JP2020534346A5 - - Google Patents
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- JP2020534346A5 JP2020534346A5 JP2020517114A JP2020517114A JP2020534346A5 JP 2020534346 A5 JP2020534346 A5 JP 2020534346A5 JP 2020517114 A JP2020517114 A JP 2020517114A JP 2020517114 A JP2020517114 A JP 2020517114A JP 2020534346 A5 JP2020534346 A5 JP 2020534346A5
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- Prior art keywords
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- 150000001875 compounds Chemical class 0.000 claims description 50
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 36
- 208000035475 disorder Diseases 0.000 claims description 36
- 238000000034 method Methods 0.000 claims description 25
- 239000013543 active substance Substances 0.000 claims description 18
- 206010006187 Breast cancer Diseases 0.000 claims description 10
- 208000026310 Breast neoplasm Diseases 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 239000012453 solvate Substances 0.000 claims description 10
- 229940122815 Aromatase inhibitor Drugs 0.000 claims description 9
- 239000003886 aromatase inhibitor Substances 0.000 claims description 9
- 239000000328 estrogen antagonist Substances 0.000 claims description 9
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 7
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 6
- 101150029707 ERBB2 gene Proteins 0.000 claims description 6
- 239000002246 antineoplastic agent Substances 0.000 claims description 6
- 231100000433 cytotoxic Toxicity 0.000 claims description 6
- 229940127089 cytotoxic agent Drugs 0.000 claims description 6
- 230000001472 cytotoxic effect Effects 0.000 claims description 6
- 230000002062 proliferating effect Effects 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 229940079593 drug Drugs 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 238000002560 therapeutic procedure Methods 0.000 claims description 5
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 claims description 4
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 4
- 229930012538 Paclitaxel Natural products 0.000 claims description 4
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 4
- 229960001592 paclitaxel Drugs 0.000 claims description 4
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 4
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-VTZDEGQISA-N 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 3
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims description 3
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 3
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims description 3
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 3
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 3
- XNRVGTHNYCNCFF-UHFFFAOYSA-N Lapatinib ditosylate monohydrate Chemical compound O.CC1=CC=C(S(O)(=O)=O)C=C1.CC1=CC=C(S(O)(=O)=O)C=C1.O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 XNRVGTHNYCNCFF-UHFFFAOYSA-N 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 201000004681 Psoriasis Diseases 0.000 claims description 3
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 3
- 229940123237 Taxane Drugs 0.000 claims description 3
- 208000036142 Viral infection Diseases 0.000 claims description 3
- TXUZVZSFRXZGTL-QPLCGJKRSA-N afimoxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=C(O)C=C1 TXUZVZSFRXZGTL-QPLCGJKRSA-N 0.000 claims description 3
- 229960002932 anastrozole Drugs 0.000 claims description 3
- 229940046836 anti-estrogen Drugs 0.000 claims description 3
- 230000001833 anti-estrogenic effect Effects 0.000 claims description 3
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims description 3
- 229960004117 capecitabine Drugs 0.000 claims description 3
- 229960004562 carboplatin Drugs 0.000 claims description 3
- 230000004663 cell proliferation Effects 0.000 claims description 3
- 229960004397 cyclophosphamide Drugs 0.000 claims description 3
- 229960003668 docetaxel Drugs 0.000 claims description 3
- 229960004679 doxorubicin Drugs 0.000 claims description 3
- 229960001904 epirubicin Drugs 0.000 claims description 3
- 229960000255 exemestane Drugs 0.000 claims description 3
- 229960002949 fluorouracil Drugs 0.000 claims description 3
- 229960005277 gemcitabine Drugs 0.000 claims description 3
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 3
- 229940022353 herceptin Drugs 0.000 claims description 3
- 238000000338 in vitro Methods 0.000 claims description 3
- 208000028867 ischemia Diseases 0.000 claims description 3
- 208000017169 kidney disease Diseases 0.000 claims description 3
- 229960004891 lapatinib Drugs 0.000 claims description 3
- 229960003881 letrozole Drugs 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 229960002087 pertuzumab Drugs 0.000 claims description 3
- 229960001603 tamoxifen Drugs 0.000 claims description 3
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims description 3
- 230000009385 viral infection Effects 0.000 claims description 3
- 230000006907 apoptotic process Effects 0.000 claims description 2
- 230000006369 cell cycle progression Effects 0.000 claims description 2
- 150000004677 hydrates Chemical class 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 230000000340 anti-metabolite Effects 0.000 claims 2
- 229940100197 antimetabolite Drugs 0.000 claims 2
- 239000002256 antimetabolite Substances 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 230000001737 promoting effect Effects 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 102000003903 Cyclin-dependent kinases Human genes 0.000 description 8
- 108090000266 Cyclin-dependent kinases Proteins 0.000 description 8
- 238000011278 co-treatment Methods 0.000 description 4
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- MRWKUIOLQRITLV-MOPGFXCFSA-N CCc(cn[n]1c(NCc2cccc(C#N)c2)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O Chemical compound CCc(cn[n]1c(NCc2cccc(C#N)c2)c2)c1nc2NC[C@@H](CCNC1)[C@H]1O MRWKUIOLQRITLV-MOPGFXCFSA-N 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000001668 ameliorated effect Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229940078010 arimidex Drugs 0.000 description 1
- 229940087620 aromasin Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229940087476 femara Drugs 0.000 description 1
- 229960002258 fulvestrant Drugs 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 229940085033 nolvadex Drugs 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 229940063683 taxotere Drugs 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1715194.5 | 2017-09-20 | ||
| GBGB1715194.5A GB201715194D0 (en) | 2017-09-20 | 2017-09-20 | Compounds and their therapeutic use |
| PCT/EP2018/075482 WO2019057825A1 (en) | 2017-09-20 | 2018-09-20 | 4 - [[(7-AMINOPYRAZOLO [1,5-A] PYRIMIDIN-5-YL) AMINO] METHYL] PIPERIDIN-3-OL COMPOUNDS AS CDK INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020534346A JP2020534346A (ja) | 2020-11-26 |
| JP2020534346A5 true JP2020534346A5 (enExample) | 2021-10-28 |
| JP7148604B2 JP7148604B2 (ja) | 2022-10-05 |
Family
ID=60159506
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020517114A Active JP7148604B2 (ja) | 2017-09-20 | 2018-09-20 | ＣＤＫ阻害剤としての４－［［（７－アミノピラゾロ［１，５－ａ］ピリミジン－５－イル）アミノ］メチル］ピペリジン－３－オール化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US11857552B2 (enExample) |
| EP (1) | EP3684769B1 (enExample) |
| JP (1) | JP7148604B2 (enExample) |
| CN (1) | CN111566106B (enExample) |
| AU (1) | AU2018335841B2 (enExample) |
| BR (1) | BR112020005279B1 (enExample) |
| CA (1) | CA3075461C (enExample) |
| GB (1) | GB201715194D0 (enExample) |
| IL (1) | IL273396B2 (enExample) |
| MA (1) | MA50161A (enExample) |
| WO (1) | WO2019057825A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201715194D0 (en) | 2017-09-20 | 2017-11-01 | Carrick Therapeutics Ltd | Compounds and their therapeutic use |
| US20220144841A1 (en) * | 2019-03-13 | 2022-05-12 | The Translational Genomics Research Institute | Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors |
| GB201918541D0 (en) * | 2019-12-16 | 2020-01-29 | Carrick Therapeutics Ltd | Therapeutic compounds and their use |
| US20230348475A1 (en) * | 2020-09-17 | 2023-11-02 | The Translational Genomics Research Institute | Imidazopyridazine and imidazopyrazine compounds as inhibitors of cdk7 |
| GB202108572D0 (en) * | 2021-06-16 | 2021-07-28 | Carrick Therapeutics Ltd | Therapeutic compounds and their use |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| 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 |
| CN117899202B (zh) * | 2024-01-19 | 2024-11-26 | 杭州师范大学 | Cdk12蛋白及其编码基因在制备抗病毒药物中的应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2396693A1 (en) | 1999-12-28 | 2001-07-05 | Stephen T. Wrobleski | Cytokine, especially tnf-alpha, inhibitors |
| CA2497440C (en) | 2002-09-04 | 2011-03-22 | Schering Corporation | Pyrazolopyrimidines as cyclin-dependent kinase inhibitors |
| WO2004069162A2 (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 |
| BRPI0407834A (pt) | 2003-02-28 | 2006-02-14 | Teijin Pharma Ltd | composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase |
| 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 |
| AU2008261027A1 (en) * | 2007-06-05 | 2008-12-11 | Emory University | Selective inhibitors for cyclin-dependent kinases |
| SG181507A1 (en) | 2009-12-04 | 2012-07-30 | Cylene Pharmaceuticals Inc | Pyrazolopyrimidines and related heterocycles as ck2 inhibitors |
| WO2012059932A1 (en) | 2010-11-01 | 2012-05-10 | Aurigene Discovery Technologies Limited | 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors |
| EP2634190A1 (en) | 2012-03-01 | 2013-09-04 | Lead Discovery Center GmbH | Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhinitors |
| EP2634189A1 (en) | 2012-03-01 | 2013-09-04 | Lead Discovery Center GmbH | Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors |
| GB201403093D0 (en) * | 2014-02-21 | 2014-04-09 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB201715194D0 (en) | 2017-09-20 | 2017-11-01 | Carrick Therapeutics Ltd | Compounds and their therapeutic use |
-
2017
- 2017-09-20 GB GBGB1715194.5A patent/GB201715194D0/en not_active Ceased
-
2018
- 2018-09-20 US US16/648,011 patent/US11857552B2/en active Active
- 2018-09-20 MA MA050161A patent/MA50161A/fr unknown
- 2018-09-20 AU AU2018335841A patent/AU2018335841B2/en active Active
- 2018-09-20 WO PCT/EP2018/075482 patent/WO2019057825A1/en not_active Ceased
- 2018-09-20 CA CA3075461A patent/CA3075461C/en active Active
- 2018-09-20 JP JP2020517114A patent/JP7148604B2/ja active Active
- 2018-09-20 BR BR112020005279-5A patent/BR112020005279B1/pt active IP Right Grant
- 2018-09-20 CN CN201880074480.2A patent/CN111566106B/zh active Active
- 2018-09-20 EP EP18773442.1A patent/EP3684769B1/en active Active
-
2020
- 2020-03-18 IL IL273396A patent/IL273396B2/en unknown