EA202190462A1 - Индольные и азаиндольные ингибиторы ферментов pad - Google Patents

Индольные и азаиндольные ингибиторы ферментов pad

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Publication number
EA202190462A1
EA202190462A1 EA202190462A EA202190462A EA202190462A1 EA 202190462 A1 EA202190462 A1 EA 202190462A1 EA 202190462 A EA202190462 A EA 202190462A EA 202190462 A EA202190462 A EA 202190462A EA 202190462 A1 EA202190462 A1 EA 202190462A1
Authority
EA
Eurasian Patent Office
Prior art keywords
azaindole
indole
enzyme inhibitors
pad enzyme
pad
Prior art date
Application number
EA202190462A
Other languages
English (en)
Inventor
Анураг С. Сривастава
Роберт Дж. Черни
Кехионг Нгу
Original Assignee
Бристол-Маерс Сквибб Компани
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Бристол-Маерс Сквибб Компани filed Critical Бристол-Маерс Сквибб Компани
Publication of EA202190462A1 publication Critical patent/EA202190462A1/ru

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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
    • C07D471/08—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
    • C07D471/04—Ortho-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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines 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
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I), применимым в качестве ингибиторов PAD4, их композициям и способам лечения PAD4-связанных нарушенийпричем каждое из кольца A, L, Q, R1, R2, R3, R4, R7 и R8 вместе с другими переменными определено в настоящем описании.
EA202190462A 2018-08-08 2019-08-07 Индольные и азаиндольные ингибиторы ферментов pad EA202190462A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862715850P 2018-08-08 2018-08-08
PCT/US2019/045466 WO2020033520A1 (en) 2018-08-08 2019-08-07 Indole and azaindole inhibitors of pad enzymes

Publications (1)

Publication Number Publication Date
EA202190462A1 true EA202190462A1 (ru) 2021-06-03

Family

ID=67766306

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202190462A EA202190462A1 (ru) 2018-08-08 2019-08-07 Индольные и азаиндольные ингибиторы ферментов pad

Country Status (18)

Country Link
US (1) US11524959B1 (ru)
EP (1) EP3833440A1 (ru)
JP (1) JP2021534108A (ru)
KR (1) KR20210042934A (ru)
CN (1) CN112805067A (ru)
AR (1) AR115920A1 (ru)
AU (1) AU2019319835A1 (ru)
BR (1) BR112021002091A2 (ru)
CA (1) CA3108791A1 (ru)
CL (1) CL2021000296A1 (ru)
CO (1) CO2021001217A2 (ru)
EA (1) EA202190462A1 (ru)
IL (1) IL280650A (ru)
MX (1) MX2021001565A (ru)
PE (1) PE20211068A1 (ru)
SG (1) SG11202101174RA (ru)
TW (1) TW202019415A (ru)
WO (1) WO2020033520A1 (ru)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7447080B2 (ja) 2018-08-08 2024-03-11 ブリストル－マイヤーズ スクイブ カンパニー Ｐａｄ４阻害剤としての置換チエノピロール
CA3108791A1 (en) 2018-08-08 2020-02-13 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes
BR112022021963A2 (pt) * 2020-04-30 2022-12-13 Gilead Sciences Inc Inibidores macrocíclicos de peptidilarginina desiminases
CN111943947B (zh) * 2020-07-24 2021-04-30 重庆文理学院 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用
EP4267587A2 (en) * 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
EP4267562A1 (en) * 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9127003B2 (en) * 2012-07-26 2015-09-08 Glaxo Group Limited 2-(azaindol-2-yl)benzimidazoles as PAD4 inhibitors
US10407407B2 (en) 2015-05-21 2019-09-10 Glaxosmithkline Intellectual Property Development Limited Benzoimidazole derivatives as PAD4 inhibitors
AR107032A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
AR107030A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
CA3007025A1 (en) 2015-12-22 2017-06-29 Kancera Ab Bicyclic hydroxamic acids useful as inhibitors of mammalian histone deacetylase activity
ES2770102T3 (es) 2016-02-23 2020-06-30 Padlock Therapeutics Inc Inhibidores de heteroarilo de PAD4
ES2828623T3 (es) 2016-07-27 2021-05-27 Padlock Therapeutics Inc Inhibidores covalentes de PAD4
MA46193A (fr) 2016-09-12 2019-07-17 Padlock Therapeutics Inc Inhibiteurs hétéroaryles de pad4
CN110582489B (zh) 2017-06-30 2023-10-27 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
DK3697785T3 (da) 2017-10-18 2023-04-03 Jubilant Epipad LLC Imidazo-pyridine forbindelser som pad-inhibitorer
US20220348562A1 (en) 2018-08-08 2022-11-03 Bristol-Myers Squibb Company Benzimidazole inhibitors of pad enzymes
JP7447080B2 (ja) 2018-08-08 2024-03-11 ブリストル－マイヤーズ スクイブ カンパニー Ｐａｄ４阻害剤としての置換チエノピロール
PE20211067A1 (es) 2018-08-08 2021-06-09 Bristol Myers Squibb Co Benzimidazoles sustituidos como inhibidores de pad4
CA3108791A1 (en) 2018-08-08 2020-02-13 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes

Also Published As

Publication number Publication date
SG11202101174RA (en) 2021-03-30
TW202019415A (zh) 2020-06-01
BR112021002091A2 (pt) 2021-05-04
CA3108791A1 (en) 2020-02-13
CO2021001217A2 (es) 2021-02-26
US11524959B1 (en) 2022-12-13
MX2021001565A (es) 2021-04-19
CL2021000296A1 (es) 2021-06-25
AR115920A1 (es) 2021-03-10
AU2019319835A1 (en) 2021-03-25
CN112805067A (zh) 2021-05-14
EP3833440A1 (en) 2021-06-16
IL280650A (en) 2021-03-25
KR20210042934A (ko) 2021-04-20
JP2021534108A (ja) 2021-12-09
PE20211068A1 (es) 2021-06-09
WO2020033520A1 (en) 2020-02-13

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