EA201492036A1 - Способ производства циклических ундекапептидов - Google Patents

Способ производства циклических ундекапептидов

Info

Publication number
EA201492036A1
EA201492036A1 EA201492036A EA201492036A EA201492036A1 EA 201492036 A1 EA201492036 A1 EA 201492036A1 EA 201492036 A EA201492036 A EA 201492036A EA 201492036 A EA201492036 A EA 201492036A EA 201492036 A1 EA201492036 A1 EA 201492036A1
Authority
EA
Eurasian Patent Office
Prior art keywords
leu
ala
subjected
ring opening
indeceptides
Prior art date
Application number
EA201492036A
Other languages
English (en)
Other versions
EA024903B1 (ru
Inventor
Фабрис Галлу
Бернард Рисс
Original Assignee
Новартис Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48444372&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201492036(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201492036A1 publication Critical patent/EA201492036A1/ru
Publication of EA024903B1 publication Critical patent/EA024903B1/ru

Links

Classifications

    • 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
    • C07K1/12—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by hydrolysis, i.e. solvolysis in general
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C07K7/645—Cyclosporins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Изобретение относится к способам и промежуточным соединениям, применимым для производства циклических ундекапептидов, таких как неиммуносупрессорное производное циклоспорина - алиспоривир. Циклоспорин ацилируют по боковой цепи бутенил-метил-треонина и затем подвергают реакции раскрытия кольца (раскрытие кольца происходит между остатками саркозина и N-метиллейцина). Это линейное пептидное промежуточное соединение подвергают расщеплению по методу Эдмана (удаление N-концевого остатка) для получения второго линейного декапептидного промежуточного соединения, например последовательности Val-N(Me)Leu-Ala-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt-Abu-Sar, если использовался CsA.
EA201492036A 2012-05-09 2013-05-08 Способ производства циклических ундекапептидов EA024903B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261644616P 2012-05-09 2012-05-09
PCT/EP2013/059672 WO2013167703A1 (en) 2012-05-09 2013-05-08 Process for the manufacture of cyclic undecapeptides

Publications (2)

Publication Number Publication Date
EA201492036A1 true EA201492036A1 (ru) 2015-02-27
EA024903B1 EA024903B1 (ru) 2016-10-31

Family

ID=48444372

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201492036A EA024903B1 (ru) 2012-05-09 2013-05-08 Способ производства циклических ундекапептидов

Country Status (24)

Country Link
US (2) US20150087808A1 (ru)
EP (1) EP2847211A1 (ru)
JP (3) JP2015517481A (ru)
KR (1) KR20150006435A (ru)
CN (2) CN108715606A (ru)
AR (1) AR090964A1 (ru)
AU (2) AU2013257989A1 (ru)
BR (1) BR112014027648A2 (ru)
CA (1) CA2868940A1 (ru)
CL (1) CL2014003014A1 (ru)
CO (1) CO7141428A2 (ru)
EA (1) EA024903B1 (ru)
EC (1) ECSP14030537A (ru)
HK (1) HK1202555A1 (ru)
IL (1) IL235428A0 (ru)
IN (1) IN2014DN08483A (ru)
MA (1) MA20150231A1 (ru)
MX (1) MX2014013613A (ru)
PE (1) PE20142433A1 (ru)
PH (1) PH12014502499A1 (ru)
SG (1) SG11201406303XA (ru)
TN (1) TN2014000411A1 (ru)
TW (1) TW201350508A (ru)
WO (1) WO2013167703A1 (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105693820A (zh) * 2014-11-27 2016-06-22 武汉药明康德新药开发有限公司 一种降解环孢菌素a的方法
KR20200007863A (ko) 2017-05-12 2020-01-22 추가이 세이야쿠 가부시키가이샤 환상 유기 화합물의 제조 방법

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AT401177B (de) 1993-10-22 1996-07-25 Biochemie Gmbh Verfahren zur herstellung von 7-amino-3-cephem-4-carbonsäure-derivaten
USRE40987E1 (en) * 1998-07-01 2009-11-17 Debiopharm S.A. Cyclosporin with improved activity profile
AU2125300A (en) * 1999-02-05 2000-08-25 Debiopharm S.A. Cyclosporin derivatives and method for the production of said derivatives
CN1507451A (zh) * 2001-04-20 2004-06-23 �±Ȱ·�ķ�ɷ����޹�˾ 可用作前体药物的修饰环孢菌素及其应用
KR100982466B1 (ko) * 2001-10-19 2010-09-16 이소테크니카 인코포레이티드 시클로스포린 유사체의 합성
TW200505946A (en) 2003-04-08 2005-02-16 Hoffmann La Roche Process for preparation of cyclosporin a analog
ATE490778T1 (de) * 2004-10-01 2010-12-15 Debiopharm Sa Verwendung von äd-mealaü3-äetvalü4-ciclosporin zur behandlung von hepatitis-c-infektion
EP1828229A4 (en) * 2004-12-17 2010-06-30 Isotechnika Inc METABOLITES OF CYCLOSPORINANALOGA
CA2674296C (en) 2007-01-04 2015-11-24 Debiopharm Sa Non-immunosuppressive cyclosporin for treatment of ullrich congenital muscular dystrophy
US8394763B2 (en) 2007-09-26 2013-03-12 Oregon Health & Science University Cyclic undecapeptides and derivatives as multiple sclerosis therapies
US7910378B2 (en) * 2007-12-14 2011-03-22 Siemens Healthcare Diagnostics Inc. Methods for detection of hydrophobic drugs
WO2009098533A1 (en) 2008-02-08 2009-08-13 Debiopharm Sa Non -immunosuppressive cyclosporin for the treatment of muscular dystrophy
CA2741829A1 (en) 2008-11-06 2010-05-14 Debio Recherche Pharmaceutique S.A. Cycloundecadepsipeptide compounds and use of said compounds as a medicament
WO2010076329A1 (en) * 2008-12-31 2010-07-08 Scynexis, Inc. Derivatives of cyclosporin a
RU2492181C2 (ru) * 2009-01-30 2013-09-10 Энанта Фармасьютикалс, Инк. Аналоги циклоспорина для предупреждения или лечения инфекции гепатита с
WO2012021796A2 (en) * 2010-08-12 2012-02-16 S&T Global, Inc. Novel cyclosporin derivatives for the treatment and prevention of a viral infection

Also Published As

Publication number Publication date
JP2015517481A (ja) 2015-06-22
AU2016222370B2 (en) 2017-10-05
WO2013167703A1 (en) 2013-11-14
IN2014DN08483A (ru) 2015-05-08
AR090964A1 (es) 2014-12-17
MA20150231A1 (fr) 2015-07-31
PE20142433A1 (es) 2015-02-02
WO2013167703A9 (en) 2014-11-20
TW201350508A (zh) 2013-12-16
BR112014027648A2 (pt) 2017-06-27
MX2014013613A (es) 2015-02-12
CN108715606A (zh) 2018-10-30
HK1202555A1 (en) 2015-10-02
US9840534B2 (en) 2017-12-12
AU2016222370A1 (en) 2016-09-15
EA024903B1 (ru) 2016-10-31
PH12014502499A1 (en) 2014-12-22
TN2014000411A1 (en) 2015-12-21
JP2018035154A (ja) 2018-03-08
CN104284902A (zh) 2015-01-14
JP2020033349A (ja) 2020-03-05
SG11201406303XA (en) 2014-11-27
KR20150006435A (ko) 2015-01-16
US20150087808A1 (en) 2015-03-26
IL235428A0 (en) 2014-12-31
US20160304554A1 (en) 2016-10-20
EP2847211A1 (en) 2015-03-18
CA2868940A1 (en) 2013-11-14
CL2014003014A1 (es) 2015-03-06
ECSP14030537A (es) 2015-09-30
CO7141428A2 (es) 2014-12-12
AU2013257989A1 (en) 2014-10-23

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU