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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (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
EP13170006.4 2013-05-31
EP13170006 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

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

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US10005794B2 (en) 2013-12-17 2018-06-26 Stella Pharma Corporation Production method for 2-fluoro-4-borono-L-phenylalanine, and precursor of 2-fluoro-4-borono-L-phenylalanine
NO2699580T3 (enExample) 2014-01-24 2018-02-24
PL3191487T3 (pl) * 2014-09-12 2020-03-31 Boehringer Ingelheim International Gmbh Spirocykliczne inhibitory katepsyny C
CA2981732C (en) 2015-04-07 2024-03-12 Boris Khalfin Compositions for treating and/or preventing cell or tissue necrosis specifically targeting cathepsin c and/or cela1 and/or cela3a and/or structurally related enzymes thereto
KR102738945B1 (ko) 2018-03-01 2024-12-04 아스트라제네카 에이비이 (2s)-n-｛(1s)-1-시아노-2-[4-(3-메틸-2-옥소-2,3-디하이드로-1,3-벤족사졸-5-일)페닐]에틸｝-1,4-옥사제판-2-카복스아미드를 포함하는 약학 조성물
KR20210032431A (ko) 2018-07-17 2021-03-24 인스메드 인코포레이티드 루푸스 신염을 치료하기 위한 특정 (2s)-n-[(1s)-1-시아노-2-페닐에틸]-1,4-옥사제판-2-카복스아미드
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
CA3181285A1 (en) 2020-07-20 2022-01-27 Jessica BASSO Methods for extracting neutrophil serine proteases and treating dipeptidyl peptidase 1-mediated conditions
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
CN120584108A (zh) 2023-01-06 2025-09-02 英斯梅德股份有限公司 新型可逆dpp1抑制剂及其用途
TW202500548A (zh) * 2023-06-27 2025-01-01 大陸商西藏海思科製藥有限公司 Dpp1抑制劑中間體及其製備方法及在醫藥中的用途

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KR100468254B1 (ko) * 1999-12-24 2005-01-27 에프. 호프만-라 로슈 아게 카텝신 ｋ 억제제로서의 니트릴 유도체
US6960597B2 (en) 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
EP1372655B1 (en) 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
US20070099958A1 (en) 2003-06-18 2007-05-03 Prozymex A/S Protease inhibitors
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
WO2006096807A1 (en) * 2005-03-08 2006-09-14 Janssen Pharmaceutica N.V. Aza-bridged-bicyclic amino acid derivatives as alpha 4 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
EA201000958A1 (ru) 2007-12-12 2010-12-30 Астразенека Аб Пептидилнитрилы и их применение в качестве ингибиторов дипептидилпептидазы i
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Also Published As

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

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