专利号:US-2024390383-A1 优先权日:2021-09-28 标题 :Dioxazines and their use in treatment of gba-related diseases 发明人:NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH 权利人:ZEVRA DENMARK AS 摘要:The present invention relates to dioxazines, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.
专利号:US-8772301-B2 优先权日:2009-12-18 标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof 发明人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D 权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-9708336-B2 优先权日:2014-01-22 标题 :Metallo-beta-lactamase inhibitors 发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-9861636-B2 优先权日:2014-04-29 标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors 发明人:HE WEI 权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD 摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
专利号:WO-2015088564-A1 优先权日:2013-12-13 标 题:P2x4 receptor modulating compounds 发明人:NEWCOM JASON S; SPEAR KERRY L 权利人:SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are P2X4 receptor modulating compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including but not limited to, chronic pain, neuropathy, inflammatory diseases and central nervous system disorders.