AR022927A1 - Inhibidores de proteasas - Google Patents

Inhibidores de proteasas

Info

Publication number
AR022927A1
AR022927A1 ARP000101121A ARP000101121A AR022927A1 AR 022927 A1 AR022927 A1 AR 022927A1 AR P000101121 A ARP000101121 A AR P000101121A AR P000101121 A ARP000101121 A AR P000101121A AR 022927 A1 AR022927 A1 AR 022927A1
Authority
AR
Argentina
Prior art keywords
alkyl
het
group
alkenyl
alkoxy
Prior art date
Application number
ARP000101121A
Other languages
English (en)
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 AR022927A1 publication Critical patent/AR022927A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D321/00—Heterocyclic compounds containing rings having two oxygen atoms as the only ring hetero atoms, not provided for by groups C07D317/00 - C07D319/00
    • C07D321/02—Seven-membered rings
    • C07D321/04—Seven-membered rings not condensed with other rings
    • C07D321/06—1,3-Dioxepines; Hydrogenated 1,3-dioxepines
    • 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
    • A61P19/08—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invencion proporciona compuestos de la formula (1): R1, R2, R3, R4, R5, R6, R7, R8, R11, R16 y R17, y R se seleccionan independientemente delgrupo que comprende: H, alquiloC1-6, alqueniloC2-6, alquiniloC2-6, Ar-alquiloC0-6, y Het-alquiloC0-6; R9 se selecciona del grupo que comprende: alquilo C3-6,Ar, Het, CH(R10)Ar, CH(R10) OAr, NR10R11 y CH(R10)NR11R12; R10 se selecciona del grupo que comprende: H, alqueniloC2-6, alquiniloC2-6, cicloalquilC3-11-alquiloC0-6, Ar-alquiloC0-6,Ar-alqueniloC2-6,Ar-alquilinoC2-6, Het-alquiloC0-6, Het-alqueniloC2-6, Het-alquiniloC2-6, y alquiloC1-6,opcionalmente sustituido con OR13,SR13,NR13R14,N(R)CO2R,C02R,CONR13R14, o N(C=NH)NH2; R12 se selecciona del grupo que comprende: R15,R15C(O),R15C(S),R15OC(O) y R15OC(O)NR11CH(R10)(CO); R13 yR14 se seleccionan independientemente del grupo que comprende: H,alquiloC1-6,alqueniloC2-6,Ar-alquiloC0-6,o Het-alquiloC0-6,y R16R17N-alquiloC2-6; R15 seselecciona del grupo que comprende: alquiloC1-6,alqueniloC2-6,Ar-alquiloC0-6,o Het-alquiloC0-6; Ar se selecciona del grup que comprende fenilo y naftilo,opcionalmente sustituidos con uno o más de Ph-alquiloC0-6,Het-alquiloC0-6, alquiloC1-6, alcoxiloC1-6, Ph-alcoxiloC0-6, Het-alcoxiloC0-6, OH, NR13R14, Het--S-alquiloC0-6, (CH2)1-6OH, (CH2)1-6NR13R14, OH(CH3)1-6NR13R14, (CH2)0-6CO2R, O(CH2)1-6C02R,(CH2)1-6SO2, CF3,OCF3 o halogeno; Ph puede estar opcionalmentesustituido con uno o más de alquiloC1-6, alcoxiC1-6,OH,(CH2)1-6NR13R14,CO2R,CF3 o halogeno; dos grupos alquiloC1-6 o alcoxiloC1-6 se pueden combinar paraformar un anillo de 5-7 miembros, saturados o no saturado,condensados sobre el anillo de Ar; y sus sales, hidratos y solvatos farmacéuticamente aceptables queinhiben proteasas incluyendo catepsina K, composiciones farmacéuticas de tales compuestos, y métodos para tratar enfermedades de pérdida osea o degradacion decartílado o matriz excesivas, incluyendo osteoporosis, enfermedad gingival incluyendo gingivitis y periodontitis; artritis, más específicamente osteoartritis yartritis reumatoide; enfermdad de Paget; hipercalcemia de carácter maligno; y enfermedad osea metabolica, que comprende inhibir dicha pérdida osea o la
ARP000101121A 1999-03-16 2000-03-14 Inhibidores de proteasas AR022927A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12465999P 1999-03-16 1999-03-16

Publications (1)

Publication Number Publication Date
AR022927A1 true AR022927A1 (es) 2002-09-04

Family

ID=22416114

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000101121A AR022927A1 (es) 1999-03-16 2000-03-14 Inhibidores de proteasas

Country Status (9)

Country Link
EP (1) EP1161237A4 (es)
JP (1) JP2002539160A (es)
AR (1) AR022927A1 (es)
AU (1) AU3888200A (es)
CO (1) CO5180542A1 (es)
HK (1) HK1043534A1 (es)
PE (1) PE20001564A1 (es)
UY (1) UY26026A1 (es)
WO (1) WO2000054769A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
AU1588901A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
JP2003513972A (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
JP2003513924A (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
SK13632002A3 (sk) 2000-03-21 2003-02-04 Smithkline Beecham Corporation C1-6-alkyl-4-amino-azepán-3-ónové zlúčeniny, spôsob ich prípravy, farmaceutický prostriedok s ich obsahom, ich použitie a medziprodukty
WO2003062192A1 (en) 2002-01-17 2003-07-31 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
JP2004196696A (ja) * 2002-12-18 2004-07-15 Kyowa Hakko Kogyo Co Ltd 関節炎の予防剤または治療剤
DK2714675T3 (en) * 2011-05-27 2019-04-15 Lexicon Pharmaceuticals Inc 4H-Thieno [3,2-c] chromium-based inhibitors of notum pectin acetyl esterase and methods for their use

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5374623A (en) * 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
DE69321087T2 (de) * 1992-12-25 1999-05-20 Mitsubishi Chem Corp Alpha-aminoketon Derivate

Also Published As

Publication number Publication date
EP1161237A1 (en) 2001-12-12
CO5180542A1 (es) 2002-07-30
WO2000054769A1 (en) 2000-09-21
EP1161237A4 (en) 2002-03-27
UY26026A1 (es) 2000-10-31
HK1043534A1 (zh) 2002-09-20
JP2002539160A (ja) 2002-11-19
PE20001564A1 (es) 2001-02-08
AU3888200A (en) 2000-10-04

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