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-7648986-B2 优先权日:2002-01-10 标题:Substituted thieno[3,2-D]pyrimidines as Rho kinase inhibitors 发明人:NAGARATHNAM DHANAPALAN; KHIRE UDAY; ASGARI DAVOUD; SHAO JIANXING; LIU XIAO-GAO; WANG CHUNGUANG; HART BARRY; WEBER OLAF; LYNCH MARK; ZHANG LEI; WANG LEI 权利人:BAYER HEALTHCARE LLC 摘要:Disclosed are compounds and derivatives thereof their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
参考文献:10.1038/ncomms15761 摘要:Collier TL, Normandin MD, Stephenson NA, Livni E, Liang SH, Wooten DW, Esfahani SA, Stabin MG, Mahmood U, Chen J, Wang W, Maresca K, Waterhouse RN, El Fakhri G, Richardson P, Vasdev N. Synthesis and preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib. Nature Communications. 2017 Jun 08;8(1):15761. doi: 10.1038/ncomms15761.