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PE20011374A1 - 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS - Google Patents

4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS

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
Spanish (es)
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/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • A61P33/12Schistosomicides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic 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
    • C07D223/12Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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, MALARIAREFERS TO 4-AMINO-AZEPAN-3-ONA COMPOUNDS OF FORMULA IA WHERE R1 IS R4 (R ') NCHR3-CO-; R4 (R ') NC (R3) (R' '' ') - CO-, GROUP a; R2 IS C1-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL, R9C (O) - AMONG OTHERS; R3 IS C1-C6 ALKYL; R4 IS R5C (O) -; R5 IS C0-C6 HET-ALKYL SUCH AS PIPERIDINYL-ETHYL, BENZO [1,3] DIOXOLYL, FURANIL, AMONG OTHERS; R9 IS C1-C6 ALKYL, C3-C6 CYCLOALKYL-C0-C6 ALKYL, Ar-C0-C6 ALKYL, AMONG OTHERS; R ', R' ', R' '' ARE H; R '' '' IS C1-C6 ALKYL, C3-C6 CYCLOALKYL-C0-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS; n IS 1 TO 5. ARE PREFERRED COMPOUNDS {(S) -1 - [(3-FLUORO-BENZENOSULFONIL) -3-OXO-AZEPAN-4-ILCARBAMOIL] -3-METHYL-1-BUTYL}-BENZOFURAN ACID AMIDE- 2-CARBOXYL; 3- [OXO-1- (PYRIDINE-2-SULFONIL) -AZEPAN-4-OL] AMIDE OF ACID (S) -4-METHYL-2- [3-PIPERIDIN-1-ILPROPANOYLAMINO) -PENTANOICO, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. COMPOUND I IS AN INHIBITOR OF CYSTINE OR SERINE PROTEASE AND MAY BE USEFUL FOR THE TREATMENT OF DISEASES WITH BONE LOSS, PERIODONTITIS, GINGIVITIS, OSTEOARTHRITIS, RHEUMATOID ARTHRITIS, SCHISTOSOMIASIS, MALARIA

PE2001000566A 2000-06-14 2001-06-14 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS PE20011374A1 (en)

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 (en) 2002-04-07

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000566A PE20011374A1 (en) 2000-06-14 2001-06-14 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS

Country Status (25)

Country Link
EP (1) EP1307204A4 (en)
JP (1) JP2004503502A (en)
KR (1) KR20030008220A (en)
CN (1) CN1444481A (en)
AP (1) AP2002002671A0 (en)
AR (1) AR032622A1 (en)
AU (1) AU2001268407A1 (en)
BG (1) BG107327A (en)
BR (1) BR0111693A (en)
CA (1) CA2412353A1 (en)
CZ (1) CZ20024086A3 (en)
EA (1) EA200300018A1 (en)
EC (1) ECSP024388A (en)
HU (1) HUP0301231A2 (en)
IL (1) IL153421A0 (en)
MA (1) MA25758A1 (en)
MX (1) MXPA02012442A (en)
NO (1) NO20025786L (en)
NZ (1) NZ522965A (en)
OA (1) OA12288A (en)
PE (1) PE20011374A1 (en)
PL (1) PL360508A1 (en)
SK (1) SK17592002A3 (en)
WO (1) WO2001095911A1 (en)
ZA (1) ZA200209808B (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001034159A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
HUP0301964A3 (en) * 2000-11-22 2007-09-28 Smithkline Beecham Corp Protease inhibitors
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
WO2002066035A2 (en) 2001-02-20 2002-08-29 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-coa decarboxylase inhibitors useful as metabolic modulators
US20040157828A1 (en) * 2001-05-17 2004-08-12 Ren Xie Protease inhibitors
GB0220187D0 (en) * 2002-08-30 2002-10-09 Novartis Ag Organic compounds
EP1653944B1 (en) * 2003-08-01 2010-11-10 Chugai Seiyaku Kabushiki Kaisha Heterocyclic compounds useful as malonyl-coa decarboxylase inhibitors
JP4773960B2 (en) 2003-08-01 2011-09-14 中外製薬株式会社 Cyanoguanidine-type azole compounds useful as malonyl-CoA decarboxylase inhibitors
ES2309563T3 (en) 2003-08-01 2008-12-16 Chugai Seiyaku Kabushiki Kaisha PIPERIDINE COMPOUNDS USED AS INHIBITORS FROM MALONIL COENZIMA TO DESCARBOXYLASE.
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
CN103275070A (en) * 2013-05-10 2013-09-04 郑彪 Tetracyclic compound for adjusting proliferation of mononuclear cells and application of tetracyclic compound
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 (en) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Cysteine protease inhibitors.
TR200101869T2 (en) * 1998-12-23 2002-01-21 Smithkline Beecham Corporation Protease Inhibitors.
JP2003513956A (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
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2004509083A (en) * 2000-09-01 2004-03-25 スミスクライン・ビーチャム・コーポレイション Method of treatment
HUP0301964A3 (en) * 2000-11-22 2007-09-28 Smithkline Beecham Corp Protease inhibitors
US20040157828A1 (en) * 2001-05-17 2004-08-12 Ren Xie Protease inhibitors

Also Published As

Publication number Publication date
JP2004503502A (en) 2004-02-05
EP1307204A4 (en) 2004-06-02
NZ522965A (en) 2004-06-25
OA12288A (en) 2003-12-12
CA2412353A1 (en) 2001-12-20
BR0111693A (en) 2004-04-06
WO2001095911A1 (en) 2001-12-20
IL153421A0 (en) 2003-07-06
SK17592002A3 (en) 2003-05-02
PL360508A1 (en) 2004-09-06
CZ20024086A3 (en) 2003-05-14
BG107327A (en) 2003-07-31
NO20025786L (en) 2003-02-12
KR20030008220A (en) 2003-01-24
EA200300018A1 (en) 2003-06-26
EP1307204A1 (en) 2003-05-07
ZA200209808B (en) 2004-07-09
AU2001268407A1 (en) 2001-12-24
HUP0301231A2 (en) 2003-08-28
ECSP024388A (en) 2003-02-06
CN1444481A (en) 2003-09-24
AP2002002671A0 (en) 2002-12-31
MXPA02012442A (en) 2003-04-25
AR032622A1 (en) 2003-11-19
NO20025786D0 (en) 2002-12-02
MA25758A1 (en) 2003-04-01

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