专利号:US-8716507-B2 优先权日:2008-10-31 标题 :Iron(II) catalysts containing diimino-diphosphine tetradentate ligands and their synthesis 发明人:MIKHAILINE ALEXANDRE; FREUTEL FRIEDERIKE; SUI-SENG CHRISTINE; MEYER NILS; MORRIS ROBERT H; LAGADITIS PARASKEVI OLYMPIA 权利人:MIKHAILINE ALEXANDRE; FREUTEL FRIEDERIKE; SUI-SENG CHRISTINE; MEYER NILS; MORRIS ROBERT H; LAGADITIS PARASKEVI OLYMPIA; GOVERNING COUNCIL OF UNIVERSITY OF TORONTO 摘要:New hexa-coordinate iron (II) complexes comprising compounds of formula (I) are described. These compounds comprise a tetradentate ligand with donor atoms comprising nitrogen and phosphorus. These complexes are shown for the first time to be useful catalysts for the hydrogenation of ketones, aldehydes, or imines to produce alcohols or amines, and the asymmetric hydrogenation of prochiral ketones or imines to produce non-racemic alcohols or amines. The source of the hydrogen can be hydrogen gas or a hydrogen-donating molecule such as isopropanol or hydrogen-donating mixture such as formic acid and an amine depending on the structure of the catalyst. In certain embodiments, the axial ligands on the catalyst comprise organonitrile ligands, carbonyl ligands, isonitrile ligands, or combinations thereof. The catalysts and the preparation thereof are disclosed. A reaction using phosphine and diamine precursors that is templated by the iron ion is the preferred route to the catalysts.
专利号:WO-2017077550-A1 优先权日:2015-11-02 标题 :A metal free process for the preparation of alpha-substituted carbonyl compounds from alkenes 发明人:SUDALAI ARUMUGAM; PRASAD PRAGATI KISHORE; REDDI RAMBABU 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses a novel metal free process for the regioselective synthesis of α-substituted carbonyl compounds of formula I from alkene, X is selected from the following compounds (A, B).
专利号:US-2018148745-A1 优先权日:2015-05-26 标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor 发明人:ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN 权利人:CALIFORNIA INST OF TECHN; PROVIVI INC 摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.
专利号:WO-2004074215-A1 优先权日:2003-02-03 标 题 :Process for preparation of clopidogrel, its salts and pharmaceutical compositions 发明人:NADKARNI SUNIL SADANAND; PATEL HASMUKH MATHURBHAI 权利人:NADKARNI SUNIL SADANAND; PATEL HASMUKH MATHURBHAI 摘要:The invention discloses an improved process for racemization of methyl (R)Â(-) alpha-(2-chlorophenyl)-6,7-dihydro-thieno[3,2-c]pyridine-5(4H)-acetate , a stereoisomer formed in the synthesis of clopidogrel i.e. methyl (S)-(+)-alpha (2-chlorophenyl)-6,7-dihydro-thieno[3,2-c]pyridine-5(4H)-acetate or its salts. The invention is also for an improved process for production of clopidogrel or its pharmaceutically acceptable salts. The invention further discloses novel clopidogrel salts and pharmaceutical compositions comprising them.
专利号:US-10888571-B2 优先权日:2015-12-18 标 题:Method and composition for increasing muscle protein synthesis and/or functional strength in mammals 发明人:BELLAMINE AOUATEF; ZHIVKOVICH ILYA; FREITAS ULLA 权利人:LONZA CONSUMER HEALTH INC 摘要:A method and composition for preserving muscle mass and function by increasing muscle protein synthesis and/or decreasing muscle protein degradation in mammals is disclosed. In one embodiment, the mammals are administered a protein building composition comprising at least two of an essential amino acid, an amino acid derivative, and a nitrogenous organic acid. In a particular embodiment, the protein building composition comprises leucine, L-carnitine, and creatine. The protein building composition can decrease TNF-α and increase mTOR expression in muscle.
专利号:CN-111699248-A 优先权日:2018-01-31 标题:Biocatalysts and methods for the synthesis of mixed disulfide conjugates of thienopyridine compounds
1. Clopidogrel Pharmacogenetics. Pereira NL, Rihal CS, So DYF, Rosenberg Y, Lennon RJ, Mathew V, Goodman SG, Weinshilboum RM, Wang L, Baudhuin LM, Lerman A, Hasan A, Iturriaga E, Fu YP, Geller N, Bailey K, Farkouh ME. 2. The Role of Clopidogrel in 2020: A Reappraisal. Patti G, Micieli G, Cimminiello C, Bolognese L. Cardiovasc Ther. 2020 Mar 16;2020:8703627. doi: 10.1155/2020/8703627. eCollection 2020. 3. Interactions between clopidogrel and traditional Chinese medicine. Hu Y, Wang J. J Thromb Thrombolysis. 2019 Oct;48(3):491-499. doi: 10.1007/s11239-019-01945-3. 382(18):1696-1707. doi: 10.1056/NEJMoa1915152. Epub 2020 Mar 29. 5. Clopidogrel versus ticagrelor or prasugrel in patients aged 70 years or older with non-ST-elevation acute coronary syndrome (POPular AGE): the randomised, open-label, non-inferiority trial. Gimbel M, Qaderdan K, Willemsen L, Hermanides R, Bergmeijer T, de Vrey E, Heestermans T, Tjon Joe Gin M, Waalewijn R, Hofma S, den Hartog F, Jukema W, von Birgelen C, Voskuil M, Kelder J, Deneer V, Ten Berg J. 6. Aspirin with or without Clopidogrel after Transcatheter Aortic-Valve Implantation. Brouwer J, Nijenhuis VJ, Delewi R, Hermanides RS, Holvoet W, Dubois CLF, Frambach P, De Bruyne B, van Houwelingen GK, Van Der Heyden JAS, Toušek P, van der Kley F, Buysschaert I, Schotborgh CE, Ferdinande B, van der Harst P, Roosen J, Peper J, Thielen FWF, Veenstra L, Chan Pin Yin DRPP, Swaans MJ, Rensing BJWM, van 't Hof AWJ, Timmers L, Kelder JC, Stella PR, Baan J, Ten Berg JM. N Engl J Med. 2020 Oct 8;383(15):1447-1457. doi: 10.1056/NEJMoa2017815. Epub 7. Compared efficacy of clopidogrel and ticagrelor in treating acute coronary syndrome: a meta-analysis. Wang D, Yang XH, Zhang JD, Li RB, Jia M, Cui XR. BMC Cardiovasc Disord. 2018 Nov 29;18(1):217. doi: 10.1186/s12872-018-0948-4. STOPDAPT-2 Investigators. JAMA. 2019 Jun 25;321(24):2414-2427. doi: 10.1001/jama.2019.8145. 9. Clopidogrel Pharmacogenetics - Why the Wait? Roden DM. N Engl J Med. 2019 Oct 24;381(17):1677-1678. doi: 10.1056/NEJMe1911496. 10. Benefits and Risks of Clopidogrel vs. Aspirin Monotherapy after Recent Ischemic Stroke: A Systematic Review and Meta-Analysis. Paciaroni M, Ince B, Hu B, Jeng JS, Kutluk K, Liu L, Lou M, Parfenov V, Wong KSL, Zamani B, Paek D, Min Han J, Del Aguila M, Girotra S.
合成参考文献
参考文献:10.1186/1476-7120-2-5 摘要:Knebel F, Gliech V, Walde T, Panda A, Sanad W, Eddicks S, Baumann G, Borges AC. Percutaneous closure of interatrial communications in adults - prospective embolism prevention study with two- and three-dimensional echocardiography. Cardiovasc Ultrasound. 2004 May 19;2():5. 参考文献:10.1007/s12272-001-1149-7 摘要:Ki MH, Choi MH, Ahn KB, Kim BS, Im DS, Ahn SK, Shin HJ. The efficacy and safety of clopidogrel resinate as a novel polymeric salt form of clopidogrel. Arch Pharm Res. 2008 Feb;31(2):250–8. doi: 10.1007/s12272-001-1149-7. 参考文献:10.1245/s10434-011-1723-2 摘要:Hammond J, Kozma C, Hart JC, Nigam S, Daskiran M, Paris A, Mackowiak JI. Rates of Venous Thromboembolism Among Patients with Major Surgery for Cancer. Annals of Surgical Oncology. 2011 May 17;18(12):3240–7. doi: 10.1245/s10434-011-1723-2.