TW202019411A - 作為pad4抑制劑之經取代苯并咪唑 - Google Patents

作為pad4抑制劑之經取代苯并咪唑 Download PDF

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Publication number
TW202019411A
TW202019411A TW108128157A TW108128157A TW202019411A TW 202019411 A TW202019411 A TW 202019411A TW 108128157 A TW108128157 A TW 108128157A TW 108128157 A TW108128157 A TW 108128157A TW 202019411 A TW202019411 A TW 202019411A
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Taiwan
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substituted
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TW108128157A
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Chinese (zh)
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丹尼爾 S 嘉納
約翰 V 鄧希亞
克揚 吳
克里斯多福 安農奇亞多
約瑟夫 B 桑提拉
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美商必治妥美雅史谷比公司
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Publication of TW202019411A publication Critical patent/TW202019411A/zh

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    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW108128157A 2018-08-08 2019-08-07 作為pad4抑制劑之經取代苯并咪唑 TW202019411A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862715858P 2018-08-08 2018-08-08
US62/715,858 2018-08-08

Publications (1)

Publication Number Publication Date
TW202019411A true TW202019411A (zh) 2020-06-01

Family

ID=67766299

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108128157A TW202019411A (zh) 2018-08-08 2019-08-07 作為pad4抑制劑之經取代苯并咪唑

Country Status (18)

Country Link
US (1) US20220402950A1 (enExample)
EP (1) EP3833438B1 (enExample)
JP (1) JP7483678B2 (enExample)
KR (1) KR102825194B1 (enExample)
CN (1) CN112805066A (enExample)
AU (1) AU2019318415A1 (enExample)
BR (1) BR112021002089A2 (enExample)
CA (1) CA3108871A1 (enExample)
CL (1) CL2021000292A1 (enExample)
CO (1) CO2021001219A2 (enExample)
EA (1) EA202190464A1 (enExample)
ES (1) ES2973714T3 (enExample)
IL (1) IL280641A (enExample)
MX (1) MX2021001471A (enExample)
PE (1) PE20211067A1 (enExample)
SG (1) SG11202101176YA (enExample)
TW (1) TW202019411A (enExample)
WO (1) WO2020033488A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3833440A1 (en) 2018-08-08 2021-06-16 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes
ES2929200T3 (es) * 2018-08-08 2022-11-25 Bristol Myers Squibb Co Tienopirroles sustituidos como inhibidores de PAD4
ES2956090T3 (es) 2018-08-08 2023-12-13 Bristol Myers Squibb Co Inhibidores de bencimidazol de enzimas PAD
CN115298175B (zh) 2020-02-06 2024-05-07 百时美施贵宝公司 可用作免疫抑制剂的大环pad4抑制剂
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
MX2022013615A (es) 2020-04-30 2022-11-16 Gilead Sciences Inc Inhibidores de macrociclo de peptidilarginina deiminasas.
EP4267562A1 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
TW202233174A (zh) 2020-12-22 2022-09-01 美商基利科學股份有限公司 肽基精胺酸去亞胺酶之抑制劑
CN116492462B (zh) * 2023-02-03 2023-09-22 山东第一医科大学附属眼科医院(山东省眼科医院) Pad4抑制剂在防治角膜移植术后免疫排斥反应中的应用
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators
WO2026020127A2 (en) 2024-07-19 2026-01-22 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad2 modulators

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2611010C2 (ru) * 2012-07-26 2017-02-17 Глаксо Груп Лимитед 2-(Азаиндол-2-ил)бензимидазолы в качестве ингибиторов PAD4
WO2016185279A1 (en) 2015-05-21 2016-11-24 Glaxosmithkline Intellectual Property Development Limited Benzoimidazole derivatives as pad4 inhibitors
AR107030A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
AR107032A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
US10703741B2 (en) 2016-07-27 2020-07-07 Padlock Therapeutics, Inc. Covalent inhibitors of PAD4

Also Published As

Publication number Publication date
CL2021000292A1 (es) 2021-06-11
IL280641A (en) 2021-03-25
CN112805066A (zh) 2021-05-14
BR112021002089A2 (pt) 2021-05-04
MX2021001471A (es) 2021-04-28
CO2021001219A2 (es) 2021-02-17
AU2019318415A1 (en) 2021-03-25
SG11202101176YA (en) 2021-03-30
WO2020033488A1 (en) 2020-02-13
US20220402950A1 (en) 2022-12-22
EP3833438B1 (en) 2024-02-07
JP7483678B2 (ja) 2024-05-15
PE20211067A1 (es) 2021-06-09
JP2021534097A (ja) 2021-12-09
KR20210042932A (ko) 2021-04-20
ES2973714T3 (es) 2024-06-24
KR102825194B1 (ko) 2025-06-24
EP3833438A1 (en) 2021-06-16
EA202190464A1 (ru) 2021-06-16
CA3108871A1 (en) 2020-02-13

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