JP2020530467A5 - - Google Patents
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- JP2020530467A5 JP2020530467A5 JP2020507545A JP2020507545A JP2020530467A5 JP 2020530467 A5 JP2020530467 A5 JP 2020530467A5 JP 2020507545 A JP2020507545 A JP 2020507545A JP 2020507545 A JP2020507545 A JP 2020507545A JP 2020530467 A5 JP2020530467 A5 JP 2020530467A5
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- JP
- Japan
- Prior art keywords
- kinase inhibitor
- medicament according
- kinase
- cdk5
- 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.)
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- 229940043355 kinase inhibitor Drugs 0.000 claims description 83
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims description 83
- 239000003814 drug Substances 0.000 claims description 54
- 108010025454 Cyclin-Dependent Kinase 5 Proteins 0.000 claims description 20
- 102100026805 Cyclin-dependent-like kinase 5 Human genes 0.000 claims description 20
- 102100033245 Cyclin-dependent kinase 16 Human genes 0.000 claims description 16
- 101000944357 Homo sapiens Cyclin-dependent kinase 16 Proteins 0.000 claims description 16
- 101000663635 Homo sapiens Sphingosine kinase 1 Proteins 0.000 claims description 16
- 102100039024 Sphingosine kinase 1 Human genes 0.000 claims description 16
- 101001042360 Homo sapiens LIM domain kinase 2 Proteins 0.000 claims description 15
- 101000628954 Homo sapiens Mitogen-activated protein kinase 12 Proteins 0.000 claims description 15
- 102100021756 LIM domain kinase 2 Human genes 0.000 claims description 15
- 102100026932 Mitogen-activated protein kinase 12 Human genes 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 15
- 201000011510 cancer Diseases 0.000 claims description 15
- -1 CAKM4 Proteins 0.000 claims description 14
- 108091000080 Phosphotransferase Proteins 0.000 claims description 14
- 102000020233 phosphotransferase Human genes 0.000 claims description 14
- 229940124597 therapeutic agent Drugs 0.000 claims description 14
- 102100023332 Dual specificity mitogen-activated protein kinase kinase 7 Human genes 0.000 claims description 12
- 101000624594 Homo sapiens Dual specificity mitogen-activated protein kinase kinase 7 Proteins 0.000 claims description 12
- 101000950687 Homo sapiens Mitogen-activated protein kinase 7 Proteins 0.000 claims description 12
- 101000687955 Homo sapiens Phosphomevalonate kinase Proteins 0.000 claims description 12
- 101000971404 Homo sapiens Protein kinase C iota type Proteins 0.000 claims description 12
- 101000987297 Homo sapiens Serine/threonine-protein kinase PAK 4 Proteins 0.000 claims description 12
- 101000841505 Homo sapiens Uridine-cytidine kinase 2 Proteins 0.000 claims description 12
- 206010027476 Metastases Diseases 0.000 claims description 12
- 102100037805 Mitogen-activated protein kinase 7 Human genes 0.000 claims description 12
- 102100024279 Phosphomevalonate kinase Human genes 0.000 claims description 12
- 102100021557 Protein kinase C iota type Human genes 0.000 claims description 12
- 102100027940 Serine/threonine-protein kinase PAK 4 Human genes 0.000 claims description 12
- 102100029150 Uridine-cytidine kinase 2 Human genes 0.000 claims description 12
- 230000009401 metastasis Effects 0.000 claims description 12
- 229920005735 poly(methyl vinyl ketone) Polymers 0.000 claims description 12
- 102100035952 Atypical kinase COQ8B, mitochondrial Human genes 0.000 claims description 10
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 10
- 102100026865 Cyclin-dependent kinase 5 activator 1 Human genes 0.000 claims description 10
- 102100040856 Dual specificity protein kinase CLK3 Human genes 0.000 claims description 10
- 101000875775 Homo sapiens Atypical kinase COQ8B, mitochondrial Proteins 0.000 claims description 10
- 101000749304 Homo sapiens Dual specificity protein kinase CLK3 Proteins 0.000 claims description 10
- 101001024118 Homo sapiens Nuclear-interacting partner of ALK Proteins 0.000 claims description 10
- 101001026854 Homo sapiens Protein kinase C delta type Proteins 0.000 claims description 10
- 101000794200 Homo sapiens Testis-specific serine/threonine-protein kinase 6 Proteins 0.000 claims description 10
- 101000944219 Homo sapiens cAMP-dependent protein kinase catalytic subunit beta Proteins 0.000 claims description 10
- 101000944207 Homo sapiens cAMP-dependent protein kinase catalytic subunit gamma Proteins 0.000 claims description 10
- 206010059282 Metastases to central nervous system Diseases 0.000 claims description 10
- 102100035376 Nuclear-interacting partner of ALK Human genes 0.000 claims description 10
- 102100037340 Protein kinase C delta type Human genes 0.000 claims description 10
- 102100030141 Testis-specific serine/threonine-protein kinase 6 Human genes 0.000 claims description 10
- 210000004556 brain Anatomy 0.000 claims description 10
- 102100033065 cAMP-dependent protein kinase catalytic subunit beta Human genes 0.000 claims description 10
- 102100033064 cAMP-dependent protein kinase catalytic subunit gamma Human genes 0.000 claims description 10
- 108010064131 neuronal Cdk5 activator (p25-p35) Proteins 0.000 claims description 10
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- 102100026859 FAD-AMP lyase (cyclizing) Human genes 0.000 claims description 9
- 101000892986 Homo sapiens Tyrosine-protein kinase FRK Proteins 0.000 claims description 9
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- HUXYBQXJVXOMKX-UHFFFAOYSA-N N-[6,6-dimethyl-5-[(1-methyl-4-piperidinyl)-oxomethyl]-1,4-dihydropyrrolo[3,4-c]pyrazol-3-yl]-3-methylbutanamide Chemical compound CC(C)CC(=O)NC1=NNC(C2(C)C)=C1CN2C(=O)C1CCN(C)CC1 HUXYBQXJVXOMKX-UHFFFAOYSA-N 0.000 claims description 4
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 4
- QQQCWVDPMPFUGF-ZDUSSCGKSA-N alpinetin Chemical compound C1([C@H]2OC=3C=C(O)C=C(C=3C(=O)C2)OC)=CC=CC=C1 QQQCWVDPMPFUGF-ZDUSSCGKSA-N 0.000 claims description 4
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- DLPIYBKBHMZCJI-WBVHZDCISA-N (2r,3s)-3-[[6-[(4,6-dimethylpyridin-3-yl)methylamino]-9-propan-2-ylpurin-2-yl]amino]pentan-2-ol Chemical compound C=12N=CN(C(C)C)C2=NC(N[C@@H](CC)[C@@H](C)O)=NC=1NCC1=CN=C(C)C=C1C DLPIYBKBHMZCJI-WBVHZDCISA-N 0.000 claims description 3
- 229960000556 fingolimod Drugs 0.000 claims description 3
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims description 3
- 230000008685 targeting Effects 0.000 claims description 3
- AOUZPXZGMZUQQS-YPAWHYETSA-N (2r)-2-[[(2r)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-n-[(2r)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide Chemical compound C([C@@H](NC(=O)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC=1C=CC=CC=1)C(N)=O)C1=CC=C(O)C=C1 AOUZPXZGMZUQQS-YPAWHYETSA-N 0.000 claims description 2
- RNOAOAWBMHREKO-QFIPXVFZSA-N (7S)-2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C(C=C)(=O)N1CCC(CC1)[C@@H]1CCNC=2N1N=C(C=2C(=O)N)C1=CC=C(C=C1)OC1=CC=CC=C1 RNOAOAWBMHREKO-QFIPXVFZSA-N 0.000 claims description 2
- RZXMIHOUHYSGJO-UHFFFAOYSA-N 1-[2-[3-(2-aminopyrimidin-4-yl)-2-(2-methoxyethylamino)benzimidazol-5-yl]ethynyl]cyclohexan-1-ol Chemical compound COCCNC1=NC2=CC=C(C#CC3(O)CCCCC3)C=C2N1C1=CC=NC(N)=N1 RZXMIHOUHYSGJO-UHFFFAOYSA-N 0.000 claims description 2
- ZGFWTMIQAJXQJS-UHFFFAOYSA-N 1-phenanthren-1-yl-1,2,3,4-tetrahydroisoquinoline Chemical class C1(=CC=CC=2C3=CC=CC=C3C=CC1=2)C1NCCC2=CC=CC=C12 ZGFWTMIQAJXQJS-UHFFFAOYSA-N 0.000 claims description 2
- XVBGRTMNFNMINE-UHFFFAOYSA-N 11-cyclopentyl-2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one Chemical compound CCOC1=CC(C(=O)N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=C12)=NC=C1N(C)C(=O)C1=CC=CC=C1N2C1CCCC1 XVBGRTMNFNMINE-UHFFFAOYSA-N 0.000 claims description 2
- DDTPGANIPBKTNU-UHFFFAOYSA-N 2-[2-methoxy-4-(4-methyl-1-piperazinyl)anilino]-5,11-dimethyl-6-pyrimido[4,5-b][1,4]benzodiazepinone Chemical compound C=1C=C(NC=2N=C3N(C)C4=CC=CC=C4C(=O)N(C)C3=CN=2)C(OC)=CC=1N1CCN(C)CC1 DDTPGANIPBKTNU-UHFFFAOYSA-N 0.000 claims description 2
- FBWZAFQEOKNGQL-UHFFFAOYSA-N 2-n-(3-methoxyphenyl)-4-n-(oxolan-2-ylmethyl)quinazoline-2,4-diamine Chemical compound COC1=CC=CC(NC=2N=C3C=CC=CC3=C(NCC3OCCC3)N=2)=C1 FBWZAFQEOKNGQL-UHFFFAOYSA-N 0.000 claims description 2
- ZGXOBLVQIVXKEB-UHFFFAOYSA-N 3-[N-[3-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-N,N-dimethyl-1H-indole-6-carboxamide Chemical compound CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N(C)C)O ZGXOBLVQIVXKEB-UHFFFAOYSA-N 0.000 claims description 2
- XVOKFRPKSAWELK-UHFFFAOYSA-N 3-methyl-n-[3-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl]-1,2-oxazole-5-carboxamide Chemical compound O1N=C(C)C=C1C(=O)NC1=CC=CC(C(=O)NC=2C=C(C=CC=2)C(F)(F)F)=C1 XVOKFRPKSAWELK-UHFFFAOYSA-N 0.000 claims description 2
- TWOSIFOFWWXXIG-PTGBLXJZSA-N 4-[(E)-[2-(2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxybutane-1,2-diol Chemical compound OCC(O)CCO\N=C1\C(=Nc2ccccc12)c1c(O)[nH]c2ccccc12 TWOSIFOFWWXXIG-PTGBLXJZSA-N 0.000 claims description 2
- SEJLPXCPMNSRAM-GOSISDBHSA-N 6-amino-9-[(3r)-1-but-2-ynoylpyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one Chemical compound C1N(C(=O)C#CC)CC[C@H]1N1C(=O)N(C=2C=CC(OC=3C=CC=CC=3)=CC=2)C2=C(N)N=CN=C21 SEJLPXCPMNSRAM-GOSISDBHSA-N 0.000 claims description 2
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound 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 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims description 2
- 101100246550 Caenorhabditis elegans pyr-1 gene Proteins 0.000 claims description 2
- 102100022789 Calcium/calmodulin-dependent protein kinase type IV Human genes 0.000 claims description 2
- 239000005461 Canertinib Substances 0.000 claims description 2
- 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 2
- 150000004922 Dasatinib derivatives Chemical group 0.000 claims description 2
- ORJDDOBAOGKRJV-UHFFFAOYSA-N Dihydrotectochrysin Natural products O1C2=CC(OC)=CC(O)=C2C(=O)CC1C1=CC=CC=C1 ORJDDOBAOGKRJV-UHFFFAOYSA-N 0.000 claims description 2
- 108010057573 Flavoproteins Proteins 0.000 claims description 2
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- 101000974816 Homo sapiens Calcium/calmodulin-dependent protein kinase type IV Proteins 0.000 claims description 2
- JZUTXVTYJDCMDU-MOPGFXCFSA-N Hydrastine Chemical compound CN1CCC2=CC=3OCOC=3C=C2[C@@H]1[C@@H]1C2=CC=C(OC)C(OC)=C2C(=O)O1 JZUTXVTYJDCMDU-MOPGFXCFSA-N 0.000 claims description 2
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 2
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- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims description 2
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims description 2
- 239000002177 L01XE27 - Ibrutinib Substances 0.000 claims description 2
- IVUGBSGLHRJSSP-UHFFFAOYSA-N LimKi 3 Chemical compound S1C(NC(=O)C(C)C)=NC=C1C1=CC(C(F)F)=NN1C1=C(Cl)C=CC=C1Cl IVUGBSGLHRJSSP-UHFFFAOYSA-N 0.000 claims description 2
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- OUSFTKFNBAZUKL-UHFFFAOYSA-N N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCNCC1 OUSFTKFNBAZUKL-UHFFFAOYSA-N 0.000 claims description 2
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- ABSXPNGWJFAPRT-UHFFFAOYSA-N benzenesulfonic acid;n-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide Chemical compound OS(=O)(=O)C1=CC=CC=C1.C1=CC(OCCOC)=CC=C1NC1=NC=C(F)C(NC=2C=C(NC(=O)C=C)C=CC=2)=N1 ABSXPNGWJFAPRT-UHFFFAOYSA-N 0.000 claims description 2
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- OMZCMEYTWSXEPZ-UHFFFAOYSA-N canertinib Chemical compound C1=C(Cl)C(F)=CC=C1NC1=NC=NC2=CC(OCCCN3CCOCC3)=C(NC(=O)C=C)C=C12 OMZCMEYTWSXEPZ-UHFFFAOYSA-N 0.000 claims description 2
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- JZUTXVTYJDCMDU-UHFFFAOYSA-N d-alpha-hydrastine Natural products CN1CCC2=CC=3OCOC=3C=C2C1C1C2=CC=C(OC)C(OC)=C2C(=O)O1 JZUTXVTYJDCMDU-UHFFFAOYSA-N 0.000 claims description 2
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Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022183795A JP7587860B2 (ja) | 2017-08-11 | 2022-11-17 | 癌転移を処置するためにキナーゼを標的とする方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762544597P | 2017-08-11 | 2017-08-11 | |
| US62/544,597 | 2017-08-11 | ||
| PCT/US2018/046329 WO2019033041A1 (en) | 2017-08-11 | 2018-08-10 | TARGETING KINASES FOR THE TREATMENT OF CANCER METASTASES |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022183795A Division JP7587860B2 (ja) | 2017-08-11 | 2022-11-17 | 癌転移を処置するためにキナーゼを標的とする方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020530467A JP2020530467A (ja) | 2020-10-22 |
| JP2020530467A5 true JP2020530467A5 (enExample) | 2021-09-24 |
Family
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| KR102141997B1 (ko) * | 2017-11-22 | 2020-08-06 | (주)인핸스드바이오 | Pmvk를 유효성분으로 포함하는 방사선 저항성 암 진단용 또는 방사선 치료 예후 예측용 바이오마커 조성물 |
| EP3781168A4 (en) * | 2018-04-16 | 2022-10-05 | The Regents of the University of California | PAK4 INHIBITORS AND METHODS OF USE |
| US20220178924A1 (en) * | 2019-03-03 | 2022-06-09 | Purdue Research Foundation | Systems and methods for identifying subtype, prognosis, and monitoring of breast cancer |
| KR20220002930A (ko) * | 2019-03-28 | 2022-01-07 | 캔써 리서치 테크놀로지 리미티드 | 비정형 단백질 키나제 c의 억제제 및 헷지호그 경로 의존성 암의 치료에서 이의 용도 |
| TWI719446B (zh) * | 2019-04-16 | 2021-02-21 | 中國醫藥大學 | 醫藥組合物及其用於製備抑制胃癌細胞增生藥物的用途 |
| CN113143525A (zh) * | 2021-05-10 | 2021-07-23 | 广东省人民医院 | 一种新型脑转移瘤动物模型的构建方法 |
| CN114410778B (zh) * | 2021-12-29 | 2024-03-19 | 中南大学湘雅医院 | Pf543在制备pd-l1/pd-1单抗肿瘤免疫治疗药物中的应用 |
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| US20100029748A1 (en) | 2008-08-04 | 2010-02-04 | Sloan-Kettering Institute For Cancer Research | Metastasis Promoting Genes and Proteins |
| MX365219B (es) | 2011-07-27 | 2019-05-27 | The Broad Inst Inc Star | Uso de una composición en un método para inhibir el crecimiento del carcinoma de células escamosas de cabeza y cuello (hnscc). |
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| AU2015317330B2 (en) * | 2014-09-19 | 2021-01-14 | Memorial Sloan-Kettering Cancer Center | Methods for treating brain metastasis |
| UY36660A (es) * | 2015-04-30 | 2016-11-30 | Bayer Pharma AG | Combinaciones de inhibidores de irak4 |
| JP2018135268A (ja) | 2015-06-05 | 2018-08-30 | 大日本住友製薬株式会社 | 新規ヘテロアリールアミノ−３−ピラゾール誘導体およびその薬理学上許容される塩 |
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