CA2994644A1 - Pyrazole pyrimidine derivative and uses thereof - Google Patents

Pyrazole pyrimidine derivative and uses thereof Download PDF

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Publication number
CA2994644A1
CA2994644A1 CA2994644A CA2994644A CA2994644A1 CA 2994644 A1 CA2994644 A1 CA 2994644A1 CA 2994644 A CA2994644 A CA 2994644A CA 2994644 A CA2994644 A CA 2994644A CA 2994644 A1 CA2994644 A1 CA 2994644A1
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Canada
Prior art keywords
branched
straight
compound according
compound
alkyl
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA2994644A
Other languages
English (en)
French (fr)
Inventor
Yinon Ben Neriah
Guy BRACHYA
Ido BURSTAIN
Waleed MINZEL
Irit SNIR-ALKALAY
Joseph Vacca
Dansu Li
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
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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Application filed by Yissum Research Development Co of Hebrew University of Jerusalem filed Critical Yissum Research Development Co of Hebrew University of Jerusalem
Publication of CA2994644A1 publication Critical patent/CA2994644A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • C07D403/04Heterocyclic 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
    • 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)
CA2994644A 2015-08-04 2016-08-04 Pyrazole pyrimidine derivative and uses thereof Pending CA2994644A1 (en)

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

Publications (1)

Publication Number Publication Date
CA2994644A1 true CA2994644A1 (en) 2017-02-09

Family

ID=56738143

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2994644A Pending CA2994644A1 (en) 2015-08-04 2016-08-04 Pyrazole pyrimidine derivative and uses thereof

Country Status (23)

Country Link
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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Publication number Priority date Publication date Assignee Title
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
GB0215844D0 (en) * 2002-07-09 2002-08-14 Novartis Ag Organic compounds
CN101693695A (zh) 2004-03-30 2010-04-14 大正制药株式会社 嘧啶衍生物以及与其应用有关的治疗方法
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
US20100063049A1 (en) * 2006-05-26 2010-03-11 Clifford Jones 2-carbocycloamino-4-imidazolylpyrimidines as agents for the inhbition of cell proliferation
CA2707989A1 (en) * 2007-12-07 2009-06-11 Novartis Ag Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
KR101990605B1 (ko) * 2011-11-04 2019-06-18 자스코 파머수티컬스, 엘엘씨 아미노피리미딘 키나아제 억제제
CN106232122A (zh) * 2013-09-27 2016-12-14 林伯士艾瑞斯公司 Irak抑制剂和其用途
EP3057956B1 (en) * 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
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

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
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
AU2016304464B2 (en) 2020-11-19
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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