WO2003020287A3 - Methods for the treatment of chronic pain anc compositions therefor - Google Patents

Methods for the treatment of chronic pain anc compositions therefor Download PDF

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Publication number
WO2003020287A3
WO2003020287A3 PCT/EP2002/009662 EP0209662W WO03020287A3 WO 2003020287 A3 WO2003020287 A3 WO 2003020287A3 EP 0209662 W EP0209662 W EP 0209662W WO 03020287 A3 WO03020287 A3 WO 03020287A3
Authority
WO
WIPO (PCT)
Prior art keywords
chronic pain
cathepsin
methods
anc
treatment
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/EP2002/009662
Other languages
French (fr)
Other versions
WO2003020287A2 (en
Inventor
Francis Paul Buxton
Pamposh Ganju
Christopher Robert Snell
Chuanzheng Song
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.)
Novartis Pharma GmbH Austria
Novartis AG
Original Assignee
Novartis Pharma GmbH Austria
Novartis AG
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 Novartis Pharma GmbH Austria, Novartis AG filed Critical Novartis Pharma GmbH Austria
Priority to EP02797651A priority Critical patent/EP1423128A2/en
Priority to JP2003524594A priority patent/JP2005502679A/en
Publication of WO2003020287A2 publication Critical patent/WO2003020287A2/en
Publication of WO2003020287A3 publication Critical patent/WO2003020287A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/711—Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Biophysics (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

The invention discloses cathepsin S as a suitable target for the development of new therapeutics to treat or ameliorate chronic pain. The invention relates to methods to treat and/or ameliorate chronic pain and pharmaceutical compositions therefor comprising modulators with inhibitory effect on cathepsin S enzyme activity and/or cathepsin S gene expression. The invention also relates to a method to identify compounds with therapeutic usefulness to treat chronic pain, comprising identifying compounds that can inhibit cathepsin S activity and/or gene expression which can also reverse the pathological effects of chronic pain in vivo.
PCT/EP2002/009662 2001-08-30 2002-08-29 Methods for the treatment of chronic pain anc compositions therefor Ceased WO2003020287A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP02797651A EP1423128A2 (en) 2001-08-30 2002-08-29 Methods for the treatment of chronic pain anc compositions therefor
JP2003524594A JP2005502679A (en) 2001-08-30 2002-08-29 Method for treating chronic pain and composition therefor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31589801P 2001-08-30 2001-08-30
US60/315,898 2001-08-30

Publications (2)

Publication Number Publication Date
WO2003020287A2 WO2003020287A2 (en) 2003-03-13
WO2003020287A3 true WO2003020287A3 (en) 2003-10-30

Family

ID=23226545

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/009662 Ceased WO2003020287A2 (en) 2001-08-30 2002-08-29 Methods for the treatment of chronic pain anc compositions therefor

Country Status (4)

Country Link
US (2) US20030144234A1 (en)
EP (1) EP1423128A2 (en)
JP (1) JP2005502679A (en)
WO (1) WO2003020287A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7326715B2 (en) 2005-09-23 2008-02-05 N.V. Organon 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA03005601A (en) * 2000-12-22 2004-12-02 Axys Pharm Inc Novel compounds and compositions as cathepsin inhibitors.
US20040147503A1 (en) * 2002-06-04 2004-07-29 Sheila Zipfeil Novel compounds and compositions as cathepsin inhibitors
GB0220187D0 (en) 2002-08-30 2002-10-09 Novartis Ag Organic compounds
PE20050068A1 (en) * 2003-02-06 2005-03-11 Novartis Ag 2-CYANOPYRROLOPYRIMIDINES AS INHIBITORS OF CATEPSIN S
US7384970B2 (en) 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7109243B2 (en) 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
EP1797883A3 (en) * 2003-04-28 2007-08-01 Novartis AG Pharmaceutical composition comprising a cathepsin S inhibitor and an opioid
US20070037835A1 (en) * 2003-04-28 2007-02-15 Pamposh Ganju Pharmaceutical composition comprising a cathepsin s inhibitor and an opioid
US7173051B2 (en) 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
WO2005014849A2 (en) * 2003-07-03 2005-02-17 Euro-Celtique, S.A. Genes associated with responses to neuropathic pain
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
GB0324542D0 (en) * 2003-10-21 2003-11-26 Novartis Ag Organic compounds
US7297714B2 (en) * 2003-10-21 2007-11-20 Irm Llc Inhibitors of cathepsin S
TW200614993A (en) 2004-06-11 2006-05-16 Akzo Nobel Nv 4-phenyl-pyrimidine-2-carbonitrile derivatives
US7309589B2 (en) 2004-08-20 2007-12-18 Vironix Llc Sensitive detection of bacteria by improved nested polymerase chain reaction targeting the 16S ribosomal RNA gene and identification of bacterial species by amplicon sequencing
EP1879923B1 (en) 2005-04-09 2015-05-27 Fusion Antibodies Limited Cathepsin s antibody
GB0507298D0 (en) 2005-04-11 2005-05-18 Novartis Ag Organic compounds
WO2006125105A2 (en) * 2005-05-19 2006-11-23 Wyeth Methods and compositions for treating and diagnosing multiple sclerosis
JP2008545720A (en) 2005-06-02 2008-12-18 メルク フロスト カナダ リミテツド Fluoroalkylamine derivatives as cathepsin inhibitors
US7687515B2 (en) 2006-01-17 2010-03-30 N.V. Organon 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
EP1991692A4 (en) * 2006-02-21 2009-07-22 Agency Science Tech & Res METHOD AND REAGENTS FOR TREATING HEPATIC FIBROSIS AND INFLAMMATION
CA2648947A1 (en) * 2006-04-10 2007-11-15 Fusion Antibodies Limited Therapy targeting cathepsin s
US20080269241A1 (en) * 2007-02-15 2008-10-30 Darin Allen Bicyclic aminopropyl tetrahydro-pyrazolo-pyridine modulators of cathepsin s
US20080207683A1 (en) * 2007-02-15 2008-08-28 Darin Allen Biaryl-substituted tetrahydro-pyrazolo-pyridine modulators of cathepsin s
US20080200454A1 (en) * 2007-02-15 2008-08-21 Ameriks Michael K Carbon-linked tetrahydro-pyrazolo-pyridine modulators of cathepsin s
US20090118274A1 (en) * 2007-02-15 2009-05-07 Darin Allen Monocyclic aminopropyl tetrahydro-pyrazolo-pyridine modulators of cathepsin s
US20090099157A1 (en) * 2007-02-15 2009-04-16 Ameriks Michael K Tetrahydro-pyrazolo-pyridine thioether modulators of cathepsin s
US7932251B2 (en) 2007-07-16 2011-04-26 N.V. Organon 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
EP2105742A1 (en) * 2008-03-26 2009-09-30 Sanofi-Aventis Use of cathepsin C
BRPI0922283A2 (en) 2008-12-19 2015-12-29 Medivir Uk Ltd cysteine protease inhibitors
US8026236B2 (en) 2009-01-16 2011-09-27 N.V. Organon 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
EP2293072A1 (en) * 2009-08-31 2011-03-09 Sanofi-Aventis Use of cathepsin H
EP2582660B1 (en) 2010-06-16 2015-07-22 Medivir UK Ltd New cathepsin s protease inhibitors, useful in the treatment of e.g. autoimmune disorders, allergy and chronic pain conditions

Citations (2)

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Publication number Priority date Publication date Assignee Title
US5795977A (en) * 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
WO2000051998A1 (en) * 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s

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US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
US5714484A (en) * 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
CA2251714A1 (en) * 1996-04-22 1997-10-30 Massachusetts Institute Of Technology Suppression of immune response via inhibition of cathepsin s
GB0121033D0 (en) * 2001-08-30 2001-10-24 Novartis Ag Organic compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5795977A (en) * 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
WO2000051998A1 (en) * 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
KATUNUMA N ET AL: "Structure based development of novel specific inhibitors for cathepsin L and cathepsin S in vitro and in vivo", FEBS LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 458, no. 1, 10 September 1999 (1999-09-10), pages 6 - 10, XP004260218, ISSN: 0014-5793 *
RIESE R J ET AL: "CATHEPSIN S ACTIVITY REGULATES ANTIGEN PRESENTATION AND IMMUNITY", JOURNAL OF CLINICAL INVESTIGATION, NEW YORK, NY, US, vol. 101, no. 11, June 1998 (1998-06-01), pages 2351 - 2363, XP002919128, ISSN: 0021-9738 *
See also references of EP1423128A2 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7326715B2 (en) 2005-09-23 2008-02-05 N.V. Organon 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives

Also Published As

Publication number Publication date
US20070129366A1 (en) 2007-06-07
JP2005502679A (en) 2005-01-27
WO2003020287A2 (en) 2003-03-13
EP1423128A2 (en) 2004-06-02
US20030144234A1 (en) 2003-07-31

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