JP2016538310A5 - - Google Patents
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- JP2016538310A5 JP2016538310A5 JP2016534995A JP2016534995A JP2016538310A5 JP 2016538310 A5 JP2016538310 A5 JP 2016538310A5 JP 2016534995 A JP2016534995 A JP 2016534995A JP 2016534995 A JP2016534995 A JP 2016534995A JP 2016538310 A5 JP2016538310 A5 JP 2016538310A5
- Authority
- JP
- Japan
- Prior art keywords
- use according
- carbon atoms
- thienotriazolodiazepine compound
- formula
- leukemia
- 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.)
- Pending
Links
- 125000004432 carbon atom Chemical group C* 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000007962 solid dispersion Substances 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- -1 methyl ( S)-{4- (3′-cyanobiphenyl-4-yl) -2,3,9-trimethyl-6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a ] [1,4] diazepin-6-yl} acetate Chemical compound 0.000 claims 3
- GNMUEVRJHCWKTO-FQEVSTJZSA-N 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- Chemical compound C([C@@H]1N=C(C2=C(N3C(C)=NN=C31)SC(=C2C)C)C=1C=CC(Cl)=CC=1)C(=O)NC1=CC=C(O)C=C1 GNMUEVRJHCWKTO-FQEVSTJZSA-N 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 2
- UHDGCWIWMRVCDJ-ZAKLUEHWSA-N cytidine Chemical class O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-ZAKLUEHWSA-N 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 239000002254 cytotoxic agent Substances 0.000 claims 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims 2
- 239000012649 demethylating agent Substances 0.000 claims 2
- 239000003862 glucocorticoid Substances 0.000 claims 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- XAUDJQYHKZQPEU-KVQBGUIXSA-N 5-aza-2'-deoxycytidine Chemical group O=C1N=C(N)N=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 XAUDJQYHKZQPEU-KVQBGUIXSA-N 0.000 claims 1
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical group O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 claims 1
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 1
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- HMKHWYHCDUFAJR-UHFFFAOYSA-N acetamide;dihydrate Chemical compound O.O.CC(N)=O HMKHWYHCDUFAJR-UHFFFAOYSA-N 0.000 claims 1
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims 1
- 229960002756 azacitidine Drugs 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229960000684 cytarabine Drugs 0.000 claims 1
- 229960000975 daunorubicin Drugs 0.000 claims 1
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin 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(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims 1
- 229960003603 decitabine Drugs 0.000 claims 1
- 229960003957 dexamethasone Drugs 0.000 claims 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 1
- 150000004683 dihydrates Chemical class 0.000 claims 1
- 230000001973 epigenetic effect Effects 0.000 claims 1
- 229960005167 everolimus Drugs 0.000 claims 1
- 230000009477 glass transition Effects 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- FWZRWHZDXBDTFK-ZHACJKMWSA-N panobinostat Chemical compound CC1=NC2=CC=C[CH]C2=C1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FWZRWHZDXBDTFK-ZHACJKMWSA-N 0.000 claims 1
- 229960005184 panobinostat Drugs 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229940037128 systemic glucocorticoids Drugs 0.000 claims 1
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical group ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 1
- 229960000237 vorinostat Drugs 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361909702P | 2013-11-27 | 2013-11-27 | |
| US61/909,702 | 2013-11-27 | ||
| US201462012128P | 2014-06-13 | 2014-06-13 | |
| US62/012,128 | 2014-06-13 | ||
| US201462080804P | 2014-11-17 | 2014-11-17 | |
| US62/080,804 | 2014-11-17 | ||
| PCT/EP2014/075709 WO2015078929A1 (en) | 2013-11-27 | 2014-11-26 | Method of treating leukemia using pharmaceutical formulation containing thienotriazolodiazepine compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016538310A JP2016538310A (ja) | 2016-12-08 |
| JP2016538310A5 true JP2016538310A5 (enExample) | 2018-01-11 |
Family
ID=52000829
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016534995A Pending JP2016538310A (ja) | 2013-11-27 | 2014-11-26 | チエノトリアゾロジアゼピン化合物を含む医薬製剤を用いる白血病の治療方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9757385B2 (enExample) |
| EP (1) | EP3074018A1 (enExample) |
| JP (1) | JP2016538310A (enExample) |
| KR (1) | KR20160079823A (enExample) |
| CN (1) | CN105960239A (enExample) |
| WO (1) | WO2015078929A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9795612B2 (en) * | 2013-08-01 | 2017-10-24 | Merck Sharp & Dohme Corp. | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
| US20170095484A1 (en) * | 2014-05-02 | 2017-04-06 | Oncoethix Gmbh | Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds |
| CA2947601A1 (en) * | 2014-05-02 | 2015-11-05 | Oncoethix Gmbh | Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds |
| CN107427524A (zh) * | 2014-08-28 | 2017-12-01 | 翁科埃斯克斯有限公司 | 利用包含噻吩并三唑并二氮杂*化合物的药物组合物治疗急性髓细胞白血病或急性淋巴性白血病的方法 |
| US10702517B2 (en) | 2015-04-22 | 2020-07-07 | Celgene Quanticel Research, Inc. | Bromodomain inhibitor |
| EP3334725B1 (en) * | 2015-08-10 | 2025-04-23 | Dana-Farber Cancer Institute, Inc. | Bromodomain and extra terminal (bet) inhibitor and a protein phosphatase 2a (pp2a) activator for treating bet inhibitor resistant cancer |
| EP3795563B1 (en) | 2016-03-31 | 2024-07-17 | Oncternal Therapeutics, Inc. | Indoline analogs and uses thereof |
| MX395539B (es) * | 2016-07-29 | 2025-03-25 | Oncternal Therapeutics Inc | Usos de compuestos de indolinona |
| AU2017345468B2 (en) * | 2016-10-20 | 2022-06-02 | Celgene Quanticel Research, Inc. | Bromodomain inhibitor |
| EA202092635A1 (ru) | 2018-06-13 | 2021-03-23 | Дибли Аг | Получение конденсированных производных триазепина и их применение в качестве ингибиторов bet |
| CN108743591A (zh) * | 2018-07-17 | 2018-11-06 | 苏州大学 | 用于治疗癌症的药物组合物及其应用 |
| BR112023025562A2 (pt) | 2021-06-08 | 2024-02-20 | Poseidon Innovation Llc | Compostos anticâncer |
| WO2023229535A1 (en) | 2022-05-27 | 2023-11-30 | Engine Biosciences Pte. Ltd. | Bet polypeptide therapeutic agents for generating synthetic lethality in tumors |
| CN116098870B (zh) * | 2023-04-10 | 2023-07-25 | 上海赛默罗生物科技有限公司 | α5-GABAA受体调节剂的固体分散体及其制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2412776C (en) * | 2000-06-16 | 2011-03-15 | Mitsubishi Pharma Corporation | Compositions controlling release ph range and/or speed |
| CA2576222C (en) | 2004-08-10 | 2014-09-30 | Inex Pharmaceuticals Corporation | Compositions and methods for treating lymphoma |
| JP2009501707A (ja) * | 2005-07-06 | 2009-01-22 | カニサ・ファーマシューティカルズ・インコーポレイテッド | 癌の処置のためのゾスキダル、ダウノルビシン、およびシタラビン |
| US20070010466A1 (en) | 2005-07-06 | 2007-01-11 | Branimir Sikic | Zosuquidar, daunorubicin, and cytarabine for the treatment of cancer |
| MX2009005946A (es) | 2006-12-04 | 2009-06-17 | Novartis Ag | Combinacion de un inhibidor de desacetilasa de histona y un antimetabolito. |
| JP5478262B2 (ja) * | 2007-12-28 | 2014-04-23 | 田辺三菱製薬株式会社 | 抗癌剤 |
| EP2569434B1 (en) | 2010-05-14 | 2019-09-04 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia and related disorders |
| CN104311562B (zh) | 2010-05-14 | 2017-07-04 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
| US10226478B2 (en) | 2011-04-14 | 2019-03-12 | Cyclacel Limited | Dosage regimen for sapacitabine and decitabine in combination for treating acute myeloid leukemia |
| DE102011082013A1 (de) * | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| CA2877434A1 (en) | 2012-06-25 | 2014-01-03 | Oncoethix Sa | Method of treating lymphoma using thienotriazolodiazepine compounds |
| BR112015006537A2 (pt) * | 2012-09-28 | 2017-07-04 | Oncoethix Sa | dispersão sólida, formulação farmacêutica, cápsula farmacêutica, e, tablete farmacêutico |
| US9795612B2 (en) * | 2013-08-01 | 2017-10-24 | Merck Sharp & Dohme Corp. | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
-
2014
- 2014-11-26 US US15/039,307 patent/US9757385B2/en not_active Expired - Fee Related
- 2014-11-26 EP EP14805555.1A patent/EP3074018A1/en not_active Withdrawn
- 2014-11-26 JP JP2016534995A patent/JP2016538310A/ja active Pending
- 2014-11-26 CN CN201480065213.0A patent/CN105960239A/zh active Pending
- 2014-11-26 WO PCT/EP2014/075709 patent/WO2015078929A1/en not_active Ceased
- 2014-11-26 KR KR1020167013580A patent/KR20160079823A/ko not_active Withdrawn
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