RU2735522C2 - Пиразолпиримидиновое производное и его применение - Google Patents

Пиразолпиримидиновое производное и его применение Download PDF

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Publication number
RU2735522C2
RU2735522C2 RU2018107668A RU2018107668A RU2735522C2 RU 2735522 C2 RU2735522 C2 RU 2735522C2 RU 2018107668 A RU2018107668 A RU 2018107668A RU 2018107668 A RU2018107668 A RU 2018107668A RU 2735522 C2 RU2735522 C2 RU 2735522C2
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compound
pharmaceutically acceptable
acceptable salt
stereoisomer
salt according
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RU2018107668A
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Russian (ru)
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RU2018107668A (ru
RU2018107668A3 (enExample
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НЕРИАХ Йинон БЕН
Гай БРАХИЯ
Идо БУРШТЕЙН
Валид МИНЗЕЛЬ
Ирит СНИР-АЛКАЛАЙ
Йозеф ВАККА
Даньсу ЛИ
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Йиссум Рисерч Дивелопмент Компани Оф Дзе Хебрю Юниверсити Оф Иерусалим Лтд
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    • 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
    • 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
    • C07D403/08—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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
RU2018107668A 2015-08-04 2016-08-04 Пиразолпиримидиновое производное и его применение RU2735522C2 (ru)

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 (3)

Publication Number Publication Date
RU2018107668A RU2018107668A (ru) 2019-09-05
RU2018107668A3 RU2018107668A3 (enExample) 2020-01-13
RU2735522C2 true RU2735522C2 (ru) 2020-11-03

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RU2018107668A RU2735522C2 (ru) 2015-08-04 2016-08-04 Пиразолпиримидиновое производное и его применение

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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.
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
WO2019155468A1 (en) 2018-02-08 2019-08-15 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
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
US11472791B2 (en) 2019-03-05 2022-10-18 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
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
SG11202113211PA (en) * 2019-06-03 2021-12-30 Biotheryx Inc Non-hygroscopic crystalline salts of a pyrazole compound, and pharmaceutical compositions and use thereof
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
BR112022002698A2 (pt) 2019-08-14 2022-07-19 Incyte Corp Compostos de imidazolil pirimidinilamina como inibidores de cdk2
AU2020364007A1 (en) 2019-10-11 2022-04-28 Incyte Corporation Bicyclic amines as CDK2 inhibitors
AU2021209057A1 (en) * 2020-01-13 2022-06-30 Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. Pyrazolylpyrimidines and use thereof
WO2021155050A1 (en) * 2020-01-29 2021-08-05 Biotheryx, Inc. Kinase modulators, pharmaceutical compositions, and therapeutic applications
WO2021191384A1 (en) * 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Aryl piperidines as monoacylglycerol lipase modulators
US20240207268A1 (en) * 2021-03-24 2024-06-27 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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RU2373197C2 (ru) * 2004-03-30 2009-11-20 Тайсо Фармасьютикал Ко., Лтд. Пиримидиновые производные, обладающие активностью в отношении мсн
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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EP1343781B1 (en) 2000-12-05 2008-09-03 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
US6884804B2 (en) 2001-05-16 2005-04-26 Vertex Pharmaceuticals Incorporated Inhibitors of Src and other protein kinases
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
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
JP2009538352A (ja) 2006-05-26 2009-11-05 アストラゼネカ アクチボラグ 細胞増殖を阻害するための薬剤としての２−カルボシクロアミノ−４−イミダゾリルピリミジン類
EP2231636B1 (en) 2007-12-07 2011-09-14 Novartis AG Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
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.
WO2019155468A1 (en) 2018-02-08 2019-08-15 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
RU2373197C2 (ru) * 2004-03-30 2009-11-20 Тайсо Фармасьютикал Ко., Лтд. Пиримидиновые производные, обладающие активностью в отношении мсн
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)

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AU2021200839A1 (en) 2021-03-04
US10960003B2 (en) 2021-03-30
EP3331877B1 (en) 2021-09-22
CY1124898T1 (el) 2023-01-05
SI3331877T1 (sl) 2022-02-28
US20180214447A1 (en) 2018-08-02
ES2901349T3 (es) 2022-03-22
MX2018001395A (es) 2018-04-13
US11925641B2 (en) 2024-03-12
PT3331877T (pt) 2021-12-27
IL257282B (en) 2021-06-30
RU2018107668A (ru) 2019-09-05
PL3331877T3 (pl) 2022-01-31
SMT202100720T1 (it) 2022-01-10
CN108137562B (zh) 2021-11-30
EP3331877A1 (en) 2018-06-13
NZ739511A (en) 2023-08-25
US20190365759A1 (en) 2019-12-05
AU2016304464B2 (en) 2020-11-19
US20250049793A1 (en) 2025-02-13
LT3331877T (lt) 2022-01-10
RS62728B1 (sr) 2022-01-31
IL257282A (en) 2018-03-29
RU2018107668A3 (enExample) 2020-01-13
KR20180043794A (ko) 2018-04-30
AU2016304464A1 (en) 2018-02-22
ZA201800671B (en) 2020-05-27
CN108137562A (zh) 2018-06-08
WO2017021969A1 (en) 2017-02-09
HRP20211949T1 (hr) 2022-03-18
KR102698366B1 (ko) 2024-08-26
JP7083309B2 (ja) 2022-06-10
MX384172B (es) 2025-03-14
JP2018525441A (ja) 2018-09-06
DK3331877T3 (da) 2022-01-03
HK1256535A1 (en) 2019-09-27
CA2994644A1 (en) 2017-02-09
US20210251992A1 (en) 2021-08-19
HUE057607T2 (hu) 2022-06-28
US10376511B2 (en) 2019-08-13

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