CA2739375C - Derivatives of 1-amino-2-cyclobutylethylboronic acid - Google Patents

Derivatives of 1-amino-2-cyclobutylethylboronic acid Download PDF

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Publication number
CA2739375C
CA2739375C CA2739375A CA2739375A CA2739375C CA 2739375 C CA2739375 C CA 2739375C CA 2739375 A CA2739375 A CA 2739375A CA 2739375 A CA2739375 A CA 2739375A CA 2739375 C CA2739375 C CA 2739375C
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Prior art keywords
amino
acid
boronic acid
compound
pharmaceutically acceptable
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CA2739375A
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English (en)
French (fr)
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CA2739375A1 (en
Inventor
Paul E. Fleming
Jing Li
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Millennium Pharmaceuticals Inc
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Millennium Pharmaceuticals Inc
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Publication of CA2739375A1 publication Critical patent/CA2739375A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
CA2739375A 2008-09-29 2009-09-25 Derivatives of 1-amino-2-cyclobutylethylboronic acid Active CA2739375C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US19461408P 2008-09-29 2008-09-29
US61/194,614 2008-09-29
PCT/US2009/005324 WO2010036357A1 (en) 2008-09-29 2009-09-25 Derivatives of 1-amino-2-cyclobutylethylboronic acid

Publications (2)

Publication Number Publication Date
CA2739375A1 CA2739375A1 (en) 2010-04-01
CA2739375C true CA2739375C (en) 2019-03-12

Family

ID=41426361

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2739375A Active CA2739375C (en) 2008-09-29 2009-09-25 Derivatives of 1-amino-2-cyclobutylethylboronic acid

Country Status (25)

Country Link
US (3) US8664200B2 (https=)
EP (1) EP2346882B1 (https=)
JP (3) JP5736314B2 (https=)
KR (1) KR101739470B1 (https=)
CN (2) CN102203103A (https=)
AR (1) AR075090A1 (https=)
AU (1) AU2009297113B2 (https=)
BR (1) BRPI0919447B8 (https=)
CA (1) CA2739375C (https=)
CL (1) CL2011000653A1 (https=)
CO (1) CO6362015A2 (https=)
CR (2) CR20160475A (https=)
DO (1) DOP2011000086A (https=)
EA (1) EA030539B1 (https=)
EC (1) ECSP11011011A (https=)
IL (1) IL211983A0 (https=)
MA (1) MA32729B1 (https=)
MX (1) MX2011003317A (https=)
MY (1) MY166653A (https=)
NZ (2) NZ606001A (https=)
SG (1) SG194388A1 (https=)
TW (2) TWI598352B (https=)
UA (1) UA105503C2 (https=)
WO (1) WO2010036357A1 (https=)
ZA (1) ZA201203615B (https=)

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Publication number Publication date
US10035811B2 (en) 2018-07-31
WO2010036357A1 (en) 2010-04-01
EP2346882B1 (en) 2017-09-20
CR20160475A (es) 2016-12-19
US20170349611A1 (en) 2017-12-07
US20100081633A1 (en) 2010-04-01
SG194388A1 (en) 2013-11-29
JP5736314B2 (ja) 2015-06-17
CN103554143B (zh) 2018-02-23
CR20110216A (es) 2011-07-14
BRPI0919447B8 (pt) 2021-05-25
JP2012504122A (ja) 2012-02-16
AR075090A1 (es) 2011-03-09
TW201641504A (zh) 2016-12-01
IL211983A0 (en) 2011-06-30
MY166653A (en) 2018-07-18
CN103554143A (zh) 2014-02-05
US9771381B2 (en) 2017-09-26
ZA201203615B (en) 2015-03-25
CN102203103A (zh) 2011-09-28
KR20110082534A (ko) 2011-07-19
JP2015143264A (ja) 2015-08-06
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US20140194387A1 (en) 2014-07-10
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TW201024313A (en) 2010-07-01
EA030539B1 (ru) 2018-08-31
AU2009297113B2 (en) 2016-11-10
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US8664200B2 (en) 2014-03-04
NZ606001A (en) 2014-08-29
AU2009297113A1 (en) 2010-04-01
EP2346882A1 (en) 2011-07-27
MA32729B1 (fr) 2011-10-02
UA105503C2 (uk) 2014-05-26
TWI598352B (zh) 2017-09-11
CA2739375A1 (en) 2010-04-01
MX2011003317A (es) 2011-04-26
ECSP11011011A (es) 2011-07-29
DOP2011000086A (es) 2011-04-15
CL2011000653A1 (es) 2011-09-30
CO6362015A2 (es) 2012-01-20
KR101739470B1 (ko) 2017-05-24
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JP2017025091A (ja) 2017-02-02

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