Monomethyl auristatin E crystal and preparation method thereof

The invention provides a monomethyl auristatin E crystal form A and a preparation method thereof, a pharmaceutical composition containing the crystal form A, and application of the crystal form A in preparation of pharmaceutical conjugates. The crystal form A is high in purity, good in stability, lo...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: WANG GUITAO, HUANG BAOHUA, SHA FEI, SHAO JUN, PAN CHANGMING, MAO SHENGFEI
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
container_end_page
container_issue
container_start_page
container_title
container_volume
creator WANG GUITAO
HUANG BAOHUA
SHA FEI
SHAO JUN
PAN CHANGMING
MAO SHENGFEI
description The invention provides a monomethyl auristatin E crystal form A and a preparation method thereof, a pharmaceutical composition containing the crystal form A, and application of the crystal form A in preparation of pharmaceutical conjugates. The crystal form A is high in purity, good in stability, low in hygroscopicity and especially suitable for industrial application, and the defects that in the prior art, amorphous MMAE is low in purity, poor in stability and not suitable for storage, and when the amorphous MMAE is used for preparing conjugates, the requirement for reaction equipment is high, and operation is complex are overcome; and secondly, the preparation method of the MMAE crystal form A provided by the invention is simple to operate, the prepared crystal form is high in purity and uniform in particle size distribution, the production cost is reduced, and the preparation method is suitable for commercial production amplification. 本发明提供了一种一甲基澳瑞他汀E的晶型A及其制备方法,包含该晶型A的药物组合物,以及这些晶型A在制备药物偶联物中的应用。所述晶型A纯度高,稳定性
format Patent
fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_CN113121640A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>CN113121640A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_CN113121640A3</originalsourceid><addsrcrecordid>eNrjZLDzzc_Lz00tyajMUUgsLcosLkksycxTcFVILqoEsoGCeSkKBUWpBYlFQIn8PAWQ2vwUhZKM1KLU_DQeBta0xJziVF4ozc2g6OYa4uyhm1qQH59aXJCYnJqXWhLv7GdoaGxoZGhmYuBoTIwaAJD8MOg</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Monomethyl auristatin E crystal and preparation method thereof</title><source>esp@cenet</source><creator>WANG GUITAO ; HUANG BAOHUA ; SHA FEI ; SHAO JUN ; PAN CHANGMING ; MAO SHENGFEI</creator><creatorcontrib>WANG GUITAO ; HUANG BAOHUA ; SHA FEI ; SHAO JUN ; PAN CHANGMING ; MAO SHENGFEI</creatorcontrib><description>The invention provides a monomethyl auristatin E crystal form A and a preparation method thereof, a pharmaceutical composition containing the crystal form A, and application of the crystal form A in preparation of pharmaceutical conjugates. The crystal form A is high in purity, good in stability, low in hygroscopicity and especially suitable for industrial application, and the defects that in the prior art, amorphous MMAE is low in purity, poor in stability and not suitable for storage, and when the amorphous MMAE is used for preparing conjugates, the requirement for reaction equipment is high, and operation is complex are overcome; and secondly, the preparation method of the MMAE crystal form A provided by the invention is simple to operate, the prepared crystal form is high in purity and uniform in particle size distribution, the production cost is reduced, and the preparation method is suitable for commercial production amplification. 本发明提供了一种一甲基澳瑞他汀E的晶型A及其制备方法,包含该晶型A的药物组合物,以及这些晶型A在制备药物偶联物中的应用。所述晶型A纯度高,稳定性</description><language>chi ; eng</language><subject>CHEMISTRY ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PEPTIDES ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2021</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20210716&amp;DB=EPODOC&amp;CC=CN&amp;NR=113121640A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20210716&amp;DB=EPODOC&amp;CC=CN&amp;NR=113121640A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>WANG GUITAO</creatorcontrib><creatorcontrib>HUANG BAOHUA</creatorcontrib><creatorcontrib>SHA FEI</creatorcontrib><creatorcontrib>SHAO JUN</creatorcontrib><creatorcontrib>PAN CHANGMING</creatorcontrib><creatorcontrib>MAO SHENGFEI</creatorcontrib><title>Monomethyl auristatin E crystal and preparation method thereof</title><description>The invention provides a monomethyl auristatin E crystal form A and a preparation method thereof, a pharmaceutical composition containing the crystal form A, and application of the crystal form A in preparation of pharmaceutical conjugates. The crystal form A is high in purity, good in stability, low in hygroscopicity and especially suitable for industrial application, and the defects that in the prior art, amorphous MMAE is low in purity, poor in stability and not suitable for storage, and when the amorphous MMAE is used for preparing conjugates, the requirement for reaction equipment is high, and operation is complex are overcome; and secondly, the preparation method of the MMAE crystal form A provided by the invention is simple to operate, the prepared crystal form is high in purity and uniform in particle size distribution, the production cost is reduced, and the preparation method is suitable for commercial production amplification. 本发明提供了一种一甲基澳瑞他汀E的晶型A及其制备方法,包含该晶型A的药物组合物,以及这些晶型A在制备药物偶联物中的应用。所述晶型A纯度高,稳定性</description><subject>CHEMISTRY</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PEPTIDES</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2021</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLDzzc_Lz00tyajMUUgsLcosLkksycxTcFVILqoEsoGCeSkKBUWpBYlFQIn8PAWQ2vwUhZKM1KLU_DQeBta0xJziVF4ozc2g6OYa4uyhm1qQH59aXJCYnJqXWhLv7GdoaGxoZGhmYuBoTIwaAJD8MOg</recordid><startdate>20210716</startdate><enddate>20210716</enddate><creator>WANG GUITAO</creator><creator>HUANG BAOHUA</creator><creator>SHA FEI</creator><creator>SHAO JUN</creator><creator>PAN CHANGMING</creator><creator>MAO SHENGFEI</creator><scope>EVB</scope></search><sort><creationdate>20210716</creationdate><title>Monomethyl auristatin E crystal and preparation method thereof</title><author>WANG GUITAO ; HUANG BAOHUA ; SHA FEI ; SHAO JUN ; PAN CHANGMING ; MAO SHENGFEI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN113121640A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>chi ; eng</language><creationdate>2021</creationdate><topic>CHEMISTRY</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PEPTIDES</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>WANG GUITAO</creatorcontrib><creatorcontrib>HUANG BAOHUA</creatorcontrib><creatorcontrib>SHA FEI</creatorcontrib><creatorcontrib>SHAO JUN</creatorcontrib><creatorcontrib>PAN CHANGMING</creatorcontrib><creatorcontrib>MAO SHENGFEI</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>WANG GUITAO</au><au>HUANG BAOHUA</au><au>SHA FEI</au><au>SHAO JUN</au><au>PAN CHANGMING</au><au>MAO SHENGFEI</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Monomethyl auristatin E crystal and preparation method thereof</title><date>2021-07-16</date><risdate>2021</risdate><abstract>The invention provides a monomethyl auristatin E crystal form A and a preparation method thereof, a pharmaceutical composition containing the crystal form A, and application of the crystal form A in preparation of pharmaceutical conjugates. The crystal form A is high in purity, good in stability, low in hygroscopicity and especially suitable for industrial application, and the defects that in the prior art, amorphous MMAE is low in purity, poor in stability and not suitable for storage, and when the amorphous MMAE is used for preparing conjugates, the requirement for reaction equipment is high, and operation is complex are overcome; and secondly, the preparation method of the MMAE crystal form A provided by the invention is simple to operate, the prepared crystal form is high in purity and uniform in particle size distribution, the production cost is reduced, and the preparation method is suitable for commercial production amplification. 本发明提供了一种一甲基澳瑞他汀E的晶型A及其制备方法,包含该晶型A的药物组合物,以及这些晶型A在制备药物偶联物中的应用。所述晶型A纯度高,稳定性</abstract><oa>free_for_read</oa></addata></record>
fulltext fulltext_linktorsrc
identifier
ispartof
issn
language chi ; eng
recordid cdi_epo_espacenet_CN113121640A
source esp@cenet
subjects CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Monomethyl auristatin E crystal and preparation method thereof
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-11T01%3A13%3A22IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=WANG%20GUITAO&rft.date=2021-07-16&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3ECN113121640A%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true