专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:WO-9747313-A1 优先权日:1996-06-10 标题:Total synthesis of bacitracin polypetides 发明人:GRIFFIN JOHN H; MCDOUGAL PATRICK G 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Methods for the total synthesis of bacitracin-type polypeptides are described, as well as useful analogs of bacitracin A, and treatment of bacterial infection using such analogs.
专利号:US-10654862-B2 优先权日:2015-03-18 标题 :Methods for the chemical synthesis of pyrrole-linked bivalent compounds, and compositions thereof 发明人:CRAN JOHN 权利人:AVEKSHAN LLC 摘要:The present invention in various aspects relates to the synthesis of pyrrole-linked bivalent compounds, including but not limited to norBNI, as well as pharmaceutical compositions comprising the same.
专利号:WO-0146695-A1 优先权日:1999-12-08 标 题:Novel supports for solid phase synthesis 发明人:ANTONENKO VALERY V; THIELE JOCHEN; ATUEGBU ANDY E 权利人:GLAXO GROUP LTD; ANTONENKO VALERY V; THIELE JOCHEN; ATUEGBU ANDY E 摘要:Novel solid supports and methods for their use in the synthesis of chemical compounds by the sequential addition of chemical building blocks are provided. The solid support comprises a polymer having reactive groups (for example, poly(styrene-co-vinylbenzyl chloride)) grafted to a chemically inert bulk material (such as a Teflon® membrane).
1: Ahmadi M, Nicholls PJ, Smith HJ, Spencer PS, Preet-Ryatt MS, Spragg BP. Metabolism of beclamide after a single oral dose in man: quantitative studies. J Pharm Pharmacol. 1995 Oct;47(10):876-8. doi: 10.1111/j.2042-7158.1995.tb05757.x. 81(2):162-7. doi: 10.1111/j.1600-0447.1990.tb06472.x. 43(6):425-9. doi: 10.1111/j.2042-7158.1991.tb03502.x. 1(5132):1275-8. doi: 10.1136/bmj.1.5132.1275. 5: Ozer AY, Hincal AA. Studies on the masking of unpleasant taste of beclamide: microencapsulation and tabletting. J Microencapsul. 1990 Jul-Sep;7(3):327-39. doi: 10.3109/02652049009021843. 24(45):11779-11784. doi: 10.1002/chem.201802208. Epub 2018 Jul 13. 40(12):891-3. doi: 10.1111/j.2042-7158.1988.tb06297.x. 42(6):447-9. doi: 10.1111/j.2042-7158.1990.tb06591.x. 2(4):377P-378P. 9(2):129-40. doi: 10.3109/00498257909038713. 2(4):364-5. doi: 10.1111/j.1365-2125.1975.tb02788.x. 12: Sawaya MC, Horton RW, Meldrum BS. Effects of anticonvulsant drugs on the cerebral enzymes metabolizing GABA. Epilepsia. 1975 Nov;16(4):649-55. doi: 10.1111/j.1528-1157.1975.tb04747.x. 32(3):365-74. French. 27 Suppl?-2:18P. 10(5):527-33. doi: 10.1111/j.1440-1681.1983.tb00221.x. 42(4):295-9. French. 1(5122):627-9. doi: 10.1136/bmj.1.5122.627.
合成参考文献
摘要:Pharmaceutical Chemistry Journal, 14(99), 1980 摘要:Psychotropic Drugs and Related Compounds, 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972, -(384), 1972 摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 摘要:REMEZOVA ES, KANTINA EA. [Application of a new anti-spastic drug chloracon in the treatment of epilepsy]. Zh Nevropatol Psikhiatr Im S S Korsakova. 1958;58(2):171–6.