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)
  • 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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (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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Family Applications (2)

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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)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017021969A1 (en) * 2015-08-04 2017-02-09 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Pyrazole pyrimidine derivative and uses thereof
WO2018142393A1 (en) * 2017-02-01 2018-08-09 Yissum Research Development Company Of The Hebrew N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
BR112020016064A2 (pt) 2018-02-08 2020-12-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Compostos de heteroarila, composições farmacêuticas dos mesmos e seu uso terapêutico
TWI898556B (zh) 2018-07-13 2025-09-21 美商基利科學股份有限公司 吡咯并[1,2-b]嗒衍生物
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
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
CN119930611A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
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
EP4126840A1 (en) * 2020-03-26 2023-02-08 Janssen Pharmaceutica NV Aryl piperidines as monoacylglycerol lipase modulators
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
WO2025199440A1 (en) * 2024-03-21 2025-09-25 Edgewood Oncology Methods of treating liposarcoma using a pyrazole compound

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015058140A1 (en) * 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2430539C (en) 2000-12-05 2010-07-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
WO2005095357A2 (en) 2004-03-30 2005-10-13 Taisho Pharmaceutical Co., Ltd. Pyrimidine derivatives and methods of treatment related to the use thereof
JP2007145819A (ja) 2005-10-28 2007-06-14 Tanabe Seiyaku Co Ltd 医薬組成物
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
WO2007138277A1 (en) 2006-05-26 2007-12-06 Astrazeneca Ab 2-carbocycloamino-4-imidaz0lylpyrimidines as agents for the inhbition of cell proliferation
WO2009071701A1 (en) 2007-12-07 2009-06-11 Novartis Ag Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
JP6215832B2 (ja) * 2011-11-04 2017-10-18 ジャスコ ファーマスーティカルズ エルエルシーJasco Pharmaceuticals, LLC アミノピリミジンキナーゼ阻害剤
KR20160092991A (ko) 2013-09-27 2016-08-05 님버스 아이리스 인코포레이티드 Irak 억제제 및 이의 용도
WO2017021969A1 (en) * 2015-08-04 2017-02-09 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Pyrazole pyrimidine derivative and uses thereof
WO2018142393A1 (en) * 2017-02-01 2018-08-09 Yissum Research Development Company Of The Hebrew N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer
BR112020016064A2 (pt) 2018-02-08 2020-12-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Compostos de heteroarila, composições farmacêuticas dos mesmos e seu uso terapêutico

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015058140A1 (en) * 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)

Also Published As

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

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