EA201990664A1 - Производные 5-[2-(пиридин-2-иламино)-1,3-тиазол-5-ил]-2,3-дигидро-1h-изоиндол-1-она и их применение в качестве двойных ингибиторов фосфатидилинозитол-3-киназ дельта и гамма - Google Patents

Производные 5-[2-(пиридин-2-иламино)-1,3-тиазол-5-ил]-2,3-дигидро-1h-изоиндол-1-она и их применение в качестве двойных ингибиторов фосфатидилинозитол-3-киназ дельта и гамма

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Publication number
EA201990664A1
EA201990664A1 EA201990664A EA201990664A EA201990664A1 EA 201990664 A1 EA201990664 A1 EA 201990664A1 EA 201990664 A EA201990664 A EA 201990664A EA 201990664 A EA201990664 A EA 201990664A EA 201990664 A1 EA201990664 A1 EA 201990664A1
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EA
Eurasian Patent Office
Prior art keywords
gamma
delta
phosphosididylinositol
isoindole
ylamino
Prior art date
Application number
EA201990664A
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English (en)
Other versions
EA036176B1 (ru
Inventor
Мэттью Перри
Константинос Карабелас
Миккаэль Могемарк
Петер Болд
Кристиан Тюркан
Антониос Никитидис
Йенс Петерсен
Ульф Бёрьессон
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Астразенека Аб
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Application filed by Астразенека Аб filed Critical Астразенека Аб
Publication of EA201990664A1 publication Critical patent/EA201990664A1/ru
Publication of EA036176B1 publication Critical patent/EA036176B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pulmonology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В заявке раскрыты некоторые новые соединения (включая их фармацевтически приемлемые соли), которые подавляют активность фосфатидилинозитол-3-киназы дельта (PI3Kδ) и фосфатидилинозитол-3-киназы гамма (PI3Kγ), их применимость в лечении и/или предупреждении клинических состояний, в том числе респираторных заболеваний, таких как астма и хроническое обструктивное заболевание легких (COPD), их применение в терапии, содержащие их фармацевтические композиции и способы получения таких соединений.
EA201990664A 2016-09-22 2017-09-21 Производные 5-[2-(пиридин-2-иламино)-1,3-тиазол-5-ил]-2,3-дигидро-1h-изоиндол-1-она и их применение в качестве двойных ингибиторов фосфатидилинозитол-3-киназ дельта и гамма EA036176B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662398006P 2016-09-22 2016-09-22
PCT/EP2017/073916 WO2018055040A1 (en) 2016-09-22 2017-09-21 5-[2-(pyridin-2-ylamino)-1,3-thiazol-5-yl]-2,3-dihydro-1 h-isoindol-1 -one derivatives and their use as dual inhibitors of phosphatidylinositol 3-kinase delta & gamma

Publications (2)

Publication Number Publication Date
EA201990664A1 true EA201990664A1 (ru) 2019-08-30
EA036176B1 EA036176B1 (ru) 2020-10-09

Family

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EA201990664A EA036176B1 (ru) 2016-09-22 2017-09-21 Производные 5-[2-(пиридин-2-иламино)-1,3-тиазол-5-ил]-2,3-дигидро-1h-изоиндол-1-она и их применение в качестве двойных ингибиторов фосфатидилинозитол-3-киназ дельта и гамма

Country Status (35)

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US (2) US10961236B2 (ru)
EP (1) EP3515910B1 (ru)
JP (1) JP6765516B2 (ru)
KR (1) KR102226098B1 (ru)
CN (1) CN109715623A (ru)
AR (1) AR109706A1 (ru)
AU (1) AU2017331940B2 (ru)
BR (1) BR112019004719A2 (ru)
CA (1) CA3036304A1 (ru)
CL (1) CL2019000707A1 (ru)
CO (1) CO2019003440A2 (ru)
CR (1) CR20190200A (ru)
CY (1) CY1123346T1 (ru)
DK (1) DK3515910T3 (ru)
DO (1) DOP2019000073A (ru)
EA (1) EA036176B1 (ru)
EC (1) ECSP19027780A (ru)
ES (1) ES2818583T3 (ru)
HR (1) HRP20201175T1 (ru)
HU (1) HUE051634T2 (ru)
IL (1) IL265298B (ru)
JO (1) JOP20190052A1 (ru)
LT (1) LT3515910T (ru)
MA (1) MA46268B1 (ru)
MX (2) MX2019003194A (ru)
PE (1) PE20190909A1 (ru)
PH (1) PH12019500615A1 (ru)
PL (1) PL3515910T3 (ru)
PT (1) PT3515910T (ru)
RS (1) RS60764B1 (ru)
SI (1) SI3515910T1 (ru)
SV (1) SV2019005857A (ru)
TW (1) TW201813967A (ru)
UA (1) UA123558C2 (ru)
WO (1) WO2018055040A1 (ru)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11396502B2 (en) 2018-11-13 2022-07-26 Incyte Corporation Substituted heterocyclic derivatives as PI3K inhibitors
WO2022017371A1 (zh) * 2020-07-21 2022-01-27 中国医药研究开发中心有限公司 具有磷脂酰肌醇3-激酶δ和γ的双重抑制剂活性的杂环化合物及其医药用途
WO2022023456A1 (en) 2020-07-29 2022-02-03 Astrazeneca Ab Pharmaceutical compositions comprising nano embedded microparticles and methods of use
CN116813608B (zh) * 2023-06-08 2024-03-22 英矽智能科技(上海)有限公司 噻唑类化合物及其应用

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DK1347971T3 (da) * 2000-12-21 2006-05-15 Bristol Myers Squibb Co Thiazolylinhibitorer af tyrosinkinaser fra Tec-familien
GB0305152D0 (en) * 2003-03-06 2003-04-09 Novartis Ag Organic compounds
GB0320197D0 (en) * 2003-08-28 2003-10-01 Novartis Ag Organic compounds
WO2006135604A2 (en) * 2005-06-09 2006-12-21 Merck & Co., Inc. Inhibitors of checkpoint kinases
ES2401557T3 (es) * 2007-08-02 2013-04-22 Amgen, Inc Moduladores de Pl3 cinasas y métodos de uso
UY33337A (es) 2010-10-18 2011-10-31 Respivert Ltd DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
JP6027611B2 (ja) 2011-07-19 2016-11-16 インフィニティー ファーマシューティカルズ, インコーポレイテッド 複素環式化合物及びその使用
CA2846431A1 (en) 2011-08-29 2013-03-07 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
CN104024257A (zh) 2011-10-04 2014-09-03 吉利德卡利斯托加有限责任公司 Pi3k的新的喹喔啉抑制剂
UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
AR094797A1 (es) 2013-02-15 2015-08-26 Almirall Sa Derivados de pirrolotriazina como inhibidores de pi3k
ES2672018T3 (es) 2013-07-02 2018-06-12 Rhizen Pharmaceuticals S.A. Inhibidores de proteína cinasa PI3K, particularmente inhibidores delta y/o gamma
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
CN106661029B (zh) 2014-06-27 2019-04-05 理森制药股份公司 作为PI3δ和γ蛋白激酶的选择性双重抑制剂的取代色烯衍生物

Also Published As

Publication number Publication date
US20210246130A1 (en) 2021-08-12
SV2019005857A (es) 2019-05-06
CN109715623A (zh) 2019-05-03
PH12019500615A1 (en) 2019-06-03
KR102226098B1 (ko) 2021-03-09
DK3515910T3 (da) 2020-08-31
MA46268B1 (fr) 2020-08-31
UA123558C2 (uk) 2021-04-21
LT3515910T (lt) 2020-10-12
CR20190200A (es) 2019-06-07
CO2019003440A2 (es) 2019-04-12
JP2019529445A (ja) 2019-10-17
HUE051634T2 (hu) 2021-03-01
AU2017331940A1 (en) 2019-05-02
MX2021004748A (es) 2021-06-08
HRP20201175T1 (hr) 2020-11-13
MA46268A (fr) 2019-07-31
DOP2019000073A (es) 2019-04-15
PL3515910T3 (pl) 2021-02-22
AU2017331940B2 (en) 2020-03-12
CY1123346T1 (el) 2022-03-24
WO2018055040A1 (en) 2018-03-29
SI3515910T1 (sl) 2020-09-30
ECSP19027780A (es) 2019-04-30
TW201813967A (zh) 2018-04-16
BR112019004719A2 (pt) 2019-05-28
EA036176B1 (ru) 2020-10-09
PE20190909A1 (es) 2019-06-26
PT3515910T (pt) 2020-09-16
ES2818583T3 (es) 2021-04-13
US20200308164A1 (en) 2020-10-01
IL265298A (en) 2019-05-30
AR109706A1 (es) 2019-01-16
US10961236B2 (en) 2021-03-30
JOP20190052A1 (ar) 2019-03-21
CL2019000707A1 (es) 2019-05-31
RS60764B1 (sr) 2020-10-30
CA3036304A1 (en) 2018-03-29
IL265298B (en) 2020-09-30
EP3515910B1 (en) 2020-07-15
JP6765516B2 (ja) 2020-10-07
KR20190049867A (ko) 2019-05-09
MX2019003194A (es) 2019-06-17
EP3515910A1 (en) 2019-07-31

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