PE20051048A1 - Compuestos heterociclicos como inhibidores de aspartil proteasa - Google Patents

Compuestos heterociclicos como inhibidores de aspartil proteasa

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Publication number
PE20051048A1
PE20051048A1 PE2005000018A PE2005000018A PE20051048A1 PE 20051048 A1 PE20051048 A1 PE 20051048A1 PE 2005000018 A PE2005000018 A PE 2005000018A PE 2005000018 A PE2005000018 A PE 2005000018A PE 20051048 A1 PE20051048 A1 PE 20051048A1
Authority
PE
Peru
Prior art keywords
aspartile
protease inhibitors
methyl
heterocyclic compounds
compounds
Prior art date
Application number
PE2005000018A
Other languages
English (en)
Inventor
William J Greenlee
Robert Mazzola
John Caldwell
Andrew Stamford
Yusheng Wu
Suresh D Babu
Tao Guo
Johannes H Voigt
Elizabeth M Smith
Yuanzan C Ye
Zhong-Yue Sun
Brian Mckittrick
Corey Strickland
Jared Cumming
Ulrich Iserloh
Zhaoning Zhu
Lingyan Wang
Kurt W Saionz
Rachel C Hunter
Thuy X H Le
Original Assignee
Schering Corp
Pharmacopeia 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 Schering Corp, Pharmacopeia Inc filed Critical Schering Corp
Publication of PE20051048A1 publication Critical patent/PE20051048A1/es

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    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/88Nitrogen atoms, e.g. allantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
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    • 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
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    • A61P31/10Antimycotics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P9/12Antihypertensives
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    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/071,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • AIDS & HIV (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE W ES UN ENLACE, -C(=S)-, -S(O)(1-2)-, -C(=O)-, -O-, -C(R6)(R7)-, ENTRE OTROS; X ES -O-, -N(R5)- O -C(R6)(R7)-, CON LA CONDICION DE QUE CUANDO X ES -O- U NO SEA -O-, -S(O)(1-2)-, -C(=O)- O -C(=NR5)-; U ES -S(O)(1-2)-, -C(O)-,-O-, -(C(R6)(R7))b-, ENTRE OTROS; R1, R2 Y R5 SON INDEPENDIENTEMENTE, H, ALQUILO, ALQUENILO, ENTRE OTROS; R3 Y R4 SON INDEPENDIENTEMENTE, H, ALQUILO, CICLOALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 5-ETILCICLOHEXIL-2-IMINO-3-METIL-5-({3-[(2-OXOETIL)AMINO]CICLOHEXIL}METIL)-IMIDAZOL-4-ONA, 5-ETILCICLOHEXIL-2-IMINO-3-METIL-5-({3-(PIRROLIDIN)-CICLOHEXIL}METIL)-IMIDAZOL-4-ONA, ENTRE OTROS. TAMBIEN SE REFIERE A UN COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA ASPARTIL PROTEASA, POR LO QUE SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES CARDIOVASCULARES, COGNITIVAS Y NEURODEGENERATIVAS
PE2005000018A 2003-12-15 2005-01-03 Compuestos heterociclicos como inhibidores de aspartil proteasa PE20051048A1 (es)

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US52953503P 2003-12-15 2003-12-15

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CN (3) CN1913886B (es)
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AU (1) AU2004299040A1 (es)
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Families Citing this family (127)

* 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
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
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