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PE20141540A1 - Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2 - Google Patents

Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2

Info

Publication number
PE20141540A1
PE20141540A1 PE2014000256A PE2014000256A PE20141540A1 PE 20141540 A1 PE20141540 A1 PE 20141540A1 PE 2014000256 A PE2014000256 A PE 2014000256A PE 2014000256 A PE2014000256 A PE 2014000256A PE 20141540 A1 PE20141540 A1 PE 20141540A1
Authority
PE
Peru
Prior art keywords
pyridin
amino
bace
alkyl
difluoro
Prior art date
Application number
PE2014000256A
Other languages
English (en)
Inventor
Rainer Martin Lueoend
Rainer Machauer
Heinrich Rueeger
Siem Jacob Veenstra
Original Assignee
Novartis Ag
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=47018309&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20141540(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20141540A1 publication Critical patent/PE20141540A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE: R1 Y R2 SON INDEPENDIENTEMENTE H O HALOGENO; R3 Y R4 SON INDEPENDIENTEMENTE H O ALQUILO C1-3, O R3 Y R4 TOMADOS JUNTOS SON CICLOPROPILO, O R1 Y R4 SON H Y R2 Y R3 TOMADOS JUNTOS SON -CH2-O-CH2; R5 ES ALQUILO C1-3, HALO-ALQUILO C1-3 O ALCOXILO C1-3-ALQUILO C1-3; R6 ES FENILO O UN HETEROARILO MONOCICLICO DE 5 O 6 MIEMBROS QUE COMPRENDE 1,2,3 O 4 HETEROATOMOS SELECCIONADOS INDEPENDIENTEMENTE DE N, O Y S, EN DONDE EL FENILO O HETEROARILO ESTA OPCIONALMENTE SUSTITUIDO. SON COMPUESTOS PREFERIDOS: [6-((R)-2-AMINO-5,5-DIFLUORO-4-METIL-5,6-DIHIDRO-4H-[1,3]OXAZIN-4-IL)-5-FLUORO-PIRIDIN-2-IL]-AMIDA DEL ACIDO 5-CIANO-3-METIL-PIRIDIN-2-CARBOXILICO; [6-((R)-2-AMINO-5,5-DIFLUORO-4-METIL-5,6-DIHIDRO-4H-[1,3]OXAZIN-4-IL)-5-FLUORO-PIRIDIN-2-IL]-AMIDA DEL ACIDO 3-AMINO-5-(1,1-DIFLUORO-ETIL)-PIRAZIN-2-CARBOXILICO; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UNA COMBINACION. DICHOS COMPUESTOS SON UTILES PARA EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER O DIABETES
PE2014000256A 2011-08-25 2012-08-23 Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2 PE20141540A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161527172P 2011-08-25 2011-08-25
US201261665395P 2012-06-28 2012-06-28

Publications (1)

Publication Number Publication Date
PE20141540A1 true PE20141540A1 (es) 2014-10-31

Family

ID=47018309

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000256A PE20141540A1 (es) 2011-08-25 2012-08-23 Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2

Country Status (28)

Country Link
US (2) US9163011B2 (es)
EP (2) EP3023423B1 (es)
JP (1) JP5816369B2 (es)
KR (1) KR101601571B1 (es)
CN (1) CN103906748B (es)
AP (1) AP2014007507A0 (es)
AR (1) AR087668A1 (es)
AU (1) AU2012298177B2 (es)
BR (1) BR112014004131A2 (es)
CA (1) CA2845093A1 (es)
CL (1) CL2014000458A1 (es)
CO (1) CO6890097A2 (es)
CR (1) CR20140084A (es)
EA (1) EA024580B1 (es)
ES (2) ES2638832T3 (es)
GT (1) GT201400031A (es)
IL (1) IL230975A0 (es)
MA (1) MA35356B1 (es)
MX (1) MX339303B (es)
PE (1) PE20141540A1 (es)
PH (1) PH12014500356A1 (es)
PL (1) PL2748162T3 (es)
SG (1) SG2014012108A (es)
TN (1) TN2014000062A1 (es)
TW (1) TW201313706A (es)
UY (1) UY34278A (es)
WO (1) WO2013027188A1 (es)
ZA (1) ZA201401139B (es)

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MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
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Also Published As

Publication number Publication date
EA024580B1 (ru) 2016-09-30
ES2638832T3 (es) 2017-10-24
US20150150877A1 (en) 2015-06-04
MX2014002230A (es) 2014-04-25
JP2014524463A (ja) 2014-09-22
IL230975A0 (en) 2014-03-31
NZ621093A (en) 2015-05-29
TW201313706A (zh) 2013-04-01
EP3023423B1 (en) 2017-05-31
AP2014007507A0 (en) 2014-03-31
CO6890097A2 (es) 2014-03-10
MX339303B (es) 2016-05-19
AR087668A1 (es) 2014-04-09
BR112014004131A2 (pt) 2017-06-13
EP2748162B1 (en) 2015-12-16
EP2748162A1 (en) 2014-07-02
PL2748162T3 (pl) 2016-06-30
ES2565229T3 (es) 2016-04-01
AU2012298177A1 (en) 2014-03-06
UY34278A (es) 2013-04-05
US9163011B2 (en) 2015-10-20
MA35356B1 (fr) 2014-08-01
CN103906748A (zh) 2014-07-02
US20130172331A1 (en) 2013-07-04
PH12014500356A1 (en) 2014-04-07
AU2012298177B2 (en) 2015-10-29
EP3023423A1 (en) 2016-05-25
JP5816369B2 (ja) 2015-11-18
CL2014000458A1 (es) 2014-09-05
WO2013027188A1 (en) 2013-02-28
TN2014000062A1 (en) 2015-07-01
EA201490491A1 (ru) 2014-06-30
KR101601571B1 (ko) 2016-03-08
CN103906748B (zh) 2017-06-16
SG2014012108A (en) 2014-05-29
ZA201401139B (en) 2014-12-23
CA2845093A1 (en) 2013-02-28
CR20140084A (es) 2014-05-02
GT201400031A (es) 2015-02-19
HK1195903A1 (en) 2014-11-28
KR20140054313A (ko) 2014-05-08

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