CY1121588T1 - Ενωσεις πυραζολο[1,5-α]πυριμιδινο-5,7-διαμινης ως αναστολεις cdk και θεραπευτικη χρηση αυτων - Google Patents
Ενωσεις πυραζολο[1,5-α]πυριμιδινο-5,7-διαμινης ως αναστολεις cdk και θεραπευτικη χρηση αυτωνInfo
- Publication number
- CY1121588T1 CY1121588T1 CY20191100425T CY191100425T CY1121588T1 CY 1121588 T1 CY1121588 T1 CY 1121588T1 CY 20191100425 T CY20191100425 T CY 20191100425T CY 191100425 T CY191100425 T CY 191100425T CY 1121588 T1 CY1121588 T1 CY 1121588T1
- Authority
- CY
- Cyprus
- Prior art keywords
- disorders
- cdk
- compounds
- disorders associated
- present
- Prior art date
Links
- 230000001225 therapeutic effect Effects 0.000 title abstract 2
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 title 1
- 108090000266 Cyclin-dependent kinases Proteins 0.000 abstract 8
- 102000003903 Cyclin-dependent kinases Human genes 0.000 abstract 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 8
- 150000001875 compounds Chemical class 0.000 abstract 3
- 238000011282 treatment Methods 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 229940122815 Aromatase inhibitor Drugs 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 abstract 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 abstract 1
- 108010025454 Cyclin-Dependent Kinase 5 Proteins 0.000 abstract 1
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 abstract 1
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 abstract 1
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 abstract 1
- 102100023263 Cyclin-dependent kinase 10 Human genes 0.000 abstract 1
- 102100038111 Cyclin-dependent kinase 12 Human genes 0.000 abstract 1
- 102100038114 Cyclin-dependent kinase 13 Human genes 0.000 abstract 1
- 102100033145 Cyclin-dependent kinase 19 Human genes 0.000 abstract 1
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 abstract 1
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 abstract 1
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 abstract 1
- 102100026810 Cyclin-dependent kinase 7 Human genes 0.000 abstract 1
- 102100024456 Cyclin-dependent kinase 8 Human genes 0.000 abstract 1
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 abstract 1
- 102100026805 Cyclin-dependent-like kinase 5 Human genes 0.000 abstract 1
- 229940125497 HER2 kinase inhibitor Drugs 0.000 abstract 1
- 101000908138 Homo sapiens Cyclin-dependent kinase 10 Proteins 0.000 abstract 1
- 101000884345 Homo sapiens Cyclin-dependent kinase 12 Proteins 0.000 abstract 1
- 101000884348 Homo sapiens Cyclin-dependent kinase 13 Proteins 0.000 abstract 1
- 101000944345 Homo sapiens Cyclin-dependent kinase 19 Proteins 0.000 abstract 1
- 101000911952 Homo sapiens Cyclin-dependent kinase 7 Proteins 0.000 abstract 1
- 101000980937 Homo sapiens Cyclin-dependent kinase 8 Proteins 0.000 abstract 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- -1 PPDA compounds Chemical class 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 229940046836 anti-estrogen Drugs 0.000 abstract 1
- 230000001833 anti-estrogenic effect Effects 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 239000003886 aromatase inhibitor Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 238000011970 concomitant therapy Methods 0.000 abstract 1
- 231100000433 cytotoxic Toxicity 0.000 abstract 1
- 229940127089 cytotoxic agent Drugs 0.000 abstract 1
- 230000001472 cytotoxic effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000328 estrogen antagonist Substances 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000035772 mutation Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000002018 overexpression Effects 0.000 abstract 1
- 230000037361 pathway Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- GLWUDZAXMREBCZ-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine-5,7-diamine Chemical class N1=C(N)C=C(N)N2N=CC=C21 GLWUDZAXMREBCZ-UHFFFAOYSA-N 0.000 abstract 1
- 238000011450 sequencing therapy Methods 0.000 abstract 1
- 238000011144 upstream manufacturing Methods 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB201403093A GB201403093D0 (en) | 2014-02-21 | 2014-02-21 | Therapeutic compounds and their use |
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| CY1121588T1 true CY1121588T1 (el) | 2020-05-29 |
Family
ID=50482596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20191100425T CY1121588T1 (el) | 2014-02-21 | 2019-04-17 | Ενωσεις πυραζολο[1,5-α]πυριμιδινο-5,7-διαμινης ως αναστολεις cdk και θεραπευτικη χρηση αυτων |
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) |
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| GB201403093D0 (en) | 2014-02-21 | 2014-04-09 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| US10131679B2 (en) | 2014-10-31 | 2018-11-20 | Ube Industries, Ltd. | Substituted dihydropyrrolopyrazole compound |
| CN107207488B (zh) | 2014-12-17 | 2020-11-17 | 伦敦皇家学院 | 作为视黄酸受体β(RARβ)激动剂的双环杂芳基-杂芳基-苯甲酸化合物 |
| US10913744B2 (en) * | 2015-02-13 | 2021-02-09 | Dana-Farber Cancer Institute, Inc. | LRRK2 inhibitors and methods of making and using the same |
| AU2016281225B2 (en) | 2015-06-15 | 2020-10-15 | Ube Corporation | 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 |
| UA125852C2 (uk) | 2016-08-31 | 2022-06-22 | Ле Лаборатуар Сервьє | Інгібітори клітинних метаболічних процесів |
| IL317854A (en) | 2017-07-28 | 2025-02-01 | Takeda Pharmaceuticals Co | TYK2 inhibitors and their uses |
| 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 |
| WO2019035866A1 (en) * | 2017-08-15 | 2019-02-21 | The Brigham & Women's Hospital, Inc. | COMPOSITIONS AND METHODS FOR TREATING THE 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 |
| MY207194A (en) * | 2018-04-11 | 2025-02-05 | Qurient Co Ltd | Pharmaceutically active pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives |
| KR102966455B1 (ko) * | 2018-04-11 | 2026-05-15 | 주식회사 큐리언트 | 사이클린 의존성 키나아제의 선택적 억제제로서의 피라졸로-트리아진 및/또는 피라졸로피리미딘 유도체 |
| WO2019213403A1 (en) | 2018-05-02 | 2019-11-07 | Kinnate Biopharma Inc. | Inhibitors of cyclin-dependent kinases |
| SG11202013175SA (en) | 2018-06-29 | 2021-01-28 | Kinnate Biopharma Inc | Inhibitors of cyclin-dependent kinases |
| KR20250174699A (ko) * | 2018-10-30 | 2025-12-12 | 크로노스 바이오, 인코포레이티드 | Cdk9 활성을 조절하기 위한 화합물, 조성물 및 방법 |
| JP7530297B2 (ja) | 2018-11-14 | 2024-08-07 | Ｕｂｅ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 |
| US20220144841A1 (en) * | 2019-03-13 | 2022-05-12 | The Translational Genomics Research Institute | Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors |
| CN114269742B (zh) * | 2019-07-10 | 2024-07-16 | 常州千红生化制药股份有限公司 | 作为治疗剂的4-(咪唑并[1,2-a]吡啶-3-基)-N-(吡啶基)嘧啶-2-胺的衍生物 |
| CN114901284A (zh) * | 2019-10-29 | 2022-08-12 | 希洛斯医药品股份有限公司 | 用细胞周期蛋白依赖性激酶7(cdk7)抑制剂治疗生物标志物鉴定的患者的癌症的方法 |
| GB201918541D0 (en) | 2019-12-16 | 2020-01-29 | Carrick Therapeutics Ltd | Therapeutic compounds and their use |
| CA3174507A1 (en) * | 2020-03-06 | 2021-09-10 | 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 |
| CA3217792A1 (en) | 2021-05-07 | 2022-11-10 | 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 |
| EP4436569A4 (en) * | 2021-11-24 | 2025-10-01 | Kronos Bio Inc | POLYMORPHIC AND SALT FORMS OF (LS,3S))-N-(5-(PENTAN-3-YL)PYRAZOLO[1,5-A]PYRIMIDIN-7-YL)CYCLOPENTANE-L,3-DIAMINE |
| CA3251059A1 (en) | 2022-05-02 | 2023-11-09 | The Board Of Trustees Of The Leland Stanford Junior University | Compositions, systems and methods for modulating a target gene |
| US20260191864A1 (en) * | 2022-11-10 | 2026-07-09 | Emory University | Uses of Hydroimidazopyridopyrimidinone Derivatives for Managing Aneurysms or Other Vascular Conditions or Diseases |
| CN120752238A (zh) * | 2023-02-20 | 2025-10-03 | 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 |
| CN120712267A (zh) * | 2023-02-21 | 2025-09-26 | 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 |
| EP4777509A1 (en) | 2023-09-11 | 2026-07-22 | Assia Chemical Industries Ltd. | Solid state forms of samuraciclib |
| 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 |
|---|---|---|---|---|
| CA2396693A1 (en) | 1999-12-28 | 2001-07-05 | Stephen T. Wrobleski | Cytokine, especially tnf-alpha, inhibitors |
| JP4881558B2 (ja) | 2002-09-04 | 2012-02-22 | シェーリング コーポレイション | サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン |
| JP2006516573A (ja) | 2003-01-31 | 2006-07-06 | メルク エンド カムパニー インコーポレーテッド | 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての３−アミノ−４−フェニルブタン酸誘導体 |
| JP4564485B2 (ja) | 2003-02-28 | 2010-10-20 | 帝人ファーマ株式会社 | ピラゾロ［１，５−ａ］ピリミジン誘導体 |
| WO2004087707A1 (en) * | 2003-03-31 | 2004-10-14 | 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 |
| US20070082900A1 (en) * | 2005-10-06 | 2007-04-12 | Schering Corporation | Methods for inhibiting protein kinases |
| JP2010529140A (ja) * | 2007-06-05 | 2010-08-26 | エモリー・ユニバーシテイ | サイクリン依存性キナーゼの選択的阻害剤 |
| PL2509602T3 (pl) | 2009-12-04 | 2017-08-31 | Senhwa Biosciences, Inc. | Pirazolopirymidyny i podobne heterocykle jako inhibitory ck2 |
| WO2012059932A1 (en) | 2010-11-01 | 2012-05-10 | Aurigene Discovery Technologies Limited | 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors |
| DK2734205T3 (en) * | 2011-07-21 | 2018-06-14 | 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 JP JP2016553387A patent/JP6498212B2/ja active Active
- 2015-02-20 ES ES15706282T patent/ES2721268T3/es active Active
- 2015-02-20 CA CA2939786A patent/CA2939786C/en active Active
- 2015-02-20 PL PL15706282T patent/PL3107914T3/pl unknown
- 2015-02-20 DK DK15706282.9T patent/DK3107914T3/en active
- 2015-02-20 SM SM20190266T patent/SMT201900266T1/it unknown
- 2015-02-20 RS RS20190487A patent/RS58704B1/sr unknown
- 2015-02-20 PT PT15706282T patent/PT3107914T/pt unknown
- 2015-02-20 BR BR112016018633-8A patent/BR112016018633B1/pt active IP Right Grant
- 2015-02-20 TR TR2019/05647T patent/TR201905647T4/tr unknown
- 2015-02-20 NZ NZ724323A patent/NZ724323A/en unknown
- 2015-02-20 WO PCT/GB2015/050494 patent/WO2015124941A1/en not_active Ceased
- 2015-02-20 HR HRP20190685TT patent/HRP20190685T1/hr unknown
- 2015-02-20 EP EP15706282.9A patent/EP3107914B8/en active Active
- 2015-02-20 CN CN201580011502.7A patent/CN106103445B/zh active Active
- 2015-02-20 ME MEP-2019-119A patent/ME03427B/me unknown
- 2015-02-20 HU HUE15706282A patent/HUE043122T2/hu unknown
- 2015-02-20 AU AU2015220560A patent/AU2015220560B2/en active Active
- 2015-02-20 SI SI201530714T patent/SI3107914T1/sl unknown
- 2015-02-20 LT LTEP15706282.9T patent/LT3107914T/lt unknown
- 2015-02-20 US US15/117,982 patent/US9932344B2/en active Active
-
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
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2021
- 2021-02-15 US US17/175,780 patent/US11566029B2/en active Active
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