ECSP024388A - Inhibidores de proteasas - Google Patents

Inhibidores de proteasas

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
English (en)
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/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • A61P33/12Schistosomicides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic 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
    • C07D223/12Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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.
EC2002004388A 2000-06-14 2002-12-12 Inhibidores de proteasas ECSP024388A (es)

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 (es) 2003-02-06

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2002004388A ECSP024388A (es) 2000-06-14 2002-12-12 Inhibidores de proteasas

Country Status (25)

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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003513926A (ja) * 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 プロテアーゼ阻害剤
JP2003513927A (ja) * 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 プロテア−ゼ阻害剤
BR0115473A (pt) * 2000-11-22 2004-09-28 Smithkline Beecham Corp Inibidores de protease
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
ATE442141T1 (de) 2001-02-20 2009-09-15 Chugai Pharmaceutical Co Ltd Verfahren zur behandlung von stoffwechselerkrankungen mit malonyl-coa- decarboxylase-hemmern
AU2002342682A1 (en) * 2001-05-17 2002-11-25 Smithkline Beecham Corporation Protease inhibitors
GB0220187D0 (en) * 2002-08-30 2002-10-09 Novartis Ag Organic compounds
ES2353306T3 (es) * 2003-08-01 2011-03-01 Chugai Seiyaku Kabushiki Kaisha Compuestos heterocíclicos útiles como inhibidores de la malonil-coa-descarboxilasa.
DE602004016530D1 (de) 2003-08-01 2008-10-23 Chugai Pharmaceutical Co Ltd Azol-verbindungen auf cyanoguanidin-basis als malonyl-coa decarboxylase-hemmer
ES2309563T3 (es) 2003-08-01 2008-12-16 Chugai Seiyaku Kabushiki Kaisha Compuestos de piperidina utiles como inhibidores de malonil coenzima a descarboxilasa.
EP2719700A1 (en) 2008-01-09 2014-04-16 Amura Therapeutics Limited Tetrahydrofuro(3,2-b)pyrrol-3-one derivatives as inhibitors of cysteine proteinases
CN103275070A (zh) * 2013-05-10 2013-09-04 郑彪 调节单核细胞增殖的四环化合物及其应用
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 (fr) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
CN1253441C (zh) * 1998-12-23 2006-04-26 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
JP2003513926A (ja) * 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 プロテアーゼ阻害剤
JP2003513956A (ja) * 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 プロテアーゼ阻害剤
WO2002017924A1 (en) * 2000-09-01 2002-03-07 Smithkline Beecham Corporation Method of treatment
BR0115473A (pt) * 2000-11-22 2004-09-28 Smithkline Beecham Corp Inibidores de protease
AU2002342682A1 (en) * 2001-05-17 2002-11-25 Smithkline Beecham Corporation Protease inhibitors

Also Published As

Publication number Publication date
MXPA02012442A (es) 2003-04-25
BG107327A (bg) 2003-07-31
KR20030008220A (ko) 2003-01-24
JP2004503502A (ja) 2004-02-05
NO20025786L (no) 2003-02-12
CN1444481A (zh) 2003-09-24
IL153421A0 (en) 2003-07-06
WO2001095911A1 (en) 2001-12-20
ZA200209808B (en) 2004-07-09
EP1307204A1 (en) 2003-05-07
EA200300018A1 (ru) 2003-06-26
SK17592002A3 (sk) 2003-05-02
HUP0301231A2 (hu) 2003-08-28
NZ522965A (en) 2004-06-25
NO20025786D0 (no) 2002-12-02
EP1307204A4 (en) 2004-06-02
PE20011374A1 (es) 2002-04-07
AR032622A1 (es) 2003-11-19
MA25758A1 (fr) 2003-04-01
AU2001268407A1 (en) 2001-12-24
OA12288A (en) 2003-12-12
BR0111693A (pt) 2004-04-06
AP2002002671A0 (en) 2002-12-31
PL360508A1 (en) 2004-09-06
CA2412353A1 (en) 2001-12-20
CZ20024086A3 (cs) 2003-05-14

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