专利号:WO-2021038581-A1 优先权日:2019-08-30 标题 :A one step synthesis of 2-substituted benzo[b]thiophenes 发明人:SEKAR GOVINDASAMY; POONGUZHALI ELAMVAZHUTHI 权利人:INDIAN INST TECH MADRAS 摘要:The invention pertains to a one step synthesis of 2-substituted benzo[ b ]thiophene of general formula wherein the synthesis of 2-substituted benzo[ b ]thiophenes is by reacting the starting materials substituted or unsubstituted 2-halogenobenzaldehyde and substituted or unsubstituted acetyl/phenacyl bromide with a catalyst, a sulphur source and phase transfer catalyst in an aqueous medium with atmospheric air and at temperature in the range of 25°C-30°C.
专利号:US-5399721-A 优先权日:1990-01-12 标题:Synthesis of optically pure 4-aryl-2-hydroxytetronic acids 发明人:HOPPER ALLEN T; WITIAK DONALD T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. the invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.
专利号:US-2004267028-A1 优先权日:2001-09-24 标题 :Preparation and use of pyrrole derivatives for treating obesity 发明人:SMITH ROGER A; KLUENDER HAROLD C; SU NING; LAVOIE RICO C; FAN JIANMEI 权利人:SMITH ROGER A; KLUENDER HAROLD C; SU NING; LAVOIE RICO C; FAN JIANMEI 摘要:This invention relates to pyrrole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:US-7816375-B2 优先权日:2000-09-11 标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-7807837-B2 优先权日:2004-05-07 标 题 :Scalable synthesis of imidazole derivatives 发明人:JONES TODD K; MANI NEELAKANDHA 权利人:JANSSEN PHARMACEUTICA NV 摘要:Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them.
专利号:US-7217823-B2 优先权日:2000-12-06 标题:4,4-Disubstituted piperidines, and methods of use thereof 发明人:HOEMANN MICHAEL Z 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
[参考文献]: Shigeo Hayashi, Et Al. Design, Synthesis And Structure-Activity Relationship Studies Of Novel And Diverse Cyclooxygenase-2 Inhibitors As Anti-Inflammatory Drugs. J Enzyme Inhib Med Chem. 2014 Dec;29(6):846-67.
合成参考文献
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