Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于氯仿,氨体系中,化学反应生成 卡巴胆碱 参考文献:Process For Preparing Therapeutically Active Substances 标题:Process For Preparing Therapeutically Active Substances
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
专利号:US-8049024-B2 优先权日:2006-09-16 标 题 :Heterogenized rhodium complexes, methods of their synthesis and application as hydrosilylation catalysts 发明人:MARCINIEC BOGDAN; FIEDOROW RYSZARD; SZUBERT KAROL; KOWNACKI IRENEUSZ; FRANCZYK ADRIAN; DUTKIEWICZ MICHAL; LESZCZAK KINGA 权利人:UNIV ADAM MICKIEWICZ 摘要:The subjects of the invention are new heterogenized rhodium complexes, the methods of their synthesis and their application as catalysts for synthesis of organosilicon compounds by hydrosilylation. The subject of the invention are new siloxide rhodium(I) complexes immobilised on the silica surface, of the general formula 1. [(≡SiO)(L)Rh(diene)] The second subject of the invention is the method of synthesis of the new rhodium complexes of the general formula 1. The third subject of the invention is the method of obtaining the organosilicon compounds in the reaction of hydrosilylation between the selected alkenes or functionalised alkenes containing the terminal Câ• C bond and the appropriate compounds containing the Siâ• H bond selected from silanes, (poly)siloxanes and (poly)carbosiloxanes, in the presence of heterogenized rhodium catalysts, of the general formula 1.
专利号:US-8278296-B2 优先权日:2006-08-10 标题:Manipulation of brain CDP-diacylglycerol and uses thereof 发明人:UNDIEH ASHIWEL S 权利人:UNDIEH ASHIWEL S 摘要:Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.
专利号:US-4331688-A 优先权日:1978-02-23 标题 :Therapeutic method for inhibiting gastric secretion by administration of 15-deoxy-16-hydroxy prostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:US-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
专利号:US-4132738-A 优先权日:1978-02-23 标 题:Preparation of 15-deoxy-16-hydroxyprostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## SUCH THAT A BICYCLOALKYL OR BICYCLOALKENYL COMPOUND IS FORMED, WHEREIN M AND N ARE INTEGERS HAVING A VALUE FROM 0 TO 3, P IS AN INTEGER HAVING A VALUE FROM 0 TO 4 AND Q IS AN INTEGER HAVING A VALUE OF FROM 1 TO 4 AND WHEREIN THE DOUBLE BOND OF SUCH BICYCLOALKENYL IS IN THE M, N, P, OR Q BRIDGE; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n Pge 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
1: Fornai M, Pellegrini C, Antonioli L, Segnani C, Ippolito C, Barocelli E, Ballabeni V, Vegezzi G, Al Harraq Z, Blandini F, Levandis G, Cerri S, Blandizzi C, Bernardini N, Colucci R. Enteric dysfunctions in experimental Parkinson's disease: alterations of excitatory cholinergic neurotransmission regulating colonic motility in rats. J Pharmacol Exp Ther. 2015 Nov 18. pii: jpet.115.228510. [Epub ahead of print] Denatonium and 6-n-propyl-2-thiouracil, agonists of bitter taste receptor, inhibit contraction of various types of smooth muscles in the rat and mouse. Biol Pharm Bull. 2015 Nov 14. [Epub ahead of print]
合成参考文献
参考文献:10.1113/expphysiol.2009.051102 摘要:Flores CA, Cid LP, Sepúlveda FV. Strain-dependent differences in electrogenic secretion of electrolytes across mouse colon epithelium. Exp Physiol. 2010 Jun;95(6):686–98. doi: 10.1113/expphysiol.2009.051102. 参考文献:10.1007/s10875-010-9370-0 摘要:Negroni MP, Fiszman GL, Azar ME, Morgado CC, Español AJ, Pelegrina LT, de la Torre E, Sales ME. Immunoglobulin G from Breast Cancer Patients in Stage I Stimulates Muscarinic Acetylcholine Receptors in MCF7 Cells and Induces Proliferation. Participation of Nitric Oxide Synthase-Derived Nitric Oxide. Journal of Clinical Immunology. 2010 Feb 16;30(3):474–84. doi: 10.1007/s10875-010-9370-0. 参考文献:10.1152/ajpendo.00773.2009 摘要:Niu W, Bilan PJ, Ishikura S, Schertzer JD, Contreras-Ferrat A, Fu Z, Liu J, Boguslavsky S, Foley KP, Liu Z, Li J, Chu G, Panakkezhum T, Lopaschuk GD, Lavandero S, Yao Z, Klip A. Contraction-related stimuli regulate GLUT4 traffic in C2C12-GLUT4mycskeletal muscle cells. American Journal of Physiology-Endocrinology and Metabolism. 2010 May;298(5):E1058–71. doi: 10.1152/ajpendo.00773.2009. 参考文献:10.1055/s-2005-871291 摘要:Gomes AY, de Fátima Souza M, Cortes SF, Lemos VS. Mechanism involved in the spasmolytic effect of a mixture of two triterpenes, cycloartenol and cycloeucalenol, isolated from Herissanthia tiubae in the guinea-pig ileum. Planta Med. 2005 Nov;71(11):1025–9. doi: 10.1055/s-2005-871291. 参考文献:10.1007/s10620-011-1821-9 摘要:Ren A, Zhang W, Thomas HG, Barish A, Berry S, Kiel JS, Naren AP. A Tannic Acid-Based Medical Food, Cesinex®, Exhibits Broad-Spectrum Antidiarrheal Properties: A Mechanistic and Clinical Study. Digestive Diseases and Sciences. 2011 Jul 12;57(1):99–108. doi: 10.1007/s10620-011-1821-9.