📜盐酸西布曲明,水 以 四氢呋喃 用作溶剂,以to Give N,N-Dimethyl-1-[1-(4-Chlorophenyl)-Cyclobutyl]-3-Methylbutylamine Hydrochloride Monohydrate (M.P. 193°-195oc.)的收率获得盐酸西布曲明水合物 参考文献:Process For The Manufacture Of 标题:Process For The Manufacture Of 摘要:一种制备n,N-二甲基-1-[1-(4-氯苯基)环丁基]-3-甲基丁胺盐酸盐一水合物的方法,该物质不吸湿,可用于治疗抑郁症的制药.
专利号:US-8378072-B2 优先权日:2006-04-13 标题 :Methods for designing and synthesizing directed sequence polymer compositions via the directed expansion of epitope permeability 发明人:BONNIN DUSTAN 权利人:DECLION PHARMACEUTICALS INC; BONNIN DUSTAN 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the modulation of unwanted immune responses, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use.
专利号:US-2011040105-A1 优先权日:2008-04-16 标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine 发明人:HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL 权利人:ARENA PHARM INC 摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
专利号:US-6894189-B2 优先权日:2001-04-13 标 题 :Methods of preparing didesmethylsibutramine and other sibutramine derivatives 发明人:SENANAYAKE CHRIS HUGH; HAN ZHENGXU; KRISHNAMURTHY DHILEEPKUMAR; PFLUM DEREK 权利人:SEPRACOR INC 摘要:This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.
专利号:WO-2004058727-A1 优先权日:2002-12-20 标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity 发明人:CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. 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-7354923-B2 优先权日:2001-08-10 标 题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:WO-2005102340-A1 优先权日:2003-05-30 标题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
参考文献:10.1177/2168479017742858 摘要:Patriarca PA, Van Auken RM, Kebschull SA. Analysis of the Risks and Benefits of New Chemical Entities Approved by the US Food and Drug Administration (FDA) and Subsequently Withdrawn From the US Market. Therapeutic Innovation & Regulatory Science. 2018 Sep;52(5):649–55. doi: 10.1177/2168479017742858. 参考文献:10.2116/analsci.21p148 摘要:Yuan Y, Chen N, Wang L, Zhang X, Chen H, Ma P. Rapid detection of illegally added nifedipine in Chinese traditional patent medicine by surface-enhanced Raman spectroscopy. Anal Sci. 2022 Feb;38(2):359–68. doi: 10.2116/analsci.21p148. 参考文献:10.1007/bf01271196 摘要:Fleischmann A, Sternheim A, Etgen AM, Li C, Grisaru N, Belmaker RH. Transcranial magnetic stimulation downregulates beta-adrenoreceptors in rat cortex. J Neural Transm (Vienna). 1996;103(11):1361–6. doi: 10.1007/bf01271196.