JP2017526716A - カテプシンｃのスピロ環状阻害剤 - Google Patents

カテプシンｃのスピロ環状阻害剤 Download PDF

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JP2017526716A
JP2017526716A JP2017513658A JP2017513658A JP2017526716A JP 2017526716 A JP2017526716 A JP 2017526716A JP 2017513658 A JP2017513658 A JP 2017513658A JP 2017513658 A JP2017513658 A JP 2017513658A JP 2017526716 A JP2017526716 A JP 2017526716A
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formula
mmol
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compound
pharmaceutically acceptable
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JP2017526716A5 (enExample
Inventor
ヴィクトル ヴィントニャック
ヴィクトル ヴィントニャック
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
アレクサンダー パウチ
アレクサンダー パウチ
Original Assignee
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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Publication of JP2017526716A publication Critical patent/JP2017526716A/ja
Publication of JP2017526716A5 publication Critical patent/JP2017526716A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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 three hetero rings
    • C07D491/20—Spiro-condensed 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2017513658A 2014-09-12 2015-09-08 カテプシンｃのスピロ環状阻害剤 Ceased JP2017526716A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14184613.9 2014-09-12
EP14184613 2014-09-12
PCT/EP2015/070449 WO2016038007A1 (en) 2014-09-12 2015-09-08 Spirocyclic inhibitors of cathepsin c

Related Child Applications (1)

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JP2017246001A Division JP6360961B2 (ja) 2014-09-12 2017-12-22 カテプシンｃのスピロ環状阻害剤

Publications (2)

Publication Number Publication Date
JP2017526716A true JP2017526716A (ja) 2017-09-14
JP2017526716A5 JP2017526716A5 (enExample) 2017-10-26

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JP2017513658A Ceased JP2017526716A (ja) 2014-09-12 2015-09-08 カテプシンｃのスピロ環状阻害剤
JP2017246001A Active JP6360961B2 (ja) 2014-09-12 2017-12-22 カテプシンｃのスピロ環状阻害剤

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US (3) US9540373B2 (enExample)
EP (2) EP3511331A1 (enExample)
JP (2) JP2017526716A (enExample)
KR (1) KR102510588B1 (enExample)
CN (2) CN107074870B (enExample)
AP (1) AP2017009733A0 (enExample)
AU (1) AU2015314355B2 (enExample)
BR (1) BR112017003433B1 (enExample)
CA (1) CA2960916C (enExample)
CL (1) CL2017000432A1 (enExample)
CO (1) CO2017002268A2 (enExample)
CY (1) CY1123033T1 (enExample)
DK (1) DK3191487T3 (enExample)
EA (1) EA031376B1 (enExample)
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HK (1) HK1255362A1 (enExample)
HR (1) HRP20191756T1 (enExample)
HU (1) HUE047208T2 (enExample)
IL (1) IL250262B (enExample)
LT (1) LT3191487T (enExample)
MX (2) MX367316B (enExample)
MY (1) MY188382A (enExample)
NZ (1) NZ728684A (enExample)
PE (1) PE20170438A1 (enExample)
PH (1) PH12017500453B1 (enExample)
PL (1) PL3191487T3 (enExample)
PT (1) PT3191487T (enExample)
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SA (1) SA517381064B1 (enExample)
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SI (1) SI3191487T1 (enExample)
TW (1) TWI687424B (enExample)
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WO (1) WO2016038007A1 (enExample)

Cited By (2)

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JP2021512904A (ja) * 2018-02-07 2021-05-20 インスメッド インコーポレイテッド Ａｎｃａ関連血管炎の治療のためのある種の（２ｓ）−ｎ−［（１ｓ）−１−シアノ−２−フェニル］−１，４−オキサゼパン−２−カルボキサミド
WO2023243601A1 (ja) * 2022-06-13 2023-12-21 モジュラス株式会社 アザシクロアルキルカルボニル環状アミン化合物

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CN110256429B (zh) * 2019-06-17 2021-06-22 广东药科大学 一种具有螺环结构的氨基嘧啶类化合物及其制备方法和应用
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CN114106005B (zh) * 2020-08-26 2025-08-01 西藏海思科制药有限公司 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途
AU2021381509A1 (en) * 2020-11-17 2023-06-22 Vertex Pharmaceuticals Incorporated Solid forms of 4-(5-(4-fluorophenyl)-6-tetrahydro-2h-pyran-4-yl)- 1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid
KR20230117738A (ko) * 2020-12-04 2023-08-09 레이스톤 바이오파마 컴퍼니 리미티드 카텝신 c의 소분자 억제제 및 이의 의약적 용도
CN114591315A (zh) * 2020-12-04 2022-06-07 瑞石生物医药有限公司 一种组织蛋白酶c小分子抑制剂
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WO2024088307A1 (zh) * 2022-10-26 2024-05-02 上海壹迪生物技术有限公司 一种新型肽基腈类化合物及其应用
JP2026503035A (ja) 2023-01-06 2026-01-27 インスメッド インコーポレイテッド 新規な可逆性ｄｐｐ１阻害剤及びその用途
WO2025214464A1 (en) * 2024-04-12 2025-10-16 Insmed Incorporated Crystalline forms of (s) -n- (1-cyano-2- (2-fluoro-4- (1' - (oxetan-3-yl) -3h-spiro [isobenzofuran-1, 4' -piperidin] -6-yl) phenyl) ethyl) -2-azabicyclo [2.2.2] octane-1-carboxamide
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