AU2010330031B2 - 2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE 1 and/or BACE 2 inhibitors - Google Patents

2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE 1 and/or BACE 2 inhibitors Download PDF

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Publication number
AU2010330031B2
AU2010330031B2 AU2010330031A AU2010330031A AU2010330031B2 AU 2010330031 B2 AU2010330031 B2 AU 2010330031B2 AU 2010330031 A AU2010330031 A AU 2010330031A AU 2010330031 A AU2010330031 A AU 2010330031A AU 2010330031 B2 AU2010330031 B2 AU 2010330031B2
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Australia
Prior art keywords
difluoro
dihydro
amino
oxazin
methyl
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Ceased
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AU2010330031A
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AU2010330031A1 (en
Inventor
David Banner
Wolfgang Guba
Hans Hilpert
Harald Mauser
Alexander V. Mayweg
Robert Narquizian
Emmanuel Pinard
Eoin Power
Mark Rogers-Evans
Thomas Woltering
Wolfgang Wostl
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F Hoffmann La Roche AG
Siena Biotech SpA
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F Hoffmann La Roche AG
Siena Biotech SpA
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Application filed by F Hoffmann La Roche AG, Siena Biotech SpA filed Critical F Hoffmann La Roche AG
Publication of AU2010330031A1 publication Critical patent/AU2010330031A1/en
Priority to AU2013202820A priority Critical patent/AU2013202820A1/en
Application granted granted Critical
Publication of AU2010330031B2 publication Critical patent/AU2010330031B2/en
Ceased legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2010330031A 2009-12-11 2010-12-06 2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE 1 and/or BACE 2 inhibitors Ceased AU2010330031B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2013202820A AU2013202820A1 (en) 2009-12-11 2013-04-08 2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE 1 and/or BACE 2 inhibitors

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09178983.4 2009-12-11
EP09178983 2009-12-11
PCT/EP2010/068912 WO2011069934A1 (en) 2009-12-11 2010-12-06 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2013202820A Division AU2013202820A1 (en) 2009-12-11 2013-04-08 2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE 1 and/or BACE 2 inhibitors

Publications (2)

Publication Number Publication Date
AU2010330031A1 AU2010330031A1 (en) 2012-06-07
AU2010330031B2 true AU2010330031B2 (en) 2013-06-20

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AU2010330031A Ceased AU2010330031B2 (en) 2009-12-11 2010-12-06 2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE 1 and/or BACE 2 inhibitors

Country Status (26)

Country Link
US (1) US8389513B2 (cg-RX-API-DMAC7.html)
EP (1) EP2509965A1 (cg-RX-API-DMAC7.html)
JP (1) JP5584778B2 (cg-RX-API-DMAC7.html)
KR (1) KR101506773B1 (cg-RX-API-DMAC7.html)
CN (1) CN102712609A (cg-RX-API-DMAC7.html)
AR (1) AR079327A1 (cg-RX-API-DMAC7.html)
AU (1) AU2010330031B2 (cg-RX-API-DMAC7.html)
BR (1) BR112012013175A2 (cg-RX-API-DMAC7.html)
CA (1) CA2776727C (cg-RX-API-DMAC7.html)
CL (1) CL2012001464A1 (cg-RX-API-DMAC7.html)
CO (1) CO6541656A2 (cg-RX-API-DMAC7.html)
CR (1) CR20120262A (cg-RX-API-DMAC7.html)
EC (1) ECSP12011961A (cg-RX-API-DMAC7.html)
IL (1) IL219107A (cg-RX-API-DMAC7.html)
IN (1) IN2012DN03043A (cg-RX-API-DMAC7.html)
MA (1) MA34779B1 (cg-RX-API-DMAC7.html)
MX (1) MX2012006493A (cg-RX-API-DMAC7.html)
MY (1) MY169962A (cg-RX-API-DMAC7.html)
NZ (1) NZ599008A (cg-RX-API-DMAC7.html)
PE (1) PE20121500A1 (cg-RX-API-DMAC7.html)
PH (1) PH12012500619A1 (cg-RX-API-DMAC7.html)
RU (1) RU2515221C2 (cg-RX-API-DMAC7.html)
SG (1) SG181610A1 (cg-RX-API-DMAC7.html)
TW (1) TWI487704B (cg-RX-API-DMAC7.html)
UA (1) UA103272C2 (cg-RX-API-DMAC7.html)
WO (1) WO2011069934A1 (cg-RX-API-DMAC7.html)

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