JP7083309B2 - ピラゾールピリミジン誘導体及びその使用 - Google Patents

ピラゾールピリミジン誘導体及びその使用 Download PDF

Info

Publication number
JP7083309B2
JP7083309B2 JP2018525826A JP2018525826A JP7083309B2 JP 7083309 B2 JP7083309 B2 JP 7083309B2 JP 2018525826 A JP2018525826 A JP 2018525826A JP 2018525826 A JP2018525826 A JP 2018525826A JP 7083309 B2 JP7083309 B2 JP 7083309B2
Authority
JP
Japan
Prior art keywords
alkyl
branched
linear
compound
independently
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2018525826A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018525441A5 (enExample
JP2018525441A (ja
Inventor
ベン ネリアフ イノン
ブラクヤ ガイ
バースタイン イド
ミンゼル ワリード
スニル‐アルカライ イリト
ヴァッカ ジョセフ
リ ダンス
Original Assignee
イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー．
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー． filed Critical イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー．
Publication of JP2018525441A publication Critical patent/JP2018525441A/ja
Publication of JP2018525441A5 publication Critical patent/JP2018525441A5/ja
Application granted granted Critical
Publication of JP7083309B2 publication Critical patent/JP7083309B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
JP2018525826A 2015-08-04 2016-08-04 ピラゾールピリミジン誘導体及びその使用 Active JP7083309B2 (ja)

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
JP2018525441A JP2018525441A (ja) 2018-09-06
JP2018525441A5 JP2018525441A5 (enExample) 2019-09-19
JP7083309B2 true JP7083309B2 (ja) 2022-06-10

Family

ID=56738143

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018525826A Active JP7083309B2 (ja) 2015-08-04 2016-08-04 ピラゾールピリミジン誘導体及びその使用

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)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS62728B1 (sr) * 2015-08-04 2022-01-31 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivat pirazol pirimidina i njegove upotrebe
IL268128B2 (en) * 2017-02-01 2023-03-01 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 cancer therapy
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
CN111971280A (zh) * 2018-02-08 2020-11-20 耶路撒冷希伯来大学伊萨姆研究发展公司 杂芳基化合物、其药物组合物和其治疗用途
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
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
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 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
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
EP4013750A1 (en) 2019-08-14 2022-06-22 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
GEAP202516803A (en) 2019-10-11 2025-10-10 Incyte Corp Bicyclic amines as cdk2 inhibitors
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
MX2022011901A (es) * 2020-03-26 2023-01-04 Janssen Pharmaceutica Nv Arilo piperidinas como moduladores de monoacilglicerol lipasa.
TW202304883A (zh) * 2021-03-24 2023-02-01 美商拜歐斯瑞克斯公司 用於治療惡性實體腫瘤之吡唑基嘧啶
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 (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002046184A1 (en) 2000-12-05 2002-06-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2004005282A1 (en) 2002-07-09 2004-01-15 Novartis Ag PHENYL-[4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES
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
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
WO2013066684A1 (en) 2011-11-04 2013-05-10 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
WO2015048281A1 (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)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002308748A1 (en) * 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
ZA200607639B (en) 2004-03-30 2008-05-28 Taisho Pharmaceutical Co Ltd Pyrimidine derivatives and methods of treatment related to the use thereof
RS62728B1 (sr) 2015-08-04 2022-01-31 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivat pirazol pirimidina i njegove upotrebe
IL268128B2 (en) * 2017-02-01 2023-03-01 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 cancer therapy
CN111971280A (zh) 2018-02-08 2020-11-20 耶路撒冷希伯来大学伊萨姆研究发展公司 杂芳基化合物、其药物组合物和其治疗用途

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002046184A1 (en) 2000-12-05 2002-06-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2004005282A1 (en) 2002-07-09 2004-01-15 Novartis Ag PHENYL-[4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES
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
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
WO2013066684A1 (en) 2011-11-04 2013-05-10 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
WO2015048281A1 (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
US20180214447A1 (en) 2018-08-02
AU2016304464A1 (en) 2018-02-22
US11925641B2 (en) 2024-03-12
RU2018107668A (ru) 2019-09-05
HRP20211949T1 (hr) 2022-03-18
RU2735522C2 (ru) 2020-11-03
IL257282B (en) 2021-06-30
CA2994644A1 (en) 2017-02-09
US12514859B2 (en) 2026-01-06
ZA201800671B (en) 2020-05-27
KR20180043794A (ko) 2018-04-30
LT3331877T (lt) 2022-01-10
US10376511B2 (en) 2019-08-13
EP3331877A1 (en) 2018-06-13
US10960003B2 (en) 2021-03-30
JP2018525441A (ja) 2018-09-06
HUE057607T2 (hu) 2022-06-28
NZ739511A (en) 2023-08-25
US20190365759A1 (en) 2019-12-05
KR102698366B1 (ko) 2024-08-26
RU2018107668A3 (enExample) 2020-01-13
PL3331877T3 (pl) 2022-01-31
IL257282A (en) 2018-03-29
US20210251992A1 (en) 2021-08-19
AU2016304464B2 (en) 2020-11-19
MX384172B (es) 2025-03-14
RS62728B1 (sr) 2022-01-31
ES2901349T3 (es) 2022-03-22
PT3331877T (pt) 2021-12-27
EP3331877B1 (en) 2021-09-22
CY1124898T1 (el) 2023-01-05
SI3331877T1 (sl) 2022-02-28
HK1256535A1 (en) 2019-09-27
DK3331877T3 (da) 2022-01-03
MX2018001395A (es) 2018-04-13
CN108137562B (zh) 2021-11-30
CN108137562A (zh) 2018-06-08
US20250049793A1 (en) 2025-02-13
WO2017021969A1 (en) 2017-02-09
SMT202100720T1 (it) 2022-01-10
AU2021200839A1 (en) 2021-03-04

Similar Documents

Publication Publication Date Title
JP7083309B2 (ja) ピラゾールピリミジン誘導体及びその使用
RU2656591C2 (ru) Модуляторы протеин-тирозинкиназы и способы их применения
CN116113633B (zh) 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途
EP3939981B1 (en) Fused thiazolopyrimidine derivatives as mnks inhibitors
JP6131272B2 (ja) キナーゼ阻害活性を有するベンズヒドロール−ピラゾール誘導体及びその使用
JP7142646B2 (ja) がんを治療するためのｃｋ１及び／又はｉｒａｋ１インヒビターとしてのｎ１－（４－（５－（シクロプロピルメチル）－１－メチル－１ｈ－ピラゾール－４－イル）ピリジン－２－イル）シクロヘキサン－１，４－ジアミン誘導体及び関連化合物
CN101287728A (zh) 新的高亲和力噻吩基和呋喃基激酶配体
WO2022057836A1 (zh) 苯并脲环衍生物及其制备方法和应用
HK40065647B (en) Fused thiazolopyrimidine derivatives as mnks inhibitors
HK40065647A (en) Fused thiazolopyrimidine derivatives as mnks inhibitors
HK1256535B (en) Pyrazole pyrimidine derivative and uses thereof
CN116783166A (zh) 二甲酰胺类化合物、其制备方法及其在医药上的应用
HK40081466A (en) Efgr inhibitor, preparation method therefor, and application thereof
NZ739511B2 (en) Pyrazole pyrimidine derivative and uses thereof
HK1253575B (en) Fused thiazolopyrimidine derivatives as mnks inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190802

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190802

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200611

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200616

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200915

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210216

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210514

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211005

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211228

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20220517

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20220531

R150 Certificate of patent or registration of utility model

Ref document number: 7083309

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250