WO2002051983A3 - Novel compounds and compositions as cathepsin inhibitors - Google Patents

Novel compounds and compositions as cathepsin inhibitors Download PDF

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Publication number
WO2002051983A3
WO2002051983A3 PCT/US2001/050680 US0150680W WO02051983A3 WO 2002051983 A3 WO2002051983 A3 WO 2002051983A3 US 0150680 W US0150680 W US 0150680W WO 02051983 A3 WO02051983 A3 WO 02051983A3
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WO
WIPO (PCT)
Prior art keywords
compositions
novel compounds
cathepsin inhibitors
inhibitors
cathepsin
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/US2001/050680
Other languages
French (fr)
Other versions
WO2002051983A2 (en
Inventor
Michael Graupe
John Patterson
Stephen D Pickett
John Link
Jiayao Li
David Aldous
Sukanthini Thurairatnam
Andreas Timm
Frank Halley
Justine Lai
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.)
Axys Pharmaceuticals Inc
Aventis Pharmaceuticals Inc
Original Assignee
Axys Pharmaceuticals Inc
Aventis 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 Axys Pharmaceuticals Inc, Aventis Pharmaceuticals Inc filed Critical Axys Pharmaceuticals Inc
Priority to CA002433520A priority Critical patent/CA2433520A1/en
Priority to MXPA03005601A priority patent/MXPA03005601A/en
Priority to IL15657701A priority patent/IL156577A0/en
Priority to JP2002553464A priority patent/JP2004523506A/en
Priority to EP01988420A priority patent/EP1383748A2/en
Publication of WO2002051983A2 publication Critical patent/WO2002051983A2/en
Anticipated expiration legal-status Critical
Publication of WO2002051983A3 publication Critical patent/WO2002051983A3/en
Ceased legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones 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 other ring carbon atoms
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract

The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making
PCT/US2001/050680 2000-12-22 2001-12-24 Novel compounds and compositions as cathepsin inhibitors Ceased WO2002051983A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CA002433520A CA2433520A1 (en) 2000-12-22 2001-12-24 Novel compounds and compositions as cathepsin inhibitors
MXPA03005601A MXPA03005601A (en) 2000-12-22 2001-12-24 Novel compounds and compositions as cathepsin inhibitors.
IL15657701A IL156577A0 (en) 2000-12-22 2001-12-24 Selective cathepsin s inhibitors and pharmaceutical compositions containing the same
JP2002553464A JP2004523506A (en) 2000-12-22 2001-12-24 Novel compounds and compositions as cathepsin inhibitors
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