CA2261835C - Long-acting drugs and pharmaceutical compositions comprising them - Google Patents

Long-acting drugs and pharmaceutical compositions comprising them Download PDF

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Publication number
CA2261835C
CA2261835C CA002261835A CA2261835A CA2261835C CA 2261835 C CA2261835 C CA 2261835C CA 002261835 A CA002261835 A CA 002261835A CA 2261835 A CA2261835 A CA 2261835A CA 2261835 C CA2261835 C CA 2261835C
Authority
CA
Canada
Prior art keywords
insulin
fmoc
radical
drug
compound according
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.)
Expired - Lifetime
Application number
CA002261835A
Other languages
English (en)
French (fr)
Other versions
CA2261835A1 (en
Inventor
Matityahu Fridkin
Yoram Shechter
Eytan Gershonov
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.)
Yeda Research and Development Co Ltd
Original Assignee
Yeda Research and Development Co Ltd
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 Yeda Research and Development Co Ltd filed Critical Yeda Research and Development Co Ltd
Publication of CA2261835A1 publication Critical patent/CA2261835A1/en
Application granted granted Critical
Publication of CA2261835C publication Critical patent/CA2261835C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/555Medicinal 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 an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • 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
    • A61K47/54Medicinal 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 an organic compound
    • 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02Local antiseptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CA002261835A 1996-08-07 1997-08-05 Long-acting drugs and pharmaceutical compositions comprising them Expired - Lifetime CA2261835C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IL11902996A IL119029A0 (en) 1996-08-07 1996-08-07 Long-acting drugs and pharamaceutical compositions comprising them
IL119029 1996-08-07
PCT/IL1997/000265 WO1998005361A2 (en) 1996-08-07 1997-08-05 Long-acting drugs and pharmaceutical compositions comprising them

Publications (2)

Publication Number Publication Date
CA2261835A1 CA2261835A1 (en) 1998-02-12
CA2261835C true CA2261835C (en) 2008-07-29

Family

ID=11069166

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002261835A Expired - Lifetime CA2261835C (en) 1996-08-07 1997-08-05 Long-acting drugs and pharmaceutical compositions comprising them

Country Status (18)

Country Link
US (1) US6504005B1 (2)
EP (1) EP1019089B1 (2)
JP (1) JP4416184B2 (2)
KR (1) KR20000029806A (2)
CN (1) CN1227501A (2)
AT (1) ATE308998T1 (2)
AU (1) AU725468B2 (2)
BR (1) BR9711045A (2)
CA (1) CA2261835C (2)
CZ (1) CZ36999A3 (2)
DE (1) DE69734607T2 (2)
DK (1) DK1019089T3 (2)
ES (1) ES2252787T3 (2)
HU (1) HUP0000809A2 (2)
IL (3) IL119029A0 (2)
NO (1) NO990518L (2)
NZ (1) NZ333845A (2)
WO (1) WO1998005361A2 (2)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL139400A0 (en) * 2000-11-01 2001-11-25 Yeda Res & Dev Long-acting cytokine derivatives and pharmaceutical compositions comprising them
US7259233B2 (en) * 2000-12-13 2007-08-21 Eli Lilly And Company Chronic treatment regimen using glucagon-like insulinotropic peptides
US6946137B2 (en) * 2001-10-19 2005-09-20 Idexx Laboratories, Inc. Methods for the controlled delivery of pharmacologically active compounds
ES2561108T3 (es) * 2001-10-19 2016-02-24 Idexx Laboratories, Inc. Composiciones inyectables para la liberación controlada de compuesto farmacológicamente activo
US20030171285A1 (en) * 2001-11-20 2003-09-11 Finn Rory F. Chemically-modified human growth hormone conjugates
BE1015608A6 (fr) * 2003-07-15 2005-06-07 Messadek Jallal Traitement des arterites.
JP4033382B2 (ja) * 2002-04-08 2008-01-16 久光製薬株式会社 インスリン投与装置
EP2259068B1 (en) * 2003-01-16 2013-08-14 caprotec bioanalytics GmbH Capture compounds and methods for analyzing the proteome
CA2521784C (en) 2003-04-08 2012-03-27 Yeda Research And Development Co. Ltd. Reversible pegylated drugs
DE602004003577T2 (de) * 2003-04-17 2007-09-20 Jallal Messadek Flottierende orale Formulierungen mit kontrollierter Freisetzung von Betain
MXPA06001283A (es) * 2003-08-05 2006-04-11 Novo Nordisk As Derivados de insulina novedosos.
BE1016128A6 (fr) * 2004-07-22 2006-03-07 Messadek Jallal Combinaisons therapeutiques
US7282487B2 (en) * 2004-10-28 2007-10-16 Idexx Laboratories Method for treating bacterial infections in horses or pigs with tilmicosin
WO2006050581A2 (en) * 2004-11-10 2006-05-18 Jallal Messadek Betaine as agent against arthropod - or mosquito -borne diseases
BRPI0610249A2 (pt) * 2005-04-27 2010-06-08 Jallal Messadek associação ou combinação farmacêutica, composição farmacêutica, processo de co-cristalização e o uso de insulina ou análogo de insulina
JP4808785B2 (ja) 2005-12-28 2011-11-02 ノボ・ノルデイスク・エー/エス インスリン組成物および組成物の製造方法
US9034818B2 (en) * 2007-06-13 2015-05-19 Novo Nordisk A/S Pharmaceutical formulations comprising an insulin derivative
WO2009065193A1 (en) * 2007-11-21 2009-05-28 Jallal Messadek Treatment of aspirin resistance with betaine and/or betaine enriched molasses
CN102037008B (zh) 2008-03-18 2016-08-31 诺沃-诺迪斯克有限公司 蛋白酶稳定化的、酰化胰岛素类似物
WO2009158668A1 (en) 2008-06-26 2009-12-30 Prolynx Llc Prodrugs and drug-macromolecule conjugates having controlled drug release rates
WO2010033220A2 (en) * 2008-09-19 2010-03-25 Nektar Therapeutics Modified therapeutics peptides, methods of their preparation and use
EP2341942A1 (en) 2008-09-19 2011-07-13 Nektar Therapeutics Polymer conjugates of therapeutic peptides
CA2740904C (en) * 2008-10-21 2019-01-15 Baxter International Inc. Methods for determining active ingredients in pro-drug peg protein conjugates with releasable peg reagents (in vitro de-pegylation)
AU2009309623B9 (en) * 2008-10-30 2014-10-02 Novo Nordisk A/S Treating diabetes melitus using insulin injections with less than daily injection frequency
EP2403537A1 (en) 2009-03-05 2012-01-11 Ascendis Pharma A/S Interferon alpha carrier prodrugs
WO2011013128A2 (en) 2009-07-31 2011-02-03 Yeda Research And Development Co. Ltd. Vectors for delivery of neurotherapeutics to the central nervous system
EP2566335B1 (en) * 2010-05-05 2016-06-29 Prolynx Llc Controlled release of active compounds from macromolecular conjugates
DK2632478T3 (da) 2010-10-27 2019-10-07 Novo Nordisk As Behandling af diabetes melitus under anvendelse af insulinindsprøjtninger indgivet med varierende indsprøjtningsintervaller
EP2490378B1 (en) 2011-02-18 2014-07-09 NTT DoCoMo, Inc. Apparatus and method for determining a control unit using feasibility requests and feasibility responses
CN104023739A (zh) 2011-06-02 2014-09-03 Opko生物科学有限公司 长效glp-1/胰高血糖素受体激动剂
US10166295B2 (en) 2011-06-02 2019-01-01 Opko Biologics Ltd. Pegylated OXM variants
US9481721B2 (en) 2012-04-11 2016-11-01 Novo Nordisk A/S Insulin formulations
MX362432B (es) 2012-06-04 2019-01-17 Opko Biologics Ltd Variantes de oxm pegilada.
US20150111820A1 (en) 2012-07-09 2015-04-23 Novo Nordisk A/S Novel use of insulin derivatives
JP2016519127A (ja) 2013-04-30 2016-06-30 ノヴォ ノルディスク アー/エス 新規投与レジメン
TWI700091B (zh) 2016-12-16 2020-08-01 丹麥商諾佛 儂迪克股份有限公司 含胰島素醫藥組成物
US10335464B1 (en) 2018-06-26 2019-07-02 Novo Nordisk A/S Device for titrating basal insulin
US12441776B2 (en) 2018-11-30 2025-10-14 Eirgen Pharma Ltd. Oxyntomodulin peptide analog formulations
EP3924369A1 (en) 2019-02-11 2021-12-22 OPKO Biologics Ltd. Long-acting glp-2 analogs
US12343383B2 (en) 2019-07-12 2025-07-01 Novo Nordisk A/S High concentration insulin formulation
CA3153644A1 (en) 2019-09-30 2021-04-08 Beijing Xuanyi Pharmasciences Co., Ltd. Protein-macromolecule conjugates and methods of use thereof
CN113773398B (zh) * 2020-06-10 2023-05-23 宁波鲲鹏生物科技有限公司 一种德谷胰岛素衍生物及其应用
CN117551008B (zh) * 2023-11-10 2025-10-17 沈阳药科大学 一种去铁胺偶联物及其制备方法和应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL194729C (nl) 1986-10-13 2003-01-07 Novartis Ag Werkwijze voor de bereiding van peptidealcoholen via vaste fase.
GB8717446D0 (en) 1987-07-23 1987-08-26 Merck Sharp & Dohme Chemical compounds
US6313094B1 (en) * 1990-12-11 2001-11-06 Japan Energy Corporation β-amino-α-hydroxycarboxylic acid derivatives and HIV protease inhibitors
JPH0687887A (ja) * 1992-08-19 1994-03-29 Upjohn Co:The ペプチドのエナミン誘導体およびそれをプロドラッグとして含有するペプチド製剤
EP0679658A4 (en) 1993-06-25 1997-06-04 Kyowa Hakko Kogyo Kk Endothelin-antagonizing peptide.
US5880131A (en) * 1993-10-20 1999-03-09 Enzon, Inc. High molecular weight polymer-based prodrugs
WO1995021622A1 (en) 1994-02-09 1995-08-17 Brigham & Women's Hospital Gel-forming polypeptide derivatives
DE4437604A1 (de) * 1994-10-21 1996-04-25 Basf Ag Konjugate aus einem Poly- oder Oligopeptid und einer niedermolekularen lipophilen Verbindung
WO1996030267A2 (en) * 1995-03-30 1996-10-03 Southpac Trust International, Inc. Self-erecting container which is collapsible to be substantially flat
US5688992A (en) * 1995-03-31 1997-11-18 The United States Of America As Represented By The Department Of Health And Human Services O-malonyltryrosyl compounds, O-malonyltryrosyl compound-containing peptides, and use thereof
US5846934A (en) * 1996-02-20 1998-12-08 American Cyanamid Company Pure somatostatin antagonist and methods of use thereof
US6057297A (en) * 1996-08-06 2000-05-02 Polifarma S.P.A. Inhibitor compounds of zinc-dependent metalloproteinases associated with pathological conditions, and therapeutic use thereof

Also Published As

Publication number Publication date
EP1019089B1 (en) 2005-11-09
CN1227501A (zh) 1999-09-01
KR20000029806A (ko) 2000-05-25
ES2252787T3 (es) 2006-05-16
CA2261835A1 (en) 1998-02-12
NZ333845A (en) 2000-09-29
NO990518D0 (no) 1999-02-04
NO990518L (no) 1999-04-06
AU3706097A (en) 1998-02-25
DK1019089T3 (da) 2006-03-13
CZ36999A3 (cs) 1999-07-14
EP1019089A2 (en) 2000-07-19
IL119029A0 (en) 1996-11-14
JP4416184B2 (ja) 2010-02-17
IL128274A (en) 2006-08-01
WO1998005361A2 (en) 1998-02-12
HUP0000809A2 (hu) 2000-11-28
BR9711045A (pt) 1999-08-17
IL128274A0 (en) 1999-11-30
DE69734607T2 (de) 2006-08-03
DE69734607D1 (de) 2005-12-15
US6504005B1 (en) 2003-01-07
WO1998005361A3 (en) 1998-06-18
ATE308998T1 (de) 2005-11-15
JP2000515542A (ja) 2000-11-21
AU725468B2 (en) 2000-10-12

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Effective date: 20170807