ECSP024388A - PROTEASE INHIBITORS - Google Patents

PROTEASE INHIBITORS

Info

Publication number
ECSP024388A
ECSP024388A EC2002004388A ECSP024388A ECSP024388A EC SP024388 A ECSP024388 A EC SP024388A EC 2002004388 A EC2002004388 A EC 2002004388A EC SP024388 A ECSP024388 A EC SP024388A EC SP024388 A ECSP024388 A EC SP024388A
Authority
EC
Ecuador
Prior art keywords
compounds
provides
proteases
cathepsin
diseases
Prior art date
Application number
EC2002004388A
Other languages
Spanish (es)
Inventor
Robert Wells Marquis
Daniel Frank Veber
Yu Ru
Scott Kevin Thompson
Dennis Shinji Yamashita
Maxwell David Cummings
Original Assignee
Smithkline Beecham 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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of ECSP024388A publication Critical patent/ECSP024388A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/12—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un objetivo de la presente invención es proveer inhibidores de proteasa 4-amino-azepan-3-ona carbonil, particularmente los inhibidores de cisteína y serina proteasas, aún más particularmente los compuestos que inhiben las cisteína proteasas de la superfamilia de la papaína, todavía más particularmente los compuestos que inhiben las cisteina proteasas de la familia catepsina, más particularmente los compuestos que inhiben catepsina K y que son útiles para el tratamiento de enfermedades que pueden ser terapéuticamente modificadas por alteración de estas proteasas. De acuerdo con estos, en el primer aspecto, esta invención provee un compuesto según la Fórmula I, En otro aspecto, esta invención provee una composición farmacéutica formada de un compuesto de acuerdo a la Fórmula I y un transportador farmacéuticamente aceptable, diluyente o excipiente. Aún más, en otro aspecto esta invención provee intermediarios útiles en la preparación de los compuestos de la Fórmula I. En todavía otro aspecto, esta invención provee un método para tratar enfermedades en las que la patología de la enfermedad puede ser terapéuticamente modificada por inhibidores de proteasas de la superfamilia de la papaína, todavía más particularmente cisteína proteasas de la familia catepsina, y más particularmente catepsina K . En un sentido particular, los compuestos de esta invención son especialmente útiles para el tratamiento de enfermedades caracterizadas por pérdida ósea, tales como osteoporosis y enfermedades gingivales, tales como gingivitis y periodontitis, o por excesiva degradación del cartílago o la matriz , tales como osteoartritis y artritis reumatoidea.An objective of the present invention is to provide inhibitors of 4-amino-azepan-3-one carbonyl protease, particularly cysteine and serine protease inhibitors, even more particularly compounds that inhibit the cysteine proteases of the papain superfamily, still more particularly the compounds that inhibit the cysteine proteases of the cathepsin family, more particularly the compounds that inhibit cathepsin K and that are useful for the treatment of diseases that can be therapeutically modified by altering these proteases. According to these, in the first aspect, this invention provides a compound according to Formula I. In another aspect, this invention provides a pharmaceutical composition formed of a compound according to Formula I and a pharmaceutically acceptable carrier, diluent or excipient. Furthermore, in another aspect this invention provides useful intermediates in the preparation of the compounds of Formula I. In yet another aspect, this invention provides a method for treating diseases in which the disease pathology can be therapeutically modified by inhibitors of Papain superfamily proteases, even more particularly cysteine proteases of the cathepsin family, and more particularly cathepsin K. In a particular sense, the compounds of this invention are especially useful for the treatment of diseases characterized by bone loss, such as osteoporosis and gingival diseases, such as gingivitis and periodontitis, or by excessive degradation of the cartilage or matrix, such as osteoarthritis and Rheumatoid arthritis.

EC2002004388A 2000-06-14 2002-12-12 PROTEASE INHIBITORS ECSP024388A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US59384500A 2000-06-14 2000-06-14

Publications (1)

Publication Number Publication Date
ECSP024388A true ECSP024388A (en) 2003-02-06

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2002004388A ECSP024388A (en) 2000-06-14 2002-12-12 PROTEASE INHIBITORS

Country Status (25)

Country Link
EP (1) EP1307204A4 (en)
JP (1) JP2004503502A (en)
KR (1) KR20030008220A (en)
CN (1) CN1444481A (en)
AP (1) AP2002002671A0 (en)
AR (1) AR032622A1 (en)
AU (1) AU2001268407A1 (en)
BG (1) BG107327A (en)
BR (1) BR0111693A (en)
CA (1) CA2412353A1 (en)
CZ (1) CZ20024086A3 (en)
EA (1) EA200300018A1 (en)
EC (1) ECSP024388A (en)
HU (1) HUP0301231A2 (en)
IL (1) IL153421A0 (en)
MA (1) MA25758A1 (en)
MX (1) MXPA02012442A (en)
NO (1) NO20025786L (en)
NZ (1) NZ522965A (en)
OA (1) OA12288A (en)
PE (1) PE20011374A1 (en)
PL (1) PL360508A1 (en)
SK (1) SK17592002A3 (en)
WO (1) WO2001095911A1 (en)
ZA (1) ZA200209808B (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003513927A (en) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2005513083A (en) * 2000-11-22 2005-05-12 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
BR0207408A (en) 2001-02-20 2004-02-25 Chugai Pharmaceutical Co Ltd Azoles as malonyl coa decarboxylase inhibitors useful as metabolic modulators
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
JP2004527575A (en) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
ATE400272T1 (en) 2003-08-01 2008-07-15 Chugai Pharmaceutical Co Ltd PIPERIDINE COMPOUNDS AS MALONYL-COA DECARBOXYLASE INHIBITORS
EP1658071B1 (en) 2003-08-01 2008-09-10 Chugai Seiyaku Kabushiki Kaisha Cyanoguanidine-based azole compounds useful as malonyl-coa decarboxylase inhibitors
ES2353306T3 (en) 2003-08-01 2011-03-01 Chugai Seiyaku Kabushiki Kaisha USEFUL HETEROCYCLIC COMPOUNDS AS INHIBITORS OF MALONIL-COA-DESCARBOXYLASE.
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
CN103275070A (en) * 2013-05-10 2013-09-04 郑彪 Tetracyclic compound for adjusting proliferation of mononuclear cells and application of tetracyclic compound
US9427441B2 (en) 2014-02-19 2016-08-30 Indiana University Research And Technology Corporation Targeting primary cilia to treat glaucoma

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DZ2285A1 (en) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Cysteine protease inhibitors.
PL350132A1 (en) * 1998-12-23 2002-11-04 Smithkline Beecham Corp Protease inhibitors
JP2003513956A (en) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2002017924A1 (en) * 2000-09-01 2002-03-07 Smithkline Beecham Corporation Method of treatment
JP2005513083A (en) * 2000-11-22 2005-05-12 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
JP2004527575A (en) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション Protease inhibitor

Also Published As

Publication number Publication date
AP2002002671A0 (en) 2002-12-31
KR20030008220A (en) 2003-01-24
PL360508A1 (en) 2004-09-06
EA200300018A1 (en) 2003-06-26
JP2004503502A (en) 2004-02-05
OA12288A (en) 2003-12-12
BR0111693A (en) 2004-04-06
CA2412353A1 (en) 2001-12-20
AR032622A1 (en) 2003-11-19
IL153421A0 (en) 2003-07-06
WO2001095911A1 (en) 2001-12-20
EP1307204A1 (en) 2003-05-07
PE20011374A1 (en) 2002-04-07
EP1307204A4 (en) 2004-06-02
SK17592002A3 (en) 2003-05-02
AU2001268407A1 (en) 2001-12-24
CZ20024086A3 (en) 2003-05-14
NO20025786D0 (en) 2002-12-02
HUP0301231A2 (en) 2003-08-28
NZ522965A (en) 2004-06-25
NO20025786L (en) 2003-02-12
BG107327A (en) 2003-07-31
ZA200209808B (en) 2004-07-09
MXPA02012442A (en) 2003-04-25
MA25758A1 (en) 2003-04-01
CN1444481A (en) 2003-09-24

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