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

    • 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

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 (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1231921A4 (en) * 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
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
JP2005513083A (ja) * 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 プロテアーゼ阻害剤
WO2002066035A2 (en) 2001-02-20 2002-08-29 Chugai Seiyaku Kabushiki Kaisha 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
EP1401453A4 (en) * 2001-05-17 2005-04-06 Smithkline Beecham Corp PROTEASE INHIBITORS
EP2208495B1 (en) 2003-08-01 2011-12-14 Chugai Seiyaku Kabushiki Kaisha Cyanoguanidine-based azole compounds useful as malonyl-CoA decarboxylase inhibitors
WO2005011670A1 (en) * 2003-08-01 2005-02-10 Chugai Seiyaku Kabushiki Kaisha Heterocyclic compounds useful as malonyl-coa decarboxylase inhibitors
ATE400272T1 (de) 2003-08-01 2008-07-15 Chugai Pharmaceutical Co Ltd Piperidin-verbindungen als malonyl-coa decarboxylase-hemmer
JP5587790B2 (ja) 2008-01-09 2014-09-10 アミュラ セラピューティクス リミティド 化合物
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.
NZ511710A (en) * 1998-12-23 2003-12-19 Smithkline Beecham Corp 4-Amino-azepan-3-one derivatives useful as protease inhibitors
EP1231921A4 (en) * 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
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
AU2001286983A1 (en) * 2000-09-01 2002-03-13 Smith Kline Beecham Corporation Method of treatment
JP2005513083A (ja) * 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 プロテアーゼ阻害剤
EP1401453A4 (en) * 2001-05-17 2005-04-06 Smithkline Beecham Corp PROTEASE INHIBITORS

Also Published As

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

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