JP2019513694A5 - - Google Patents
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- JP2019513694A5 JP2019513694A5 JP2018544781A JP2018544781A JP2019513694A5 JP 2019513694 A5 JP2019513694 A5 JP 2019513694A5 JP 2018544781 A JP2018544781 A JP 2018544781A JP 2018544781 A JP2018544781 A JP 2018544781A JP 2019513694 A5 JP2019513694 A5 JP 2019513694A5
- Authority
- JP
- Japan
- Prior art keywords
- idh2
- flt3
- mutant allele
- pharmaceutical composition
- subject
- 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.)
- Granted
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- 108700028369 Alleles Proteins 0.000 claims description 51
- 206010028980 Neoplasm Diseases 0.000 claims description 45
- 238000000034 method Methods 0.000 claims description 44
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims description 40
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims description 40
- 239000003112 inhibitor Substances 0.000 claims description 33
- 201000011510 cancer Diseases 0.000 claims description 31
- 229940125904 compound 1 Drugs 0.000 claims description 21
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 18
- 150000001875 compounds Chemical class 0.000 claims description 18
- 206010066476 Haematological malignancy Diseases 0.000 claims description 16
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 11
- 239000002207 metabolite Substances 0.000 claims description 10
- 239000000651 prodrug Substances 0.000 claims description 10
- 229940002612 prodrug Drugs 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 239000012453 solvate Substances 0.000 claims description 10
- 238000006467 substitution reaction Methods 0.000 claims description 10
- 206010002449 angioimmunoblastic T-cell lymphoma Diseases 0.000 claims description 9
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 8
- UIARLYUEJFELEN-LROUJFHJSA-N LSM-1231 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3C(=O)NCC3=C2C2=CC=CC=C2N1[C@]1(C)[C@](CO)(O)C[C@H]4O1 UIARLYUEJFELEN-LROUJFHJSA-N 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 229960001796 sunitinib Drugs 0.000 claims description 8
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims description 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 8
- 102000012011 Isocitrate Dehydrogenase Human genes 0.000 claims description 7
- 108010075869 Isocitrate Dehydrogenase Proteins 0.000 claims description 7
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 7
- 230000036210 malignancy Effects 0.000 claims description 7
- 239000012472 biological sample Substances 0.000 claims description 6
- DYLUUSLLRIQKOE-UHFFFAOYSA-N enasidenib Chemical compound N=1C(C=2N=C(C=CC=2)C(F)(F)F)=NC(NCC(C)(O)C)=NC=1NC1=CC=NC(C(F)(F)F)=C1 DYLUUSLLRIQKOE-UHFFFAOYSA-N 0.000 claims description 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 4
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 4
- GKEYKDOLBLYGRB-LGMDPLHJSA-N 5-[2-(diethylamino)ethyl]-2-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1h-pyrrolo[3,2-c]pyridin-4-one Chemical compound O=C\1NC2=CC=C(F)C=C2C/1=C/C(N1)=C(C)C2=C1CCN(CCN(CC)CC)C2=O GKEYKDOLBLYGRB-LGMDPLHJSA-N 0.000 claims description 4
- WVXNSAVVKYZVOE-UHFFFAOYSA-N DCC-2036 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C4C=CC=NC4=CC=3)=CC=2)=C1 WVXNSAVVKYZVOE-UHFFFAOYSA-N 0.000 claims description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 4
- YYLKKYCXAOBSRM-JXMROGBWSA-N [4-[(e)-2-(1h-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone Chemical compound C=1C=C(\C=C\C=2C3=CC=CC=C3NN=2)C=CC=1C(=O)N1CCNCC1 YYLKKYCXAOBSRM-JXMROGBWSA-N 0.000 claims description 4
- 229940125199 famitinib Drugs 0.000 claims description 4
- GYQYAJJFPNQOOW-UHFFFAOYSA-N gilteritinib Chemical compound N1=C(NC2CCOCC2)C(CC)=NC(C(N)=O)=C1NC(C=C1OC)=CC=C1N(CC1)CCC1N1CCN(C)CC1 GYQYAJJFPNQOOW-UHFFFAOYSA-N 0.000 claims description 4
- 229950001845 lestaurtinib Drugs 0.000 claims description 4
- BMGQWWVMWDBQGC-IIFHNQTCSA-N midostaurin Chemical compound CN([C@H]1[C@H]([C@]2(C)O[C@@H](N3C4=CC=CC=C4C4=C5C(=O)NCC5=C5C6=CC=CC=C6N2C5=C43)C1)OC)C(=O)C1=CC=CC=C1 BMGQWWVMWDBQGC-IIFHNQTCSA-N 0.000 claims description 4
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims description 4
- JGWRKYUXBBNENE-UHFFFAOYSA-N pexidartinib Chemical compound C1=NC(C(F)(F)F)=CC=C1CNC(N=C1)=CC=C1CC1=CNC2=NC=C(Cl)C=C12 JGWRKYUXBBNENE-UHFFFAOYSA-N 0.000 claims description 4
- PHXJVRSECIGDHY-UHFFFAOYSA-N ponatinib Chemical compound C1CN(C)CCN1CC(C(=C1)C(F)(F)F)=CC=C1NC(=O)C1=CC=C(C)C(C#CC=2N3N=CC=CC3=NC=2)=C1 PHXJVRSECIGDHY-UHFFFAOYSA-N 0.000 claims description 4
- CVWXJKQAOSCOAB-UHFFFAOYSA-N quizartinib Chemical group O1C(C(C)(C)C)=CC(NC(=O)NC=2C=CC(=CC=2)C=2N=C3N(C4=CC=C(OCCN5CCOCC5)C=C4S3)C=2)=N1 CVWXJKQAOSCOAB-UHFFFAOYSA-N 0.000 claims description 4
- 238000012216 screening Methods 0.000 claims description 4
- IVDHYUQIDRJSTI-UHFFFAOYSA-N sorafenib tosylate Chemical compound [H+].CC1=CC=C(S([O-])(=O)=O)C=C1.C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 IVDHYUQIDRJSTI-UHFFFAOYSA-N 0.000 claims description 4
- 208000005243 Chondrosarcoma Diseases 0.000 claims description 3
- 208000032612 Glial tumor Diseases 0.000 claims description 3
- 206010018338 Glioma Diseases 0.000 claims description 3
- 206010039491 Sarcoma Diseases 0.000 claims description 3
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 3
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 3
- 102200116484 rs121913502 Human genes 0.000 claims description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 3
- 208000003950 B-cell lymphoma Diseases 0.000 claims description 2
- 206010008583 Chloroma Diseases 0.000 claims description 2
- 208000017815 Dendritic cell tumor Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 2
- 238000002648 combination therapy Methods 0.000 claims description 2
- 201000005987 myeloid sarcoma Diseases 0.000 claims description 2
- 210000005134 plasmacytoid dendritic cell Anatomy 0.000 claims description 2
- 230000000306 recurrent effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 238000010276 construction Methods 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 230000037361 pathway Effects 0.000 description 2
- 208000025324 B-cell acute lymphoblastic leukemia Diseases 0.000 description 1
- 0 CC(C)(CNc1nc(Nc2ccnc(*)c2)nc(-c2nc(C(F)(F)F)ccc2)n1)O Chemical compound CC(C)(CNc1nc(Nc2ccnc(*)c2)nc(-c2nc(C(F)(F)F)ccc2)n1)O 0.000 description 1
- RRHGJUQNOFWUDK-UHFFFAOYSA-N Isoprene Chemical compound CC(=C)C=C RRHGJUQNOFWUDK-UHFFFAOYSA-N 0.000 description 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 description 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 description 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 201000011649 lymphoblastic lymphoma Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662300673P | 2016-02-26 | 2016-02-26 | |
| US62/300,673 | 2016-02-26 | ||
| PCT/US2016/064615 WO2017146794A1 (en) | 2016-02-26 | 2016-12-02 | Idh2 inhibitors for the treatment of haematological maligancies and solid tumours |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019513694A JP2019513694A (ja) | 2019-05-30 |
| JP2019513694A5 true JP2019513694A5 (enExample) | 2020-01-23 |
| JP6930991B2 JP6930991B2 (ja) | 2021-09-01 |
Family
ID=57610404
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018544781A Expired - Fee Related JP6930991B2 (ja) | 2016-02-26 | 2016-12-02 | 血液学的悪性腫瘍及び固形腫瘍の治療のためのｉｄｈ２阻害剤 |
| JP2018544835A Expired - Fee Related JP6856657B2 (ja) | 2016-02-26 | 2016-12-02 | 血液学的悪性疾患および固形腫瘍の処置のためのｉｄｈ１阻害剤 |
| JP2021044546A Withdrawn JP2021102630A (ja) | 2016-02-26 | 2021-03-18 | 血液学的悪性疾患および固形腫瘍の処置のためのｉｄｈ１阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018544835A Expired - Fee Related JP6856657B2 (ja) | 2016-02-26 | 2016-12-02 | 血液学的悪性疾患および固形腫瘍の処置のためのｉｄｈ１阻害剤 |
| JP2021044546A Withdrawn JP2021102630A (ja) | 2016-02-26 | 2021-03-18 | 血液学的悪性疾患および固形腫瘍の処置のためのｉｄｈ１阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20190046512A1 (enExample) |
| EP (2) | EP3419593B1 (enExample) |
| JP (3) | JP6930991B2 (enExample) |
| KR (2) | KR20180113540A (enExample) |
| CN (1) | CN109069410B (enExample) |
| AU (2) | AU2016393869B2 (enExample) |
| CA (2) | CA3015757A1 (enExample) |
| ES (1) | ES2912909T3 (enExample) |
| IL (2) | IL261353A (enExample) |
| MA (1) | MA43640A (enExample) |
| MX (3) | MX390396B (enExample) |
| WO (2) | WO2017146795A1 (enExample) |
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| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| US20150031627A1 (en) | 2013-07-25 | 2015-01-29 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
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| HUE062424T2 (hu) | 2014-09-19 | 2023-11-28 | Forma Therapeutics Inc | Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok |
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2016
- 2016-12-02 EP EP16816810.2A patent/EP3419593B1/en active Active
- 2016-12-02 AU AU2016393869A patent/AU2016393869B2/en not_active Ceased
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- 2016-12-02 CN CN201680082688.XA patent/CN109069410B/zh not_active Expired - Fee Related
- 2016-12-02 KR KR1020187024384A patent/KR20180113540A/ko not_active Ceased
- 2016-12-02 CA CA3015757A patent/CA3015757A1/en active Pending
- 2016-12-02 WO PCT/US2016/064845 patent/WO2017146795A1/en not_active Ceased
- 2016-12-02 JP JP2018544781A patent/JP6930991B2/ja not_active Expired - Fee Related
- 2016-12-02 MA MA043640A patent/MA43640A/fr unknown
- 2016-12-02 CA CA3015753A patent/CA3015753A1/en not_active Abandoned
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- 2016-12-02 EP EP16819389.4A patent/EP3419594B1/en active Active
- 2016-12-02 US US16/079,802 patent/US20190046512A1/en not_active Abandoned
- 2016-12-02 KR KR1020187027740A patent/KR20180114202A/ko not_active Ceased
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2018
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2020
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2021
- 2021-03-18 JP JP2021044546A patent/JP2021102630A/ja not_active Withdrawn
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