JP2017506250A5 - - Google Patents
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- Publication number
- JP2017506250A5 JP2017506250A5 JP2016553387A JP2016553387A JP2017506250A5 JP 2017506250 A5 JP2017506250 A5 JP 2017506250A5 JP 2016553387 A JP2016553387 A JP 2016553387A JP 2016553387 A JP2016553387 A JP 2016553387A JP 2017506250 A5 JP2017506250 A5 JP 2017506250A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- alkyl
- piperazino
- saturated
- compound according
- 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.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 34
- 229920006395 saturated elastomer Polymers 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 27
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 208000035475 disorder Diseases 0.000 claims 13
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims 11
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 108091007914 CDKs Proteins 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- -1 pyrrolidino, piperidino, morpholino , Piperazino Chemical group 0.000 claims 7
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 229940122815 Aromatase inhibitor Drugs 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 101150029707 ERBB2 gene Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 230000001668 ameliorated effect Effects 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 239000003886 aromatase inhibitor Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 231100000433 cytotoxic Toxicity 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 230000001472 cytotoxic effect Effects 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 239000000328 estrogen antagonist Substances 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 238000011144 upstream manufacturing Methods 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 229940046836 anti-estrogen Drugs 0.000 claims 1
- 230000001833 anti-estrogenic effect Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000003725 azepanyl group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000005959 diazepanyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- OFPDDUJAJMRDEF-MJGOQNOKSA-N CC(C)c(cn[n]1c(NCC2CCCCC2)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O Chemical compound CC(C)c(cn[n]1c(NCC2CCCCC2)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O OFPDDUJAJMRDEF-MJGOQNOKSA-N 0.000 description 1
- YCVGLKWJKIKVBI-MJGOQNOKSA-N CC(C)c(cn[n]1c(NCc2ccccc2)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O Chemical compound CC(C)c(cn[n]1c(NCc2ccccc2)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O YCVGLKWJKIKVBI-MJGOQNOKSA-N 0.000 description 1
- TUXGZDGYDSKKTA-JHQNIPJKSA-N CC(C)c(cn[n]1c(NCc2ccncc2N(CC[C@]2(CNc3nc4c(C(C)C)cn[n]4c(NCc4ccccc4)c3)O)C[C@H]2O)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O Chemical compound CC(C)c(cn[n]1c(NCc2ccncc2N(CC[C@]2(CNc3nc4c(C(C)C)cn[n]4c(NCc4ccccc4)c3)O)C[C@H]2O)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O TUXGZDGYDSKKTA-JHQNIPJKSA-N 0.000 description 1
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 true JP2017506250A5 (enExample) | 2018-03-08 |
| JP6498212B2 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)
| 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)
| 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 |
-
2014
- 2014-02-21 GB GB201403093A patent/GB201403093D0/en not_active Ceased
-
2015
- 2015-02-20 CN CN201580011502.7A patent/CN106103445B/zh active Active
- 2015-02-20 RS RS20190487A patent/RS58704B1/sr unknown
- 2015-02-20 WO PCT/GB2015/050494 patent/WO2015124941A1/en not_active Ceased
- 2015-02-20 CA CA2939786A patent/CA2939786C/en active Active
- 2015-02-20 US US15/117,982 patent/US9932344B2/en active Active
- 2015-02-20 JP JP2016553387A patent/JP6498212B2/ja active Active
- 2015-02-20 PL PL15706282T patent/PL3107914T3/pl unknown
- 2015-02-20 LT LTEP15706282.9T patent/LT3107914T/lt unknown
- 2015-02-20 AU AU2015220560A patent/AU2015220560B2/en active Active
- 2015-02-20 PT PT15706282T patent/PT3107914T/pt unknown
- 2015-02-20 HR HRP20190685TT patent/HRP20190685T1/hr unknown
- 2015-02-20 TR TR2019/05647T patent/TR201905647T4/tr unknown
- 2015-02-20 ME MEP-2019-119A patent/ME03427B/me unknown
- 2015-02-20 DK DK15706282.9T patent/DK3107914T3/en active
- 2015-02-20 ES ES15706282T patent/ES2721268T3/es active Active
- 2015-02-20 HU HUE15706282A patent/HUE043122T2/hu unknown
- 2015-02-20 SI SI201530714T patent/SI3107914T1/sl unknown
- 2015-02-20 EP EP15706282.9A patent/EP3107914B8/en active Active
- 2015-02-20 SM SM20190266T patent/SMT201900266T1/it unknown
- 2015-02-20 BR BR112016018633-8A patent/BR112016018633B1/pt active IP Right Grant
- 2015-02-20 NZ NZ724323A patent/NZ724323A/en unknown
-
2018
- 2018-03-30 US US15/941,063 patent/US10414772B2/en active Active
-
2019
- 2019-04-17 CY CY20191100425T patent/CY1121588T1/el unknown
- 2019-09-04 US US16/559,735 patent/US10927119B2/en active Active
-
2021
- 2021-02-15 US US17/175,780 patent/US11566029B2/en active Active
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