专利号:US-2023174477-A1 优先权日:2021-12-03 标题:Methods for synthesis of the tricyclic prostaglandin d2 metabolite methyl ester 发明人:DAI MINGJI; SIMS HUNTER 权利人:PURDUE RESEARCH FOUNDATION 摘要:Methods for the synthesis of a tricyclic-prostaglandin D 2 metabolite methyl ester or a pharmaceutically acceptable salt thereof.
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:US-9328061-B2 优先权日:2012-03-01 标题:Simple organic molecules as catalysts for practical and efficient enantioselective synthesis of amines and alcohols 发明人:HOVEYDA AMIR H; SILVERIO DANIEL L; PILYUGINA TATIANA; TORKER SEBASTIAN; ROBBINS DANIEL 权利人:TRUSTEES BOSTON COLLEGE 摘要:The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
专利号:US-9243004-B2 优先权日:2011-07-22 标题 :Synthesis of boronic esters and boronic acids using grignard reagents 发明人:CLARY JACOB W; SINGARAM BAKTHAN 权利人:CLARY JACOB W; SINGARAM BAKTHAN; UNIV CALIFORNIA 摘要:Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg 0 . When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
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-7977371-B2 优先权日:2007-02-26 标题 :Pyrrole derivative having ureido group and aminocarbonyl group as substituents 发明人:KAWASHIMA KENJI; ENOMOTO HIROSHI; ISHIZAKA NORIKO; YAMAMOTO MINORU; KUDOU KAZUHIRO; MURAI MASAAKI; INABA TAKAAKI; OKAMOTO KAZUYOSHI 权利人:SANTEN PHARMACEUTICAL CO LTD 摘要:Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R 1 represents a halogen atom, a hydrogen atom, a lower alkyl group or the like; R 2 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like.
摘要:Diver, S. T., Science of Synthesis, (2009) 46, 135. 摘要:Gandon, V.; Thorimbert, S.; Malacria, M., Science of Synthesis, (2009) 46, 190. 摘要:Michalak, M.; Gulajski, L.; Grela, K., Science of Synthesis, (2010) 47, 340. 摘要:Bubnov, Yu. N.; Kolomnikova, G. D., Science of Synthesis Knowledge Updates, (2012) 3, 296. 摘要:Bubnov, Yu. N.; Kolomnikova, G. D., Science of Synthesis Knowledge Updates, (2012) 3, 303.