JP6441831B2 - カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤 - Google Patents

カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤 Download PDF

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JP6441831B2
JP6441831B2 JP2015562120A JP2015562120A JP6441831B2 JP 6441831 B2 JP6441831 B2 JP 6441831B2 JP 2015562120 A JP2015562120 A JP 2015562120A JP 2015562120 A JP2015562120 A JP 2015562120A JP 6441831 B2 JP6441831 B2 JP 6441831B2
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alkylene
alkyl
ring
independently selected
haloalkyl
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JP2016515110A5 (enExample
JP2016515110A (ja
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ラルフ アンデルスケーヴィッツ
ラルフ アンデルスケーヴィッツ
マティアス グラウエルト
マティアス グラウエルト
マルク グルンドル
マルク グルンドル
トルステン ウースト
トルステン ウースト
アレクサンダー パウチ
アレクサンダー パウチ
シュテファン ペーテルス
シュテファン ペーテルス
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015562120A 2013-03-14 2014-03-12 カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤 Active JP6441831B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP13159242.0 2013-03-14
EP13159242 2013-03-14
EP13170006 2013-05-31
EP13170006.4 2013-05-31
PCT/EP2014/054827 WO2014140091A1 (en) 2013-03-14 2014-03-12 Substituted 2-aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

Publications (3)

Publication Number Publication Date
JP2016515110A JP2016515110A (ja) 2016-05-26
JP2016515110A5 JP2016515110A5 (enExample) 2017-04-13
JP6441831B2 true JP6441831B2 (ja) 2018-12-19

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JP2015562120A Active JP6441831B2 (ja) 2013-03-14 2014-03-12 カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤

Country Status (4)

Country Link
US (2) US8877775B2 (enExample)
EP (1) EP2970252B1 (enExample)
JP (1) JP6441831B2 (enExample)
WO (1) WO2014140091A1 (enExample)

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MY183427A (en) * 2013-12-17 2021-02-18 Stella Pharma Corp A method for producing 2-fluoro-4-borono-l-phenylalanine, and precursor of 2-fluoro-4-borono-l-phenylalanine
NO2699580T3 (enExample) 2014-01-24 2018-02-24
CN108047240B (zh) * 2014-09-12 2020-08-04 勃林格殷格翰国际有限公司 组织蛋白酶c的螺环化合物抑制剂
ES2912276T3 (es) 2015-04-07 2022-05-25 Ela Pharma Ltd Composiciones para tratar y/o prevenir necrosis celular o tisular que seleccionan como diana específicamente catepsina C y/o CELA1 y/o CELA3A y/o enzimas estructuralmente relacionadas con las mismas
HRP20250115T1 (hr) 2018-03-01 2025-05-23 Astrazeneca Ab Farmaceutski pripravci koji sadrže (2s)-{(1s)-1-cijano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil} -1,4-oksazepan-2-karboksamid
CA3106269A1 (en) * 2018-07-17 2020-01-23 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis
CN110452139B (zh) * 2019-08-23 2021-07-09 黄河三角洲京博化工研究院有限公司 一种2-甲基-3-溴-6-甲砜基苯腈的制备方法
EP4182700A4 (en) 2020-07-20 2024-11-13 Insmed Incorporated METHODS FOR EXTRACTING NEUTROPHIL SERINE PROTEASES AND TREATMENT OF DIPETIDYL PEPTIDASE-1-MEDIATED DISEASES
TWI834476B (zh) * 2022-01-27 2024-03-01 禾榮科技股份有限公司 中間體、其製備方法和製備藥物的方法
US20230234973A1 (en) * 2022-01-27 2023-07-27 Heron Neutron Medical Corp. Intermediate, preparing method thereof, and method of preparing drug
EP4646265A1 (en) 2023-01-06 2025-11-12 Insmed Incorporated Novel, reversible dpp1 inhibitors and uses thereof
WO2025002093A1 (zh) * 2023-06-27 2025-01-02 西藏海思科制药有限公司 一种dpp1抑制剂中间体及其制备方法及在医药中的用途

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US4125727A (en) 1976-10-18 1978-11-14 American Cyanamid Company Method of preparing imidazoisoindolediones
WO2001047886A1 (en) * 1999-12-24 2001-07-05 F. Hoffmann-La Roche Ag Nitrile derivatives as cathepsin k inhibitors
US6960597B2 (en) 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
WO2002069901A2 (en) 2001-03-02 2002-09-12 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
JP2006527704A (ja) 2003-06-18 2006-12-07 プロザイメックス・アクティーゼルスカブ プロテアーゼ阻害剤
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
US20060223846A1 (en) * 2005-03-08 2006-10-05 Dyatkin Alexey B Aza-bridged-bicyclic amino acid derivatives as alpha4 integrin antagonists
JP5240201B2 (ja) 2007-10-12 2013-07-17 富士通株式会社 Ｉｐ電話自動試験システム及び方法
WO2009074829A1 (en) 2007-12-12 2009-06-18 Astrazeneca Ab Peptidyl nitriles and use thereof as dipeptidyl peptidase i inhibitors
EA201190235A1 (ru) 2009-05-07 2012-05-30 Астразенека Аб Замещенные 1-цианоэтилгетероциклилкарбоксамидные соединения 750
WO2010142985A1 (en) * 2009-06-10 2010-12-16 Astrazeneca Ab Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761
WO2011154677A1 (en) * 2010-06-09 2011-12-15 Astrazeneca Ab Substituted n-[1-cyano-2-(phenyl)ethyl] 1-aminocycloalk-1-ylcarboxamide compounds - 760
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
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Also Published As

Publication number Publication date
US20140275159A1 (en) 2014-09-18
EP2970252A1 (en) 2016-01-20
EP2970252B1 (en) 2020-06-03
JP2016515110A (ja) 2016-05-26
US8877775B2 (en) 2014-11-04
WO2014140091A1 (en) 2014-09-18
US9073869B2 (en) 2015-07-07
US20140378504A1 (en) 2014-12-25

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