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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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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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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    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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

Publications (2)

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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)
CR (1) CR20190200A (enExample)
CY (1) CY1123346T1 (enExample)
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DO (1) DOP2019000073A (enExample)
EA (1) EA036176B1 (enExample)
EC (1) ECSP19027780A (enExample)
ES (1) ES2818583T3 (enExample)
HR (1) HRP20201175T1 (enExample)
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IL (1) IL265298B (enExample)
JO (1) JOP20190052A1 (enExample)
LT (1) LT3515910T (enExample)
MA (1) MA46268B1 (enExample)
MX (2) MX381898B (enExample)
PE (1) PE20190909A1 (enExample)
PH (1) PH12019500615A1 (enExample)
PL (1) PL3515910T3 (enExample)
PT (1) PT3515910T (enExample)
RS (1) RS60764B1 (enExample)
SI (1) SI3515910T1 (enExample)
SM (1) SMT202000481T1 (enExample)
SV (1) SV2019005857A (enExample)
TW (1) TW201813967A (enExample)
UA (1) UA123558C2 (enExample)
WO (1) WO2018055040A1 (enExample)

Families Citing this family (8)

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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
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
CA3134173A1 (en) * 2019-04-10 2020-10-15 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphatidylinositol 3-kinase inhibitors
EP3980010A4 (en) 2019-06-04 2023-06-07 Arcus Biosciences, Inc. 2,3,5-TRISUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS
CN114258393B (zh) * 2020-07-21 2024-11-22 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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HUP0303538A2 (hu) * 2000-12-21 2005-02-28 Bristol-Myers Squibb Co. Tirozin kinázok Tec családjának tiazolil-vegyület inhibitorai és ezeket tartalmazó gyógyszerkészítmények
GB0320197D0 (en) * 2003-08-28 2003-10-01 Novartis Ag Organic compounds
US20090233896A1 (en) * 2005-06-09 2009-09-17 Arrington Kenneth L Inhibitors of checkpoint kinases
TW200911798A (en) * 2007-08-02 2009-03-16 Amgen Inc PI3 kinase modulators and methods of use
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
WO2013012918A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
CA2846431A1 (en) 2011-08-29 2013-03-07 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
CA2850763A1 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
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
US11352359B2 (en) 2013-07-02 2022-06-07 Rhizen Pharmaceuticals Ag PI3K protein kinase inhibitors
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
SG11201610745XA (en) 2014-06-27 2017-01-27 Rhizen Pharmaceuticals Sa Substituted chromene derivatives as selective dual inhibitors of pi3 delta and gamma protein kinases

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

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