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 |
| US20210161943A1 (en) * | 2018-04-16 | 2021-06-03 | 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 |
| JP7603605B2 (ja) * | 2019-03-28 | 2024-12-20 | キャンサー・リサーチ・テクノロジー・リミテッド | 非定型プロテインキナーゼｃの阻害剤およびヘッジホッグ経路依存性癌の治療におけるその使用 |
| 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 |
| KR102658209B1 (ko) * | 2021-10-05 | 2024-04-18 | 재단법인 아산사회복지재단 | Cdk 억제제 및 id2 활성화제를 포함하는 방광암의 예방 또는 치료용 약학 조성물 |
| 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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| US20060183893A1 (en) * | 2005-01-25 | 2006-08-17 | North Don A | Nucleic acids for apoptosis of cancer cells |
| WO2007044571A2 (en) | 2005-10-06 | 2007-04-19 | President And Fellows Of Harvard College | Methods for identifying proteins essential for human cell proliferation and therapeutic agents that target them |
| EP1961825A1 (en) | 2007-02-26 | 2008-08-27 | INSERM (Institut National de la Santé et de la Recherche Medicale) | Method for predicting the occurrence of metastasis in breast cancer patients |
| GB0706633D0 (en) * | 2007-04-04 | 2007-05-16 | Cyclacel Ltd | Combination |
| US20100029748A1 (en) | 2008-08-04 | 2010-02-04 | Sloan-Kettering Institute For Cancer Research | Metastasis Promoting Genes and Proteins |
| WO2013016434A1 (en) | 2011-07-27 | 2013-01-31 | The Board Institute, Inc. | Compositions and methods of treating head and neck cancer |
| EP2829880A1 (en) * | 2013-07-26 | 2015-01-28 | Energeia Biosciences | Method for identifying modulators of BCRP/ABCG2-mediated ATP release and use of said modulators for treating diseases |
| ES2873959T3 (es) * | 2014-05-28 | 2021-11-04 | Piramal Entpr Ltd | Combinación farmacéutica que comprende un inhibidor de CDK y un inhibidor de tiorredoxina reductasa para el tratamiento del cáncer |
| US20160008366A1 (en) | 2014-07-14 | 2016-01-14 | Pharmacyclics Llc | Btk inhibitors for the treatment of cns malignancies |
| GB201414542D0 (en) * | 2014-08-15 | 2014-10-01 | Imp Innovations Ltd | Novel therapy |
| CA2961894C (en) * | 2014-09-19 | 2023-12-12 | Memorial Sloan-Kettering Cancer Center | Methods for treating brain metastatis using gap junction inhibitors |
| TW201701879A (zh) * | 2015-04-30 | 2017-01-16 | 拜耳製藥公司 | Ｉｒａｋ４抑制劑組合 |
| 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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2018
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- 2018-08-10 WO PCT/US2018/046329 patent/WO2019033041A1/en not_active Ceased
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2022
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