WO2006138266A3 - The preparation and use of compounds as aspartyl protease inhibitors - Google Patents

The preparation and use of compounds as aspartyl protease inhibitors Download PDF

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Publication number
WO2006138266A3
WO2006138266A3 PCT/US2006/022920 US2006022920W WO2006138266A3 WO 2006138266 A3 WO2006138266 A3 WO 2006138266A3 US 2006022920 W US2006022920 W US 2006022920W WO 2006138266 A3 WO2006138266 A3 WO 2006138266A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
formula
disclosed
methods
aspartyl protease
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2006/022920
Other languages
French (fr)
Other versions
WO2006138266A2 (en
Inventor
Brian Mckittrick
Zhaoning Zhu
Andrew Stamford
Elizabeth M Smith
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering 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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37388420&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2006138266(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to CA002610829A priority Critical patent/CA2610829A1/en
Priority to AU2006259574A priority patent/AU2006259574A1/en
Priority to EP06784809A priority patent/EP1896430B1/en
Priority to AT06784809T priority patent/ATE489370T1/en
Priority to MX2007016177A priority patent/MX2007016177A/en
Application filed by Schering Corp filed Critical Schering Corp
Priority to CN200680021093XA priority patent/CN101198597B/en
Priority to JP2008516999A priority patent/JP4859922B2/en
Priority to DE602006018456T priority patent/DE602006018456D1/en
Publication of WO2006138266A2 publication Critical patent/WO2006138266A2/en
Publication of WO2006138266A3 publication Critical patent/WO2006138266A3/en
Priority to IL187453A priority patent/IL187453A0/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/10—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/72—Heterocyclic compounds containing 1,3,5-triazine rings condensed with carbocyclic rings or ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biochemistry (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Disclosed are compounds of the formula I (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, -C(O)-, or -C(R3’)(R4’)-; X is -N(R1)- or -C(R6)(R7)-; Y is -S(O)2-, -C(=O)-, -PO(OR9) or -C(R6’R7’)-; is a single or double bond and R, R1, R2, R3, R4, R3’, R4’, R5, R6, R6’, R7 and R7’ are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
PCT/US2006/022920 2005-06-14 2006-06-12 The preparation and use of compounds as aspartyl protease inhibitors Ceased WO2006138266A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
DE602006018456T DE602006018456D1 (en) 2005-06-14 2006-06-12 PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE HEMMER
JP2008516999A JP4859922B2 (en) 2005-06-14 2006-06-12 Preparation and use of compounds as aspartyl protease inhibitors
EP06784809A EP1896430B1 (en) 2005-06-14 2006-06-12 The preparation and use of compounds as aspartyl protease inhibitors
AT06784809T ATE489370T1 (en) 2005-06-14 2006-06-12 PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE INHIBITORS
MX2007016177A MX2007016177A (en) 2005-06-14 2006-06-12 The preparation and use of compounds as aspartyl protease inhibitors.
CA002610829A CA2610829A1 (en) 2005-06-14 2006-06-12 The preparation and use of compounds as aspartyl protease inhibitors
CN200680021093XA CN101198597B (en) 2005-06-14 2006-06-12 Preparation and use of compounds as aspartyl protease inhibitors
AU2006259574A AU2006259574A1 (en) 2005-06-14 2006-06-12 The preparation and use of compounds as aspartyl protease inhibitors
IL187453A IL187453A0 (en) 2005-06-14 2007-11-18 The preparation and uses of compounds as aspartyl protease inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US69041305P 2005-06-14 2005-06-14
US60/690,413 2005-06-14

Publications (2)

Publication Number Publication Date
WO2006138266A2 WO2006138266A2 (en) 2006-12-28
WO2006138266A3 true WO2006138266A3 (en) 2007-03-08

Family

ID=37388420

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/022920 Ceased WO2006138266A2 (en) 2005-06-14 2006-06-12 The preparation and use of compounds as aspartyl protease inhibitors

Country Status (16)

Country Link
US (1) US8110682B2 (en)
EP (2) EP2194047A1 (en)
JP (1) JP4859922B2 (en)
KR (1) KR20080015861A (en)
CN (1) CN101198597B (en)
AR (1) AR054510A1 (en)
AT (1) ATE489370T1 (en)
AU (1) AU2006259574A1 (en)
CA (1) CA2610829A1 (en)
DE (1) DE602006018456D1 (en)
IL (1) IL187453A0 (en)
MX (1) MX2007016177A (en)
PE (1) PE20070115A1 (en)
TW (1) TW200716574A (en)
WO (1) WO2006138266A2 (en)
ZA (1) ZA200710342B (en)

Cited By (1)

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US8691833B2 (en) 2007-02-23 2014-04-08 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8691833B2 (en) 2007-02-23 2014-04-08 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US8691831B2 (en) 2007-02-23 2014-04-08 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US8829036B2 (en) 2007-02-23 2014-09-09 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors

Also Published As

Publication number Publication date
EP1896430A2 (en) 2008-03-12
TW200716574A (en) 2007-05-01
PE20070115A1 (en) 2007-02-13
CN101198597B (en) 2011-11-16
ZA200710342B (en) 2008-12-31
CN101198597A (en) 2008-06-11
MX2007016177A (en) 2008-03-07
ATE489370T1 (en) 2010-12-15
KR20080015861A (en) 2008-02-20
IL187453A0 (en) 2008-02-09
JP4859922B2 (en) 2012-01-25
US8110682B2 (en) 2012-02-07
EP1896430B1 (en) 2010-11-24
DE602006018456D1 (en) 2011-01-05
AU2006259574A1 (en) 2006-12-28
JP2008546697A (en) 2008-12-25
CA2610829A1 (en) 2006-12-28
US20070010667A1 (en) 2007-01-11
AR054510A1 (en) 2007-06-27
WO2006138266A2 (en) 2006-12-28
EP2194047A1 (en) 2010-06-09

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