AU2017331940B2 - 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 - Google Patents

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 Download PDF

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Publication number
AU2017331940B2
AU2017331940B2 AU2017331940A AU2017331940A AU2017331940B2 AU 2017331940 B2 AU2017331940 B2 AU 2017331940B2 AU 2017331940 A AU2017331940 A AU 2017331940A AU 2017331940 A AU2017331940 A AU 2017331940A AU 2017331940 B2 AU2017331940 B2 AU 2017331940B2
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Australia
Prior art keywords
methyl
dihydro
thiazol
oxo
amino
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AU2017331940A
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AU2017331940A1 (en
Inventor
Peter Bold
Ulf BÖRJESSON
Konstantinos Karabelas
Mickael Mogemark
Antonios Nikitidis
Matthew Perry
Jens Petersen
Christian Tyrchan
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AstraZeneca AB
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AstraZeneca AB
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    • 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
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-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)
AU2017331940A 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 Ceased AU2017331940B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662398006P 2016-09-22 2016-09-22
US62/398,006 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

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AU2017331940A1 AU2017331940A1 (en) 2019-05-02
AU2017331940B2 true AU2017331940B2 (en) 2020-03-12

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US (2) US10961236B2 (enExample)
EP (1) EP3515910B1 (enExample)
JP (1) JP6765516B2 (enExample)
KR (1) KR102226098B1 (enExample)
CN (1) CN109715623A (enExample)
AR (1) AR109706A1 (enExample)
AU (1) AU2017331940B2 (enExample)
BR (1) BR112019004719A2 (enExample)
CA (1) CA3036304A1 (enExample)
CL (1) CL2019000707A1 (enExample)
CO (1) CO2019003440A2 (enExample)
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DO (1) DOP2019000073A (enExample)
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HR (1) HRP20201175T1 (enExample)
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MA (1) MA46268B1 (enExample)
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SV (1) SV2019005857A (enExample)
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Publication number Priority date Publication date Assignee Title
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020210379A1 (en) * 2019-04-10 2020-10-15 Hangzhou Zhengxiang Pharmaceuticals Co., Ltd. Phosphatidylinositol 3-kinase inhibitors
AU2020288610A1 (en) 2019-06-04 2022-01-27 Arcus Biosciences, Inc. 2,3,5-trisubstituted pyrazolo[1,5-a]pyrimidine compounds
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

Citations (1)

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WO2004078754A1 (en) * 2003-03-06 2004-09-16 Novartis Ag 5-phenylthiazole derivatives and their use as p13 kinase inhibitors

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ES2257461T3 (es) * 2000-12-21 2006-08-01 Bristol-Myers Squibb Company Inhibidores de tiazolilo de tirosina quinasas de la familia tec.
GB0320197D0 (en) * 2003-08-28 2003-10-01 Novartis Ag Organic compounds
JP2008543754A (ja) * 2005-06-09 2008-12-04 メルク エンド カムパニー インコーポレーテッド チェックポイントキナーゼの阻害剤
US7928140B2 (en) * 2007-08-02 2011-04-19 Amgen Inc. Benzothiazole PI3 kinase modulators for cancer treatment
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
EP2734520B1 (en) 2011-07-19 2016-09-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20141371A1 (es) 2011-08-29 2014-10-13 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
EP2763994A4 (en) 2011-10-04 2015-08-26 Gilead Calistoga Llc NEW QUINOXALINE INHIBITORS OF THE PI3K PATH
UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
TW201446767A (zh) 2013-02-15 2014-12-16 Almirall Sa 作為磷脂肌醇3-激酶抑製劑之吡咯並三嗪衍生物
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

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WO2004078754A1 (en) * 2003-03-06 2004-09-16 Novartis Ag 5-phenylthiazole derivatives and their use as p13 kinase inhibitors

Also Published As

Publication number Publication date
PT3515910T (pt) 2020-09-16
MA46268B1 (fr) 2020-08-31
CN109715623A (zh) 2019-05-03
UA123558C2 (uk) 2021-04-21
KR102226098B1 (ko) 2021-03-09
CR20190200A (es) 2019-06-07
KR20190049867A (ko) 2019-05-09
US20200308164A1 (en) 2020-10-01
US10961236B2 (en) 2021-03-30
PH12019500615A1 (en) 2019-06-03
MX381898B (es) 2025-03-13
ES2818583T3 (es) 2021-04-13
MX2019003194A (es) 2019-06-17
TW201813967A (zh) 2018-04-16
AU2017331940A1 (en) 2019-05-02
CA3036304A1 (en) 2018-03-29
EP3515910B1 (en) 2020-07-15
CL2019000707A1 (es) 2019-05-31
CY1123346T1 (el) 2022-03-24
SI3515910T1 (sl) 2020-09-30
JP2019529445A (ja) 2019-10-17
HUE051634T2 (hu) 2021-03-01
SV2019005857A (es) 2019-05-06
BR112019004719A2 (pt) 2019-05-28
RS60764B1 (sr) 2020-10-30
US20210246130A1 (en) 2021-08-12
SMT202000481T1 (it) 2020-11-10
EA201990664A1 (ru) 2019-08-30
EA036176B1 (ru) 2020-10-09
EP3515910A1 (en) 2019-07-31
DOP2019000073A (es) 2019-04-15
MX2021004748A (es) 2021-06-08
LT3515910T (lt) 2020-10-12
PL3515910T3 (pl) 2021-02-22
MA46268A (fr) 2019-07-31
ECSP19027780A (es) 2019-04-30
JOP20190052A1 (ar) 2019-03-21
HRP20201175T1 (hr) 2020-11-13
DK3515910T3 (da) 2020-08-31
IL265298A (en) 2019-05-30
CO2019003440A2 (es) 2019-04-12
IL265298B (en) 2020-09-30
WO2018055040A1 (en) 2018-03-29
PE20190909A1 (es) 2019-06-26
AR109706A1 (es) 2019-01-16
JP6765516B2 (ja) 2020-10-07

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