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PE20070645A1 - HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS - Google Patents

HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS

Info

Publication number
PE20070645A1
PE20070645A1 PE2006001476A PE2006001476A PE20070645A1 PE 20070645 A1 PE20070645 A1 PE 20070645A1 PE 2006001476 A PE2006001476 A PE 2006001476A PE 2006001476 A PE2006001476 A PE 2006001476A PE 20070645 A1 PE20070645 A1 PE 20070645A1
Authority
PE
Peru
Prior art keywords
beta
acetamide
tetrahydro
alkenyl
amino
Prior art date
Application number
PE2006001476A
Other languages
Spanish (es)
Inventor
Wenge Zhong
Stephen Hitchcock
Brian K Albrecht
Michael Bartberger
James Brown
Ryan Brown
Stuart Charles Chaffee
Yuan Cheng
Michael Croghan
Russell Graceffa
Scott Harried
Dean Hickman
Daniel Horne
Randall W Hungate
Ted Judd
Matthew Kaller
Charles Kreiman
Daniel La
Patricia Lopez
Craig E Masse
Holger Monenschein
Thomas Nguyen
Thomas Nixey
Vinod F Patel
Lewis Pennigton
Matthew Weiss
Qiufen Xue
Bryant Yang
Original Assignee
Amgen 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39708735&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20070645(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of PE20070645A1 publication Critical patent/PE20070645A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/68Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
    • 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE A ES ALQUILO(C1-C10), ALQUENILO(C2-C10), ALQUINILO(C2-C10), ENTRE OTROS; W ES -C(=O)-, -OC(=O)-, -NHC(=O)-, ENTRE OTROS; B ES R2-(CR2aR2a)h-, R2-O-(CR2aR2a)h, ENTRE OTROS, DONDE R2 ES ALQUILO(C1-C10), HALOALQUILO(C1-C10), ALQUENILO(C2-C10), ENTRE OTROS; R2a ES H, OH, NO2, CN, ENTRE OTROS; h ES DE 0 A 3; i ES DE 1 A 3; j ES DE 0 A 2; R3 ES H, CN, ALQUILO(C1-C10), ENTRE OTROS; R4 ES H, CN, ALQUENILO(C2-C10), ENTRE OTROS; R5 ES UN COMPUESTO DE FORMULA (a), (b), (c), ENTRE OTROS; DONDE X1 ES CR12, O, S O NR12; X2 ES CR12R12; Y1, Y2 E Y3 SON CADA UNO CR12R12, O, S O NR12; m ES DE 0 A 2; o ES DE 0 A 5; R10 ES H, HALO, CN, OH, ENTRE OTROS; R12 ES H, HALO, NH2, NO2, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-((1S,2R)-2-HIDROXI-1-(FENILMETIL)-3-(((4S)-2,6,6-TRIMETIL-4,5,6,7-TETRAHIDRO-1-BENZOFURAN-4-IL)AMINO)PROPIL)ACETAMIDA, N-((1S,2R)-3-(((4S)-2-ETIL-6,6-DIMETIL-4,5,6,7-TETRAHIDRO-1-BENZOTIEN-4-IL)AMINO)-2-HIDROXI-1-(FENILMETIL)PROPIL)-2-(2-OXO-1-PIRROLIDINIL)ACETAMIDA, N-((1S,2R)-1-((3-CIANOFENIL)METIL)-3-(((1R)-3,3-DIMETIL-7-(METILOXI)-4-OXO-1,2,3,4-TETRAHIDRO-1-NAFTALENIL)AMINO)-2-HIDROXIPROPIL)-2-(METILOXI)ACETAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON MODULADORES DE LA ENZIMA BETA-SECRETASA SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMERREFERS TO COMPOUNDS OF FORMULA (I) WHERE A IS ALKYL (C1-C10), ALKENYL (C2-C10), ALKINYL (C2-C10), AMONG OTHERS; W IS -C (= O) -, -OC (= O) -, -NHC (= O) -, AMONG OTHERS; B IS R2- (CR2aR2a) h-, R2-O- (CR2aR2a) h, AMONG OTHERS, WHERE R2 IS ALKYL (C1-C10), HALOALKYL (C1-C10), ALKENYL (C2-C10), AMONG OTHERS; R2a IS H, OH, NO2, CN, AMONG OTHERS; h IS 0 TO 3; i IS FROM 1 TO 3; j IS FROM 0 TO 2; R3 IS H, CN, (C1-C10) ALKYL, AMONG OTHERS; R4 IS H, CN, ALKENYL (C2-C10), AMONG OTHERS; R5 IS A COMPOUND OF FORMULA (a), (b), (c), AMONG OTHERS; WHERE X1 IS CR12, O, S OR NR12; X2 IS CR12R12; Y1, Y2 AND Y3 ARE EACH CR12R12, O, S OR NR12; m IS 0 TO 2; o IS FROM 0 TO 5; R10 IS H, HALO, CN, OH, AMONG OTHERS; R12 IS H, HALO, NH2, NO2, AMONG OTHERS. THE PREFERRED COMPOUNDS ARE: N - ((1S, 2R) -2-HYDROXY-1- (PHENYLMETHYL) -3 - (((4S) -2,6,6-TRIMETHYL-4,5,6,7-TETRAHYDRO-1 -BENZOFURAN-4-IL) AMINO) PROPYL) ACETAMIDE, N - ((1S, 2R) -3 - (((4S) -2-ETHYL-6,6-DIMETHYL-4,5,6,7-TETRAHYDRO- 1-BENZOTHEN-4-IL) AMINO) -2-HYDROXY-1- (PHENYLMETHYL) PROPYL) -2- (2-OXO-1-PYRROLIDINYL) ACETAMIDE, N - ((1S, 2R) -1 - ((3 -CYANOPHENYL) METHYL) -3 - (((1R) -3,3-DIMETHYL-7- (METHYLOXY) -4-OXO-1,2,3,4-TETRAHYDRO-1-NAPHTHALENYL) AMINO) -2-HYDROXYPROPIL ) -2- (METHYLOXY) ACETAMIDE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCEDURE. SUCH COMPOUNDS ARE MODULATORS OF THE BETA-SECRETASE ENZYME, BEING USEFUL IN THE TREATMENT OF ALZHEIMER'S DISEASE

PE2006001476A 2005-11-21 2006-11-20 HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS PE20070645A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73910805P 2005-11-21 2005-11-21
US85482406P 2006-10-27 2006-10-27

Publications (1)

Publication Number Publication Date
PE20070645A1 true PE20070645A1 (en) 2007-08-24

Family

ID=39708735

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001476A PE20070645A1 (en) 2005-11-21 2006-11-20 HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS

Country Status (8)

Country Link
EP (1) EP1971598A1 (en)
JP (1) JP5274258B2 (en)
AR (1) AR057985A1 (en)
AU (1) AU2006316620B2 (en)
CA (1) CA2629402C (en)
PE (1) PE20070645A1 (en)
TW (1) TW200800966A (en)
WO (1) WO2007061670A1 (en)

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TW200901991A (en) * 2007-05-25 2009-01-16 Amgen Inc Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
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US8946483B2 (en) 2011-07-21 2015-02-03 Ge Healthcare Limited Precursor compounds and methods for making same
BR112014023384A8 (en) * 2012-03-20 2018-01-16 R Artis Dean spirocyclic bace inhibitors of dihydro-thiazine and dihydro-oxazine, and compositions and uses thereof.
EP3170820B1 (en) 2014-07-16 2019-02-20 Japan Science and Technology Agency Benzothiazole compound and medicine containing same
JP7413346B2 (en) 2019-03-06 2024-01-15 第一三共株式会社 Pyrrolopyrazole derivative

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Also Published As

Publication number Publication date
AU2006316620A1 (en) 2007-05-31
CA2629402A1 (en) 2007-05-31
CA2629402C (en) 2011-07-26
AR057985A1 (en) 2008-01-09
AU2006316620B2 (en) 2011-03-03
EP1971598A1 (en) 2008-09-24
TW200800966A (en) 2008-01-01
WO2007061670A1 (en) 2007-05-31
JP5274258B2 (en) 2013-08-28
JP2009516684A (en) 2009-04-23

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