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PE20001607A1 - 4-AMINO-4,5-DIHYDRO-BENZO [b] [1,4] DIOXOCIN-3-ONA AS PROTEASE INHIBITORS - Google Patents

4-AMINO-4,5-DIHYDRO-BENZO [b] [1,4] DIOXOCIN-3-ONA AS PROTEASE INHIBITORS

Info

Publication number
PE20001607A1
PE20001607A1 PE2000000283A PE0002832000A PE20001607A1 PE 20001607 A1 PE20001607 A1 PE 20001607A1 PE 2000000283 A PE2000000283 A PE 2000000283A PE 0002832000 A PE0002832000 A PE 0002832000A PE 20001607 A1 PE20001607 A1 PE 20001607A1
Authority
PE
Peru
Prior art keywords
alkyl
het
dioxocin
ona
benzo
Prior art date
Application number
PE2000000283A
Other languages
Spanish (es)
Inventor
Dennis Shinji Yamashita
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 PE20001607A1 publication Critical patent/PE20001607A1/en

Links

Classifications

    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D321/12—Eight-membered rings
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A 4-AMINO-4,5-DIHIDRO-BENZO[b][1,4]DIOXOCIN-3-ONA DE FORMULA I DONDE R1 ES R", R"SO2, R"OC(O), R"R`NC(O), R"OC(O)NR'CH(R6)C(O); R2 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, CICLOALQUIL C3-C6-ALQUILO C0-C6, ENTRE OTROS; R4 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R5 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R6 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, CICLOALQUILO C3-C6-ALQUILO C0-C6, Ar-ALQUILO C0-C6; R7 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R8 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, CICLOALQUIL C3-C6-ALQUILO C0-C6, ENTRE OTROS; R' ES H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R" ES ALQUILO C1-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6, Ar-ALQUENILO C2-C6, ENTRE OTROS; X ES O, S; Y ES O, S. SON COMPUESTOS PREFERIDOS [(S)-3-METIL-1-(4-OXO-2,3,4,5-TETRAHIDROBENZO[b][1,4]DIOXOCIN-3-ILCARBAMOIL)-BUTIL]-AMIDA DEL ACIDO QUINOLINA-2-CARBOXILICO, [(S)-3-METIL-1-(4-OXO-2,3,4,5-TETRAHIDROBENZO[b][1,4]DIOXO-CIN-3-ILCARBAMOIL)-BUTIL]-AMIDA DEL ACIDO BENZOFURANO-2-CARBOXILICO, ENTRE OTROS. EL COMPUESTO DE FORMULA I SON INHIBIDORES DE CISTEINA Y SERINA PROTEASA Y PUEDEN SER UTILES EN EL TRATAMIENTO DE OSTEOPOROSIS, PERIODONTITIS, GINGIVITISREFERS TO 4-AMINO-4,5-DIHYDRO-BENZO [b] [1,4] DIOXOCIN-3-ONA OF FORMULA I WHERE R1 IS R ", R" SO2, R "OC (O), R" R `NC (O), R" OC (O) NR'CH (R6) C (O); R2 IS H, C1-C6 ALKYL, C2-C6 ALKYL, C0-C6 Ar-ALKYL, C0-C6 HET-ALKYL ; R3 IS H, C1-C6 ALKYL, C2-C6 ALKYL, C2-C6 ALKYNYL, C3-C6 CYCLOALKYL-C0-C6 ALKYL, AMONG OTHERS; R4 IS H, C1-C6 ALKYL, C2-C6 ALKYL, Ar-ALKYL C0-C6, HET-C0-C6 ALKYL; R5 IS H, C1-C6 ALKYL, C2-C6 ALKENYL, C0-C6 Ar-ALKYL, C0-C6 HET-ALKYL; R6 IS H, C1-C6 ALKYL, C2 ALKYL -C6, C3-C6 CYCLOALKYL-C0-C6 ALKYL, Ar-C0-C6 ALKYL; R7 IS H, C1-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS; R8 IS H, C1-C6 ALKYL, C2-C6 ALKYL , C3-C6-ALKYL C3-C6-ALKYL C0-C6, AMONG OTHERS; R 'IS H, C1-C6 ALKYL, C2-C6 ALKENYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R "IS C1-C6 ALKYL , Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL, Ar-C2-C6 ALKYL, AMONG OTHERS; X IS O, S; Y ES O, S. PREFERRED COMPOUNDS ARE [(S) -3-METHYL-1- (4-OXO-2,3,4,5-TETRAHIDROBENZO [b] [1,4] DIOXOCIN-3-ILCARBAMOIL) -BUTIL ] -QUINOLINE-2-CARBOXYL ACID AMIDE, [(S) -3-METHYL-1- (4-OXO-2,3,4,5-TETRAHIDROBENZO [b] [1,4] DIOXO-CIN-3- ILCARBAMOIL) -BUTIL] -AMIDE OF BENZOFURAN-2-CARBOXYL ACID, AMONG OTHERS. THE COMPOUND OF FORMULA I ARE INHIBITORS OF CYSTEINE AND SERINE PROTEASE AND MAY BE USEFUL IN THE TREATMENT OF OSTEOPOROSIS, PERIODONTITIS, GINGIVITIS

PE2000000283A 1999-03-31 2000-03-31 4-AMINO-4,5-DIHYDRO-BENZO [b] [1,4] DIOXOCIN-3-ONA AS PROTEASE INHIBITORS PE20001607A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12725099P 1999-03-31 1999-03-31

Publications (1)

Publication Number Publication Date
PE20001607A1 true PE20001607A1 (en) 2001-03-07

Family

ID=22429122

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000283A PE20001607A1 (en) 1999-03-31 2000-03-31 4-AMINO-4,5-DIHYDRO-BENZO [b] [1,4] DIOXOCIN-3-ONA AS PROTEASE INHIBITORS

Country Status (8)

Country Link
EP (1) EP1173429A4 (en)
JP (1) JP2002540199A (en)
AU (1) AU4066900A (en)
CO (1) CO5180536A1 (en)
HK (1) HK1044758A1 (en)
PE (1) PE20001607A1 (en)
UY (1) UY26088A1 (en)
WO (1) WO2000058296A1 (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
CN113651795B (en) * 2021-09-14 2022-09-02 江西开源香料有限公司 Synthesis method of watermelon ketone

Family Cites Families (1)

* 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

Also Published As

Publication number Publication date
JP2002540199A (en) 2002-11-26
AU4066900A (en) 2000-10-16
WO2000058296A1 (en) 2000-10-05
HK1044758A1 (en) 2002-11-01
EP1173429A4 (en) 2002-06-19
EP1173429A1 (en) 2002-01-23
UY26088A1 (en) 2000-10-31
CO5180536A1 (en) 2002-07-30

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