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HUP0301231A2 - Proteáz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Proteáz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

Info

Publication number
HUP0301231A2
HUP0301231A2 HU0301231A HUP0301231A HUP0301231A2 HU P0301231 A2 HUP0301231 A2 HU P0301231A2 HU 0301231 A HU0301231 A HU 0301231A HU P0301231 A HUP0301231 A HU P0301231A HU P0301231 A2 HUP0301231 A2 HU P0301231A2
Authority
HU
Hungary
Prior art keywords
alkyl
group
het
general formula
hydrogen atom
Prior art date
Application number
HU0301231A
Other languages
English (en)
Inventor
Maxwell D. Cummings
Robert W. Marquis
Yu Ru
Scott K. Thompson
Daniel F. Veber
Dennis 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 HUP0301231A2 publication Critical patent/HUP0301231A2/hu

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    • 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

A találmány (IA) általános képletű vegyületekre - amelyek képletébenR1 jelentése általános képletű csoport; R2 jelentése 1-6 szénatomosalkilcsoport, Ar-(0-6 szénatomos alkil)- csoport, Het-(0-6 szénatomosalkil)-csoport, R9C(O)-, R9SO2-, R9R11NC(O)- vagy R9SO2R11NC(O)-általános képletű csoport; R3 jelentése 1-6 szénatomos alkilcsoport;R4 jelentése R5C(O)- általános képletű csoport; R5 jelentése Het-(0-6szénatomos alkil)-csoport; R9 jelentése 1-6 szénatomos alkilcsoport,(3-6 szénatomos cikloalkil)-(0-6 szénatomos alkil)-csoport, Ar-(0-6szénatomos alkil)-csoport és Het-(0-6 szénatomos alkil)-csoport; R11jelentése hidrogénatom, 1-6 szénatomos alkilcsoport, Ar -(0-6szénatomos alkil)-csoport és Het-(0-6 szénatomos alkil)-csoport; R'jelentése hidrogénatom; R< jelentése hidrogénatom; R<' jelentésehidrogénatom; R<< jelentése 1-6 szénatomos alkilcsoport, (3-6szénatomos cikloalkil)-(0-6 szénatomos alkil)-csoport, 2-6 szénatomosalkenilcsoport, 2-6 szénatomos alkinilcsoport, Ar-(0-6 szénatomosalkil)-csoport és Het-(0-6 szénatomos alkil)- csoport; és n értéke 1,2, 3, 4 vagy 5 valamint gyógyászatilag elfogadható sóik, hidrátjaik ésszolvátjaikra vonatkozik. A találmány magában foglalja a hatóanyagként(I) általános képletű vegyületeket tartalmazó gyógyszerkészítményeketés a vegyületek gyógyászati alkalmazását is. A találmány szerintivegyületek és gyógyszerkészítmények különösen jól alkalmazhatók azolyan betegségek kezelésére, amelyekben jelentős szerepet játszanakcisztein proteázok, különösen az excesszív csont- és porcvesztésesbetegségek, például az osteoporosis, a periodontitis és az arthritiskezelésére. Ó
HU0301231A 2000-06-14 2001-06-14 Proteáz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk HUP0301231A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US59384500A 2000-06-14 2000-06-14
PCT/US2001/019062 WO2001095911A1 (en) 2000-06-14 2001-06-14 Protease inhibitors

Publications (1)

Publication Number Publication Date
HUP0301231A2 true HUP0301231A2 (hu) 2003-08-28

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0301231A HUP0301231A2 (hu) 2000-06-14 2001-06-14 Proteáz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

Country Status (25)

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

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
PE20011374A1 (es) 2002-04-07
CN1444481A (zh) 2003-09-24
NO20025786D0 (no) 2002-12-02
MXPA02012442A (es) 2003-04-25

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