AU2004266740B2 - Cathepsin cysteine protease inhibitors - Google Patents

Cathepsin cysteine protease inhibitors Download PDF

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Publication number
AU2004266740B2
AU2004266740B2 AU2004266740A AU2004266740A AU2004266740B2 AU 2004266740 B2 AU2004266740 B2 AU 2004266740B2 AU 2004266740 A AU2004266740 A AU 2004266740A AU 2004266740 A AU2004266740 A AU 2004266740A AU 2004266740 B2 AU2004266740 B2 AU 2004266740B2
Authority
AU
Australia
Prior art keywords
alkyl
amino
cyanocyclopropyl
pharmaceutically acceptable
fluoro
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2004266740A
Other languages
English (en)
Other versions
AU2004266740A1 (en
Inventor
Jacques Yves Gauthier
Vouy Linh Truong
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Canada Inc
Original Assignee
Merck Frosst Canada Ltd
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 Merck Frosst Canada Ltd filed Critical Merck Frosst Canada Ltd
Publication of AU2004266740A1 publication Critical patent/AU2004266740A1/en
Application granted granted Critical
Publication of AU2004266740B2 publication Critical patent/AU2004266740B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/45Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C255/46Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of non-condensed 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
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P19/08Drugs 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/26Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2004266740A 2003-08-21 2004-08-19 Cathepsin cysteine protease inhibitors Ceased AU2004266740B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US49682503P 2003-08-21 2003-08-21
US60/496,825 2003-08-21
PCT/CA2004/001524 WO2005019161A1 (en) 2003-08-21 2004-08-19 Cathepsin cysteine protease inhibitors

Publications (2)

Publication Number Publication Date
AU2004266740A1 AU2004266740A1 (en) 2005-03-03
AU2004266740B2 true AU2004266740B2 (en) 2010-08-26

Family

ID=34216040

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2004266740A Ceased AU2004266740B2 (en) 2003-08-21 2004-08-19 Cathepsin cysteine protease inhibitors

Country Status (7)

Country Link
US (1) US7312353B2 (enExample)
EP (1) EP1673336B1 (enExample)
JP (1) JP4553899B2 (enExample)
CN (1) CN1839114A (enExample)
AU (1) AU2004266740B2 (enExample)
CA (1) CA2535359A1 (enExample)
WO (1) WO2005019161A1 (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021487A1 (en) * 2003-08-27 2005-03-10 Merck Frosst Canada Ltd. Cathepsin inhibitors
CA2548600A1 (en) * 2003-12-12 2005-06-23 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
US8013186B2 (en) * 2004-12-01 2011-09-06 Virobay, Inc. Haloalkyl containing compounds as cysteine protease inhibitors
EP1841730A4 (en) * 2005-01-19 2010-10-27 Merck Frosst Canada Ltd CATHEPSIN K INHIBITORS AND ATHEROSCLEROSIS
WO2006076796A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and obesity
JP2008546651A (ja) * 2005-06-14 2008-12-25 メルク フロスト カナダ リミテツド モノアミンオキシダーゼa及びbの可逆的阻害剤
US20090264479A1 (en) * 2005-07-26 2009-10-22 Cameron Black Papain Family Cysteine Protease Inhibitors for the Treatment of Parasitic Diseases
AU2006301896A1 (en) * 2005-10-12 2007-04-19 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
EP2132173B1 (en) * 2007-02-26 2015-10-07 Merck Sharp & Dohme Corp. Formulations for cathepsin k inhibitors
CN101668736B (zh) * 2007-04-02 2013-06-12 默克弗罗斯特加拿大有限公司 用于制备组织蛋白酶k抑制剂的酰胺化反应
WO2010023931A1 (ja) 2008-08-29 2010-03-04 興和株式会社 1-アダマンチルアゼチジン-2-オン誘導体及びこれを含有する医薬
GB2463788B (en) 2008-09-29 2010-12-15 Amira Pharmaceuticals Inc Heteroaryl antagonists of prostaglandin D2 receptors
TWI519530B (zh) 2009-02-20 2016-02-01 艾伯維德國有限及兩合公司 羰醯胺化合物及其作為鈣蛋白酶(calpain)抑制劑之用途
WO2016027285A2 (en) * 2014-08-22 2016-02-25 Alkem Laboratories Ltd. Bicyclic heteroaryl amides as cathepsin cysteine protease inhibitors
EP3302448B1 (en) 2015-06-04 2023-10-25 Aurigene Oncology Limited Substituted heterocyclyl derivatives as cdk inhibitors
EP3342765B1 (en) * 2015-08-29 2021-09-15 Sunshine Lake Pharma Co., Ltd. Cathepsin k inhibitor and application thereof
AU2020250933A1 (en) 2019-04-05 2021-10-28 Centre Hospitalier Régional Et Universitaire De Brest Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning
CN115637275A (zh) * 2022-10-14 2023-01-24 天津药明康德新药开发有限公司 一种(s)-2-(4-溴苯基)丙酸的制备方法

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2002069901A2 (en) * 2001-03-02 2002-09-12 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors

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Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002069901A2 (en) * 2001-03-02 2002-09-12 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors

Also Published As

Publication number Publication date
US7312353B2 (en) 2007-12-25
WO2005019161A1 (en) 2005-03-03
AU2004266740A1 (en) 2005-03-03
CN1839114A (zh) 2006-09-27
EP1673336A1 (en) 2006-06-28
EP1673336A4 (en) 2007-05-30
JP2007502781A (ja) 2007-02-15
CA2535359A1 (en) 2005-03-03
EP1673336B1 (en) 2014-06-04
US20060287373A1 (en) 2006-12-21
JP4553899B2 (ja) 2010-09-29

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Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired