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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stereoisomer
pharmaceutically acceptable
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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
Original Assignee
이섬 리서치 디벨러프먼트 컴파니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디.
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    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
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 (OSRAM)
EP (1) EP3331877B1 (OSRAM)
JP (1) JP7083309B2 (OSRAM)
KR (1) KR102698366B1 (OSRAM)
CN (1) CN108137562B (OSRAM)
AU (2) AU2016304464B2 (OSRAM)
CA (1) CA2994644A1 (OSRAM)
CY (1) CY1124898T1 (OSRAM)
DK (1) DK3331877T3 (OSRAM)
ES (1) ES2901349T3 (OSRAM)
HR (1) HRP20211949T1 (OSRAM)
HU (1) HUE057607T2 (OSRAM)
IL (1) IL257282B (OSRAM)
LT (1) LT3331877T (OSRAM)
MX (1) MX384172B (OSRAM)
PL (1) PL3331877T3 (OSRAM)
PT (1) PT3331877T (OSRAM)
RS (1) RS62728B1 (OSRAM)
RU (1) RU2735522C2 (OSRAM)
SI (1) SI3331877T1 (OSRAM)
SM (1) SMT202100720T1 (OSRAM)
WO (1) WO2017021969A1 (OSRAM)
ZA (1) ZA201800671B (OSRAM)

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ES2902885T3 (es) * 2017-02-01 2022-03-30 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 el tratamiento del cáncer
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
MX2020008375A (es) 2018-02-08 2020-09-25 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Compuestos de heteroarilo, composiciones farmaceuticas de los mismos y su uso terapeutico.
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
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
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
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
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
CN114127058B (zh) * 2019-07-04 2024-06-25 深圳国顺康医药科技有限公司 一种杂环化合物、其药物组合物及用途
PH12022550361A1 (en) 2019-08-14 2023-02-27 Incyte Corp Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
JP7693656B2 (ja) 2019-10-11 2025-06-17 インサイト・コーポレイション Cdk2阻害剤としての二環式アミン
WO2021146220A1 (en) * 2020-01-13 2021-07-22 Biotheryx, Inc. Pyrazolylpyrimidines and use thereof
WO2021155050A1 (en) * 2020-01-29 2021-08-05 Biotheryx, Inc. Kinase modulators, pharmaceutical compositions, and therapeutic applications
BR112022019155A2 (pt) * 2020-03-26 2022-12-06 Janssen Pharmaceutica Nv Aril piperidinas como moduladores da monoacilglicerol lipase
WO2022204220A1 (en) * 2021-03-24 2022-09-29 Biotheryx, Inc. 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

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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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MXPA03005001A (es) 2000-12-05 2003-09-05 Vertex Pharma Inhibidores de n- terminal c-jun cinasas (jnk) y otras proteinas cinasas.
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
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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
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DK3331877T3 (da) 2015-08-04 2022-01-03 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Pyrazolpyrimidinderivat og anvendelser deraf
ES2902885T3 (es) * 2017-02-01 2022-03-30 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 el tratamiento del cáncer
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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
US20210251992A1 (en) 2021-08-19
MX2018001395A (es) 2018-04-13
CN108137562A (zh) 2018-06-08
AU2016304464B2 (en) 2020-11-19
EP3331877A1 (en) 2018-06-13
JP2018525441A (ja) 2018-09-06
RU2735522C2 (ru) 2020-11-03
ZA201800671B (en) 2020-05-27
US10960003B2 (en) 2021-03-30
US20180214447A1 (en) 2018-08-02
WO2017021969A1 (en) 2017-02-09
ES2901349T3 (es) 2022-03-22
AU2016304464A1 (en) 2018-02-22
US20250049793A1 (en) 2025-02-13
HUE057607T2 (hu) 2022-06-28
SI3331877T1 (sl) 2022-02-28
RU2018107668A (ru) 2019-09-05
CA2994644A1 (en) 2017-02-09
RU2018107668A3 (OSRAM) 2020-01-13
US11925641B2 (en) 2024-03-12
KR20180043794A (ko) 2018-04-30
IL257282B (en) 2021-06-30
IL257282A (en) 2018-03-29
PT3331877T (pt) 2021-12-27
MX384172B (es) 2025-03-14
NZ739511A (en) 2023-08-25
US20190365759A1 (en) 2019-12-05
US10376511B2 (en) 2019-08-13
EP3331877B1 (en) 2021-09-22
DK3331877T3 (da) 2022-01-03
HRP20211949T1 (hr) 2022-03-18
LT3331877T (lt) 2022-01-10
PL3331877T3 (pl) 2022-01-31
HK1256535A1 (en) 2019-09-27
CY1124898T1 (el) 2023-01-05
AU2021200839A1 (en) 2021-03-04
CN108137562B (zh) 2021-11-30
SMT202100720T1 (it) 2022-01-10
JP7083309B2 (ja) 2022-06-10
RS62728B1 (sr) 2022-01-31

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