JP2017514909A5 - - Google Patents
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- Publication number
- JP2017514909A5 JP2017514909A5 JP2017510455A JP2017510455A JP2017514909A5 JP 2017514909 A5 JP2017514909 A5 JP 2017514909A5 JP 2017510455 A JP2017510455 A JP 2017510455A JP 2017510455 A JP2017510455 A JP 2017510455A JP 2017514909 A5 JP2017514909 A5 JP 2017514909A5
- Authority
- JP
- Japan
- Prior art keywords
- therapeutic agent
- acute
- leukemia
- thieno
- triazolo
- 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
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 43
- 239000003814 drug Substances 0.000 claims description 38
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 26
- 239000007962 solid dispersion Substances 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 19
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 16
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 14
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 14
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 11
- 229920000642 polymer Polymers 0.000 claims description 9
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims description 6
- 239000002243 precursor Substances 0.000 claims description 6
- 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 description 5
- 230000001154 acute effect Effects 0.000 claims description 5
- 208000032839 leukemia Diseases 0.000 claims description 5
- -1 (S) -2- [4- (4-chlorophenyl) -2,3, 9-Trimethyl-6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-6-yl] -N- (4-hydroxyphenyl) acetamide compound Chemical class 0.000 claims description 4
- 208000025324 B-cell acute lymphoblastic leukemia Diseases 0.000 claims description 4
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 claims description 4
- 230000005856 abnormality Effects 0.000 claims description 4
- 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 description 4
- 230000009477 glass transition Effects 0.000 claims description 4
- 230000035800 maturation Effects 0.000 claims description 4
- 230000000306 recurrent effect Effects 0.000 claims description 4
- 230000002068 genetic effect Effects 0.000 claims description 3
- 208000016557 Acute basophilic leukemia Diseases 0.000 claims description 2
- 206010000871 Acute monocytic leukaemia Diseases 0.000 claims description 2
- 206010000890 Acute myelomonocytic leukaemia Diseases 0.000 claims description 2
- 208000016585 Acute panmyelosis with myelofibrosis Diseases 0.000 claims description 2
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims description 2
- 208000033775 Basophilic Acute Leukemia Diseases 0.000 claims description 2
- 208000023611 Burkitt leukaemia Diseases 0.000 claims description 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims description 2
- 206010008583 Chloroma Diseases 0.000 claims description 2
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims description 2
- 206010058314 Dysplasia Diseases 0.000 claims description 2
- 206010014950 Eosinophilia Diseases 0.000 claims description 2
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims description 2
- 208000036566 Erythroleukaemia Diseases 0.000 claims description 2
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims description 2
- 241000124008 Mammalia Species 0.000 claims description 2
- 208000035490 Megakaryoblastic Acute Leukemia Diseases 0.000 claims description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 2
- 208000033835 Myelomonocytic Acute Leukemia Diseases 0.000 claims description 2
- 208000008601 Polycythemia Diseases 0.000 claims description 2
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims description 2
- 201000011176 T-cell adult acute lymphocytic leukemia Diseases 0.000 claims description 2
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims description 2
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims description 2
- 208000021841 acute erythroid leukemia Diseases 0.000 claims description 2
- 208000013593 acute megakaryoblastic leukemia Diseases 0.000 claims description 2
- 208000020700 acute megakaryocytic leukemia Diseases 0.000 claims description 2
- 208000011912 acute myelomonocytic leukemia M4 Diseases 0.000 claims description 2
- 229940100198 alkylating agent Drugs 0.000 claims description 2
- 239000002168 alkylating agent Substances 0.000 claims description 2
- 210000001185 bone marrow Anatomy 0.000 claims description 2
- 230000002559 cytogenic effect Effects 0.000 claims description 2
- 230000004069 differentiation Effects 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 230000001973 epigenetic effect Effects 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 230000004927 fusion Effects 0.000 claims description 2
- 239000003862 glucocorticoid Substances 0.000 claims description 2
- 210000003714 granulocyte Anatomy 0.000 claims description 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims description 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 2
- 201000005987 myeloid sarcoma Diseases 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
- 239000000651 prodrug Substances 0.000 claims description 2
- 230000029058 respiratory gaseous exchange Effects 0.000 claims description 2
- 238000001694 spray drying Methods 0.000 claims description 2
- 230000009885 systemic effect Effects 0.000 claims description 2
- 229940037128 systemic glucocorticoids Drugs 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims 36
- 208000026661 Acute myeloid leukemia with 11q23 abnormalities Diseases 0.000 claims 1
- CWHGYLGCKHZVHG-UHFFFAOYSA-N CC(=O)NC1=CC=C(C=C1)O.O.O Chemical compound CC(=O)NC1=CC=C(C=C1)O.O.O CWHGYLGCKHZVHG-UHFFFAOYSA-N 0.000 claims 1
- HMKHWYHCDUFAJR-UHFFFAOYSA-N acetamide;dihydrate Chemical compound O.O.CC(N)=O HMKHWYHCDUFAJR-UHFFFAOYSA-N 0.000 claims 1
- 239000003697 methyltransferase inhibitor Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 34
- 125000004432 carbon atom Chemical group C* 0.000 description 12
- 125000000217 alkyl group Chemical group 0.000 description 7
- 125000005843 halogen group Chemical group 0.000 description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 238000000634 powder X-ray diffraction Methods 0.000 description 2
- 125000004076 pyridyl group Chemical group 0.000 description 2
- 208000033826 Promyelocytic Acute Leukemia Diseases 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
- 150000004683 dihydrates Chemical class 0.000 description 1
- 239000003968 dna methyltransferase inhibitor Substances 0.000 description 1
- 230000005861 gene abnormality Effects 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
Applications Claiming Priority (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461987822P | 2014-05-02 | 2014-05-02 | |
| US61/987,822 | 2014-05-02 | ||
| US201461990465P | 2014-05-08 | 2014-05-08 | |
| US61/990,465 | 2014-05-08 | ||
| US201462012128P | 2014-06-13 | 2014-06-13 | |
| US201462012135P | 2014-06-13 | 2014-06-13 | |
| US62/012,128 | 2014-06-13 | ||
| US62/012,135 | 2014-06-13 | ||
| US201462080771P | 2014-11-17 | 2014-11-17 | |
| US201462080804P | 2014-11-17 | 2014-11-17 | |
| US62/080,771 | 2014-11-17 | ||
| US62/080,804 | 2014-11-17 | ||
| US201462086456P | 2014-12-02 | 2014-12-02 | |
| US62/086,456 | 2014-12-02 | ||
| PCT/US2015/028891 WO2015168621A1 (en) | 2014-05-02 | 2015-05-01 | Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017514909A JP2017514909A (ja) | 2017-06-08 |
| JP2017514909A5 true JP2017514909A5 (enExample) | 2018-06-14 |
Family
ID=54359398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017510455A Pending JP2017514909A (ja) | 2014-05-02 | 2015-05-01 | チエノトリアゾロジアゼピン化合物を用いる急性骨髄性白血病及び／又は急性リンパ芽球性白血病の治療方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9956228B2 (enExample) |
| EP (1) | EP3137085A4 (enExample) |
| JP (1) | JP2017514909A (enExample) |
| KR (1) | KR20160145833A (enExample) |
| CN (1) | CN107073014A (enExample) |
| AU (1) | AU2015252844A1 (enExample) |
| CA (1) | CA2947601A1 (enExample) |
| MX (1) | MX2016014301A (enExample) |
| RU (1) | RU2016146099A (enExample) |
| WO (1) | WO2015168621A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA035469B1 (ru) | 2013-03-15 | 2020-06-22 | Инсайт Холдингс Корпорейшн | Трициклические гетероциклы как ингибиторы белков бэт |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| SMT202000133T1 (it) | 2014-04-23 | 2020-05-08 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CN109715625B (zh) | 2016-06-20 | 2022-04-19 | 因赛特公司 | Bet抑制剂的结晶固体形式 |
| CN110573151A (zh) * | 2017-04-26 | 2019-12-13 | 辛辛那提大学 | 用于治疗急性髓性白血病的方法、试剂和组合物 |
| EA202092635A1 (ru) | 2018-06-13 | 2021-03-23 | Дибли Аг | Получение конденсированных производных триазепина и их применение в качестве ингибиторов bet |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| EP4351560A4 (en) | 2021-06-08 | 2025-06-04 | The Regents of the University of California | ANTI-CANCER COMPOUNDS |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4875277B2 (ja) | 2000-06-16 | 2012-02-15 | 田辺三菱製薬株式会社 | 放出ｐＨ域及び／又は速度制御組成物 |
| EP1170008A1 (en) * | 2000-07-07 | 2002-01-09 | Chemotherapeutisches Forschungsinstitut Georg-Speyer-Haus | Valproic acid and derivatives thereof as histone deacetylase inhibitors |
| EP1781255B1 (en) * | 2004-08-10 | 2012-02-15 | Talon Therapeutics, Inc. | Compositions and methods for treating leukemia |
| CA2677651A1 (en) * | 2007-02-15 | 2008-08-21 | Novartis Ag | Combinations of therapeutic agents for treating cancer |
| CN101910182B (zh) * | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| PL2307002T3 (pl) * | 2008-06-09 | 2013-05-31 | Cyclacel Ltd | Kombinacje sapacytabiny lub cndac z inhibitorami metylotransferazy dna, takimi jak decytabina i prokaina |
| ES2606958T3 (es) * | 2010-05-14 | 2017-03-28 | Dana-Farber Cancer Institute, Inc. | Compuestos de tienotriazolodiazepina para tratar una neoplasia |
| CN103154246B (zh) * | 2010-05-14 | 2015-11-25 | 达那-法伯癌症研究所 | 用于治疗白血病的组合物和方法 |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| WO2012112847A1 (en) * | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| 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 |
| WO2014068402A2 (en) | 2012-09-28 | 2014-05-08 | Oncoethix Sa | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
| EP3027194A1 (en) * | 2013-08-01 | 2016-06-08 | Oncoethix GmbH | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
| JP2016538310A (ja) * | 2013-11-27 | 2016-12-08 | オンコエシックス ゲーエムベーハー | 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 |
| 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 |
-
2015
- 2015-05-01 WO PCT/US2015/028891 patent/WO2015168621A1/en not_active Ceased
- 2015-05-01 KR KR1020167033946A patent/KR20160145833A/ko not_active Withdrawn
- 2015-05-01 AU AU2015252844A patent/AU2015252844A1/en not_active Abandoned
- 2015-05-01 JP JP2017510455A patent/JP2017514909A/ja active Pending
- 2015-05-01 MX MX2016014301A patent/MX2016014301A/es unknown
- 2015-05-01 EP EP15785547.9A patent/EP3137085A4/en not_active Withdrawn
- 2015-05-01 CA CA2947601A patent/CA2947601A1/en not_active Abandoned
- 2015-05-01 US US15/308,540 patent/US9956228B2/en not_active Expired - Fee Related
- 2015-05-01 RU RU2016146099A patent/RU2016146099A/ru not_active Application Discontinuation
- 2015-05-01 CN CN201580036473.XA patent/CN107073014A/zh active Pending
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