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-2024351965-A1 优先权日:2021-08-23 标 题 :Synthesis and Evaluation of Novel (4-Hydroxyphenyl) Substituted Carbocycles as Potent and Selective Estrogen Receptor Beta Agonists 发明人:DONALDSON WILLIAM A; SEM DANIEL S; WETZEL EDWARD A 权利人:UNIV MARQUETTE; CONCORDIA UNIV INC 摘要:Disclosed are 4-hydroxylphenyl substituted carbocycles and there use as selective agonists of the estrogen receptor beta isoform (ERβ). The disclosed compounds may be formulated as pharmaceutical compositions and administered to treat diseases associated with ER activity, such as proliferative diseases and disorders and/or psychiatric diseases or disorders.
专利号:US-9056876-B2 优先权日:2011-09-16 标 题:Substituted 1H-pyrazolo[3′,4′,4,5]thieno[2,3-b]pyridin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 发明人:CONN JEFFREY P; LINDSLEY CRAIG W; WOOD MICHAEL R; HOPKINS COREY R; SALOVICH JAMES M; MELANCON BRUCE J 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted 1H-pyrazolo[3′,4′:4,5]thieno[2,3-b]pyridin-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-9351974-B2 优先权日:2011-11-10 标题 :Substituted pteridinones for the treatment of cancer 发明人:JIN MEIZHONG; KADALBAJOO MRIDULA; LI AN-HU; MULVIHILL MARK J; SIU KAM W; STEINIG ARNO G; WANG JING 权利人:OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula I, as shown below and defined herein: n npharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
专利号:WO-2023028074-A1 优先权日:2021-08-23 标 题 :Synthesis and evaluation of novel (4-hydroxyphenyl) substituted carbocycles as potent and selective estrogen receptor beta agonists
专利号:EP-4392487-A1 优先权日:2021-08-23 标题:Synthesis and evaluation of novel (4-hydroxyphenyl) substituted carbocycles as potent and selective estrogen receptor beta agonists
摘要:Jie, X.; Su, W., Science of Synthesis, (2022) , 14. 参考文献:10.1038/ncomms14190 摘要:Meng Q, Hou M, Liu H, Song J, Han B. Synthesis of ketones from biomass-derived feedstock. Nature Communications. 2017 Jan 31;8(1):14190. doi: 10.1038/ncomms14190.