JP2020514409A5 - - Google Patents
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- JP2020514409A5 JP2020514409A5 JP2019560071A JP2019560071A JP2020514409A5 JP 2020514409 A5 JP2020514409 A5 JP 2020514409A5 JP 2019560071 A JP2019560071 A JP 2019560071A JP 2019560071 A JP2019560071 A JP 2019560071A JP 2020514409 A5 JP2020514409 A5 JP 2020514409A5
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- 206010028980 Neoplasm Diseases 0.000 claims description 105
- 201000011510 cancer Diseases 0.000 claims description 75
- 150000003839 salts Chemical class 0.000 claims description 65
- 150000001875 compounds Chemical class 0.000 claims description 57
- 239000002246 antineoplastic agent Substances 0.000 claims description 44
- -1 Ikochinibu Chemical compound 0.000 claims description 29
- 229940121647 egfr inhibitor Drugs 0.000 claims description 26
- 210000004027 cell Anatomy 0.000 claims description 25
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims description 24
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 24
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims description 24
- 239000003112 inhibitor Substances 0.000 claims description 24
- 150000003384 small molecules Chemical group 0.000 claims description 24
- 201000002510 thyroid cancer Diseases 0.000 claims description 24
- 206010006187 Breast cancer Diseases 0.000 claims description 23
- 208000026310 Breast neoplasm Diseases 0.000 claims description 23
- 201000009030 Carcinoma Diseases 0.000 claims description 22
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 22
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 22
- 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 22
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 17
- 206010009944 Colon cancer Diseases 0.000 claims description 16
- 206010014733 Endometrial cancer Diseases 0.000 claims description 16
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 16
- 201000003803 Inflammatory myofibroblastic tumor Diseases 0.000 claims description 16
- 206010067917 Inflammatory myofibroblastic tumour Diseases 0.000 claims description 16
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 16
- 206010060862 Prostate cancer Diseases 0.000 claims description 16
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 16
- 208000029742 colonic neoplasm Diseases 0.000 claims description 16
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- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 16
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- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 15
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 15
- 229960005395 cetuximab Drugs 0.000 claims description 15
- 229960002584 gefitinib Drugs 0.000 claims description 15
- 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 15
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims description 15
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- 206010038038 rectal cancer Diseases 0.000 claims description 10
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- 229960001972 panitumumab Drugs 0.000 claims description 9
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 9
- NERXPXBELDBEPZ-RMKNXTFCSA-N (e)-n-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC(F)=C1 NERXPXBELDBEPZ-RMKNXTFCSA-N 0.000 claims description 8
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 8
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- 206010010356 Congenital anomaly Diseases 0.000 claims description 8
- 206010065859 Congenital fibrosarcoma Diseases 0.000 claims description 8
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims description 8
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- 208000017604 Hodgkin disease Diseases 0.000 claims description 8
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 8
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 8
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 8
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 8
- 206010023825 Laryngeal cancer Diseases 0.000 claims description 8
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 8
- 208000003445 Mouth Neoplasms Diseases 0.000 claims description 8
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 8
- 241000232901 Nephroma Species 0.000 claims description 8
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- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 8
- 206010033128 Ovarian cancer Diseases 0.000 claims description 8
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 8
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 8
- 206010038389 Renal cancer Diseases 0.000 claims description 8
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 8
- 206010039491 Sarcoma Diseases 0.000 claims description 8
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 8
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 8
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 8
- 206010057644 Testis cancer Diseases 0.000 claims description 8
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 8
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 8
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 8
- 210000000013 bile duct Anatomy 0.000 claims description 8
- 201000007983 brain glioma Diseases 0.000 claims description 8
- 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 8
- 201000010881 cervical cancer Diseases 0.000 claims description 8
- 201000010180 childhood kidney cell carcinoma Diseases 0.000 claims description 8
- 201000010897 colon adenocarcinoma Diseases 0.000 claims description 8
- 230000003511 endothelial effect Effects 0.000 claims description 8
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- 206010017758 gastric cancer Diseases 0.000 claims description 8
- 210000003228 intrahepatic bile duct Anatomy 0.000 claims description 8
- 201000010982 kidney cancer Diseases 0.000 claims description 8
- 229960004891 lapatinib Drugs 0.000 claims description 8
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 8
- 206010023841 laryngeal neoplasm Diseases 0.000 claims description 8
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims description 8
- 201000007270 liver cancer Diseases 0.000 claims description 8
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- 210000004072 lung Anatomy 0.000 claims description 8
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- 208000029559 malignant endocrine neoplasm Diseases 0.000 claims description 8
- 201000001441 melanoma Diseases 0.000 claims description 8
- 208000025351 nephroma Diseases 0.000 claims description 8
- 229950008835 neratinib Drugs 0.000 claims description 8
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims description 8
- 201000010302 ovarian serous cystadenocarcinoma Diseases 0.000 claims description 8
- 230000003248 secreting effect Effects 0.000 claims description 8
- 201000000849 skin cancer Diseases 0.000 claims description 8
- 210000004500 stellate cell Anatomy 0.000 claims description 8
- 201000011549 stomach cancer Diseases 0.000 claims description 8
- 201000003120 testicular cancer Diseases 0.000 claims description 8
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 8
- 206010046766 uterine cancer Diseases 0.000 claims description 8
- 230000002792 vascular Effects 0.000 claims description 8
- 201000000787 conjunctival cancer Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 230000001093 anti-cancer Effects 0.000 claims 3
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 35
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 35
- 125000003118 aryl group Chemical group 0.000 description 35
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 35
- 230000002195 synergetic effect Effects 0.000 description 32
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 28
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 21
- 229910052805 deuterium Inorganic materials 0.000 description 21
- 229910052736 halogen Inorganic materials 0.000 description 21
- 150000002367 halogens Chemical class 0.000 description 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 21
- 238000000034 method Methods 0.000 description 20
- 239000003795 chemical substances by application Substances 0.000 description 17
- 125000001072 heteroaryl group Chemical group 0.000 description 14
- 229950007440 icotinib Drugs 0.000 description 14
- QQLKULDARVNMAL-UHFFFAOYSA-N icotinib Chemical compound C#CC1=CC=CC(NC=2C3=CC=4OCCOCCOCCOC=4C=C3N=CN=2)=C1 QQLKULDARVNMAL-UHFFFAOYSA-N 0.000 description 14
- 125000002950 monocyclic group Chemical group 0.000 description 14
- 229950000908 nazartinib Drugs 0.000 description 14
- 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 description 14
- 229960003278 osimertinib Drugs 0.000 description 14
- DUYJMQONPNNFPI-UHFFFAOYSA-N osimertinib Chemical compound COC1=CC(N(C)CCN(C)C)=C(NC(=O)C=C)C=C1NC1=NC=CC(C=2C3=CC=CC=C3N(C)C=2)=N1 DUYJMQONPNNFPI-UHFFFAOYSA-N 0.000 description 14
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 7
- AILRADAXUVEEIR-UHFFFAOYSA-N 5-chloro-4-n-(2-dimethylphosphorylphenyl)-2-n-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=1)=NC=C(Cl)C=1NC1=CC=CC=C1P(C)(C)=O AILRADAXUVEEIR-UHFFFAOYSA-N 0.000 description 7
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 description 7
- 206010005949 Bone cancer Diseases 0.000 description 7
- 208000018084 Bone neoplasm Diseases 0.000 description 7
- UFHFLCQGNIYNRP-VVKOMZTBSA-N Dideuterium Chemical compound [2H][2H] UFHFLCQGNIYNRP-VVKOMZTBSA-N 0.000 description 7
- 239000005551 L01XE03 - Erlotinib Substances 0.000 description 7
- 239000002118 L01XE12 - Vandetanib Substances 0.000 description 7
- 229960001686 afatinib Drugs 0.000 description 7
- 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 description 7
- 125000000217 alkyl group Chemical group 0.000 description 7
- 229950004272 brigatinib Drugs 0.000 description 7
- 125000000753 cycloalkyl group Chemical group 0.000 description 7
- LVXJQMNHJWSHET-AATRIKPKSA-N dacomitinib Chemical compound C=12C=C(NC(=O)\C=C\CN3CCCCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 LVXJQMNHJWSHET-AATRIKPKSA-N 0.000 description 7
- 229950002205 dacomitinib Drugs 0.000 description 7
- 229960001433 erlotinib Drugs 0.000 description 7
- 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 description 7
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- 229960000513 necitumumab Drugs 0.000 description 7
- 229960000241 vandetanib Drugs 0.000 description 7
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 description 7
- 230000001394 metastastic effect Effects 0.000 description 3
- 206010061289 metastatic neoplasm Diseases 0.000 description 3
- 206010023256 Juvenile melanoma benign Diseases 0.000 description 2
- 201000005243 lung squamous cell carcinoma Diseases 0.000 description 2
- 206010052358 Colorectal cancer metastatic Diseases 0.000 description 1
- 239000003183 carcinogenic agent Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762450455P | 2017-01-25 | 2017-01-25 | |
| US62/450,455 | 2017-01-25 | ||
| US201862619165P | 2018-01-19 | 2018-01-19 | |
| US62/619,165 | 2018-01-19 | ||
| PCT/US2018/015150 WO2018140554A1 (en) | 2017-01-25 | 2018-01-25 | Combination therapy involving diaryl macrocyclic compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020514409A JP2020514409A (ja) | 2020-05-21 |
| JP2020514409A5 true JP2020514409A5 (cg-RX-API-DMAC10.html) | 2021-02-25 |
| JP7193475B2 JP7193475B2 (ja) | 2022-12-20 |
Family
ID=62979021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019560071A Active JP7193475B2 (ja) | 2017-01-25 | 2018-01-25 | ジアリール大環状化合物を含む併用療法 |
Country Status (13)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9714258B2 (en) | 2014-01-24 | 2017-07-25 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| JP6871903B2 (ja) | 2015-07-02 | 2021-05-19 | ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
| PT3733187T (pt) | 2015-07-21 | 2024-11-08 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro |
| JP2019527230A (ja) | 2016-07-28 | 2019-09-26 | ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | 大環状キナーゼ阻害剤 |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| HRP20241197T1 (hr) | 2017-07-28 | 2024-11-22 | Turning Point Therapeutics, Inc. | Makrociklični spojevi i primjene istih |
| PL3728271T3 (pl) | 2017-12-19 | 2023-01-23 | Turning Point Therapeutics, Inc. | Związki makrocykliczne do leczenia chorób |
| CN113490664B (zh) | 2018-10-22 | 2025-05-16 | 阿鲁米斯公司 | Tyk2抑制剂和其用途 |
| CN111171049B (zh) * | 2018-11-09 | 2021-06-04 | 山东轩竹医药科技有限公司 | 酪氨酸激酶抑制剂及其用途 |
| IL293206A (en) * | 2019-11-27 | 2022-07-01 | Turning Point Therapeutics Inc | Combination therapy involving diaryl macrocyclic compounds |
| US11666574B2 (en) * | 2019-11-27 | 2023-06-06 | Turning Point Therapeutics, Inc. | Combination therapy involving diaryl macrocyclic compounds |
| CN113121568A (zh) * | 2019-12-31 | 2021-07-16 | 成都倍特药业股份有限公司 | 一种大环结构化合物的盐及其制备方法 |
| WO2021244609A1 (zh) * | 2020-06-04 | 2021-12-09 | 成都倍特药业股份有限公司 | 具有大环结构的化合物及其用途 |
| IL301385A (en) * | 2020-09-16 | 2023-05-01 | Alumis Inc | TYK2 inhibitors and their use |
| WO2022117051A1 (zh) * | 2020-12-03 | 2022-06-09 | 北京鞍石生物科技有限责任公司 | 大环化合物及其制备方法和应用 |
| CN116063326B (zh) * | 2021-11-02 | 2025-08-05 | 赛诺哈勃药业（成都）有限公司 | 作为蛋白激酶调节剂的含氨基大环化合物 |
| EP4370506A1 (en) | 2021-12-30 | 2024-05-22 | Biomea Fusion, Inc. | Pyrazine compounds as inhibitors of flt3 |
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-
2018
- 2018-01-24 TW TW107102558A patent/TWI808958B/zh active
- 2018-01-25 AU AU2018212647A patent/AU2018212647B2/en active Active
- 2018-01-25 MX MX2019008701A patent/MX2019008701A/es unknown
- 2018-01-25 US US16/480,557 patent/US11291667B2/en active Active
- 2018-01-25 EP EP18745012.7A patent/EP3573991A4/en not_active Withdrawn
- 2018-01-25 KR KR1020197021227A patent/KR102618773B1/ko active Active
- 2018-01-25 BR BR112019015115-0A patent/BR112019015115A2/pt not_active Application Discontinuation
- 2018-01-25 JP JP2019560071A patent/JP7193475B2/ja active Active
- 2018-01-25 CN CN201880008596.6A patent/CN110291092A/zh active Pending
- 2018-01-25 WO PCT/US2018/015150 patent/WO2018140554A1/en not_active Ceased
- 2018-01-25 CA CA3049548A patent/CA3049548A1/en active Pending
- 2018-01-25 SG SG11201906386XA patent/SG11201906386XA/en unknown
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2019
- 2019-07-11 IL IL267992A patent/IL267992B2/en unknown
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