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AR079327A1 - Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida - Google Patents

Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida

Info

Publication number
AR079327A1
AR079327A1 ARP100104535A ARP100104535A AR079327A1 AR 079327 A1 AR079327 A1 AR 079327A1 AR P100104535 A ARP100104535 A AR P100104535A AR P100104535 A ARP100104535 A AR P100104535A AR 079327 A1 AR079327 A1 AR 079327A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
halogen
cyano
alkoxy
lower alkoxy
Prior art date
Application number
ARP100104535A
Other languages
English (en)
Inventor
Harald Mauser
Alexander V Mayweg
Robert Narquizian
Emmanuel Pinard
Eoin Power
Mark Rogers-Evans
Thomas Woltering
David Banner
Wolfgang Guba
Wolfgang Wostl
Hans Hilpert
Original Assignee
Hoffmann La Roche
Siena Biotech Spa
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43585547&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR079327(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche, Siena Biotech Spa filed Critical Hoffmann La Roche
Publication of AR079327A1 publication Critical patent/AR079327A1/es

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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
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    • 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)
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  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
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  • Cardiology (AREA)
  • Endocrinology (AREA)
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  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Emergency 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)

Abstract

Compuestos derivados que tienen actividad inhibidora de la BACE 1 y/o de la BACE2, a su obtencion, a composiciones farmacéuticas que los contienen y a su utilizacion como sustancias terapéuticamente activas. Los compuestos activos de la presente son utiles para el tratamiento terapéutico y/o profiláctico p.ej. de la enfermedad de Alzheimer y de la diabetes de tipo 2. Reivindicacion 1: Un compuesto de la formula 1, en la que R1 se elige entre el grupo formado por arilo, arilo sustituido por 1-4 sustituyentes elegidos individualmente entre ciano, ciano-alquilo inferior, halogeno, halogeno-alcoxi inferior, halogeno-alquilo inferior, alcoxi inferior, alcoxi inferior-alquilo inferior y alquilo inferior, heteroarilo y heteroarilo sustituido por 1-4 sustituyentes elegidos individualmente entre amido, ciano, ciano-alquilo inferior, cicloalquilo, cicloalquilalquenilo inferior, cicloalquil-alquinilo inferior, cicloalquil-alquilo inferior, cicloalquil-alcoxi inferior, halogeno, halogeno-alcoxi inferior, halogeno-alquilo inferior, alcoxi inferior, alcoxi inferior-alquilo inferior, alquenilo inferior, alquinilo inferior, alquilo inferior y nitro; alquilo inferior, alquilo inferior sustituido por 1-5 sustituyentes elegidos individualmente entre ciano, halogeno, hidroxi y alcoxi inferior; alquenilo inferior, alquenilo inferior sustituido por 1-4 sustituyentes elegidos individualmente entre ciano, ciano-alquilo inferior, halogeno, halogeno-alcoxi inferior, halogeno-alquilo inferior, heteroarilo, alcoxi inferior, alcoxi inferior-alquilo inferior y alquilo inferior, cicloalquilo, cicloalquilo sustituido por 1-4 sustituyentes elegidos individualmente entre ciano, ciano-alquilo inferior, halogeno, halogeno-alcoxi inferior, halogeno-alquilo inferior, alcoxi inferior, alcoxi inferior-alquilo inferior y alquilo inferior, R2 se elige entre el grupo formado por hidrogeno, halogeno y alquilo inferior; R3 es alquilo inferior; R4 se elige entre el grupo formado por hidrogeno y alquilo inferior; R5 se elige entre el grupo formado por hidrogeno y alquilo inferior; n es el numero 0, 1 o 2; o sus sales farmacéuticamente aceptables.
ARP100104535A 2009-12-11 2010-12-09 Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida AR079327A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09178983 2009-12-11

Publications (1)

Publication Number Publication Date
AR079327A1 true AR079327A1 (es) 2012-01-18

Family

ID=43585547

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104535A AR079327A1 (es) 2009-12-11 2010-12-09 Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida

Country Status (26)

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

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