KR102698366B1 - 피라졸 피리미딘 유도체 및 이의 용도 - Google Patents

피라졸 피리미딘 유도체 및 이의 용도 Download PDF

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KR102698366B1
KR102698366B1 KR1020187006128A KR20187006128A KR102698366B1 KR 102698366 B1 KR102698366 B1 KR 102698366B1 KR 1020187006128 A KR1020187006128 A KR 1020187006128A KR 20187006128 A KR20187006128 A KR 20187006128A KR 102698366 B1 KR102698366 B1 KR 102698366B1
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compound
stereoisomer
pharmaceutically acceptable
branched
alkyl
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KR20180043794A (ko
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이논 벤 네리아
가이 브라치야
이도 버스테인
웰리드 민젤
이리트 스니어-알카레이
조셉 보카
단수 리
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이섬 리서치 디벨러프먼트 컴파니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디.
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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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)
KR1020187006128A 2015-08-04 2016-08-04 피라졸 피리미딘 유도체 및 이의 용도 Active KR102698366B1 (ko)

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 (2)

Publication Number Publication Date
KR20180043794A KR20180043794A (ko) 2018-04-30
KR102698366B1 true KR102698366B1 (ko) 2024-08-26

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KR1020187006128A Active KR102698366B1 (ko) 2015-08-04 2016-08-04 피라졸 피리미딘 유도체 및 이의 용도

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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US20150094305A1 (en) 2013-09-27 2015-04-02 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
US20150202205A1 (en) 2011-11-04 2015-07-23 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors

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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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US20150202205A1 (en) 2011-11-04 2015-07-23 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
US20150094305A1 (en) 2013-09-27 2015-04-02 Nimbus Iris, Inc. Irak inhibitors and uses thereof
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
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
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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