AU2016304464B2 - Pyrazole pyrimidine derivative and uses thereof - Google Patents

Pyrazole pyrimidine derivative and uses thereof Download PDF

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Publication number
AU2016304464B2
AU2016304464B2 AU2016304464A AU2016304464A AU2016304464B2 AU 2016304464 B2 AU2016304464 B2 AU 2016304464B2 AU 2016304464 A AU2016304464 A AU 2016304464A AU 2016304464 A AU2016304464 A AU 2016304464A AU 2016304464 B2 AU2016304464 B2 AU 2016304464B2
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Prior art keywords
compound
mmol
cancer
mixture
pyrazol
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AU2016304464A
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AU2016304464A1 (en
Inventor
Yinon Ben Neriah
Guy BRACHYA
Ido BURSTAIN
Dansu Li
Waleed MINZEL
Irit SNIR-ALKALAY
Joseph Vacca
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Yissum Research Development Co of Hebrew University of Jerusalem
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Yissum Research Development Co of Hebrew University of Jerusalem
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2016304464A 2015-08-04 2016-08-04 Pyrazole pyrimidine derivative and uses thereof Active AU2016304464B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2021200839A AU2021200839A1 (en) 2015-08-04 2021-02-10 Pyrazole pyrimidine derivative and uses thereof

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562200846P 2015-08-04 2015-08-04
US62/200,846 2015-08-04
US201562268750P 2015-12-17 2015-12-17
US62/268,750 2015-12-17
PCT/IL2016/050852 WO2017021969A1 (en) 2015-08-04 2016-08-04 Pyrazole pyrimidine derivative and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2021200839A Division AU2021200839A1 (en) 2015-08-04 2021-02-10 Pyrazole pyrimidine derivative and uses thereof

Publications (2)

Publication Number Publication Date
AU2016304464A1 AU2016304464A1 (en) 2018-02-22
AU2016304464B2 true AU2016304464B2 (en) 2020-11-19

Family

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AU2016304464A Active AU2016304464B2 (en) 2015-08-04 2016-08-04 Pyrazole pyrimidine derivative and uses thereof
AU2021200839A Abandoned AU2021200839A1 (en) 2015-08-04 2021-02-10 Pyrazole pyrimidine derivative and uses thereof

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AU2021200839A Abandoned AU2021200839A1 (en) 2015-08-04 2021-02-10 Pyrazole pyrimidine derivative and uses thereof

Country Status (23)

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US (4) US10376511B2 (enExample)
EP (1) EP3331877B1 (enExample)
JP (1) JP7083309B2 (enExample)
KR (1) KR102698366B1 (enExample)
CN (1) CN108137562B (enExample)
AU (2) AU2016304464B2 (enExample)
CA (1) CA2994644A1 (enExample)
CY (1) CY1124898T1 (enExample)
DK (1) DK3331877T3 (enExample)
ES (1) ES2901349T3 (enExample)
HR (1) HRP20211949T1 (enExample)
HU (1) HUE057607T2 (enExample)
IL (1) IL257282B (enExample)
LT (1) LT3331877T (enExample)
MX (1) MX384172B (enExample)
PL (1) PL3331877T3 (enExample)
PT (1) PT3331877T (enExample)
RS (1) RS62728B1 (enExample)
RU (1) RU2735522C2 (enExample)
SI (1) SI3331877T1 (enExample)
SM (1) SMT202100720T1 (enExample)
WO (1) WO2017021969A1 (enExample)
ZA (1) ZA201800671B (enExample)

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US10376511B2 (en) * 2015-08-04 2019-08-13 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Pyrazole pyrimidine derivative and uses thereof
MX394556B (es) * 2017-02-01 2025-03-24 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer.
TW202340194A (zh) 2017-02-16 2023-10-16 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
EP3749666A1 (en) * 2018-02-08 2020-12-16 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
BR112021024330A2 (pt) * 2019-06-03 2022-01-11 Biotheryx Inc Sais cristalinos não higroscópicos de um composto de pirazol, e composições farmacêuticas e uso dos mesmos
WO2021000957A1 (zh) * 2019-07-04 2021-01-07 北京国鸿生物医药科技有限公司 一种杂环化合物、其药物组合物及用途
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
EP4090159A4 (en) * 2020-01-13 2024-01-24 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd PYRAZOLYLPYRIMIDINES AND THEIR USE
WO2021155050A1 (en) * 2020-01-29 2021-08-05 Biotheryx, Inc. Kinase modulators, pharmaceutical compositions, and therapeutic applications
CN115362151B (zh) * 2020-03-26 2025-02-11 詹森药业有限公司 作为单酰基甘油脂肪酶调节剂的芳基哌啶
EP4313053A4 (en) * 2021-03-24 2025-03-05 Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd. Pyrazolylpyrimidines for treating malignant solid tumor
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11752151B2 (en) * 2021-07-12 2023-09-12 Buddhist Tzu Chi Medical Foundation Method for enhancing hair growth
US20230053307A1 (en) * 2021-07-19 2023-02-16 Buddhist Tzu Chi Medical Foundation Method for preventing or treating skin disorders and conditions
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2025199434A1 (en) * 2024-03-21 2025-09-25 Edgewood Oncology Methods of treating breast cancer using a pyrazole compound
WO2025199440A1 (en) * 2024-03-21 2025-09-25 Edgewood Oncology Methods of treating liposarcoma using a pyrazole compound

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WO2015058140A1 (en) * 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)

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ATE407132T1 (de) * 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
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US10376511B2 (en) 2015-08-04 2019-08-13 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Pyrazole pyrimidine derivative and uses thereof
MX394556B (es) * 2017-02-01 2025-03-24 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer.
EP3749666A1 (en) 2018-02-08 2020-12-16 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use

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Also Published As

Publication number Publication date
PT3331877T (pt) 2021-12-27
KR20180043794A (ko) 2018-04-30
US10960003B2 (en) 2021-03-30
HK1256535A1 (en) 2019-09-27
CA2994644A1 (en) 2017-02-09
EP3331877A1 (en) 2018-06-13
RU2018107668A (ru) 2019-09-05
IL257282A (en) 2018-03-29
NZ739511A (en) 2023-08-25
US20190365759A1 (en) 2019-12-05
SI3331877T1 (sl) 2022-02-28
ZA201800671B (en) 2020-05-27
RU2018107668A3 (enExample) 2020-01-13
KR102698366B1 (ko) 2024-08-26
CY1124898T1 (el) 2023-01-05
AU2016304464A1 (en) 2018-02-22
JP2018525441A (ja) 2018-09-06
ES2901349T3 (es) 2022-03-22
SMT202100720T1 (it) 2022-01-10
CN108137562B (zh) 2021-11-30
MX384172B (es) 2025-03-14
US20210251992A1 (en) 2021-08-19
AU2021200839A1 (en) 2021-03-04
WO2017021969A1 (en) 2017-02-09
LT3331877T (lt) 2022-01-10
US11925641B2 (en) 2024-03-12
JP7083309B2 (ja) 2022-06-10
IL257282B (en) 2021-06-30
CN108137562A (zh) 2018-06-08
HRP20211949T1 (hr) 2022-03-18
EP3331877B1 (en) 2021-09-22
US10376511B2 (en) 2019-08-13
US12514859B2 (en) 2026-01-06
DK3331877T3 (da) 2022-01-03
PL3331877T3 (pl) 2022-01-31
MX2018001395A (es) 2018-04-13
US20250049793A1 (en) 2025-02-13
US20180214447A1 (en) 2018-08-02
RU2735522C2 (ru) 2020-11-03
RS62728B1 (sr) 2022-01-31
HUE057607T2 (hu) 2022-06-28

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