JP7776453B2 - 血漿カリクレイン阻害剤 - Google Patents

血漿カリクレイン阻害剤

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Publication number
JP7776453B2
JP7776453B2 JP2022577145A JP2022577145A JP7776453B2 JP 7776453 B2 JP7776453 B2 JP 7776453B2 JP 2022577145 A JP2022577145 A JP 2022577145A JP 2022577145 A JP2022577145 A JP 2022577145A JP 7776453 B2 JP7776453 B2 JP 7776453B2
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Japan
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mmol
chloro
methyl
title compound
mixture
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JP2022577145A
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English (en)
Japanese (ja)
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JPWO2021257353A5 (https=
JP2023531411A (ja
JP2023531411A5 (https=
Inventor
ジャブリ，サルマン
オガワ，アンソニー・ケン
ジンツ，クリストファー・ジェイ
ヒックス，ジャクリーン・ディー
チェン，アラン・シー
ガオ，イン－デュオ
ヤン，ソン
バオ，ジェンミン
ヘイズ，ドナ・エー・エー・ダブリュ
ラング，サイモン・ビー
タオカ，ブランドン・エム
ティアン，マオカン
シェイン－ナンス，ガレン，ポール
クアン，ロンゼ
ロンバルド，マシュー・ジェイ
ウー，チーカイ
ザオ，チーチャン
Original Assignee
メルク・シャープ・アンド・ドーム・エルエルシー
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Publication of JP2023531411A publication Critical patent/JP2023531411A/ja
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Publication of JP2023531411A5 publication Critical patent/JP2023531411A5/ja
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Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • C07D471/04—Ortho-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
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
JP2022577145A 2020-06-16 2021-06-10 血漿カリクレイン阻害剤 Active JP7776453B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063039873P 2020-06-16 2020-06-16
US63/039,873 2020-06-16
PCT/US2021/036706 WO2021257353A1 (en) 2020-06-16 2021-06-10 Plasma kallikrein inhibitors

Publications (4)

Publication Number Publication Date
JP2023531411A JP2023531411A (ja) 2023-07-24
JPWO2021257353A5 JPWO2021257353A5 (https=) 2024-05-08
JP2023531411A5 JP2023531411A5 (https=) 2024-05-08
JP7776453B2 true JP7776453B2 (ja) 2025-11-26

Family

ID=79268261

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022577145A Active JP7776453B2 (ja) 2020-06-16 2021-06-10 血漿カリクレイン阻害剤

Country Status (10)

Country Link
US (1) US12459927B2 (https=)
EP (1) EP4164634A4 (https=)
JP (1) JP7776453B2 (https=)
KR (1) KR102931248B1 (https=)
CN (1) CN115989224B (https=)
AU (1) AU2021292449A1 (https=)
BR (1) BR112022025528A2 (https=)
CA (1) CA3182626A1 (https=)
MX (1) MX2022016321A (https=)
WO (1) WO2021257353A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230038526A (ko) 2020-07-10 2023-03-20 머크 샤프 앤드 돔 엘엘씨 혈장 칼리크레인 억제제
US20230416227A1 (en) * 2020-09-10 2023-12-28 Merck Sharp & Dohme Llc Plasma kallikrein inhibitors
CN116120272A (zh) * 2022-12-31 2023-05-16 淮北师范大学 一种合成咯菌腈中间体2,2-二氟-1,3-苯并二噁茂-4-甲醛的方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
JP2017507160A (ja) 2014-03-07 2017-03-16 バイオクリスト ファーマスーティカルズ，インコーポレイテッドＢｉｏｃｒｙｓｔ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． ヒト血漿カリクレイン阻害剤
JP2018535963A (ja) 2015-10-27 2018-12-06 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 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体
WO2019012003A1 (en) 2017-07-13 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES
JP2019517464A (ja) 2016-05-31 2019-06-24 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
JP2017507160A (ja) 2014-03-07 2017-03-16 バイオクリスト ファーマスーティカルズ，インコーポレイテッドＢｉｏｃｒｙｓｔ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． ヒト血漿カリクレイン阻害剤
JP2018535963A (ja) 2015-10-27 2018-12-06 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 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体
JP2019517464A (ja) 2016-05-31 2019-06-24 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体
WO2019012003A1 (en) 2017-07-13 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Xie, Zhouling et al.，Discovery and development of plasma kallikrein inhibitors for multiple diseases，European Journal of Medicinal Chemistry，2020年，190，112137

Also Published As

Publication number Publication date
CN115989224B (zh) 2025-02-25
US12459927B2 (en) 2025-11-04
EP4164634A1 (en) 2023-04-19
KR20230024981A (ko) 2023-02-21
MX2022016321A (es) 2023-01-24
WO2021257353A1 (en) 2021-12-23
CN115989224A (zh) 2023-04-18
AU2021292449A1 (en) 2023-02-02
EP4164634A4 (en) 2024-08-14
KR102931248B1 (ko) 2026-03-03
JP2023531411A (ja) 2023-07-24
US20230286958A1 (en) 2023-09-14
CA3182626A1 (en) 2021-12-23
BR112022025528A2 (pt) 2023-01-17

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