JP6498212B2 - Cdk阻害剤としてのピラゾロ[1,5‐a]ピリミジン‐5,7‐ジアミン化合物及びその治療用途 - Google Patents

Cdk阻害剤としてのピラゾロ[1,5‐a]ピリミジン‐5,7‐ジアミン化合物及びその治療用途 Download PDF

Info

Publication number
JP6498212B2
JP6498212B2 JP2016553387A JP2016553387A JP6498212B2 JP 6498212 B2 JP6498212 B2 JP 6498212B2 JP 2016553387 A JP2016553387 A JP 2016553387A JP 2016553387 A JP2016553387 A JP 2016553387A JP 6498212 B2 JP6498212 B2 JP 6498212B2
Authority
JP
Japan
Prior art keywords
independently
alkyl
compound according
compound
saturated
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
JP2016553387A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017506250A5 (enExample
JP2017506250A (ja
Inventor
ボンドケ,アレクサンダー
クロル,セバスティアン
バレット,アンソニー
フヒター,マシュー
スラファー,ブライアン
アリ,シマック
クームズ,チャールズ
パトリック スナイダー,ジェームズ
パトリック スナイダー,ジェームズ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cancer Research Technology Ltd
Ip2ipo Innovations Ltd
Original Assignee
Imperial Innovations Ltd
Cancer Research Technology Ltd
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 Imperial Innovations Ltd, Cancer Research Technology Ltd filed Critical Imperial Innovations Ltd
Publication of JP2017506250A publication Critical patent/JP2017506250A/ja
Publication of JP2017506250A5 publication Critical patent/JP2017506250A5/ja
Application granted granted Critical
Publication of JP6498212B2 publication Critical patent/JP6498212B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2016553387A 2014-02-21 2015-02-20 Cdk阻害剤としてのピラゾロ[1,5‐a]ピリミジン‐5,7‐ジアミン化合物及びその治療用途 Active JP6498212B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201403093A GB201403093D0 (en) 2014-02-21 2014-02-21 Therapeutic compounds and their use
GB1403093.6 2014-02-21
PCT/GB2015/050494 WO2015124941A1 (en) 2014-02-21 2015-02-20 Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as cdk inhibitors and their therapeutic use

Publications (3)

Publication Number Publication Date
JP2017506250A JP2017506250A (ja) 2017-03-02
JP2017506250A5 JP2017506250A5 (enExample) 2018-03-08
JP6498212B2 true JP6498212B2 (ja) 2019-04-10

Family

ID=50482596

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016553387A Active JP6498212B2 (ja) 2014-02-21 2015-02-20 Cdk阻害剤としてのピラゾロ[1,5‐a]ピリミジン‐5,7‐ジアミン化合物及びその治療用途

Country Status (23)

Country Link
US (4) US9932344B2 (enExample)
EP (1) EP3107914B8 (enExample)
JP (1) JP6498212B2 (enExample)
CN (1) CN106103445B (enExample)
AU (1) AU2015220560B2 (enExample)
BR (1) BR112016018633B1 (enExample)
CA (1) CA2939786C (enExample)
CY (1) CY1121588T1 (enExample)
DK (1) DK3107914T3 (enExample)
ES (1) ES2721268T3 (enExample)
GB (1) GB201403093D0 (enExample)
HR (1) HRP20190685T1 (enExample)
HU (1) HUE043122T2 (enExample)
LT (1) LT3107914T (enExample)
ME (1) ME03427B (enExample)
NZ (1) NZ724323A (enExample)
PL (1) PL3107914T3 (enExample)
PT (1) PT3107914T (enExample)
RS (1) RS58704B1 (enExample)
SI (1) SI3107914T1 (enExample)
SM (1) SMT201900266T1 (enExample)
TR (1) TR201905647T4 (enExample)
WO (1) WO2015124941A1 (enExample)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201403093D0 (en) 2014-02-21 2014-04-09 Cancer Rec Tech Ltd Therapeutic compounds and their use
JP6690543B2 (ja) 2014-10-31 2020-04-28 宇部興産株式会社 置換ジヒドロピロロピラゾール化合物
BR112017012588B8 (pt) 2014-12-17 2024-02-15 King S College London Compostos heteroaril-heteroarila bicíclicos de ácido benzoico, seus usos, composições farmacêuticas, métodos de preparação destas e métodos para provocar ou promover o desenvolvimento de neuritos, o crescimento de neuritos e/ou a regeneração de neuritos e para ativar o receptor beta do ácido retinoico
EP3778605A3 (en) * 2015-02-13 2021-03-10 Dana Farber Cancer Institute, Inc. Lrrk2 inhibitors and methods of making and using the same
US10273252B2 (en) 2015-06-15 2019-04-30 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole derivative
WO2017096326A1 (en) 2015-12-02 2017-06-08 Massachusetts Institute Of Technology Method for efficient generation of neurons from non-neuronal cells
SG11201901747VA (en) 2016-08-31 2019-03-28 Agios Pharmaceuticals Inc Inhibitors of cellular metabolic processes
WO2019023468A1 (en) 2017-07-28 2019-01-31 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
JP7365332B2 (ja) * 2017-08-07 2023-10-19 ジョイント・ストック・カンパニー “バイオキャド” Cdk8/19阻害薬としての新規ヘテロ環式化合物
US20200197392A1 (en) * 2017-08-15 2020-06-25 The Brigham & Women's Hospital, Inc. Compositions and methods for treating tuberous sclerosis complex
GB201715194D0 (en) * 2017-09-20 2017-11-01 Carrick Therapeutics Ltd Compounds and their therapeutic use
TWI703149B (zh) * 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
US11945822B2 (en) * 2018-04-11 2024-04-02 Qurient Co., Ltd. Pyrazolo-triazine and/or pyrazolo-pxrimidine derivatives as selective inhibitor of cyclin dependent kinase
WO2019213403A1 (en) 2018-05-02 2019-11-07 Kinnate Biopharma Inc. Inhibitors of cyclin-dependent kinases
US10894788B2 (en) 2018-06-29 2021-01-19 Kinnate Biopharma Inc. Inhibitors of cyclin-dependent kinases
IL282254B2 (en) 2018-10-30 2025-08-01 Kronos Bio Inc Compounds, compositions, and methods for modulating cdk9 activity
WO2020100944A1 (ja) 2018-11-14 2020-05-22 宇部興産株式会社 ジヒドロピロロピラゾール誘導体
CN109860354B (zh) * 2018-12-28 2020-05-19 南京邮电大学 同质集成红外光子芯片及其制备方法
WO2020186196A1 (en) * 2019-03-13 2020-09-17 The Translational Genomics Research Institute Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors
CA3146375A1 (en) * 2019-07-10 2021-01-14 Aucentra Therapeutics Pty Ltd Derivatives of 4-(imidazo[l,2-a]pyridin-3-yl)-n-(pyridinyl)pyrimidin-2-amine as therapeutic agents
US20230000870A1 (en) * 2019-10-29 2023-01-05 Syros Pharmaceuticals, Inc. Methods of treating cancer in biomarker-identified patients with inhibitors of cyclin-dependent kinase 7 (cdk7)
GB201918541D0 (en) * 2019-12-16 2020-01-29 Carrick Therapeutics Ltd Therapeutic compounds and their use
US20230106032A1 (en) * 2020-03-06 2023-04-06 Bayer Aktiengesellschaft Imidazotriazines acting on cancer via inhibition of cdk12
US20230158159A1 (en) * 2020-04-24 2023-05-25 Massachusetts Institute Of Technology Chimeric degraders of cyclin-dependent kinase 9 and uses thereof
AU2022211514B2 (en) * 2021-01-22 2024-06-13 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Substituted pyrazolo[1,5-a]pyrimidine-7-amine derivative, and compositions and medical use thereof
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
GB202108572D0 (en) * 2021-06-16 2021-07-28 Carrick Therapeutics Ltd Therapeutic compounds and their use
WO2023001061A1 (en) * 2021-07-17 2023-01-26 Jingrui Biopharma Co., Ltd. Cdk7 selective inhibitors as anticancer agents
US20250059193A1 (en) * 2021-11-24 2025-02-20 Kronos Bio, Inc. Polymorphic and salt forms of (1s,3s)-n1-(5-(pentan-3-yl)pyrazolo[1,5-a]pyrimidin-7-yl) cyclopentane-1,3-diamine
WO2024102447A1 (en) * 2022-11-10 2024-05-16 Emory University Uses of hydroimidazopyridopyrimidinone derivatives for managing aneurysms or other vascular conditions or diseases
WO2024174949A1 (zh) * 2023-02-20 2024-08-29 江苏正大丰海制药有限公司 作为cdk7激酶抑制剂的杂芳环化合物及其制备和应用
WO2024175024A1 (zh) * 2023-02-21 2024-08-29 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
WO2025006569A1 (en) 2023-06-27 2025-01-02 Arvinas Operations, Inc. Combinations of estrogen receptor degraders and cdk7 inhibitors for the treatment of cancer
CN122029165A (zh) 2023-09-11 2026-05-12 阿西亚化学工业有限公司 Samuraciclib的固态形式
WO2025208104A1 (en) * 2024-03-29 2025-10-02 The Translational Genomics Research Institute Cdk7 inhibitors and methods of use thereof
WO2025208097A1 (en) * 2024-03-29 2025-10-02 The Translational Genomics Research Institute Cdk7 inhibitors and methods of use thereof
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers
WO2026057043A1 (zh) * 2024-09-14 2026-03-19 正大天晴药业集团股份有限公司 作为cdk抑制剂的三并环化合物及其应用
EP4717312A1 (en) * 2024-09-27 2026-04-01 Perha Pharmaceuticals Pyrazolo[1,5-a]pyrimidine derivatives useful as a medicament

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE449764T1 (de) 1999-12-28 2009-12-15 Pharmacopeia Inc Cytokine, insbesondere tnf-alpha, hemmer
MXPA05002571A (es) 2002-09-04 2005-09-08 Schering Corp Pirazolopirimidinas como inhibidores de cinasa dependientes de ciclina.
US7388019B2 (en) 2003-01-31 2008-06-17 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
KR20050115252A (ko) 2003-02-28 2005-12-07 데이진 화-마 가부시키가이샤 피라졸로[1,5-a]피리미딘 유도체
US20070179161A1 (en) * 2003-03-31 2007-08-02 Vernalis (Cambridge) Limited. Pyrazolopyrimidine compounds and their use in medicine
JO2478B1 (en) 2003-06-19 2009-01-20 جانسين فارماسوتيكا ان. في. (Aminomethyl) -biperidine benzamides as 5 HT4 antagonists
BRPI0616985B1 (pt) * 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
CA2688616A1 (en) 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
RU2607453C2 (ru) * 2009-12-04 2017-01-10 Сенхва Байосайенсиз, Инк. Пиразолопиримидины и родственные гетероциклы как ск2 ингибиторы
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
EP2734205B1 (en) * 2011-07-21 2018-03-21 Tolero Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors
EP2634189A1 (en) 2012-03-01 2013-09-04 Lead Discovery Center GmbH Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors
EP2634190A1 (en) 2012-03-01 2013-09-04 Lead Discovery Center GmbH Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhinitors
GB201403093D0 (en) 2014-02-21 2014-04-09 Cancer Rec Tech Ltd Therapeutic compounds and their use

Also Published As

Publication number Publication date
US10414772B2 (en) 2019-09-17
ES2721268T3 (es) 2019-07-30
WO2015124941A1 (en) 2015-08-27
PT3107914T (pt) 2019-05-20
US20210253583A1 (en) 2021-08-19
CA2939786C (en) 2022-03-08
PL3107914T3 (pl) 2019-09-30
CN106103445B (zh) 2019-08-09
SI3107914T1 (sl) 2019-05-31
RS58704B1 (sr) 2019-06-28
US20160362410A1 (en) 2016-12-15
GB201403093D0 (en) 2014-04-09
AU2015220560A1 (en) 2016-10-06
HUE043122T2 (hu) 2019-08-28
US20200055862A1 (en) 2020-02-20
ME03427B (me) 2020-01-20
BR112016018633B1 (pt) 2022-08-30
DK3107914T3 (en) 2019-04-29
AU2015220560B2 (en) 2019-05-16
US10927119B2 (en) 2021-02-23
EP3107914A1 (en) 2016-12-28
EP3107914B1 (en) 2019-01-30
EP3107914B8 (en) 2019-07-17
US11566029B2 (en) 2023-01-31
HRP20190685T1 (hr) 2019-06-14
US20180273540A1 (en) 2018-09-27
BR112016018633A2 (enExample) 2017-08-08
CY1121588T1 (el) 2020-05-29
TR201905647T4 (tr) 2019-05-21
CN106103445A (zh) 2016-11-09
LT3107914T (lt) 2019-05-27
CA2939786A1 (en) 2015-08-27
JP2017506250A (ja) 2017-03-02
US9932344B2 (en) 2018-04-03
NZ724323A (en) 2022-02-25
SMT201900266T1 (it) 2019-07-11

Similar Documents

Publication Publication Date Title
US11566029B2 (en) Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as CDK inhibitors and their therapeutic use
CA3075461C (en) 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds as cdk inhibitors
JP7348665B2 (ja) 選択的エストロゲン受容体分解剤としての置換ベンゾチオフェン類似体
WO2022263604A1 (en) Substituted pyrazolo[1,5-a]pyrimidine-7-amine compounds as cdk inhibitors and their therapeutic use
EP4077330A1 (en) 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds and their therapeutic use
EP2476682A1 (en) 8-oxodihydropurine derivative
HK1231852A1 (en) Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as cdk inhibitors and their therapeutic use
HK1231852B (en) Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as cdk inhibitors and their therapeutic use
NZ763316B2 (en) 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds as cdk inhibitors

Legal Events

Date Code Title Description
RD01 Notification of change of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7426

Effective date: 20170208

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20170208

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180129

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180129

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180911

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180913

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181206

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: 20190305

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190312

R150 Certificate of patent or registration of utility model

Ref document number: 6498212

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250