AR081369A1 - Compuestos de 2-5-6-7-tetrahidro-(1,4) oxazepin-3-ilamina o 2,3,6,7-tetrahidro-(1,4) oxazepin-5-ilamina, sus procesos de obtencion y composiciones farmaceuticas que los contienen - Google Patents

Compuestos de 2-5-6-7-tetrahidro-(1,4) oxazepin-3-ilamina o 2,3,6,7-tetrahidro-(1,4) oxazepin-5-ilamina, sus procesos de obtencion y composiciones farmaceuticas que los contienen

Info

Publication number
AR081369A1
AR081369A1 ARP110101549A ARP110101549A AR081369A1 AR 081369 A1 AR081369 A1 AR 081369A1 AR P110101549 A ARP110101549 A AR P110101549A AR P110101549 A ARP110101549 A AR P110101549A AR 081369 A1 AR081369 A1 AR 081369A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
group
cycloalkyl
hydrogen
Prior art date
Application number
ARP110101549A
Other languages
English (en)
Inventor
Hans Hilpert
Roland Humm
David Banner
Wolfgang Guba
Harald Mauser
Mark Rogers-Evans
Didier Rombach
Thomas Woltering
Wolfgang Wostl
Alexander V Mayweg
Eoin Power
Robert Narquizian
Original Assignee
Siena Biotech Spa
Hoffmann La Roche
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 Siena Biotech Spa, Hoffmann La Roche filed Critical Siena Biotech Spa
Publication of AR081369A1 publication Critical patent/AR081369A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (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)

Abstract

Estos compuestos son inhibidores de la BACE1 y/o de la BACE2 y pueden utilizarse como medicamentos para el tratamiento terapéutico y/o profiláctico de enfermedades tales como la enfermedad de Alzheimer, la diabetes, en particular la diabetes de tipo 2, y otros trastornos metabolicos. Reivindicacion 1: Compuestos de la formula en la que A es O y B es -CR8R9-; o B es O y A es -CR8R9; R1 se elige entre el grupo formado por hidrogeno, alquilo C1-7 y cicloalquilo C3-7; R2 se elige entre el grupo formado por hidrogeno, alquilo C1-7 y cicloalquilo C3-7; R3 se elige entre el grupo formado por hidrogeno, halogeno, alquilo C1-7 y cicloalquilo C3-7; R4 se elige entre el grupo formado por hidrogeno, halogeno, alquilo C1-7 y cicloalquilo C3-7; R5 es alquilo C1-7 o cicloalquilo C3-7; o R3 y R5 junto con el átomo de C al que están unidos forman un anillo ciclopropilo; R6a, R6b, R6c y R6d se eligen con independencia entre sí entre el grupo formado por hidrogeno, alquilo C1-7, halogeno y halogeno-alquilo C1-7; R7 es -(CO)-R10 o R11, en el que R10 se elige entre el grupo formado por: arilo, dicho arilo está sin sustituir o sustituido por uno, dos o tres grupos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano, hidroxi-alquilo C1-7, oxo y fenilo, heteroarilo, dicho heteroarilo está sin sustituir o sustituido por uno, dos o tres grupos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano, hidroxi-alquilo C1-7, oxo y fenilo, alquilo C1-7, halogeno-alquilo C1-7, cicloalquilo C3-7, dicho cicloalquilo está sin sustituir o sustituido por uno, dos, tres o cuatro grupos elegidos entre el grupo formado por alquilo C1-7, halogeno y halogeno-alquilo C1-7, y alcoxi C1-7-alquilo C1-7; R11se elige entre el grupo formado por alquilo C1-7, y cicloalquilo C3-7, dicho cicloalquilo está sin sustituir o sustituido por uno, dos, tres o cuatro grupos elegidos entre el grupo formado por alquilo C1-7, halogeno y halogeno-alquilo C1-7, R8 y R9 con independencia entre sí se eligen entre hidrogeno, alquilo C1-7 y cicloalquilo C3-7 o sus sales farmacéuticamente aceptables.
ARP110101549A 2010-05-07 2011-05-05 Compuestos de 2-5-6-7-tetrahidro-(1,4) oxazepin-3-ilamina o 2,3,6,7-tetrahidro-(1,4) oxazepin-5-ilamina, sus procesos de obtencion y composiciones farmaceuticas que los contienen AR081369A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10162340 2010-05-07

Publications (1)

Publication Number Publication Date
AR081369A1 true AR081369A1 (es) 2012-08-29

Family

ID=44168838

Family Applications (1)

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ARP110101549A AR081369A1 (es) 2010-05-07 2011-05-05 Compuestos de 2-5-6-7-tetrahidro-(1,4) oxazepin-3-ilamina o 2,3,6,7-tetrahidro-(1,4) oxazepin-5-ilamina, sus procesos de obtencion y composiciones farmaceuticas que los contienen

Country Status (14)

Country Link
US (2) US8673894B2 (es)
EP (1) EP2566855B1 (es)
JP (1) JP5823503B2 (es)
KR (1) KR20130100241A (es)
CN (1) CN102958922B (es)
AR (1) AR081369A1 (es)
BR (1) BR112012028519A2 (es)
CA (1) CA2797622A1 (es)
ES (1) ES2481409T3 (es)
HK (1) HK1179617A1 (es)
MX (1) MX2012012952A (es)
RU (1) RU2570796C2 (es)
TW (1) TW201144302A (es)
WO (1) WO2011138293A1 (es)

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JPWO2012147763A1 (ja) 2011-04-26 2014-07-28 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
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TW201144302A (en) 2011-12-16
US20140045820A1 (en) 2014-02-13
CN102958922B (zh) 2015-09-30
CA2797622A1 (en) 2011-11-10
KR20130100241A (ko) 2013-09-10
RU2570796C2 (ru) 2015-12-10
CN102958922A (zh) 2013-03-06
JP5823503B2 (ja) 2015-11-25
HK1179617A1 (en) 2013-10-04
EP2566855B1 (en) 2014-05-21
JP2013525506A (ja) 2013-06-20
EP2566855A1 (en) 2013-03-13
WO2011138293A1 (en) 2011-11-10
ES2481409T3 (es) 2014-07-30
US20110312937A1 (en) 2011-12-22
US8673894B2 (en) 2014-03-18
RU2012148818A (ru) 2014-06-20
BR112012028519A2 (pt) 2016-07-19
MX2012012952A (es) 2012-12-17

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