JP6703553B2 - Pad4阻害剤としてのベンゾイミダゾール誘導体 - Google Patents

Pad4阻害剤としてのベンゾイミダゾール誘導体 Download PDF

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JP6703553B2
JP6703553B2 JP2017560547A JP2017560547A JP6703553B2 JP 6703553 B2 JP6703553 B2 JP 6703553B2 JP 2017560547 A JP2017560547 A JP 2017560547A JP 2017560547 A JP2017560547 A JP 2017560547A JP 6703553 B2 JP6703553 B2 JP 6703553B2
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methyl
alkyl
indol
ethyl
mmol
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JP2018520105A5 (enExample
JP2018520105A (ja
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ドミニク・アマンズ
スティーブン・ジョン・アトキンソン
マイケル・デイビッド・バーカー
マシュー・キャンベル
ハワ・ディアロ
クレメント・ドゥオー
ニール・スチュアート・ガートン
ジョン・リドル
ジェシカ・ファニー・ルノー
ロバート・ジョン・シェパード
アン・ルイーズ・ウォーカー
クリストファー・ローランド・ウェラウェイ
デイビッド・マシュー・ウィルソン
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GlaxoSmithKline Intellectual Property Development Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06Peri-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Materials For Medical Uses (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
JP2017560547A 2015-05-21 2016-05-19 Pad4阻害剤としてのベンゾイミダゾール誘導体 Active JP6703553B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562164906P 2015-05-21 2015-05-21
US62/164,906 2015-05-21
PCT/IB2016/000761 WO2016185279A1 (en) 2015-05-21 2016-05-19 Benzoimidazole derivatives as pad4 inhibitors

Publications (3)

Publication Number Publication Date
JP2018520105A JP2018520105A (ja) 2018-07-26
JP2018520105A5 JP2018520105A5 (enExample) 2019-06-20
JP6703553B2 true JP6703553B2 (ja) 2020-06-03

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JP2017560547A Active JP6703553B2 (ja) 2015-05-21 2016-05-19 Pad4阻害剤としてのベンゾイミダゾール誘導体

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US (2) US10407407B2 (enExample)
EP (1) EP3298003B1 (enExample)
JP (1) JP6703553B2 (enExample)
KR (1) KR20180005250A (enExample)
CN (1) CN107849015B (enExample)
AR (1) AR106863A1 (enExample)
AU (1) AU2016264958B2 (enExample)
BR (1) BR112017024678A2 (enExample)
CA (2) CA3199601A1 (enExample)
EA (1) EA033680B1 (enExample)
ES (1) ES2945314T3 (enExample)
IL (2) IL255666A (enExample)
MX (1) MX387321B (enExample)
TW (1) TW201706263A (enExample)
WO (1) WO2016185279A1 (enExample)

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WO2018022897A1 (en) 2016-07-27 2018-02-01 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
US11026937B2 (en) 2016-09-12 2021-06-08 Padlock Therapeutics, Inc. Heteroaryl inhibitors of PAD4
PL3684767T3 (pl) * 2017-09-22 2024-10-14 Jubilant Epipad LLC Związki heterocykliczne jako inhibitory pad
PL3697785T3 (pl) * 2017-10-18 2023-08-07 Jubilant Epipad LLC Związki imidazopirydynowe jako inhibitory pad
AU2018362046B2 (en) 2017-11-06 2023-04-13 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
SI3704120T1 (sl) 2017-11-24 2024-07-31 Jubilant Episcribe Llc Heterociklične spojine kot inhibitorji prmt5
JP7269943B2 (ja) 2018-01-08 2023-05-09 エフ. ホフマン-ラ ロシュ アーゲー Magl阻害剤としてのオクタヒドロピリド[1,2-アルファ]ピラジン
WO2019152883A1 (en) * 2018-02-02 2019-08-08 Padforward Llc Inhibitors of protein arginine deiminases
EP3765453A1 (en) 2018-03-13 2021-01-20 Jubilant Prodel LLC Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation
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US11524959B1 (en) * 2018-08-08 2022-12-13 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes
TW202019411A (zh) * 2018-08-08 2020-06-01 美商必治妥美雅史谷比公司 作為pad4抑制劑之經取代苯并咪唑
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KR20220137694A (ko) * 2020-02-06 2022-10-12 브리스톨-마이어스 스큅 컴퍼니 면역억제제로서 유용한 마크로시클릭 pad4 억제제
TW202140477A (zh) 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環pad4抑制劑
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Also Published As

Publication number Publication date
IL255666A (en) 2018-01-31
BR112017024678A2 (pt) 2018-07-31
US20200095227A1 (en) 2020-03-26
JP2018520105A (ja) 2018-07-26
ES2945314T3 (es) 2023-06-30
AR106863A1 (es) 2018-02-28
EP3298003A1 (en) 2018-03-28
EP3298003B1 (en) 2023-04-19
TW201706263A (zh) 2017-02-16
IL278916A (en) 2021-01-31
AU2016264958B2 (en) 2020-10-29
CA3199601A1 (en) 2016-11-24
MX2017014714A (es) 2018-01-25
MX387321B (es) 2025-03-11
KR20180005250A (ko) 2018-01-15
EA201792517A1 (ru) 2018-04-30
AU2016264958A1 (en) 2017-12-07
US10815218B2 (en) 2020-10-27
US10407407B2 (en) 2019-09-10
CN107849015B (zh) 2021-03-19
CN107849015A (zh) 2018-03-27
EA033680B1 (ru) 2019-11-15
CA2986199C (en) 2023-07-18
WO2016185279A1 (en) 2016-11-24
CA2986199A1 (en) 2016-11-24
US20180297983A1 (en) 2018-10-18

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