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
fmoc
otbu
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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 (https=)
EP (2) EP4549450A3 (https=)
JP (1) JP6801835B2 (https=)
KR (1) KR102056257B1 (https=)
CN (2) CN107849089B (https=)
AU (1) AU2016290654C1 (https=)
TW (1) TWI708779B (https=)
WO (1) WO2017005902A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6801835B2 (ja) * 2015-07-09 2020-12-16 ミメトゲン ファーマシュウティカルズ インコーポレイテッドＭｉｍｅｔｏｇｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． β−ターンペプチド模倣環状塩の液相合成及び結晶化
EP4067368A1 (en) 2016-06-01 2022-10-05 Athira Pharma, Inc. Compounds
CA3098707A1 (en) * 2018-05-31 2019-12-05 Gap Peptides Llc Method for solution-phase peptide synthesis and protecting strategies thereof
US11427612B2 (en) * 2018-08-21 2022-08-30 Wayne State University Epimerization-free N to C solid-phase peptide synthesis

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
DE60123399T2 (de) 2000-01-18 2007-08-23 The Texas A & M University System, College Station Pharmazeutische zubereitungen enthaltend beta-turn peptidomimetische zyklische substanzen
EP1517915B1 (en) * 2002-06-11 2009-01-21 Eli Lilly And Company Prodrugs of excitatory amino acids
WO2012013281A1 (de) * 2010-07-29 2012-02-02 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
WO2014204681A1 (en) * 2013-06-20 2014-12-24 Exxonmobil Chemical Patents Inc. Long-bridged salen catalyst
JP6801835B2 (ja) * 2015-07-09 2020-12-16 ミメトゲン ファーマシュウティカルズ インコーポレイテッドＭｉｍｅｔｏｇｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． β−ターンペプチド模倣環状塩の液相合成及び結晶化

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

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