CA2265454A1 - Peptide prodrugs containing an alpha-hydroxyacid linker - Google Patents

Peptide prodrugs containing an alpha-hydroxyacid linker Download PDF

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Publication number
CA2265454A1
CA2265454A1 CA002265454A CA2265454A CA2265454A1 CA 2265454 A1 CA2265454 A1 CA 2265454A1 CA 002265454 A CA002265454 A CA 002265454A CA 2265454 A CA2265454 A CA 2265454A CA 2265454 A1 CA2265454 A1 CA 2265454A1
Authority
CA
Canada
Prior art keywords
peptide
glu
lys
alkyl
amino
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002265454A
Other languages
English (en)
French (fr)
Inventor
Bjarne Due Larsen
Arne Holm
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Zealand Pharma AS
Original Assignee
Individual
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
Application filed by Individual filed Critical Individual
Publication of CA2265454A1 publication Critical patent/CA2265454A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General 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
    • C07K1/1072General 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 by covalent attachment of residues or functional groups
    • C07K1/1075General 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 by covalent attachment of residues or functional groups by covalent attachment of amino acids or peptide residues
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA002265454A 1996-09-09 1997-09-09 Peptide prodrugs containing an alpha-hydroxyacid linker Abandoned CA2265454A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DK97296 1996-09-09
DK0972/96 1996-09-09
PCT/DK1997/000376 WO1998011126A1 (de) 1996-09-09 1997-09-09 Peptide prodrugs

Publications (1)

Publication Number Publication Date
CA2265454A1 true CA2265454A1 (en) 1998-03-19

Family

ID=8099572

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002265454A Abandoned CA2265454A1 (en) 1996-09-09 1997-09-09 Peptide prodrugs containing an alpha-hydroxyacid linker

Country Status (8)

Country Link
EP (1) EP0932614A1 (de)
JP (1) JP2001505872A (de)
KR (1) KR20000036015A (de)
AU (1) AU724326B2 (de)
CA (1) CA2265454A1 (de)
IL (1) IL128828A0 (de)
NZ (1) NZ334595A (de)
WO (1) WO1998011126A1 (de)

Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0967999A2 (de) * 1997-02-14 2000-01-05 The Salk Institute For Biological Studies Verfahren und zusammensetzungen zur abgabe therapeutischer mittel an knochen mit conjugaten von negativ geladenen peptidoligomeren mit therapeutischen mittel
EP1062229A1 (de) 1998-03-09 2000-12-27 Zealand Pharmaceuticals A/S Pharmakologisch aktive peptid-konjugate mit verringerter neigung enzymatisch hydrolysiert zu werden
EP1076066A1 (de) * 1999-07-12 2001-02-14 Zealand Pharmaceuticals A/S Peptide zur Senkung des Blutglukosespiegels
US6528486B1 (en) 1999-07-12 2003-03-04 Zealand Pharma A/S Peptide agonists of GLP-1 activity
US6908900B2 (en) * 2001-01-17 2005-06-21 Zimmer & Associates Ag Compositions and methods for enhanced pharmacological activity through oral and parenteral administration of compositions comprising polypeptide drug substances and other poorly absorbed active ingredients
US7671029B2 (en) 1999-08-06 2010-03-02 Immupharma Sa Compositions and methods for enhanced pharmacological activity of compositions comprising peptide drug substances
EP1224318A2 (de) * 1999-10-29 2002-07-24 Novus International, Inc. Oligomere und oligomerische teilstücke von alpha-hydroxy-carboxysäuren und alpha-
US6939693B2 (en) 1999-10-29 2005-09-06 Novus International, Inc. Enantioselective oligomerization of α-hydroxy carboxylic acids and α-amino acids
DE10018617A1 (de) * 2000-01-13 2001-10-31 Joerg G Moser Cyclodextrin-Dimere mit Peptid-Spacerstrukturen zur Entgiftung von pharmazeutischen Wirkstoffen hohen Nebenwirkungspotentials
WO2002030460A2 (en) 2000-10-09 2002-04-18 Isis Innovation Ltd. Therapeutic antibodies
US6881829B2 (en) * 2002-04-26 2005-04-19 Chimeracom, L.L.C. Chimeric hybrid analgesics
JP2009508885A (ja) 2005-09-21 2009-03-05 7ティーエム ファーマ エイ/エス 治療的介入のためのy4選択性レセプターアゴニスト
AU2005337101A1 (en) 2005-09-21 2007-04-12 7Tm Pharma A/S Y2 selective receptor agonists for therapeutic interventions
CA2628241C (en) 2005-11-07 2016-02-02 Indiana University Research And Technology Corporation Glucagon analogs exhibiting physiological solubility and stability
AU2008205229B2 (en) 2007-01-05 2014-03-27 Indiana University Research And Technology Corporation Glucagon analogs exhibiting enhanced solubility in physiological pH buffers
AU2008216265B2 (en) 2007-02-15 2014-04-03 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
EP3492488A1 (de) 2007-08-22 2019-06-05 The Regents of The University of California Aktivierbare bindende polypeptide und verfahren zu deren identifikation und anwendung
MX2010004297A (es) 2007-10-30 2010-05-03 Univ Indiana Res & Tech Corp Antagonistas de glucagon.
CA2702289A1 (en) 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Compounds exhibiting glucagon antagonist and glp-1 agonist activity
JP2011511778A (ja) 2008-01-30 2011-04-14 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーション エステルに基づいたペプチドプロドラッグ
NZ589847A (en) 2008-06-17 2013-01-25 Univ Indiana Res & Tech Corp Glucagon/glp-1 receptor co-agonists
CN104945500B (zh) 2008-06-17 2019-07-09 印第安纳大学研究及科技有限公司 基于gip的混合激动剂用于治疗代谢紊乱和肥胖症
US8450270B2 (en) 2008-06-17 2013-05-28 Indiana University Research And Technology Corporation Glucagon analogs exhibiting enhanced solubility and stability in physiological pH buffers
WO2010070252A1 (en) 2008-12-15 2010-06-24 Zealand Pharma A/S Glucagon analogues
KR101593406B1 (ko) 2008-12-15 2016-02-12 질랜드 파마 에이/에스 글루카곤 유사체
CN102282166B (zh) 2008-12-15 2015-04-01 西兰制药公司 胰高血糖素类似物
UA104605C2 (uk) 2008-12-15 2014-02-25 Зіленд Фарма А/С Аналоги глюкагону
CA2744558A1 (en) 2008-12-19 2010-07-15 Indiana University Research And Technology Corporation Amide-based insulin prodrugs
AU2009335712B2 (en) 2008-12-19 2015-09-17 Indiana University Research And Technology Corporation Insulin analogs
JP2012512903A (ja) * 2008-12-19 2012-06-07 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーション アミド系グルカゴンスーパーファミリーペプチドプロドラッグ
AU2010203353B2 (en) 2009-01-12 2016-06-16 Cytomx Therapeutics, Inc Modified antibody compositions, methods of making and using thereof
RU2012101274A (ru) 2009-06-16 2013-07-27 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Соединения глюкагона, активные в отношении рецептора gip
PL2454282T3 (pl) 2009-07-13 2015-08-31 Zealand Pharma As Acylowane analogi glukagonu
WO2011075393A2 (en) 2009-12-18 2011-06-23 Indiana University Research And Technology Corporation Glucagon/glp-1 receptor co-agonists
WO2011094337A1 (en) 2010-01-27 2011-08-04 Indiana University Research And Technology Corporation Glucagon antagonist - gip agonist conjugates and compositions for the treatment of metabolic disorders and obesity
SG184988A1 (en) 2010-04-27 2012-11-29 Zealand Pharma As Peptide conjugates of glp-1 receptor agonists and gastrin and their use
EP2569000B1 (de) 2010-05-13 2017-09-27 Indiana University Research and Technology Corporation Glucagon-superfamilien-peptide mit nuklearhormon-rezeptoraktivität
CN103179976A (zh) 2010-05-13 2013-06-26 印第安纳大学研究及科技有限公司 呈现g蛋白偶联受体活性的胰高血糖素超家族肽
EP2582719B1 (de) 2010-06-16 2016-08-10 Indiana University Research and Technology Corporation Einkettige insulinagonisten mit hoher aktivität am insulinrezeptor
UY33462A (es) 2010-06-23 2012-01-31 Zealand Pharma As Analogos de glucagon
KR20130102470A (ko) 2010-06-24 2013-09-17 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 아미드계 글루카곤 슈퍼패밀리 펩티드 프로드러그
CN103119057B (zh) 2010-06-24 2016-06-15 印第安纳大学研究及科技有限公司 基于酰胺的胰岛素前药
JP6023048B2 (ja) 2010-06-24 2016-11-09 ジーランド ファーマ アクティーゼルスカブ グルカゴン類似体
US8507428B2 (en) 2010-12-22 2013-08-13 Indiana University Research And Technology Corporation Glucagon analogs exhibiting GIP receptor activity
PE20140724A1 (es) 2011-06-22 2014-07-10 Univ Indiana Res & Tech Corp Coagonistas del receptor de glucagon/glp-1
US9309301B2 (en) 2011-06-22 2016-04-12 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US20140249093A1 (en) * 2011-08-12 2014-09-04 Ascendis Pharma A/S Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages
CA2853884A1 (en) 2011-11-03 2013-05-10 Zealand Pharma A/S Glp-1 receptor agonist peptide gastrin conjugates
KR20140097151A (ko) 2011-11-17 2014-08-06 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 글루코코르티코이드 수용체 활성을 나타내는 글루카곤 슈퍼패밀리 펩티드
CN104114183A (zh) 2011-12-20 2014-10-22 印第安纳大学研究及科技有限公司 用于治疗糖尿病的基于ctp的胰岛素类似物
PE20150605A1 (es) 2012-04-27 2015-05-28 Cytomx Therapeutics Inc Anticuerpos activables que se unen al receptor del factor de crecimiento epidermico
KR102184241B1 (ko) 2012-05-03 2020-12-01 질랜드 파마 에이/에스 Gip-glp-1 이원 작용제 화합물 및 방법
WO2013192129A1 (en) 2012-06-21 2013-12-27 Indiana University Research And Technology Corporation Glucagon analogs exhibiting gip receptor activity
PL2875043T3 (pl) 2012-07-23 2017-06-30 Zealand Pharma A/S Analogi glukagonu
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
EP3395358B1 (de) 2012-09-26 2019-11-06 Indiana University Research and Technology Corporation Insulinanalogdimere
CN104936613B (zh) 2012-11-30 2018-05-22 株式会社糖锁工学研究所 糖链加成连接子、含有糖链加成连接子与生理活性物质的化合物或其盐、以及其制造方法
AU2014241743B2 (en) 2013-03-14 2018-07-05 Indiana University Research And Technology Corporation Insulin-incretin conjugates
HUE034308T2 (en) 2013-03-21 2018-02-28 Sanofi Aventis Deutschland Preparation of hydantoin-containing peptide products
HUE033371T2 (en) 2013-03-21 2017-11-28 Sanofi Aventis Deutschland Process for the preparation of peptide products containing a ring imide
LT2994153T (lt) * 2013-05-07 2018-11-26 Merck Patent Gmbh Peptidų ir peptidų aktyvių ingredientų konjugatas, skirtas vaisto nukreipimui į inkstus
LT2994152T (lt) * 2013-05-07 2018-11-26 Merck Patent Gmbh Konjugatai, skirti apsaugai nuo nefrotoksinių aktyvių medžiagų
US9988429B2 (en) 2013-10-17 2018-06-05 Zealand Pharma A/S Glucagon analogues
EP3057984B1 (de) 2013-10-17 2018-07-11 Zealand Pharma A/S Acylierte glucagon-analoga
WO2015066279A2 (en) 2013-10-30 2015-05-07 Cytomx Therapeutics, Inc. Activatable antibodies that bind epidermal growth factor receptor and methods of use thereof
KR102310389B1 (ko) 2013-11-06 2021-10-13 질랜드 파마 에이/에스 Gip-glp-1 이원 효능제 화합물 및 방법
TR201902516T4 (tr) 2013-11-06 2019-03-21 Zealand Pharma As Glukagon-glp-1-gıp üçlü agonist bileşikleri.
US9737623B2 (en) 2013-12-11 2017-08-22 Cytomx Therapeutics, Inc. Antibodies that bind activatable antibodies and methods of use thereof
JP6701208B2 (ja) 2014-09-24 2020-05-27 インディアナ ユニヴァーシティ リサーチ アンド テクノロジー コーポレイション 脂質化アミド系インスリンプロドラッグ
WO2016049190A1 (en) 2014-09-24 2016-03-31 Indiana University Research And Technology Corporation Incretin-insulin conjugates
US10253078B2 (en) 2014-10-29 2019-04-09 Zealand Pharma A/S GIP agonist compounds and methods
MX2017012864A (es) 2015-04-16 2018-06-12 Zealand Pharma As Analogo acilado del glucagon.
CN110088125B (zh) 2016-12-09 2023-10-03 西兰制药公司 酰化的glp-1/glp-2双重激动剂
AU2018368769B2 (en) * 2017-11-17 2024-05-09 Cytogel Pharma, Llc Polymer agonists of mu opioid receptors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5589356A (en) * 1993-06-21 1996-12-31 Vanderbilt University Litigation of sidechain unprotected peptides via a masked glycoaldehyde ester and O,N-acyl rearrangement

Also Published As

Publication number Publication date
AU4199497A (en) 1998-04-02
AU724326B2 (en) 2000-09-14
NZ334595A (en) 2000-08-25
EP0932614A1 (de) 1999-08-04
KR20000036015A (ko) 2000-06-26
JP2001505872A (ja) 2001-05-08
IL128828A0 (en) 2000-01-31
WO1998011126A1 (de) 1998-03-19

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Legal Events

Date Code Title Description
FZDE Discontinued