EA201201482A1 - SELECTIVE INTEGRINE INHIBITORS - Google Patents

SELECTIVE INTEGRINE INHIBITORS

Info

Publication number
EA201201482A1
EA201201482A1 EA201201482A EA201201482A EA201201482A1 EA 201201482 A1 EA201201482 A1 EA 201201482A1 EA 201201482 A EA201201482 A EA 201201482A EA 201201482 A EA201201482 A EA 201201482A EA 201201482 A1 EA201201482 A1 EA 201201482A1
Authority
EA
Eurasian Patent Office
Prior art keywords
integrine
inhibitors
selective
methods
selectively
Prior art date
Application number
EA201201482A
Other languages
Russian (ru)
Inventor
Энтони Пепио
Гордон Фрэнсис
Теодор А. Йеднок
Алисса Чекериан
Брайан Тодд Уипк
Original Assignee
Элан Фармасьютикалз, Инк.
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 Элан Фармасьютикалз, Инк. filed Critical Элан Фармасьютикалз, Инк.
Publication of EA201201482A1 publication Critical patent/EA201201482A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/56—Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Это изобретение предусматривает способы для селективного антагонизирования гетеродимера интегрина α4β1 у субъекта, который в этом нуждается, а предпочтительно - у человека. Способы этого изобретения используют конъюгаты, включающие два или более мелкомолекулярных антагонистов α4β1, ковалентно присоединенных к биосовместимому полимеру. Эти способы селективного ингибирования α4β1 могут быть использованы для модулирования как нормальных, так и патологических биологических процессов, опосредованных, по меньшей мере, частично активностью α4β1.This invention provides methods for selectively antagonizing the α4β1 integrin heterodimer in a subject that needs it, and preferably in humans. The methods of this invention use conjugates comprising two or more small molecule α4β1 antagonists covalently attached to a biocompatible polymer. These methods of selectively inhibiting α4β1 can be used to modulate both normal and pathological biological processes mediated, at least in part, by α4β1 activity.

EA201201482A 2010-04-30 2011-05-02 SELECTIVE INTEGRINE INHIBITORS EA201201482A1 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US33012210P 2010-04-30 2010-04-30
US39228810P 2010-10-12 2010-10-12
US201161516846P 2011-04-08 2011-04-08
PCT/US2011/034721 WO2011137418A1 (en) 2010-04-30 2011-05-02 Selective integrin inhibitors

Publications (1)

Publication Number Publication Date
EA201201482A1 true EA201201482A1 (en) 2013-03-29

Family

ID=44260795

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201201482A EA201201482A1 (en) 2010-04-30 2011-05-02 SELECTIVE INTEGRINE INHIBITORS

Country Status (8)

Country Link
EP (1) EP2563405A1 (en)
JP (1) JP2013525435A (en)
KR (1) KR20130081651A (en)
CN (1) CN102883750A (en)
AU (1) AU2011245140A1 (en)
CA (1) CA2797974A1 (en)
EA (1) EA201201482A1 (en)
WO (1) WO2011137418A1 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2632492B1 (en) * 2010-10-25 2017-10-04 Biogen MA Inc. METHODS FOR DETERMINING DIFFERENCES IN ALPHA-4 INTEGRIN ACTIVITY BY CORRELATING DIFFERENCES IN sVCAM AND/OR sMAdCAM LEVELS
US20180206726A1 (en) 2016-12-07 2018-07-26 Progenity Inc. Gastrointestinal tract detection methods, devices and systems
US20200253506A1 (en) 2016-12-14 2020-08-13 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an integrin inhibitor
WO2019246455A1 (en) 2018-06-20 2019-12-26 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an integrin inhibitor
WO2020106704A2 (en) 2018-11-19 2020-05-28 Progenity, Inc. Ingestible device for delivery of therapeutic agent to the gastrointestinal tract
WO2021119482A1 (en) 2019-12-13 2021-06-17 Progenity, Inc. Ingestible device for delivery of therapeutic agent to the gastrointestinal tract

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1765412A2 (en) * 2004-07-08 2007-03-28 Elan Pharmaceuticals, Inc. Multivalent vla-4 antagonists comprising polyethylene glycol moieties
WO2006127584A1 (en) 2005-05-20 2006-11-30 Elan Pharmaceuticals, Inc. Imidazolone phenylalanine derivatives as vla-4 antagonists
SG196786A1 (en) * 2005-07-08 2014-02-13 Elan Pharm Inc Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds
US8138272B2 (en) 2006-05-22 2012-03-20 Elan Pharmaceuticals, Inc. Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds
EP2231185A4 (en) * 2007-12-07 2012-06-27 Elan Pharm Inc Methods and compositions for treating liquid tumors

Also Published As

Publication number Publication date
CN102883750A (en) 2013-01-16
WO2011137418A1 (en) 2011-11-03
KR20130081651A (en) 2013-07-17
EP2563405A1 (en) 2013-03-06
AU2011245140A1 (en) 2012-12-20
CA2797974A1 (en) 2011-11-03
JP2013525435A (en) 2013-06-20

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