JP2017521474A5 - - Google Patents
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- Publication number
- JP2017521474A5 JP2017521474A5 JP2017505465A JP2017505465A JP2017521474A5 JP 2017521474 A5 JP2017521474 A5 JP 2017521474A5 JP 2017505465 A JP2017505465 A JP 2017505465A JP 2017505465 A JP2017505465 A JP 2017505465A JP 2017521474 A5 JP2017521474 A5 JP 2017521474A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- combination
- alkyl
- treatment
- tyrosine kinase
- 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 27
- 201000011510 cancer Diseases 0.000 claims description 23
- 238000000034 method Methods 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 13
- QMEZUZOCLYUADC-UHFFFAOYSA-N hydrate;dihydrochloride Chemical class O.Cl.Cl QMEZUZOCLYUADC-UHFFFAOYSA-N 0.000 claims description 11
- LIOLIMKSCNQPLV-UHFFFAOYSA-N 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1C1=NN2C(CC=3C=C4C=CC=NC4=CC=3)=CN=C2N=C1 LIOLIMKSCNQPLV-UHFFFAOYSA-N 0.000 claims description 9
- 229940121647 egfr inhibitor Drugs 0.000 claims description 8
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 8
- -1 1- (4- (dimethylamino) but-2-enoyl) azepan-3-yl Chemical group 0.000 claims description 6
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 6
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 6
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 206010052358 Colorectal cancer metastatic Diseases 0.000 claims description 4
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 4
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 4
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 4
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 4
- 206010039491 Sarcoma Diseases 0.000 claims description 4
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 229960001433 erlotinib Drugs 0.000 claims description 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 4
- 229960002584 gefitinib Drugs 0.000 claims description 4
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 4
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims description 4
- 230000001394 metastastic effect Effects 0.000 claims description 4
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- 229940122661 MET tyrosine kinase inhibitor Drugs 0.000 claims description 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- IOMMMLWIABWRKL-WUTDNEBXSA-N nazartinib Chemical compound C1N(C(=O)/C=C/CN(C)C)CCCC[C@H]1N1C2=C(Cl)C=CC=C2N=C1NC(=O)C1=CC=NC(C)=C1 IOMMMLWIABWRKL-WUTDNEBXSA-N 0.000 claims description 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 206010003571 Astrocytoma Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims description 2
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 2
- 208000018142 Leiomyosarcoma Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 2
- 208000000389 T-cell leukemia Diseases 0.000 claims description 2
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims description 2
- 208000008383 Wilms tumor Diseases 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- 229960001686 afatinib Drugs 0.000 claims description 2
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims description 2
- 230000003321 amplification Effects 0.000 claims description 2
- 210000000481 breast Anatomy 0.000 claims description 2
- 210000003679 cervix uteri Anatomy 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 210000003238 esophagus Anatomy 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 210000003128 head Anatomy 0.000 claims description 2
- 230000009033 hematopoietic malignancy Effects 0.000 claims description 2
- 210000003734 kidney Anatomy 0.000 claims description 2
- 210000004185 liver Anatomy 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 210000001989 nasopharynx Anatomy 0.000 claims description 2
- 210000003739 neck Anatomy 0.000 claims description 2
- 201000008026 nephroblastoma Diseases 0.000 claims description 2
- 238000003199 nucleic acid amplification method Methods 0.000 claims description 2
- 201000008968 osteosarcoma Diseases 0.000 claims description 2
- 210000001672 ovary Anatomy 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 210000002784 stomach Anatomy 0.000 claims description 2
- 206010042863 synovial sarcoma Diseases 0.000 claims description 2
- 210000001685 thyroid gland Anatomy 0.000 claims description 2
- 210000003932 urinary bladder Anatomy 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 description 46
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 24
- 125000005842 heteroatom Chemical group 0.000 description 24
- 229910052739 hydrogen Inorganic materials 0.000 description 22
- 239000001257 hydrogen Substances 0.000 description 22
- 229910052760 oxygen Inorganic materials 0.000 description 20
- 229910052717 sulfur Inorganic materials 0.000 description 20
- 125000005843 halogen group Chemical group 0.000 description 14
- 150000002431 hydrogen Chemical class 0.000 description 14
- 125000004043 oxo group Chemical group O=* 0.000 description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 8
- 125000003545 alkoxy group Chemical group 0.000 description 8
- 125000004093 cyano group Chemical group *C#N 0.000 description 8
- 125000000623 heterocyclic group Chemical group 0.000 description 8
- 125000002950 monocyclic group Chemical group 0.000 description 8
- 229910052698 phosphorus Inorganic materials 0.000 description 8
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 description 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 description 4
- 125000001188 haloalkyl group Chemical group 0.000 description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 description 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 229940126062 Compound A Drugs 0.000 description 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 2
- 125000004429 atom Chemical group 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 125000000753 cycloalkyl group Chemical group 0.000 description 2
- 125000004438 haloalkoxy group Chemical group 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- 238000009097 single-agent therapy Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462031583P | 2014-07-31 | 2014-07-31 | |
| US62/031,583 | 2014-07-31 | ||
| PCT/IB2015/055737 WO2016016822A1 (en) | 2014-07-31 | 2015-07-29 | Combination therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017521474A JP2017521474A (ja) | 2017-08-03 |
| JP2017521474A5 true JP2017521474A5 (cg-RX-API-DMAC7.html) | 2018-06-14 |
| JP6526789B2 JP6526789B2 (ja) | 2019-06-05 |
Family
ID=53783790
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017505465A Expired - Fee Related JP6526789B2 (ja) | 2014-07-31 | 2015-07-29 | 組み合わせ療法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10195208B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3174869B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6526789B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR20170036037A (cg-RX-API-DMAC7.html) |
| CN (1) | CN107207510B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2015294889B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BR112017001695A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2954862A1 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2831416T3 (cg-RX-API-DMAC7.html) |
| MX (1) | MX373272B (cg-RX-API-DMAC7.html) |
| RU (1) | RU2695230C2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2016016822A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015512425A (ja) | 2012-04-03 | 2015-04-27 | ノバルティス アーゲー | チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用 |
| UY38349A (es) | 2018-08-30 | 2020-03-31 | Array Biopharma Inc | Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met |
| SG11202106897XA (en) | 2019-01-03 | 2021-07-29 | Array Biopharma Inc | Quinoline compounds as inhibitors of tam and met kinases |
| IL296060A (en) * | 2020-03-03 | 2022-10-01 | Array Biopharma Inc | Use of (r)-n-(3-fluoro-4-((3-((1-hydroxypropan-2-yl)amino)-1h-pyrazolo[3,4-b]pyridin-4-yl)oxy) phenyl)-3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide for cancer treatment |
| KR102522963B1 (ko) * | 2020-11-12 | 2023-04-19 | 중앙대학교 산학협력단 | 캡마티닙을 포함하는 항비만 조성물 |
| JP2024540399A (ja) * | 2021-11-05 | 2024-10-31 | ハイファ バイオファーマ カンパニー リミテッド | Ｍｅｔ受容体チロシンキナーゼ阻害剤を含む薬物の組み合わせ及びその使用 |
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| US20080032960A1 (en) * | 2006-04-04 | 2008-02-07 | Regents Of The University Of California | PI3 kinase antagonists |
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| JP2015512425A (ja) * | 2012-04-03 | 2015-04-27 | ノバルティス アーゲー | チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用 |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| KR101418970B1 (ko) * | 2013-03-20 | 2014-07-11 | (주)제욱 | 야생형 EGFR를 가진 비소세포폐암에서 EGFR 억제제와 c-MET 억제제 병용투여에 대한 반응 예측 인자 |
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-
2015
- 2015-07-29 WO PCT/IB2015/055737 patent/WO2016016822A1/en not_active Ceased
- 2015-07-29 BR BR112017001695A patent/BR112017001695A2/pt not_active Application Discontinuation
- 2015-07-29 ES ES15747562T patent/ES2831416T3/es active Active
- 2015-07-29 US US15/328,710 patent/US10195208B2/en not_active Expired - Fee Related
- 2015-07-29 JP JP2017505465A patent/JP6526789B2/ja not_active Expired - Fee Related
- 2015-07-29 CA CA2954862A patent/CA2954862A1/en not_active Abandoned
- 2015-07-29 RU RU2017105827A patent/RU2695230C2/ru active
- 2015-07-29 KR KR1020177005144A patent/KR20170036037A/ko not_active Ceased
- 2015-07-29 MX MX2017001461A patent/MX373272B/es active IP Right Grant
- 2015-07-29 CN CN201580053665.1A patent/CN107207510B/zh not_active Expired - Fee Related
- 2015-07-29 EP EP15747562.5A patent/EP3174869B1/en active Active
- 2015-07-29 AU AU2015294889A patent/AU2015294889B2/en not_active Ceased
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