CN108137562B - 吡唑嘧啶衍生物及其用途 - Google Patents

吡唑嘧啶衍生物及其用途 Download PDF

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Publication number
CN108137562B
CN108137562B CN201680059148.XA CN201680059148A CN108137562B CN 108137562 B CN108137562 B CN 108137562B CN 201680059148 A CN201680059148 A CN 201680059148A CN 108137562 B CN108137562 B CN 108137562B
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pharmaceutically acceptable
stereoisomer
acceptable salt
straight
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CN108137562A (zh
Inventor
伊农·本内里艾
盖·布雷加
伊多·伯斯泰
瓦利德·门策尔
艾里特·思尼尔-奥克利
约瑟夫·瓦卡
李丹素
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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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    • 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)
  • 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)
CN201680059148.XA 2015-08-04 2016-08-04 吡唑嘧啶衍生物及其用途 Active CN108137562B (zh)

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

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Publication Number Publication Date
CN108137562A CN108137562A (zh) 2018-06-08
CN108137562B true CN108137562B (zh) 2021-11-30

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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)
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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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HRP20211949T1 (hr) * 2015-08-04 2022-03-18 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Derivat pirazol primidina i njegove uporabe
NZ755447A (en) 2017-02-01 2023-05-26 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd 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
AU2019219678A1 (en) * 2018-02-08 2020-08-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
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
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
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
CN114423752B (zh) * 2019-06-03 2025-06-24 耶路撒冷希伯来大学伊萨姆研究发展公司 吡唑化合物的非吸湿性结晶盐和其药物组合物与用途
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
MX2022001940A (es) 2019-08-14 2022-05-10 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2.
CN119930610A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
US20230047732A1 (en) * 2020-01-13 2023-02-16 Biotheryx, Inc. Pyrazolylpyrimidines and use thereof
WO2021155050A1 (en) * 2020-01-29 2021-08-05 Biotheryx, Inc. Kinase modulators, pharmaceutical compositions, and therapeutic applications
JP7729832B2 (ja) * 2020-03-26 2025-08-26 ヤンセン ファーマシューティカ エヌ．ベー． モノアシルグリセロールリパーゼ調節因子としてのアリールピペリジン
AU2022242818A1 (en) * 2021-03-24 2023-10-05 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
WO2025199434A1 (en) * 2024-03-21 2025-09-25 Edgewood Oncology Methods of treating breast cancer using a pyrazole compound

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WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
WO2007129195A2 (en) * 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
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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ATE407132T1 (de) 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
RU2373197C2 (ru) * 2004-03-30 2009-11-20 Тайсо Фармасьютикал Ко., Лтд. Пиримидиновые производные, обладающие активностью в отношении мсн
JP2007145819A (ja) 2005-10-28 2007-06-14 Tanabe Seiyaku Co Ltd 医薬組成物
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
CA2707989A1 (en) 2007-12-07 2009-06-11 Novartis Ag Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
ES2629690T3 (es) 2011-11-04 2017-08-14 Jasco Pharmaceuticals, LLC Inhibidores de aminopirimidina quinasa
KR20160092991A (ko) 2013-09-27 2016-08-05 님버스 아이리스 인코포레이티드 Irak 억제제 및 이의 용도
HRP20211949T1 (hr) * 2015-08-04 2022-03-18 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Derivat pirazol primidina i njegove uporabe
NZ755447A (en) * 2017-02-01 2023-05-26 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd 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
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Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
WO2007129195A2 (en) * 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
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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JP7083309B2 (ja) 2022-06-10
CN108137562A (zh) 2018-06-08
KR102698366B1 (ko) 2024-08-26
PL3331877T3 (pl) 2022-01-31
KR20180043794A (ko) 2018-04-30
US11925641B2 (en) 2024-03-12
EP3331877A1 (en) 2018-06-13
MX2018001395A (es) 2018-04-13
AU2021200839A1 (en) 2021-03-04
CA2994644A1 (en) 2017-02-09
RU2018107668A (ru) 2019-09-05
US20250049793A1 (en) 2025-02-13
LT3331877T (lt) 2022-01-10
NZ739511A (en) 2023-08-25
US20190365759A1 (en) 2019-12-05
US20210251992A1 (en) 2021-08-19
CY1124898T1 (el) 2023-01-05
HRP20211949T1 (hr) 2022-03-18
HK1256535A1 (en) 2019-09-27
AU2016304464B2 (en) 2020-11-19
HUE057607T2 (hu) 2022-06-28
ES2901349T3 (es) 2022-03-22
RU2018107668A3 (enExample) 2020-01-13
US10376511B2 (en) 2019-08-13
US20180214447A1 (en) 2018-08-02
SI3331877T1 (sl) 2022-02-28
PT3331877T (pt) 2021-12-27
AU2016304464A1 (en) 2018-02-22
IL257282B (en) 2021-06-30
US10960003B2 (en) 2021-03-30
SMT202100720T1 (it) 2022-01-10
DK3331877T3 (da) 2022-01-03
IL257282A (en) 2018-03-29
RU2735522C2 (ru) 2020-11-03
US12514859B2 (en) 2026-01-06
WO2017021969A1 (en) 2017-02-09
MX384172B (es) 2025-03-14
RS62728B1 (sr) 2022-01-31
EP3331877B1 (en) 2021-09-22
JP2018525441A (ja) 2018-09-06
ZA201800671B (en) 2020-05-27

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