EA201792517A1 - Производные бензоимидазола в качестве ингибиторов pad4 - Google Patents

Производные бензоимидазола в качестве ингибиторов pad4

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Publication number
EA201792517A1
EA201792517A1 EA201792517A EA201792517A EA201792517A1 EA 201792517 A1 EA201792517 A1 EA 201792517A1 EA 201792517 A EA201792517 A EA 201792517A EA 201792517 A EA201792517 A EA 201792517A EA 201792517 A1 EA201792517 A1 EA 201792517A1
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EA
Eurasian Patent Office
Prior art keywords
benzoimidazole
derivatives
pad4 inhibitors
lupus erythematosus
pad4
Prior art date
Application number
EA201792517A
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English (en)
Other versions
EA033680B1 (ru
Inventor
Доминик Аманс
Стивен Джон Аткинсон
Майкл Дэвид Баркер
Мэттью Кэмпбелл
Хава Диалло
Клемент Дуалт
Нил Стюарт Гартон
Джон Лиддл
Джессика Фанни Рено
Роберт Джон Шеппард
Энн Луис Уолкер
Кристофер Роланд Уэллавей
Дэвид Мэттью Уилсон
Original Assignee
Глаксосмиткляйн Интеллекчуал Проперти Девелопмент Лимитед
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Publication of EA201792517A1 publication Critical patent/EA201792517A1/ru
Publication of EA033680B1 publication Critical patent/EA033680B1/ru

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    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • 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
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    • 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]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/06—Peri-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Materials For Medical Uses (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Соединение формулы (I)где X, Y, Rи R-Rимеют значение, определённое в данной заявке, и его соли являются ингибиторами PAD4 и могут применяться в лечении различных заболеваний, например ревматоидного артрита, васкулита, системной красной волчанки, язвенного колита, ракового заболевания, муковисцидоза, астмы, кожной формы красной волчанки и псориаза.
EA201792517A 2015-05-21 2016-05-19 Производные бензоимидазола в качестве ингибиторов pad4 EA033680B1 (ru)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
EA201792517A1 true EA201792517A1 (ru) 2018-04-30
EA033680B1 EA033680B1 (ru) 2019-11-15

Family

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Family Applications (1)

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EA201792517A EA033680B1 (ru) 2015-05-21 2016-05-19 Производные бензоимидазола в качестве ингибиторов pad4

Country Status (15)

Country Link
US (2) US10407407B2 (ru)
EP (1) EP3298003B1 (ru)
JP (1) JP6703553B2 (ru)
KR (1) KR20180005250A (ru)
CN (1) CN107849015B (ru)
AR (1) AR106863A1 (ru)
AU (1) AU2016264958B2 (ru)
BR (1) BR112017024678A2 (ru)
CA (2) CA3199601A1 (ru)
EA (1) EA033680B1 (ru)
ES (1) ES2945314T3 (ru)
IL (2) IL255666A (ru)
MX (1) MX2017014714A (ru)
TW (1) TW201706263A (ru)
WO (1) WO2016185279A1 (ru)

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WO2021057910A1 (zh) * 2019-09-27 2021-04-01 南京药捷安康生物科技有限公司 肽酰精氨酸脱亚胺酶抑制剂及其用途
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BR112017024678A2 (pt) 2018-07-31
ES2945314T3 (es) 2023-06-30
US20200095227A1 (en) 2020-03-26
CN107849015A (zh) 2018-03-27
AU2016264958A1 (en) 2017-12-07
AU2016264958B2 (en) 2020-10-29
IL255666A (en) 2018-01-31
AR106863A1 (es) 2018-02-28
CA2986199A1 (en) 2016-11-24
WO2016185279A1 (en) 2016-11-24
EA033680B1 (ru) 2019-11-15
CA2986199C (en) 2023-07-18
US10815218B2 (en) 2020-10-27
MX2017014714A (es) 2018-01-25
EP3298003A1 (en) 2018-03-28
CA3199601A1 (en) 2016-11-24
US20180297983A1 (en) 2018-10-18
TW201706263A (zh) 2017-02-16
KR20180005250A (ko) 2018-01-15
JP6703553B2 (ja) 2020-06-03
EP3298003B1 (en) 2023-04-19
US10407407B2 (en) 2019-09-10
CN107849015B (zh) 2021-03-19
IL278916A (en) 2021-01-31
JP2018520105A (ja) 2018-07-26

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