JP2019510746A5 - - Google Patents
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- JP2019510746A5 JP2019510746A5 JP2018544835A JP2018544835A JP2019510746A5 JP 2019510746 A5 JP2019510746 A5 JP 2019510746A5 JP 2018544835 A JP2018544835 A JP 2018544835A JP 2018544835 A JP2018544835 A JP 2018544835A JP 2019510746 A5 JP2019510746 A5 JP 2019510746A5
- Authority
- JP
- Japan
- Prior art keywords
- idh1
- flt3
- inhibitor
- composition
- cancer
- 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
Links
- 206010028980 Neoplasm Diseases 0.000 claims description 69
- 239000003112 inhibitor Substances 0.000 claims description 63
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims description 61
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims description 61
- 238000000034 method Methods 0.000 claims description 54
- 201000011510 cancer Diseases 0.000 claims description 39
- 108700028369 Alleles Proteins 0.000 claims description 34
- 229940125782 compound 2 Drugs 0.000 claims description 33
- 230000035772 mutation Effects 0.000 claims description 28
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 26
- 206010066476 Haematological malignancy Diseases 0.000 claims description 24
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 19
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 18
- 102000012011 Isocitrate Dehydrogenase Human genes 0.000 claims description 16
- 108010075869 Isocitrate Dehydrogenase Proteins 0.000 claims description 16
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 16
- 239000002207 metabolite Substances 0.000 claims description 16
- 229940002612 prodrug Drugs 0.000 claims description 16
- 239000000651 prodrug Substances 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 16
- 239000012453 solvate Substances 0.000 claims description 16
- 229960001796 sunitinib Drugs 0.000 claims description 16
- 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 16
- 201000007450 intrahepatic cholangiocarcinoma Diseases 0.000 claims description 12
- 230000036210 malignancy Effects 0.000 claims description 12
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 12
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 12
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 11
- 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 10
- WIJZXSAJMHAVGX-DHLKQENFSA-N ivosidenib Chemical compound FC1=CN=CC(N([C@H](C(=O)NC2CC(F)(F)C2)C=2C(=CC=CC=2)Cl)C(=O)[C@H]2N(C(=O)CC2)C=2N=CC=C(C=2)C#N)=C1 WIJZXSAJMHAVGX-DHLKQENFSA-N 0.000 claims description 9
- 238000011282 treatment Methods 0.000 claims description 9
- 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 8
- 208000025324 B-cell acute lymphoblastic leukemia Diseases 0.000 claims description 8
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 8
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 8
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims description 8
- 229940125199 famitinib Drugs 0.000 claims description 8
- 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 8
- 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 8
- 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 8
- 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 8
- 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 8
- 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 7
- 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 7
- 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 7
- 229950001845 lestaurtinib Drugs 0.000 claims description 7
- 208000005243 Chondrosarcoma Diseases 0.000 claims description 6
- 208000032612 Glial tumor Diseases 0.000 claims description 6
- 206010018338 Glioma Diseases 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 201000001441 melanoma Diseases 0.000 claims description 6
- 230000000306 recurrent effect Effects 0.000 claims description 6
- 239000012472 biological sample Substances 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 230000003211 malignant effect Effects 0.000 claims description 5
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims description 4
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 4
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 4
- 210000001072 colon Anatomy 0.000 claims description 4
- 102200069690 rs121913500 Human genes 0.000 claims description 4
- 238000012216 screening Methods 0.000 claims description 4
- 239000000523 sample Substances 0.000 claims description 3
- 238000002648 combination therapy Methods 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 38
- MWUFVYLAWAXDHQ-HMNLTAHHSA-N (2e,5s,6s,8z,10r,11s)-17-(ethylamino)-5,6,15-trihydroxy-10,11-dimethyl-12-oxabicyclo[12.4.0]octadeca-1(18),2,8,14,16-pentaene-7,13-dione Chemical compound O([C@@H](C)[C@H](C)\C=C/C(=O)[C@@H](O)[C@@H](O)C/C=C/1)C(=O)C=2C\1=CC(NCC)=CC=2O MWUFVYLAWAXDHQ-HMNLTAHHSA-N 0.000 claims 2
- JLRIJKVMMZEKDF-UHFFFAOYSA-N 3-n-(1h-indol-5-yl)-5-pyridin-4-ylpyrazine-2,3-diamine Chemical compound N1=C(NC=2C=C3C=CNC3=CC=2)C(N)=NC=C1C1=CC=NC=C1 JLRIJKVMMZEKDF-UHFFFAOYSA-N 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 239000002137 L01XE24 - Ponatinib Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 238000011284 combination treatment Methods 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 229960001131 ponatinib Drugs 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 description 21
- 230000006872 improvement Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- -1 1- (2-chlorophenyl) -2-((3,3-difluorocyclobutyl) amino) -2-oxoethyl Chemical group 0.000 description 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021044546A 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 |
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/US2016/064845 WO2017146795A1 (en) | 2016-02-26 | 2016-12-02 | Idh1 inhibitors for the treatment of haematological malignancies and solid tumours |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021044546A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019510746A JP2019510746A (ja) | 2019-04-18 |
| JP2019510746A5 true JP2019510746A5 (enExample) | 2020-01-16 |
| JP6856657B2 JP6856657B2 (ja) | 2021-04-07 |
Family
ID=57610404
Family Applications (3)
| 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 |
| 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 |
| 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 |
|---|---|---|---|
| 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 |
| 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) | US10137130B2 (enExample) |
| EP (2) | EP3419593B1 (enExample) |
| JP (3) | JP6856657B2 (enExample) |
| KR (2) | KR20180113540A (enExample) |
| CN (1) | CN109069410B (enExample) |
| AU (2) | AU2016393869B2 (enExample) |
| CA (2) | CA3015757A1 (enExample) |
| ES (1) | ES2912909T3 (enExample) |
| IL (2) | IL261333B (enExample) |
| MA (1) | MA43640A (enExample) |
| MX (3) | MX390396B (enExample) |
| WO (2) | WO2017146795A1 (enExample) |
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2016
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2018
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2020
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2021
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