专利号:US-8236960-B2 优先权日:2004-09-27 标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl)carbamide and its tartrate salt and crystalline forms 发明人:THYGESEN MIKKEL BOAS; SCHLIENGER NATHALIE; TOLF BO-RAGNAR; ANDERSSON CARL-MAGNUS A; BLATTER FRITZ; BERGHAUSEN JOERG 权利人:THYGESEN MIKKEL BOAS; SCHLIENGER NATHALIE; TOLF BO-RAGNAR; ANDERSSON CARL-MAGNUS A; BLATTER FRITZ; BERGHAUSEN JOERG; ACADIA PHARM INC 摘要:Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl) -N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2 -methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.
专利号:WO-9412651-A1 优先权日:1992-12-01 标题 :Enzymatic synthesis of sugar alcohol esters 发明人:BARFOED MARTIN; SKAGERLIND JAN PETER 权利人:NOVO NORDISK AS; BARFOED MARTIN; SKAGERLIND JAN PETER 摘要:A method of preparing a compound of the general formula (I): R1-COO-X-O-R2, wherein R1-CO is the acyl group of a carboxylic acid which may be saturated or unsaturated, O-X-O is a saccharide moiety or a sugar alcohol moiety corresponding to a saccharide or a sugar alcohol of the general formula X(OH)¿2 , and R 2¿ is hydrogen, acetyl, or an alkyl group.
专利号:US-7790899-B2 优先权日:2004-09-27 标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms 发明人:TOLF BO-RAGNAR; SCHLIENGER NATHALIE; THYGESEN MIKKEL BOAS 权利人:ACADIA PHARM INC 摘要:Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.
专利号:US-8871926-B1 优先权日:2010-09-28 标题:Synthesis of porphyrin nanostructures 发明人:FAN HONGYOU; BAI FENG 权利人:FAN HONGYOU; BAI FENG; SANDIA CORP 摘要:The present disclosure generally relates to self-assembly methods for generating porphyrin nanostructures. For example, in one embodiment a method is provided that includes preparing a porphyrin solution and a surfactant solution. The porphyrin solution is then mixed with the surfactant solution at a concentration sufficient for confinement of the porphyrin molecules by the surfactant molecules. In some embodiments, the concentration of the surfactant is at or above its critical micelle concentration (CMC), which allows the surfactant to template the growth of the nanostructure over time. The size and morphology of the nanostructures may be affected by the type of porphyrin molecules used, the type of surfactant used, the concentration of the porphyrin and surfactant the pH of the mixture of the solutions, and the order of adding the reagents to the mixture, to name a few variables.
专利号:US-7799829-B2 优先权日:2006-07-28 标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use 发明人:DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A 权利人:XENOPORT INC 摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
专利号:US-2006205714-A1 优先权日:2004-04-01 标 题 :Method of synthesis and isolation of solid N-desmethylclozapine and crystalline forms thereof 发明人:TOLF BO-RAGNAR; THYGESEN MIKKEL B; BLATTER FRITZ; BERGHAUSEN JORG 权利人:TOLF BO-RAGNAR; THYGESEN MIKKEL B; BLATTER FRITZ; BERGHAUSEN JORG 摘要:Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms.
1: Duan X, Xiang M, Wang L, Yan Q, Yang S, Jiang Z. Biochemical characterization of a novel lipase from Malbranchea cinnamomea suitable for production of lipolyzed milkfat flavor and biodegradation of phthalate esters. Food Chem. 2019 Nov 1;297:124925. doi: 10.1016/j.foodchem.2019.05.199. Epub 2019 May 31. doi: 10.3389/fphys.2019.00657. eCollection 2019. 3: Hvid H, Kildegaard J, Kristensen K, Porsgaard T, Jørgensen MS, Ballarín-González B, Ahnfelt-Rønne J, Hansen BF, Nishimura E. Intraintestinal and Parenteral Administration of an Insulin Analogue Leads to Comparable Activation of Signaling Downstream of the Insulin Receptor in the Small Intestine. J Diabetes Sci Technol. 2019 Jun 12:1932296819855075. doi: 10.1177/1932296819855075. [Epub ahead of print] pii: giz061. doi: 10.1093/gigascience/giz061.
合成参考文献
摘要:Final Report 04/2019 Available from CIR 参考文献:10.1023/a:1016080723968 摘要:Okumura S, Fukuda Y, Takahashi K, Fujita T, Yamamoto A, Muranishi S. Transport of drugs across the Xenopus pulmonary membrane and their absorption enhancement by various absorption enhancers. Pharm Res. 1996 Aug;13(8):1247–51. doi: 10.1023/a:1016080723968. 参考文献:10.1186/s13568-018-0605-4 摘要:Sugiharto YEC, Lee H, Fitriana AD, Lee H, Jeon W, Park K, Ahn J, Lee H. Effect of decanoic acid and 10-hydroxydecanoic acid on the biotransformation of methyl decanoate to sebacic acid. AMB Express. 2018 May 05;8(1):75. 参考文献:10.1208/s12248-021-00670-1 摘要:Metry M, Polli JE. Evaluation of Excipient Risk in BCS Class I and III Biowaivers. The AAPS Journal. 2022 Jan 05;24(1):20. doi: 10.1208/s12248-021-00670-1. 参考文献:10.1023/a:1016188312399 摘要:González Ferreiro M, Tillman LG, Hardee G, Bodmeier R. Alginate/poly-L-lysine microparticles for the intestinal delivery of antisense oligonucleotides. Pharm Res. 2002 Jun;19(6):755–64. doi: 10.1023/a:1016188312399.