA; DESROY NICOLAS; DENIS ALEXIS; GERUSZ VINCENT; OLIVEIRA CHRYSTELLE; VONGSOUTHI VANIDA; MOREAU FRANCOISE; ESCAICH SONIA 摘要:The invention relates to new 1,2,4-triazine derivatives of formula (I): wherein A, B, R2 and Y are defined in the application, their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.
专利号:CN-117603193-A 优先权日:2023-12-20 标题:A kind of synthesis method of β-cyanopyrazole compounds
参考文献:10.1007/s00044-023-03092-0 摘要:Gupta M, Canziani G, Ang C, Mohammadi M, Abrams CF, Yang D, Smith AB, Chaiken I. Pharmacophore variants of the macrocyclic peptide triazole inactivator of HIV-1 Env. Med Chem Res. 2023 Jun 27;32(7):1497–509. doi: 10.1007/s00044-023-03092-0. 参考文献:10.1007/s00044-024-03245-9 摘要:Zhang Y, Dai L, Tan Y, Yu Y, Xing J, Yang F, Ren B, Xu Y, Li Q. Design and synthesis of novel factor XIa Inhibitors with bicyclic isoquinoline and naphthalene fragments. Med Chem Res. 2024 May 30;33(6):1003–23. doi: 10.1007/s00044-024-03245-9.