H-D-β-Nal-Cys-(Acm)-Tyr-D-Trp-Lys-Val-Cys(Acm)-Thr-Nh2置于碘,溶剂黄146体系中,用 甲醇 用作溶剂,化学反应 0.25H,以350 Mg的收率获得兰瑞肽 参考文献:Boc And Fmoc Solid Phase Peptide Synthesis 标题:Boc And Fmoc Solid Phase Peptide Synthesis 摘要:使用boc和fmoc保护的氨基酸以及氯甲基化聚苯乙烯树脂合成含有三个或更多氨基酸残基的肽的固相方法.
专利信息
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-2005164912-A1 优先权日:2003-12-31 标 题:Methods for recovering cleaved peptide from a support after solid phase synthesis 发明人:BIGELOW ROGER D; CAIN ROBERT O 摘要:Methods for the solid phase synthesis of peptides and peptide intermediates, in particular methods involving recovering peptides from resin supports at excellent yield. In this invention, an alternating at least partially repeating cycle of shrinking and swelling treatments are used. Each shrinking or swelling part of a cycle may involve one or more washes. The process provides excellent recovery of peptide in a very efficient manner in terms of the number of individual washes and the total volume of wash reagents used.
专利号:US-9388212-B2 优先权日:2013-02-21 标 题:Solid phase peptide synthesis via side chain attachment 发明人:BARLOS KLEOMENIS K 权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A 摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
专利号:US-2009162290-A1 优先权日:2005-09-09 标 题 :Method for the synthesis of penta-pendant enantiomer-pure chelators and process for therapeutically active bioconjugates preparation by a covalent binding thereof 发明人:BENES IVAN; CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R 1 , R 2 , R 3 , R 4 are groups forming an adequate enantiomer of the chelator; and X 1 -X 5 , Y 1 -Y 5 , Z 1 -Z 5 each individually forming pendant chelating groups.
1: Caplin ME, Pavel M, Ćwikła JB, Phan AT, Raderer M, Sedláčková E, Cadiot G, Wolin EM, Capdevila J, Wall L, Rindi G, Langley A, Martinez S, Blumberg J, Ruszniewski P; CLARINET Investigators. Lanreotide in metastatic enteropancreatic neuroendocrine tumors. N Engl J Med. 2014 Jul 17;371(3):224-33. doi: 10.1056/NEJMoa1316158. doi: 10.1007/s40265-014-0283-8. Review. doi: 10.1186/s12885-015-1512-6. 4: Zheng N, Dai W, Zhang H, Wang X, Wang J, Zhang X, Wang K, Li J, Zhang Q. Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors. J Drug Target. 2015 Jan;23(1):67-78. doi: 10.3109/1061186X.2014.954118. Epub 2014 Nov 4. Pasireotide versus continued treatment with octreotide or lanreotide in patients with inadequately controlled acromegaly (PAOLA): a randomised, phase 3 trial. Lancet Diabetes Endocrinol. 2014 Nov;2(11):875-84. doi: 10.1016/S2213-8587(14)70169-X. Epub 2014 Sep 24. doi: 10.1111/liv.12726. Epub 2014 Dec 1. e1. doi: 10.1016/j.cgh.2015.05.039. Epub 2015 Jun 12. doi: 10.1007/s11102-016-0724-3. Review. 10: Hernández B, Coïc YM, Baron B, Kruglik SG, Pflüger F, Cohen R, Carelli C, Ghomi M. Low concentration structural dynamics of lanreotide and somatostatin-14. Biopolymers. 2014 Oct;101(10):1019-28. doi: 10.1002/bip.22491. Review. Lanreotide Autogel 120 mg at extended dosing intervals in patients with acromegaly biochemically controlled with octreotide LAR: the LEAD study. Eur J Endocrinol. 2015 Sep;173(3):313-23. doi: 10.1530/EJE-15-0215. Epub 2015 Jun 5.
合成参考文献
参考文献:10.1530/eje-09-0769 摘要:Auriemma RS, Galdiero M, Grasso LF, Vitale P, Cozzolino A, Lombardi G, Colao A, Pivonello R. Complete disappearance of a GH-secreting pituitary macroadenoma in a patient with acromegaly: effect of treatment with lanreotide Autogel and consequence of treatment withdrawal. Eur J Endocrinol. 2010 May;162(5):993–9. doi: 10.1530/eje-09-0769.