ES2721268T3 - Compuestos de pirazolo[1,5-a]pirimidina-5,7-diamina como inhibidores de CDK y su uso terapéutico - Google Patents
Compuestos de pirazolo[1,5-a]pirimidina-5,7-diamina como inhibidores de CDK y su uso terapéutico Download PDFInfo
- Publication number
- ES2721268T3 ES2721268T3 ES15706282T ES15706282T ES2721268T3 ES 2721268 T3 ES2721268 T3 ES 2721268T3 ES 15706282 T ES15706282 T ES 15706282T ES 15706282 T ES15706282 T ES 15706282T ES 2721268 T3 ES2721268 T3 ES 2721268T3
- Authority
- ES
- Spain
- Prior art keywords
- piperazino
- independently
- branched
- linear
- alkyl
- 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
Links
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 title 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 title 1
- 230000001225 therapeutic effect Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 13
- 229920006395 saturated elastomer Polymers 0.000 abstract 12
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 7
- -1 pyrrolidino, piperidino, morpholino, piperazino Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 102100037241 Endoglin Human genes 0.000 abstract 1
- 101000881679 Homo sapiens Endoglin Proteins 0.000 abstract 1
- 101000799194 Homo sapiens Serine/threonine-protein kinase receptor R3 Proteins 0.000 abstract 1
- 102100034136 Serine/threonine-protein kinase receptor R3 Human genes 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 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)
- 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 Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 |
|---|---|
| ES2721268T3 true ES2721268T3 (es) | 2019-07-30 |
Family
ID=50482596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES15706282T Active ES2721268T3 (es) | 2014-02-21 | 2015-02-20 | Compuestos de pirazolo[1,5-a]pirimidina-5,7-diamina como inhibidores de CDK y su uso terapéutico |
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 |
| CA2966164C (en) | 2014-10-31 | 2023-10-17 | Ube Industries, Ltd. | Substituted dihydropyrrolopyrazole compound |
| JP6596090B2 (ja) | 2014-12-17 | 2019-10-23 | キングス カレッジ ロンドン | レチノイン酸受容体ベータ（ＲＡＲβ）アゴニストとしてのビシクロヘテロアリール−ヘテロアリール−安息香酸化合物 |
| CN107801397B (zh) * | 2015-02-13 | 2021-07-30 | 达纳－法伯癌症研究所公司 | Lrrk2抑制剂及其制备和使用方法 |
| MX394157B (es) | 2015-06-15 | 2025-03-24 | Ube Corp | Derivado de dihidropirrolopirazol sustituido. |
| WO2017096326A1 (en) | 2015-12-02 | 2017-06-08 | Massachusetts Institute Of Technology | Method for efficient generation of neurons from non-neuronal cells |
| JP6832430B2 (ja) | 2016-08-31 | 2021-02-24 | アジオス ファーマシューティカルズ， インコーポレイテッド | 細胞代謝過程の阻害剤 |
| SI3658557T1 (sl) | 2017-07-28 | 2024-10-30 | Takeda Pharmaceutical Company Limited | Zaviralci TYK2 in njihova uporaba |
| 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 |
| KR20200141487A (ko) * | 2018-04-11 | 2020-12-18 | 주식회사 큐리언트 | 사이클린 의존성 키나아제의 선택적 억제제로서의 피라졸로-트리아진 및/또는 피라졸로피리미딘 유도체 |
| US11447493B2 (en) | 2018-05-02 | 2022-09-20 | Kinnate Biopharma Inc. | Inhibitors of cyclin-dependent kinases |
| EP3813819A4 (en) | 2018-06-29 | 2022-08-17 | Kinnate Biopharma Inc. | CYCLIN-DEPENDENT KINASE INHIBITORS |
| US11155560B2 (en) * | 2018-10-30 | 2021-10-26 | Kronos Bio, Inc. | Substituted pyrazolo[1,5-a]pyrimidines for modulating CDK9 activity |
| EP3885347B1 (en) | 2018-11-14 | 2023-11-22 | UBE Corporation | Dihydropyrrolopyrazole derivative |
| 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 |
| US12398132B2 (en) * | 2019-07-10 | 2025-08-26 | Aucentra Therapeutics Pty Ltd | Derivatives of 4-(imidazo[1,2-a]pyridin-3-yl)-n-(pyridinyl)pyrimidin-2-amine as therapeutic agents |
| WO2021087138A1 (en) * | 2019-10-29 | 2021-05-06 | 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 |
| WO2021176045A1 (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 |
| EP4282868B1 (en) * | 2021-01-22 | 2026-03-04 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Substituted pyrazolo[1,5-a]pyrimidine-7-amine derivative, and compositions and medical use thereof |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| 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 |
| JP2024543136A (ja) * | 2021-11-24 | 2024-11-19 | クロノス バイオ インコーポレイテッド | （１Ｓ，３Ｓ）－Ｎ１－（５－（ペンタン－３－イル）ピラゾロ［１，５－ａ］ピリミジン－７－イル）シクロペンタン－１，３－ジアミンの多形性形態および塩形態 |
| WO2024102447A1 (en) * | 2022-11-10 | 2024-05-16 | 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 |
| TW202500147A (zh) | 2023-06-27 | 2025-01-01 | 美商亞文納營運公司 | 雌激素受體降解劑與ｃｄｋ７抑制劑之組合 |
| WO2025057087A1 (en) | 2023-09-11 | 2025-03-20 | Assia Chemical Industries Ltd. | Solid state forms of samuraciclib |
| WO2025208097A1 (en) * | 2024-03-29 | 2025-10-02 | The Translational Genomics Research Institute | Cdk7 inhibitors and methods of use thereof |
| WO2025208104A1 (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 |
|---|---|---|---|---|
| EP1246823A1 (en) | 1999-12-28 | 2002-10-09 | Pharmacopeia, Inc. | Pyrimidine and triazine kinase inhibitors |
| MXPA05002571A (es) | 2002-09-04 | 2005-09-08 | Schering Corp | Pirazolopirimidinas como inhibidores de cinasa dependientes de ciclina. |
| CA2513684A1 (en) | 2003-01-31 | 2004-08-19 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| US7557110B2 (en) | 2003-02-28 | 2009-07-07 | Teijin Pharma Limited | Pyrazolo[1,5-A] pyrimidine derivatives |
| 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 |
| AU2008261027A1 (en) * | 2007-06-05 | 2008-12-11 | Emory University | Selective inhibitors for cyclin-dependent kinases |
| JP5802676B2 (ja) * | 2009-12-04 | 2015-10-28 | センワ バイオサイエンシズ インコーポレイテッド | Ｃｋ２阻害剤としてのピラゾロピリミジンおよび関連複素環化合物 |
| WO2012059932A1 (en) | 2010-11-01 | 2012-05-10 | Aurigene Discovery Technologies Limited | 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors |
| EP3812387A1 (en) * | 2011-07-21 | 2021-04-28 | Sumitomo Dainippon Pharma Oncology, 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 ME MEP-2019-119A patent/ME03427B/me unknown
- 2015-02-20 HR HRP20190685TT patent/HRP20190685T1/hr unknown
- 2015-02-20 CA CA2939786A patent/CA2939786C/en active Active
- 2015-02-20 BR BR112016018633-8A patent/BR112016018633B1/pt active IP Right Grant
- 2015-02-20 HU HUE15706282A patent/HUE043122T2/hu unknown
- 2015-02-20 LT LTEP15706282.9T patent/LT3107914T/lt unknown
- 2015-02-20 SI SI201530714T patent/SI3107914T1/sl unknown
- 2015-02-20 RS RS20190487A patent/RS58704B1/sr unknown
- 2015-02-20 AU AU2015220560A patent/AU2015220560B2/en active Active
- 2015-02-20 WO PCT/GB2015/050494 patent/WO2015124941A1/en not_active Ceased
- 2015-02-20 ES ES15706282T patent/ES2721268T3/es active Active
- 2015-02-20 SM SM20190266T patent/SMT201900266T1/it unknown
- 2015-02-20 PT PT15706282T patent/PT3107914T/pt unknown
- 2015-02-20 PL PL15706282T patent/PL3107914T3/pl unknown
- 2015-02-20 JP JP2016553387A patent/JP6498212B2/ja active Active
- 2015-02-20 TR TR2019/05647T patent/TR201905647T4/tr unknown
- 2015-02-20 NZ NZ724323A patent/NZ724323A/en unknown
- 2015-02-20 EP EP15706282.9A patent/EP3107914B8/en active Active
- 2015-02-20 US US15/117,982 patent/US9932344B2/en active Active
- 2015-02-20 DK DK15706282.9T patent/DK3107914T3/en active
- 2015-02-20 CN CN201580011502.7A patent/CN106103445B/zh 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
-
2021
- 2021-02-15 US US17/175,780 patent/US11566029B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2721268T3 (es) | Compuestos de pirazolo[1,5-a]pirimidina-5,7-diamina como inhibidores de CDK y su uso terapéutico | |
| AR106806A1 (es) | Inhibidores triazol de acc y usos de los mismos | |
| PE20190339A1 (es) | 1h-pirazolo[4,3-b] piridinas como inhibidores de pde1 | |
| PE20210469A1 (es) | Compuestos de naftiridinona sustituidos utiles como activadores de celulas t | |
| CO2019003349A2 (es) | Compuestos de benzo[b]tiofeno como agonistas de sting | |
| AR067757A1 (es) | Derivados de imidazo[4,5-c]piridin-2-ona, composiciones farmaceuticas que los contienen, procedimiento para su preparacion y uso de los mismos como agentes antivirales. | |
| MX2016014238A (es) | Composicion limpiadora. | |
| AR054560A1 (es) | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer | |
| AR107966A2 (es) | Derivados de pirimidina y piridina inhibidores de la proteína quinasa | |
| PE20151764A1 (es) | Derivados de pirrolo[2,3-d]pirimidina | |
| PE20151413A1 (es) | Inhibidores de bmi-1 de pirimidina inversa sustituida | |
| CO5580788A2 (es) | Compuestos de bencimidazol sustituidos utiles como inhibidores de proteina cinasas | |
| CO6170361A2 (es) | Composiciones y metodos para modular receptores de c-kit y pdgfr | |
| AR052682A1 (es) | DERIVADOS DE 5, 6, 7, 8 - TETRAHIDROTIEN[2, 3 - B]QUINOLINA uTILES PARA INHIBIR LA ACTIVIDAD DE QUINESINA DE KSP, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y SU USO EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS. | |
| CL2022000551A1 (es) | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl | |
| BR112017028075A2 (pt) | material de base sólida para uso externo na pele, composição aquosa e método de para sua produção | |
| AR058701A1 (es) | Derivados de piracinil-s-espiro-oxacinoquinolin-pirimidin-triona como agentes antibacterianos | |
| PE20200932A1 (es) | Novedosos derivados de pirazolo-pirrolo-pirimidina como inhibidores de p2x3 | |
| UY25265A1 (es) | Procedimiento para la preparacion de acidos 8-alcoxi-quinoloncarboxilicos. | |
| AR120452A1 (es) | Compuestos heterocíclicos y usos de los mismos | |
| PE20190109A1 (es) | Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina | |
| AR045326A1 (es) | Derivados de aminoquinolina y su uso como ligandos a3 de adenosina | |
| PE20190803A1 (es) | 1-arilnaftiridin-3-carboxamidas 7-sustituidas y su uso | |
| AR028714A1 (es) | Piridin-2-il-aminoalquilcarbonilglicil-beta-alanina y derivados | |
| PE20181895A1 (es) | Compuestos de cinnolin-4-amina y su uso en el tratamiento del cancer |