📜(S)-托非索泮置于potassium Tert-Butylate,水体系中,用 四氢呋喃 用作溶剂,化学反应 2.0H,反应生成托非索泮 参考文献:Conversion Process For 2,3-Benzodiazepine Enantiomers 标题:Conversion Process For 2,3-Benzodiazepine Enantiomers 摘要:描述了将2,3-苯二氮䓬啉分子的一个对映异构体在碱性或酸性条件下转化为相应的混合物的消旋方法.此外,该发明涉及将托非索帕姆或其代谢物的一个对映异构体转化为相应的对映异构体的过程.
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-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-2006084805-A1 优先权日:2004-09-30 标题:Synthesis of thienopyridinone compounds and related intermediates
专利号:US-7982040-B2 优先权日:2004-05-17 标题 :Thienopyridinone compounds and methods of treatment 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; MOHANTY PRADYUMNA; CHEN DONGLI; LOBERA MERCEDES; WU LAURENCE; MARANTZ YAEL; INBAL BOAZ; HEIFETZ ALEXANDER; BAR-HAIM SHAY; SHACHAM SHARON 权利人:NANOTHERAPEUTICS 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-2004138238-A1 优先权日:2002-08-08 标题 :Substituted aminopyrimidine compounds as neurokinin antagonists 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY 摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:CN-107915688-A 优先权日:2016-10-09 标题 :A kind of synthesis process improvement method of tofisopam
1: Abdelmonaem AA, Abdel-Aziz AM, Ibrahim YF, Abdelzaher WY, Amgad Mohammed N, Marey H, S Taghian A, Setouhi A, Radi A, Ahmed SM. Cardioprotective effect of tofisopam against isoprenaline-induced myocardial infarction in rats via modulation of NLRP3\IL-1β\caspase-1 pathway. Immunopharmacol Immunotoxicol. 2024 Dec;46(6):902-911. doi: 10.1080/08923973.2024.2421528. Epub 2024 Nov 5. 89(8):5298-5303. doi: 10.1021/acs.joc.3c02660. Epub 2024 Apr 1. 17(1):140. doi: 10.3390/ph17010140. 4: Pálovics E, Madarász J, Pokol G, Fogassy E, Bánhegyi DF. Economic Separations of Organic Acidic or Basic Enantiomeric Mixtures-A Protocol Suggestion. Int J Mol Sci. 2023 Jan 3;24(1):846. doi: 10.3390/ijms24010846. 5: Matsuda K, Watanabe K, Miyagawa Y, Maruyama K, Konno N, Nakamachi T. Distribution of neuromedin U (NMU)-like immunoreactivity in the goldfish brain, and effect of intracerebroventricular administration of NMU on emotional behavior in goldfish. Peptides. 2022 Oct;156:170846. doi: 10.1016/j.peptides.2022.170846. Epub 2022 Jul 26. 36(7):819-835. doi: 10.1177/02698811221095528. Epub 2022 May 30. 43(2):174-176. doi: 10.1177/0253717621994285. Epub 2021 Feb 26.
合成参考文献
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