CR20130339A - Nuevos derivados heterocíclicos y su uso en el tratamiento de desordenes neurológicos - Google Patents

Nuevos derivados heterocíclicos y su uso en el tratamiento de desordenes neurológicos

Info

Publication number
CR20130339A
CR20130339A CR20130339A CR20130339A CR20130339A CR 20130339 A CR20130339 A CR 20130339A CR 20130339 A CR20130339 A CR 20130339A CR 20130339 A CR20130339 A CR 20130339A CR 20130339 A CR20130339 A CR 20130339A
Authority
CR
Costa Rica
Prior art keywords
treatment
neurological disorders
heterocyclic derivatives
new heterocyclic
new
Prior art date
Application number
CR20130339A
Other languages
English (en)
Inventor
Sangamesh Badiger
Murali Chebrolu
Konstanze Hurth
Sébastien Jacquier
Rainer Martin Lueoend
Rainer Machauer
Heinrich Rueeger
Marina Tintelnot-Blomley
Siem Jacob Veenstra
Markus Voegtle
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46491227&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CR20130339(A) "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 CR20130339A publication Critical patent/CR20130339A/es

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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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds

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

Abstract

LA PRESENTE INVENCIÓN SE REFIERE A COMPUESTOS HETEROCÍCLICOS NOVEDOSOS DE LA FÓRMULA (I), EN LA CUAL TODAS LAS VARIABLES SON COMO SE DEFINEN EN LA ESPECIFICACIÓN, COMPOSICIONES FARMACÉUTICAS DE LOS MISMO, COMBINACIONES DE LOS MISMOS, Y SU USO COMO MEDICAMENTOS, PARTICULARMENTE PARA EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER Ó LA DIABETES MEDIANTE LA INHIBICIÓN DE LA BACE-1 Ó BACE-2.-
CR20130339A 2011-01-13 2013-07-10 Nuevos derivados heterocíclicos y su uso en el tratamiento de desordenes neurológicos CR20130339A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN77DE2011 2011-01-13
US201161534591P 2011-09-14 2011-09-14

Publications (1)

Publication Number Publication Date
CR20130339A true CR20130339A (es) 2013-09-04

Family

ID=46491227

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20130339A CR20130339A (es) 2011-01-13 2013-07-10 Nuevos derivados heterocíclicos y su uso en el tratamiento de desordenes neurológicos

Country Status (40)

Country Link
US (6) US8637508B2 (es)
EP (1) EP2663561B1 (es)
JP (1) JP5715710B2 (es)
KR (1) KR101569260B1 (es)
CN (2) CN103403001B (es)
AP (1) AP3807A (es)
AR (1) AR084849A1 (es)
AU (1) AU2012206561B2 (es)
CA (1) CA2824220C (es)
CL (2) CL2013001964A1 (es)
CO (1) CO6751293A2 (es)
CR (1) CR20130339A (es)
CU (1) CU20130101A7 (es)
CY (1) CY1117580T1 (es)
DK (1) DK2663561T3 (es)
EA (1) EA024059B1 (es)
ES (1) ES2576182T3 (es)
GT (1) GT201300179A (es)
HR (1) HRP20160647T1 (es)
HU (1) HUE029226T2 (es)
IL (1) IL227294A (es)
JO (1) JO3146B1 (es)
MA (1) MA34898B1 (es)
ME (1) ME02409B (es)
MX (1) MX336966B (es)
MY (1) MY162413A (es)
PE (1) PE20141110A1 (es)
PH (1) PH12013501480A1 (es)
PL (1) PL2663561T3 (es)
PT (1) PT2663561E (es)
RS (1) RS54782B1 (es)
SG (1) SG191812A1 (es)
SI (1) SI2663561T1 (es)
SM (1) SMT201600144B (es)
TN (1) TN2013000285A1 (es)
TW (1) TWI531570B (es)
UA (1) UA113051C2 (es)
UY (1) UY33865A (es)
WO (1) WO2012095469A1 (es)
ZA (1) ZA201304921B (es)

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