📜盐酸西布曲明置于sodium Hydroxide体系中,用 水,甲苯 用作溶剂,化学反应 0.25H,以93%的收率获得西布曲明 参考文献: Sibutramine Free Base In Crystalline Form And Its Pharmaceutical Use[fr] Base Libre De Sibutramine Sous Forme Cristalline Et Utilisation Pharmaceutique De Celle-Ci 标题: Sibutramine Free Base In Crystalline Form And Its Pharmaceutical Use[fr] Base Libre De Sibutramine Sous Forme Cristalline Et Utilisation Pharmaceutique De Celle-Ci 摘要:西布曲明,N-{1-[1-(4-氯苯基) 环丁基]-3-甲基丁基}-N,N-二甲基胺,以晶体形式存在的自由基,含有其的组合物和其用途.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-2009156465-A1 优先权日:2005-12-30 标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors 发明人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:US-2008300251-A1 优先权日:2005-09-05 标 题 :Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors 发明人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:US-2008207950-A1 优先权日:2004-12-22 标 题:Enantioselective Synthesis of a Sterically Hindered Amine 发明人:BERENS ULRICH; MALAN CHRISTOPHE; KIRNER HANS JURG 权利人:CIBA SC HOLDING AG 摘要:Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C 1 -C 4 alkyl or CF 3 ; R 1 is H or methyl or ethyl; R 2 is H or methyl or acyl; R 3 is H or methyl; R′ 4 is —CH 3 or â• CH 2 ; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R 3 are as in formula (I); A is acyl; and R 4 is —CH 3 or â• CH 2 ; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R 1 as methyl or ethyl and/or R 2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.
专利号:US-2013243770-A1 优先权日:2005-10-14 标 题:Treating diabetes using inhibitors of il-1 发明人:LAU JESPER 权利人:NOVO NORDISK AS 摘要:The present invention describes a method of treating diabetes or metabolic syndrome with a compound that inhibits (a) IL-1, (b) the synthesis of IL-1, or (c) the release of IL-1.
参考文献:10.2165/11530130-000000000-00000 摘要:Hasnain M, Vieweg WV, Fredrickson SK. Metformin for atypical antipsychotic-induced weight gain and glucose metabolism dysregulation: review of the literature and clinical suggestions. CNS Drugs. 2010 Mar;24(3):193–206. doi: 10.2165/11530130-000000000-00000. 参考文献:10.2165/11592040-000000000-00000 摘要:Cheung BM. Drug treatment for obesity in the post-sibutramine era. Drug Saf. 2011 Aug 01;34(8):641–50. doi: 10.2165/11592040-000000000-00000. 参考文献:10.3109/09513590.2011.588745 摘要:Koiou E, Tziomalos K, Katsikis I, Kandaraki EA, Kalaitzakis E, Delkos D, Vosnakis C, Panidis D. Weight loss significantly reduces serum lipocalin-2 levels in overweight and obese women with polycystic ovary syndrome. Gynecol Endocrinol. 2012 Jan;28(1):20–4. doi: 10.3109/09513590.2011.588745. 参考文献:10.2164/jandrol.111.013466 摘要:Bellentani FF, Fernandes GSA, Perobelli JE, Pacini ESA, Kiguti LRA, Pupo AS, Kempinas WDG. Acceleration of Sperm Transit Time and Reduction of Sperm Reserves in the Epididymis of Rats Exposed to Sibutramine. Journal of Andrology. 2011 Jul 15;32(6):718–24. doi: 10.2164/jandrol.111.013466. 摘要:Nagayama D, Shirai K. [Sibutramine and its adequate usage]. Nihon Rinsho. 2011 Jan;69 Suppl 1():678–82.