PE20080744A1 - IMIDAZOLE AMINES AS ß-SECRETASE INHIBITORS - Google Patents

IMIDAZOLE AMINES AS ß-SECRETASE INHIBITORS

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Publication number
PE20080744A1
PE20080744A1 PE2007001049A PE2007001049A PE20080744A1 PE 20080744 A1 PE20080744 A1 PE 20080744A1 PE 2007001049 A PE2007001049 A PE 2007001049A PE 2007001049 A PE2007001049 A PE 2007001049A PE 20080744 A1 PE20080744 A1 PE 20080744A1
Authority
PE
Peru
Prior art keywords
som
pyrimidin
halogen
amine
phenyl
Prior art date
Application number
PE2007001049A
Other languages
Spanish (es)
Inventor
Michael Sotirios Malamas
Keith Douglas Barnes
Matthew Robert Johnson
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of PE20080744A1 publication Critical patent/PE20080744A1/en

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Classifications

    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/20Spiro-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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

REFERIDA A UN DERIVADO DE IMIDAZOL DE FORMULA (I), DONDE Q ES O, S O CH2; W ES O, S O CH2; X ES N, NO, SOm, O O CH; Y ES N, NO, SOm, O, CR10; Z ES N, NO, O, SOm O CR11; m ES 0, 1 O 2; n ES 0 O 1; R1 Y R2 SON H, ALQUILO C1-C4, ENTRE OTROS; R3 Y R4 SON H, ALQUILO C1-C4, ENTRE OTROS; R5 Y R6 SON H, HALOGENO, NO2, ENTRE OTROS; R7 Y R8 SON H, HALOGENO, NO2, CN, ENTRE OTROS; R9 ES H, HALOGENO, NO2, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 8-[3-(2-FLUOROPIRIDIN-3-IL)-FENIL]-8-PIRIDIN-4-IL-2,3,4,8-TETRAHIDROIMIDAZO[1,5-a]PIRIMIDIN-6-AMINA, 8-(2,6-DIETILPIRIDIN-4-IL)-8-[3-(2-FLUROPIRIDIN-3-IL)-FENIL]-2,3,4,8-TETRAHIDRO-IMIDAZO[1,5-a]PIRIMIDIN-6-AMINA, 8-(1-ETIL-1H-PIRAZOL-4-IL)-8-[3-(2-FLUOROPIRIDIN-3-IL)FENIL]-2,3,4,8-TETRAHIDRO-IMIDAZOL[1,5-a]PIRIMIDIN-6-AMINA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y UN PROCESO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA ß-SECRETASA Y SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, SINDROME DE DOWN, HEMORRAGIA CEREBRAL HEREDITARIA CON AMILOIDOSIS DEL TIPO DUTCH, ENTRE OTROSREFERRING TO AN IMIDAZOLE DERIVATIVE OF FORMULA (I), WHERE Q IS O, S OR CH2; W IS O, S O CH2; X IS N, NO, SOm, O OR CH; Y IS N, NO, SOm, O, CR10; Z IS N, NO, O, SOm OR CR11; m IS 0, 1 O 2; n IS 0 O 1; R1 AND R2 ARE H, C1-C4 ALKYL, AMONG OTHERS; R3 AND R4 ARE H, C1-C4 ALKYL, AMONG OTHERS; R5 AND R6 ARE H, HALOGEN, NO2, AMONG OTHERS; R7 AND R8 ARE H, HALOGEN, NO2, CN, AMONG OTHERS; R9 IS H, HALOGEN, NO2, CN, AMONG OTHERS. THE PREFERRED COMPOUNDS ARE: 8- [3- (2-FLUOROPYRIDIN-3-IL) -PHENYL] -8-PYRIDIN-4-IL-2,3,4,8-TETRAHYDROIMIDAZO [1,5-a] PYRIMIDIN-6- AMINE, 8- (2,6-DIETHYLPYRIDIN-4-IL) -8- [3- (2-FLUROPYRIDIN-3-IL) -PHENYL] -2,3,4,8-TETRAHYDRO-IMIDAZO [1,5- a] PYRIMIDIN-6-AMINE, 8- (1-ETHYL-1H-PYRAZOLE-4-IL) -8- [3- (2-FLUOROPYRIDIN-3-IL) PHENYL] -2,3,4,8-TETRAHYDRO -IMIDAZOLE [1,5-a] PYRIMIDIN-6-AMINE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCESS. SUCH COMPOUNDS ARE INHIBITORS OF ß-SECRETASE AND ARE USEFUL IN THE TREATMENT OF ALZHEIMER'S DISEASE, DOWN'S SYNDROME, HEREDITARY BRAIN HEMORRHAGE WITH DUTCH-TYPE AMYLOIDOSIS, AMONG OTHERS

PE2007001049A 2006-08-17 2007-08-07 IMIDAZOLE AMINES AS ß-SECRETASE INHIBITORS PE20080744A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US83835706P 2006-08-17 2006-08-17

Publications (1)

Publication Number Publication Date
PE20080744A1 true PE20080744A1 (en) 2008-05-24

Family

ID=38988046

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007001049A PE20080744A1 (en) 2006-08-17 2007-08-07 IMIDAZOLE AMINES AS ß-SECRETASE INHIBITORS

Country Status (9)

Country Link
EP (1) EP2054414A2 (en)
JP (1) JP2010500999A (en)
AR (1) AR062409A1 (en)
CA (1) CA2660441A1 (en)
CL (1) CL2007002288A1 (en)
MX (1) MX2009001699A (en)
PE (1) PE20080744A1 (en)
TW (1) TW200817406A (en)
WO (1) WO2008022024A2 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
KR20080029965A (en) 2005-06-14 2008-04-03 쉐링 코포레이션 Aspartyl protease inhibitors
BRPI0612545A2 (en) 2005-06-14 2010-11-23 Schering Corp protease inhibiting compounds, pharmaceutical compositions and their use
ES2572263T3 (en) 2005-10-25 2016-05-31 Shionogi & Co Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors
CA2653650A1 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co Pharmaceutical composition for treatment of alzheimer's disease
EP2283016B1 (en) 2008-04-22 2014-09-24 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
KR101324426B1 (en) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING β-SECRETASE-INHIBITING ACTIVITY
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-aminopyridin-4-one and 2-aminopyridine derivative both having bace1-inhibiting activity
UA108363C2 (en) 2009-10-08 2015-04-27 IMINOTIADIASIADIOXIDE OXIDES AS BACE INHIBITORS, COMPOSITIONS THEREOF AND THEIR APPLICATIONS
CN102834384A (en) 2009-12-11 2012-12-19 盐野义制药株式会社 Oxazine derivative
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
WO2012057248A1 (en) 2010-10-29 2012-05-03 塩野義製薬株式会社 Naphthyridine derivative
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2703399A4 (en) 2011-04-26 2014-10-15 Shionogi & Co Oxazine derivative and bace 1 inhibitor containing same
JP2014524472A (en) 2011-08-22 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション 2-Spiro-substituted iminothiazines and their monooxides and dioxides as BACE inhibitors, compositions, and uses thereof
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA06014792A (en) * 2004-06-16 2007-02-16 Wyeth Corp Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase.
ATE444962T1 (en) * 2004-06-16 2009-10-15 Wyeth Corp AMINO-5,5-DIPHENYLIMIDAZOLONE DERIVATIVES FOR BETA SECRETASE INHIBITION
BRPI0606690A2 (en) * 2005-01-14 2009-07-14 Wyeth Corp compound; use of the compound to treat a disease or disorder associated with excessive bace activity; and pharmaceutical composition
AU2006266167A1 (en) * 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation

Also Published As

Publication number Publication date
TW200817406A (en) 2008-04-16
JP2010500999A (en) 2010-01-14
EP2054414A2 (en) 2009-05-06
WO2008022024A2 (en) 2008-02-21
MX2009001699A (en) 2009-02-25
CL2007002288A1 (en) 2008-02-08
AR062409A1 (en) 2008-11-05
WO2008022024A3 (en) 2008-05-22
CA2660441A1 (en) 2008-02-21

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