[go: up one dir, main page]

PE20011374A1 - 4-amino-azepan-3-ona como inhibidores de proteasas - Google Patents

4-amino-azepan-3-ona como inhibidores de proteasas

Info

Publication number
PE20011374A1
PE20011374A1 PE2001000566A PE2001000566A PE20011374A1 PE 20011374 A1 PE20011374 A1 PE 20011374A1 PE 2001000566 A PE2001000566 A PE 2001000566A PE 2001000566 A PE2001000566 A PE 2001000566A PE 20011374 A1 PE20011374 A1 PE 20011374A1
Authority
PE
Peru
Prior art keywords
alkyl
azepan
amino
ona
het
Prior art date
Application number
PE2001000566A
Other languages
English (en)
Inventor
Maxwell D Cummings
Marquis
Dennin S Yamashita
Scott K Thompson
Daniel F Veber
Yu Ru
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 PE20011374A1 publication Critical patent/PE20011374A1/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

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)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (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

SE REFIERE A COMPUESTOS DE 4-AMINO-AZEPAN-3-ONA DE FORMULA IA DONDE R1 ES R4(R')NCHR3-CO-; R4(R')NC(R3)(R'''')-CO-, GRUPO a; R2 ES ALQUILO C1-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6, R9C(O)- ENTRE OTROS; R3 ES ALQUILO C1-C6; R4 ES R5C(O)-; R5 ES HET-ALQUILO C0-C6 TAL COMO PIPERIDINIL-ETILO, BENZO[1,3]DIOXOLILO, FURANILO, ENTRE OTROS; R9 ES ALQUILO C1-C6, CICLOALQUIL C3-C6-ALQUILO C0-C6, Ar-ALQUILO C0-C6, ENTRE OTROS; R' , R'', R''' SON H; R'''' ES ALQUILO C1-C6, CICLOALQUILO C3-C6-ALQUILO C0-C6, ALQUENILO C2-C6, ENTRE OTROS; n ES 1 A 5. SON COMPUESTOS PREFERIDOS {(S)-1-[(3-FLUORO-BENCENOSULFONIL)-3-OXO-AZEPAN-4-ILCARBAMOIL]-3-METIL-1-BUTIL}-AMIDA DE ACIDO BENZOFURAN-2-CARBOXILICO; 3-[OXO-1-(PIRIDINA-2-SULFONIL)-AZEPAN-4-OL]AMIDA DE ACIDO (S)-4-METIL-2-[3-PIPERIDIN-1-ILPROPANOILAMINO)-PENTANOICO, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. EL COMPUESTO I ES UN INHIBIDOR DE CISTEINA O SERINA PROTEASA Y PUEDE SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES CON PERDIDA OSEA, PERIODONTITIS, GINGIVITIS, OSTEOARTRITIS, ARTRITIS REUMATOIDE, ESQUISTOSOMIASIS, MALARIA
PE2001000566A 2000-06-14 2001-06-14 4-amino-azepan-3-ona como inhibidores de proteasas PE20011374A1 (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
PE20011374A1 true PE20011374A1 (es) 2002-04-07

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000566A PE20011374A1 (es) 2000-06-14 2001-06-14 4-amino-azepan-3-ona como 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
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034159A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
BR0115473A (pt) * 2000-11-22 2004-09-28 Smithkline Beecham Corp Inibidores de protease
EP1370260B1 (en) 2001-02-20 2010-11-24 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
JP2004527575A (ja) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害物質
ES2353306T3 (es) 2003-08-01 2011-03-01 Chugai Seiyaku Kabushiki Kaisha Compuestos heterocíclicos útiles como inhibidores de la malonil-coa-descarboxilasa.
ES2314491T3 (es) 2003-08-01 2009-03-16 Chugai Seiyaku Kabushiki Kaisha Compuestos azol basados en cianoguanidina utiles como inhibidores de la manonil-coa descaraboxilasa.
DE602004014937D1 (de) 2003-08-01 2008-08-21 Chugai Pharmaceutical Co Ltd Piperidin-verbindungen als malonyl-coa decarboxylase-hemmer
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.
KR100630986B1 (ko) * 1998-12-23 2006-10-09 스미스클라인 비참 코포레이션 프로테아제 억제제
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1235577A4 (en) * 1999-11-10 2003-04-09 Smithkline Beecham Corp PROTEASE INHIBITORS
EP1320370A4 (en) * 2000-09-01 2008-10-22 Smithkline Beecham Corp TREATMENT METHOD
BR0115473A (pt) * 2000-11-22 2004-09-28 Smithkline Beecham Corp Inibidores de protease
JP2004527575A (ja) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害物質

Also Published As

Publication number Publication date
CA2412353A1 (en) 2001-12-20
NZ522965A (en) 2004-06-25
CZ20024086A3 (cs) 2003-05-14
BR0111693A (pt) 2004-04-06
KR20030008220A (ko) 2003-01-24
EA200300018A1 (ru) 2003-06-26
SK17592002A3 (sk) 2003-05-02
BG107327A (bg) 2003-07-31
IL153421A0 (en) 2003-07-06
AP2002002671A0 (en) 2002-12-31
MA25758A1 (fr) 2003-04-01
WO2001095911A1 (en) 2001-12-20
NO20025786L (no) 2003-02-12
EP1307204A1 (en) 2003-05-07
PL360508A1 (en) 2004-09-06
JP2004503502A (ja) 2004-02-05
ZA200209808B (en) 2004-07-09
AU2001268407A1 (en) 2001-12-24
OA12288A (en) 2003-12-12
EP1307204A4 (en) 2004-06-02
AR032622A1 (es) 2003-11-19
ECSP024388A (es) 2003-02-06
HUP0301231A2 (hu) 2003-08-28
CN1444481A (zh) 2003-09-24
NO20025786D0 (no) 2002-12-02
MXPA02012442A (es) 2003-04-25

Similar Documents

Publication Publication Date Title
PE20011233A1 (es) Compuestos alquil aminoazepan-3-ona como inhibidores de proteasas
PE20011374A1 (es) 4-amino-azepan-3-ona como inhibidores de proteasas
PE20010984A1 (es) Derivados de nitrilo como inhibidores de catepsina k
PE110899A1 (es) Derivados de acidos ariloxiarilsulfonilamino hidroxamicos
AR029870A1 (es) Proceso para la preparacion de amidas de octanoilo sustituido
PE73699A1 (es) Inhibidores de proteasas
PE71599A1 (es) Inhibidores de proteasas
PE20081583A1 (es) Agentes antibacterianos derivados de compuestos carbonilamino
AU4688301A (en) Stabilized pharmaceutical compositions containing calcium channel blockers
PE128799A1 (es) Quinolinas antimicrobianas y sus composiciones
PE20020786A1 (es) Derivados de azaindol antiviral
PE20021014A1 (es) Derivados de glutaramida sustituida con n-fenpropilciclopentilo como inhibidores de nep para fsad
DE69615058D1 (de) Metalloproteinase inhibitoren
PE64398A1 (es) Derivados de azetidinona
PE20050012A1 (es) Compuestos de benzopirano como inhibidores de la ciclooxigenasa-2
UY26820A1 (es) Derivados de ciclopentil-glutaramida como inhibidores de endopeptidasa neutra
PE20090548A1 (es) Compuestos aza-biciclohexano como inhibidores de trombina
PE20040666A1 (es) Derivados novedosos de piperidina
ES2062486T3 (es) 3-fenilbenzofuran-2-onas.
AR008621A1 (es) Un compuesto derivado de amina succinica, un procedimiento para llevar a cabo su preparacion y una composicion farmaceutica que comprende dichocompuesto
PE20050312A1 (es) Compuestos de peptidilo como inhibidores de catepsina s
PE20050160A1 (es) 3-aminopirrolidinas como inhibidores de la captacion de monoaminas
PE20001486A1 (es) Compuestos etereos anular de 7 a 14 miembros como inhibidores de proteasas
PE20001241A1 (es) Ciertas caprolactamas sustituidas, composiciones farmaceuticas que las contienen, y su uso en el tratamiento de tumores
HUT39966A (en) Insecticides containing as active substance acetilized sacharin-derivatives and process for production of this active substance

Legal Events

Date Code Title Description
FC Refusal