PE20120219A1 - Inhibidores de beta-secretasa - Google Patents

Inhibidores de beta-secretasa

Info

Publication number
PE20120219A1
PE20120219A1 PE2011001640A PE2011001640A PE20120219A1 PE 20120219 A1 PE20120219 A1 PE 20120219A1 PE 2011001640 A PE2011001640 A PE 2011001640A PE 2011001640 A PE2011001640 A PE 2011001640A PE 20120219 A1 PE20120219 A1 PE 20120219A1
Authority
PE
Peru
Prior art keywords
ring
beta
compounds
spyro
oxadiazol
Prior art date
Application number
PE2011001640A
Other languages
English (en)
Inventor
Salvacion Cacatian
David A Claremon
Lawrence W Dillard
Klaus Fuchs
Niklas Heine
Lanqi Jia
Katerina Leftheris
Brian Mckeever
Ramos Angel Morales
Suresh Singh
Shankar Venkatraman
Guosheng Wu
Zhongren Wu
Zhenrong Xu
Jing Yuan
Yajun Zheng
Original Assignee
Boehringer Ingelheim Int
Vitae Pharmaceuticals Inc
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 Boehringer Ingelheim Int, Vitae Pharmaceuticals Inc filed Critical Boehringer Ingelheim Int
Publication of PE20120219A1 publication Critical patent/PE20120219A1/es

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    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • 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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
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    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/10—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 carbon chain containing aromatic rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMUESTOS HETEROCICLICOS DE FORMULA (I) DONDE EL ANILLO HET ES UN HETEROCICLO DE 5 A 6 MIEMBROS; X ES O, -C(RaRb)-C(R3R4), -C(R3R4), ENTRE OTROS, EN DONDE Ra Y Rb SON CADA UNO H, HALOGENO, METOXI, ENTRE OTROS; R3 Y R4 SON CADA UNO H, CN, ALQUENILO(C2-C6), ENTRE OTROS; R0 ES H, =O, =S, ALQUILO(C1-C6), ENTRE OTROS; R1 ES H, OH, ALCOXI(C1-C4), ENTRE OTROS; R2 ES H, HALOGENO, CN, NO2, ENTRE OTROS; R8 Y R9 JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS FORMAN UN ANILLO (A) QUE ES UN ANILLO MONOCICLICO DE 3-14 MIEMBROS, UN ANILLO BICICLICO O POLICICLICO DE 9-14 MIEMBROS; p ES DE 1 A 4; q ES DE 1 A 3. SON COMPUESTOS PREFERIDOS: 3-(ESPIRO[ESPIRO[2,3-DIHIDRO-INDENO-2,2'-TETRAHIDRONAFTALENO]-1,5'-(3-AMINO-2-METIL-2H-[1,2,4]OXADIAZOL)]-6-IL)BENZONITRILO; 3-(ESPIRO[ESPIRO[2,3-DIHIDRO-INDENO-2,1'-(4-OXACICLOHEXANO)]-1,5'-(3-AMINO-2-METIL-2H-[1,2,4]OXADIAZOL)]-6-IL)BENZONITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA BETA-SECRETASA SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, DEMENCIA SENIL
PE2011001640A 2009-03-13 2010-03-12 Inhibidores de beta-secretasa PE20120219A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21014609P 2009-03-13 2009-03-13
US30754210P 2010-02-24 2010-02-24

Publications (1)

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PE20120219A1 true PE20120219A1 (es) 2012-03-19

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PE2011001640A PE20120219A1 (es) 2009-03-13 2010-03-12 Inhibidores de beta-secretasa

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US (3) US8633212B2 (es)
EP (2) EP2406240B1 (es)
JP (2) JP5731414B2 (es)
KR (2) KR20120001756A (es)
CN (1) CN102348698B (es)
AP (1) AP2866A (es)
AR (1) AR075854A1 (es)
AU (1) AU2010223937B2 (es)
BR (1) BRPI1009333B8 (es)
CA (1) CA2753730C (es)
CO (1) CO6450683A2 (es)
DK (1) DK2406240T3 (es)
EA (1) EA020875B1 (es)
EC (1) ECSP11011398A (es)
ES (1) ES2571057T3 (es)
GE (1) GEP20135964B (es)
IL (1) IL214226A (es)
MA (1) MA33240B1 (es)
MX (1) MX2011009571A (es)
NZ (1) NZ594230A (es)
PE (1) PE20120219A1 (es)
PT (1) PT2406240E (es)
SG (1) SG173466A1 (es)
TN (1) TN2011000400A1 (es)
TW (1) TWI464153B (es)
UY (1) UY32490A (es)
WO (1) WO2010105179A2 (es)
ZA (2) ZA201106002B (es)

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EP2324032B1 (en) * 2008-08-19 2014-10-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
KR20120001756A (ko) 2009-03-13 2012-01-04 비타이 파마슈티컬즈, 인코포레이티드 베타세크리타아제 저해제
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
EP2539322B1 (en) 2010-02-24 2014-01-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
US8415483B2 (en) * 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
WO2012109165A1 (en) 2011-02-07 2012-08-16 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
ES2566373T3 (es) 2011-10-10 2016-04-12 Astrazeneca Ab Inhibidores monofluoro beta-secretasa
TWI557112B (zh) * 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
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