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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
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

Publications (2)

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

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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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ES2901349T3 (es) * 2015-08-04 2022-03-22 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivado de pirazol pirimidina y usos del mismo
US11072599B2 (en) 2017-02-01 2021-07-27 Biotheryx, Inc. Pyrazole compounds and uses thereof
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
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
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
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020247345A1 (en) * 2019-06-03 2020-12-10 Biotheryx, Inc. Non-hygroscopic crystalline salts of a pyrazole compound, and pharmaceutical compositions and use thereof
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
TW202115024A (zh) 2019-08-14 2021-04-16 美商英塞特公司 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物
CN119930610A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
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
AU2021243726A1 (en) * 2020-03-26 2022-09-29 Janssen Pharmaceutica Nv Aryl piperidines as monoacylglycerol lipase modulators
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

Citations (3)

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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
CN1976905A (zh) * 2004-03-30 2007-06-06 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
WO2007138277A1 (en) * 2006-05-26 2007-12-06 Astrazeneca Ab 2-carbocycloamino-4-imidaz0lylpyrimidines as agents for the inhbition of cell proliferation
WO2009071701A1 (en) * 2007-12-07 2009-06-11 Novartis Ag Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
RU2674017C2 (ru) 2011-11-04 2018-12-04 ДЖАСКО ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Аминопиримидиновые ингибиторы киназ
BR112016006319A2 (pt) 2013-09-27 2017-08-01 Nimbus Iris Inc inibidores de irak e usos dos mesmos
ES2901349T3 (es) * 2015-08-04 2022-03-22 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivado de pirazol pirimidina y usos del mismo
US11072599B2 (en) * 2017-02-01 2021-07-27 Biotheryx, Inc. Pyrazole compounds and uses thereof
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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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SI3331877T1 (sl) 2022-02-28
EP3331877B1 (en) 2021-09-22
EP3331877A1 (en) 2018-06-13
HK1256535A1 (en) 2019-09-27
JP7083309B2 (ja) 2022-06-10
AU2021200839A1 (en) 2021-03-04
AU2016304464B2 (en) 2020-11-19
KR20180043794A (ko) 2018-04-30
RU2018107668A (ru) 2019-09-05
DK3331877T3 (da) 2022-01-03
US10376511B2 (en) 2019-08-13
CN108137562A (zh) 2018-06-08
PT3331877T (pt) 2021-12-27
US20250049793A1 (en) 2025-02-13
IL257282A (en) 2018-03-29
RS62728B1 (sr) 2022-01-31
RU2018107668A3 (enExample) 2020-01-13
JP2018525441A (ja) 2018-09-06
RU2735522C2 (ru) 2020-11-03
SMT202100720T1 (it) 2022-01-10
HRP20211949T1 (hr) 2022-03-18
US10960003B2 (en) 2021-03-30
CY1124898T1 (el) 2023-01-05
IL257282B (en) 2021-06-30
LT3331877T (lt) 2022-01-10
ZA201800671B (en) 2020-05-27
HUE057607T2 (hu) 2022-06-28
NZ739511A (en) 2023-08-25
ES2901349T3 (es) 2022-03-22
MX384172B (es) 2025-03-14
WO2017021969A1 (en) 2017-02-09
US11925641B2 (en) 2024-03-12
AU2016304464A1 (en) 2018-02-22
CA2994644A1 (en) 2017-02-09
PL3331877T3 (pl) 2022-01-31
US20190365759A1 (en) 2019-12-05
US20210251992A1 (en) 2021-08-19
KR102698366B1 (ko) 2024-08-26
MX2018001395A (es) 2018-04-13
US20180214447A1 (en) 2018-08-02

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