CN107849089B - β-转角环状模拟肽盐的溶液相合成和结晶 - Google Patents

β-转角环状模拟肽盐的溶液相合成和结晶 Download PDF

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Publication number
CN107849089B
CN107849089B CN201680040450.0A CN201680040450A CN107849089B CN 107849089 B CN107849089 B CN 107849089B CN 201680040450 A CN201680040450 A CN 201680040450A CN 107849089 B CN107849089 B CN 107849089B
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formula
compound
hcl
salt
fmoc
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CN107849089A (zh
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尚塔尔·德温
田伟
马丁·博林
塞巴斯蒂安·罗基
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Mimetogen Pharmaceuticals Inc
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Mimetogen Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14—Extraction; Separation; Purification
    • C07K1/30—Extraction; Separation; Purification by precipitation
    • C07K1/306—Extraction; Separation; Purification by precipitation by crystallization
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201680040450.0A 2015-07-09 2016-07-08 β-转角环状模拟肽盐的溶液相合成和结晶 Active CN107849089B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210654769.XA CN114874288A (zh) 2015-07-09 2016-07-08 β-转角环状模拟肽盐的溶液相合成和结晶

Applications Claiming Priority (3)

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US201562190596P 2015-07-09 2015-07-09
US62/190,596 2015-07-09
PCT/EP2016/066281 WO2017005902A1 (en) 2015-07-09 2016-07-08 Solution phase synthesis and crystallization of beta-turn peptidomimetic cyclic salts

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CN107849089A CN107849089A (zh) 2018-03-27
CN107849089B true CN107849089B (zh) 2022-07-05

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CN202210654769.XA Pending CN114874288A (zh) 2015-07-09 2016-07-08 β-转角环状模拟肽盐的溶液相合成和结晶

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US (4) US10125165B2 (enExample)
EP (2) EP3319978B1 (enExample)
JP (1) JP6801835B2 (enExample)
KR (1) KR102056257B1 (enExample)
CN (2) CN107849089B (enExample)
AU (1) AU2016290654C1 (enExample)
TW (1) TWI708779B (enExample)
WO (1) WO2017005902A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102056257B1 (ko) * 2015-07-09 2019-12-16 미메토젠 파르마슈티칼스 인크. 베타-턴 펩티도미메틱 사이클릭 염의 용액상 합성 및 결정화
SI3464336T1 (sl) 2016-06-01 2022-06-30 Athira Pharma, Inc. Spojine
KR102826649B1 (ko) * 2018-05-31 2025-06-30 쎄데르마 용액-상 펩티드의 합성 방법 및 그에 따른 보호 전략
US11427612B2 (en) * 2018-08-21 2022-08-30 Wayne State University Epimerization-free N to C solid-phase peptide synthesis
CN117279928A (zh) * 2021-05-07 2023-12-22 中外制药株式会社 包含n-取代氨基酸残基的环状化合物的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102046166A (zh) * 2008-04-04 2011-05-04 米梅托根药物公司 治疗干眼症的方法
CN102333537A (zh) * 2009-02-27 2012-01-25 米梅托根药物公司 用于治疗色素性视网膜炎的模拟肽环状化合物
CN104619717A (zh) * 2012-06-22 2015-05-13 米梅奥亨制药公司 β-转角模拟肽环状化合物的合成

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AUPP254898A0 (en) * 1998-03-24 1998-04-23 University Of Queensland, The Peptide turn mimetics
WO2001052843A1 (en) 2000-01-18 2001-07-26 Mcgill University β-TURN PEPTIDOMIMETIC CYCLIC COMPOUNDS
HRP20041179B1 (hr) * 2002-06-11 2012-11-30 Eli Lilly And Company Prekursorski oblici lijekova za aminokiseline s pobuđivačkom aktivnosti
EP2598604B1 (de) * 2010-07-29 2015-11-25 Merck Patent GmbH Flüssigkristallines medium enthaltend thiophenderivate
JP5710436B2 (ja) * 2011-09-26 2015-04-30 株式会社東芝 パターン形成方法
JP6516974B2 (ja) * 2013-06-14 2019-05-22 豊田合成株式会社 ゴム組成物及びゴム製品
CN105142777B (zh) * 2013-06-20 2017-12-26 埃克森美孚化学专利公司 长桥Salen催化剂
KR102056257B1 (ko) * 2015-07-09 2019-12-16 미메토젠 파르마슈티칼스 인크. 베타-턴 펩티도미메틱 사이클릭 염의 용액상 합성 및 결정화

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102046166A (zh) * 2008-04-04 2011-05-04 米梅托根药物公司 治疗干眼症的方法
CN102333537A (zh) * 2009-02-27 2012-01-25 米梅托根药物公司 用于治疗色素性视网膜炎的模拟肽环状化合物
CN104619717A (zh) * 2012-06-22 2015-05-13 米梅奥亨制药公司 β-转角模拟肽环状化合物的合成

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Rapid, Continuous Solution-Phase Peptide Synthesis: Application to Peptides of Pharmaceutical Interest;Louis A. Carpino 等;《Organic Process Research & Development》;20031231;第7卷(第1期);第32-37页experimental section部分 *
β2-Amino Acids in the Design of Conformationally Homogeneous cyclo-Peptide Scaffolds;Anna S. Norgren等;《The journal of organic chemistry》;20060901;第71卷(第18期);第6816页右栏最后一段,第6817页左栏第1-12行,图2,3 *

Also Published As

Publication number Publication date
CN114874288A (zh) 2022-08-09
WO2017005902A1 (en) 2017-01-12
TWI708779B (zh) 2020-11-01
JP6801835B2 (ja) 2020-12-16
AU2016290654A2 (en) 2020-08-06
AU2016290654A1 (en) 2018-01-25
EP3319978C0 (en) 2025-02-19
EP4549450A2 (en) 2025-05-07
US20230357318A1 (en) 2023-11-09
US12281179B2 (en) 2025-04-22
AU2016290654C1 (en) 2021-11-11
US20170008923A1 (en) 2017-01-12
KR20180036982A (ko) 2018-04-10
US11078234B2 (en) 2021-08-03
TW201716425A (zh) 2017-05-16
AU2016290654B2 (en) 2021-07-08
CN107849089A (zh) 2018-03-27
US11753441B2 (en) 2023-09-12
HK1255355A1 (en) 2019-08-16
KR102056257B1 (ko) 2019-12-16
CA2991661A1 (en) 2017-01-12
EP3319978A1 (en) 2018-05-16
EP4549450A3 (en) 2025-07-02
US20190194251A1 (en) 2019-06-27
US20210300966A1 (en) 2021-09-30
US10125165B2 (en) 2018-11-13
EP3319978B1 (en) 2025-02-19
JP2018528928A (ja) 2018-10-04

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