专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:WO-2017004172-A1 优先权日:2015-06-29 标题:Total synthesis of shishijimicin a and analogs thereof
专利号:US-10233182-B2 优先权日:2014-04-04 标题 :Substituted spirocyclic inhibitors of autotaxin 发明人:BABISS LEE; CLARK MATTHEW; KEEFE ANTHONY D; MULVIHILL MARK J; NI HAIHONG; RENZETTI LOUIS; RUEBSAM FRANK; WANG CE; XIE ZHIFENG; ZHANG YING 权利人:X RX INC 摘要:The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
专利号:CN-113828342-A 优先权日:2021-09-30 标 题:Cu-Pd-CeO2/γ-Al2O3Preparation of @ NP catalyst and synthesis of benzopyrazine compounds
专利号:CN-113828342-B 优先权日:2021-09-30 标题 :Preparation of Cu-Pd-CeO2/γ-Al2O3@NP catalyst and synthesis of benzopyrazine compounds
专利号:WO-2022202643-A1 优先权日:2021-03-23 标 题:Method for producing s,s-(6-methylquinoxaline-2,3-diyl)dithiocarbonate 发明人:SHIGENOBU MASASHI; FUJIMOTO RYOSUKE; OKITA CHIAKI 权利人:OSAKA SODA CO LTD 摘要:The purpose of the present invention is to provide a method for producing high-purity S,S-(6-methylquinoxaline-2,3-diyl)dithiocarbonate by efficiently removing starting materials used for the synthesis and specific impurities produced during the synthesis from S,S-(6-methylquinoxaline-2,3-diyl)dithiocarbonate. The present invention provides a method for producing S,S-(6-methylquinoxaline-2,3-diyl)dithiocarbonate, the method comprising: a step (reaction step) in which 2,3-dimercapto-6-methylquinoxaline is converted into an alkali metal salt or an alkaline earth metal salt, and is subsequently reacted with a phenyl chloroformate in the presence of a phase-transfer catalyst; and a purification step which is characterized by purifying S,S-(6-methylquinoxaline-2,3-diyl)dithiocarbonate with use of an acetic acid ester, the S,S-(6-methylquinoxaline-2,3-diyl)dithiocarbonate having been obtained by the reaction.