NO318910B1 - Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat - Google Patents

Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat Download PDF

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Publication number
NO318910B1
NO318910B1 NO20013124A NO20013124A NO318910B1 NO 318910 B1 NO318910 B1 NO 318910B1 NO 20013124 A NO20013124 A NO 20013124A NO 20013124 A NO20013124 A NO 20013124A NO 318910 B1 NO318910 B1 NO 318910B1
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Norway
Prior art keywords
methyl
carboxylic acid
azepan
amide
butyl
Prior art date
Application number
NO20013124A
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English (en)
Norwegian (no)
Other versions
NO20013124D0 (no
NO20013124L (no
Inventor
Daniel Frank Veber
Dennis Shinji Yamashita
Jr Robert Wells Marquis
Maxwell David Cummings
Yu Ru
Scott Kevin Thompson
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Smithkline Beecham Corp
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Publication date
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of NO20013124D0 publication Critical patent/NO20013124D0/no
Publication of NO20013124L publication Critical patent/NO20013124L/no
Publication of NO318910B1 publication Critical patent/NO318910B1/no

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • A61P19/08Drugs 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]
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P33/06Antimalarials
    • 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
    • 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
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    • 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
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    • 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
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    • 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
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    • C07D405/02Heterocyclic 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
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    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D495/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
NO20013124A 1998-12-23 2001-06-22 Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat NO318910B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11363698P 1998-12-23 1998-12-23
US16458199P 1999-11-10 1999-11-10
PCT/US1999/030730 WO2000038687A1 (en) 1998-12-23 1999-12-21 Protease inhibitors

Publications (3)

Publication Number Publication Date
NO20013124D0 NO20013124D0 (no) 2001-06-22
NO20013124L NO20013124L (no) 2001-06-22
NO318910B1 true NO318910B1 (no) 2005-05-23

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Family Applications (1)

Application Number Title Priority Date Filing Date
NO20013124A NO318910B1 (no) 1998-12-23 2001-06-22 Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat

Country Status (24)

Country Link
US (2) US20020147188A1 (es)
EP (1) EP1158986A4 (es)
JP (1) JP2002533397A (es)
KR (1) KR100630986B1 (es)
CN (1) CN1253441C (es)
AT (1) ATE411294T1 (es)
AU (1) AU768565B2 (es)
BR (1) BR9916488A (es)
CA (1) CA2356671A1 (es)
CZ (1) CZ20012277A3 (es)
DE (1) DE69939752D1 (es)
DZ (1) DZ2977A1 (es)
ES (1) ES2315456T3 (es)
GC (1) GC0000178A (es)
HK (1) HK1043536A1 (es)
HU (1) HUP0104768A3 (es)
IL (2) IL143142A0 (es)
NO (1) NO318910B1 (es)
NZ (1) NZ511710A (es)
PE (1) PE20001340A1 (es)
PL (1) PL350132A1 (es)
TR (1) TR200101869T2 (es)
UY (1) UY25874A1 (es)
WO (1) WO2000038687A1 (es)

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US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
WO2001034599A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1229914A4 (en) * 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
WO2001034600A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2003513928A (ja) * 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 プロテアーゼ阻害剤
JP2003513922A (ja) * 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 プロテアーゼ阻害剤
AU1474601A (en) * 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
EP1231922A4 (en) * 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
JP2003513926A (ja) * 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 プロテアーゼ阻害剤
JP2003533432A (ja) * 1999-11-10 2003-11-11 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
WO2001034153A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034157A1 (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
NZ520588A (en) 2000-03-21 2004-06-25 Smithkline Beecham Corp Protease inhibitors
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EP1320370A4 (en) * 2000-09-01 2008-10-22 Smithkline Beecham Corp TREATMENT METHOD
HUP0301964A3 (en) * 2000-11-22 2007-09-28 Smithkline Beecham Corp Protease inhibitors
PT1370260E (pt) 2001-02-20 2011-02-01 Chugai Pharmaceutical Co Ltd Azóis como inibidores da malonil-coa-descarboxilase úteis como moduladores metabólicos
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
EP1401453A4 (en) * 2001-05-17 2005-04-06 Smithkline Beecham Corp PROTEASE INHIBITORS
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
EP1511745A4 (en) * 2002-05-22 2006-11-15 Smithkline Beecham Corp PROTEASE INHIBITORS
EP1534292A4 (en) * 2002-05-22 2008-04-02 Smithkline Beecham Corp PROTEASE INHIBITORS
KR100962972B1 (ko) 2002-07-26 2010-06-09 주식회사유한양행 1-페닐피페리딘-3-온 유도체 및 그의 제조방법
WO2004033445A1 (en) * 2002-10-08 2004-04-22 Merck Frosst Canada & Co. 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
SI3345895T1 (sl) 2003-04-11 2020-03-31 Ptc Therapeutics, Inc. Spojina 1,2,4-oksadiazol benzojske kisline in njena uporaba za supresijo nesmiselne in zdravljenje bolezni
CA2533749C (en) 2003-08-01 2012-07-10 Chugai Seiyaku Kabushiki Kaisha Piperidine compounds useful as malonyl-coa decarboxylase inhibitors
EP1653944B1 (en) 2003-08-01 2010-11-10 Chugai Seiyaku Kabushiki Kaisha Heterocyclic compounds useful as malonyl-coa decarboxylase inhibitors
EP1658071B1 (en) 2003-08-01 2008-09-10 Chugai Seiyaku Kabushiki Kaisha Cyanoguanidine-based azole compounds useful as malonyl-coa decarboxylase inhibitors
CN1910175A (zh) * 2004-01-08 2007-02-07 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
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JP2003513922A (ja) * 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 プロテアーゼ阻害剤
AU1474601A (en) * 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
JP2003513928A (ja) * 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 プロテアーゼ阻害剤
WO2001034599A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034153A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034600A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1229914A4 (en) * 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
EP1235577A4 (en) * 1999-11-10 2003-04-09 Smithkline Beecham Corp PROTEASE INHIBITORS
JP2003513926A (ja) * 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 プロテアーゼ阻害剤
NL1013996C2 (nl) * 1999-12-30 2001-07-03 Innas Free Piston Bv Vrijezuiger aggregaat voor opwekken van hydraulische energie.

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AU1941100A (en) 2000-07-31
HUP0104768A2 (hu) 2002-04-29
DZ2977A1 (fr) 2004-03-15
CN1350458A (zh) 2002-05-22
CA2356671A1 (en) 2000-07-06
HUP0104768A3 (en) 2002-05-28
IL143142A0 (en) 2002-04-21
CZ20012277A3 (cs) 2001-11-14
AU768565B2 (en) 2003-12-18
US20020147188A1 (en) 2002-10-10
CN1253441C (zh) 2006-04-26
EP1158986A1 (en) 2001-12-05
ATE411294T1 (de) 2008-10-15
EP1158986A4 (en) 2002-03-27
PL350132A1 (en) 2002-11-04
WO2000038687A1 (en) 2000-07-06
KR20010089677A (ko) 2001-10-08
NO20013124D0 (no) 2001-06-22
JP2002533397A (ja) 2002-10-08
BR9916488A (pt) 2001-10-09
KR100630986B1 (ko) 2006-10-09
NZ511710A (en) 2003-12-19
TR200101869T2 (tr) 2002-01-21
US20030225061A1 (en) 2003-12-04
NO20013124L (no) 2001-06-22
ES2315456T3 (es) 2009-04-01
IL143142A (en) 2006-08-20
HK1043536A1 (zh) 2002-09-20
UY25874A1 (es) 2001-08-27
GC0000178A (en) 2006-03-29
PE20001340A1 (es) 2001-01-28
DE69939752D1 (de) 2008-11-27

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