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PE20001564A1 - 1,3-DIOXEPIN-5-ONA WITH A 7-MEMBER RING AS PROTEASE INHIBITORS - Google Patents

1,3-DIOXEPIN-5-ONA WITH A 7-MEMBER RING AS PROTEASE INHIBITORS

Info

Publication number
PE20001564A1
PE20001564A1 PE2000000226A PE0002262000A PE20001564A1 PE 20001564 A1 PE20001564 A1 PE 20001564A1 PE 2000000226 A PE2000000226 A PE 2000000226A PE 0002262000 A PE0002262000 A PE 0002262000A PE 20001564 A1 PE20001564 A1 PE 20001564A1
Authority
PE
Peru
Prior art keywords
alkyl
dioxepin
ona
het
alkenyl
Prior art date
Application number
PE2000000226A
Other languages
Spanish (es)
Inventor
Stacie Marie Halbert
Scott Kevin Thompson
Daniel Frank Veber
Sirishkumar Nidamarthy
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 PE20001564A1 publication Critical patent/PE20001564A1/en

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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A 1,3-DIOXEPIN-5-ONA CON UN ANILLO DE 7 MIEMBROS DE FORMULA I, DONDE: R1-R8, R11, R16, R17, R` SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R9 ES ALQUILO C3-C6, Ar, HET, CH(R10)Ar, CH(R10)OAr, NR10R11, CH(R10)NR11R12; R10 ES H, ALQUENILO C2-C6, ALQUINILO C2-C6, CICLOALQUIL C3-C11-ALQUILO C0-C6, Ar-ALQUILO C0-C6, Ar-ALQUENILO C2-C6, OPCIONALMENTE SUSTITUIDO CON OR13, SR13, NR13R14, N(R')CO2R', ENTRE OTROS; R12 ES R15, R15C(O), R15C(S), R15OC(O), R15OC(O)NR11CH(R10)(CO); R13 Y R14 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6, R16R17N-ALQUILO C2-C6; R15 ES ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; Ar ES FENILO, NAFTILO OPCIONALMENTE SUSTITUIDO CON Ph-ALQUILO C0-C6, HET-ALQUILO C0-C6, ALQUILO C1-C6, NR13R14, ENTRE OTROS. SON COMPUESTOS PREFERIDOS (6-RS)-6-[N-(N-BENZOFURAN-2-OIL-L-LEUCINIL)AMINO]-1,3-DIOXEPIN-5-ONA, (6-RS)-6-[N-[N-(5,6-DIMETOXIBENZOFURAN-2-OIL-L-LEUCINIL]-AMINO]-1,3-DIOXEPIN-5-ONA, (6RS)-6[N-[N-(N-BENZOTIOFEN-2-OIL-L-LEUCINIL)AMINO]-1,3-DIOXEPIN-5-ONA, ENTRE OTROS. EL COMPUESTO I ES UN INHIBIDOR DE PROTEASAS DE PREFERENCIA CISTEINA O SERINA PROTEASAS Y PUEDE SER UTIL PARA EL TRATAMIENTO DE UNA ENFERMEDAD CARACTERIZADA POR PERDIDA OSEA, OSTEOPOROSIS, PERIODONTITIS, GINGIVITIS, ARTRITIS REUMATOIDEREFERS TO 1,3-DIOXEPIN-5-ONA WITH A 7-MEMBER RING OF FORMULA I, WHERE: R1-R8, R11, R16, R17, R` SON H, C1-C6 ALKYL, C2-C6 ALKENYL, ALKINYL C2-C6, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R9 IS C3-C6 ALKYL, Ar, HET, CH (R10) Ar, CH (R10) OAr, NR10R11, CH (R10) NR11R12; R10 IS H, C2-C6 ALKYNYL, C2-C6 ALKYNYL, C3-C11-CYCLOALKYL C0-C6 ALKYL, C0-C6 Ar-ALKYL, C2-C6 Ar-ALKENYL, OPTIONALLY REPLACED WITH OR13, SR13, NR13R14, N (R ') CO2R', AMONG OTHERS; R12 IS R15, R15C (O), R15C (S), R15OC (O), R15OC (O) NR11CH (R10) (CO); R13 AND R14 ARE H, C1-C6 ALKYL, C2-C6 ALKENYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL, R16R17N-C2-C6 ALKYL; R15 IS C1-C6 ALKYL, C2-C6 ALKENYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; Ar IS PHENYL, NAPHTHYLL OPTIONALLY SUBSTITUTED WITH Ph-ALKYL C0-C6, HET-ALKYL C0-C6, ALKYL C1-C6, NR13R14, AMONG OTHERS. THE PREFERRED COMPOUNDS ARE (6-RS) -6- [N- (N-BENZOFURAN-2-OIL-L-LEUKINYL) AMINO] -1,3-DIOXEPIN-5-ONA, (6-RS) -6- [N - [N- (5,6-DIMETOXIBENZOFURAN-2-OIL-L-LEUCINIL] -AMINO] -1,3-DIOXEPIN-5-ONA, (6RS) -6 [N- [N- (N-BENZOTIOFEN-2 -OIL-L-LEUKINYL) AMINO] -1,3-DIOXEPIN-5-ONA, AMONG OTHERS COMPOUND I IS AN INHIBITOR OF PROTEASES OF PREFERENCE CYSTEINE OR SERINE PROTEASES AND MAY BE USEFUL FOR THE TREATMENT OF A DISEASE CHARACTERIZED BY LOSS OSEA, OSTEOPOROSIS, PERIODONTITIS, GINGIVITIS, RHEUMATOID ARTHRITIS

PE2000000226A 1999-03-16 2000-03-16 1,3-DIOXEPIN-5-ONA WITH A 7-MEMBER RING AS PROTEASE INHIBITORS PE20001564A1 (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20001564A1 true PE20001564A1 (en) 2001-02-08

Family

ID=22416114

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000226A PE20001564A1 (en) 1999-03-16 2000-03-16 1,3-DIOXEPIN-5-ONA WITH A 7-MEMBER RING AS PROTEASE INHIBITORS

Country Status (9)

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

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
JP2003513924A (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
WO2001034600A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1232155A4 (en) 1999-11-10 2002-11-20 Smithkline Beecham Corp Protease inhibitors
CZ20023168A3 (en) 2000-03-21 2003-02-12 Smithkline Beecham Corporation Protease inhibitors
JP2005515254A (en) 2002-01-17 2005-05-26 スミスクライン ビーチャム コーポレーション Cycloalkylketoamide derivatives useful as cathepsin K inhibitors
JP2004196696A (en) * 2002-12-18 2004-07-15 Kyowa Hakko Kogyo Co Ltd Prophylactic or therapeutic agent for arthritis
PL2714675T3 (en) * 2011-05-27 2019-07-31 Lexicon Pharmaceuticals, Inc. 4h-thieno[3,2-c]chromene-based inhibitors of notum pectinacetylesterase and methods of 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
EP0603769B1 (en) * 1992-12-25 1998-09-16 Mitsubishi Chemical Corporation Alpha-Aminoketone derivatives

Also Published As

Publication number Publication date
WO2000054769A1 (en) 2000-09-21
UY26026A1 (en) 2000-10-31
JP2002539160A (en) 2002-11-19
HK1043534A1 (en) 2002-09-20
AU3888200A (en) 2000-10-04
AR022927A1 (en) 2002-09-04
CO5180542A1 (en) 2002-07-30
EP1161237A1 (en) 2001-12-12
EP1161237A4 (en) 2002-03-27

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