JP2019516749A5 - - Google Patents
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- Publication number
- JP2019516749A5 JP2019516749A5 JP2018561474A JP2018561474A JP2019516749A5 JP 2019516749 A5 JP2019516749 A5 JP 2019516749A5 JP 2018561474 A JP2018561474 A JP 2018561474A JP 2018561474 A JP2018561474 A JP 2018561474A JP 2019516749 A5 JP2019516749 A5 JP 2019516749A5
- Authority
- JP
- Japan
- Prior art keywords
- crystals
- formula
- cancer
- crystalline form
- crystal
- 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
- 239000013078 crystal Substances 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 238000001816 cooling Methods 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 238000010438 heat treatment Methods 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 238000001959 radiotherapy Methods 0.000 claims 3
- 238000010992 reflux Methods 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- YDTDKKULPWTHRV-UHFFFAOYSA-N 1H-indazol-3-amine Chemical compound C1=CC=C2C(N)=NNC2=C1 YDTDKKULPWTHRV-UHFFFAOYSA-N 0.000 claims 2
- GNFTZDOKVXKIBK-UHFFFAOYSA-N 3-(2-methoxyethoxy)benzohydrazide Chemical compound COCCOC1=CC=CC(C(=O)NN)=C1 GNFTZDOKVXKIBK-UHFFFAOYSA-N 0.000 claims 2
- FGUUSXIOTUKUDN-IBGZPJMESA-N C1(=CC=CC=C1)N1C2=C(NC([C@H](C1)NC=1OC(=NN=1)C1=CC=CC=C1)=O)C=CC=C2 Chemical compound C1(=CC=CC=C1)N1C2=C(NC([C@H](C1)NC=1OC(=NN=1)C1=CC=CC=C1)=O)C=CC=C2 FGUUSXIOTUKUDN-IBGZPJMESA-N 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 238000001914 filtration Methods 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 102100035080 BDNF/NT-3 growth factors receptor Human genes 0.000 claims 1
- 102100035108 High affinity nerve growth factor receptor Human genes 0.000 claims 1
- 101000596896 Homo sapiens BDNF/NT-3 growth factors receptor Proteins 0.000 claims 1
- 101000596894 Homo sapiens High affinity nerve growth factor receptor Proteins 0.000 claims 1
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 claims 1
- 102100029166 NT-3 growth factor receptor Human genes 0.000 claims 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 150000001263 acyl chlorides Chemical class 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 230000004077 genetic alteration Effects 0.000 claims 1
- 231100000118 genetic alteration Toxicity 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 239000002002 slurry Substances 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 108010064892 trkC Receptor Proteins 0.000 claims 1
- HAYYBYPASCDWEQ-UHFFFAOYSA-N CN(CC1)CCN1c1ccc(C(Nc2n[nH]c3c2cc(Cc2cc(F)cc(F)c2)cc3)=O)c(NC2CCOCC2)c1 Chemical compound CN(CC1)CCN1c1ccc(C(Nc2n[nH]c3c2cc(Cc2cc(F)cc(F)c2)cc3)=O)c(NC2CCOCC2)c1 HAYYBYPASCDWEQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662340797P | 2016-05-24 | 2016-05-24 | |
| US62/340,797 | 2016-05-24 | ||
| PCT/EP2017/061919 WO2017202674A1 (en) | 2016-05-24 | 2017-05-18 | New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020185594A Division JP7154271B2 (ja) | 2016-05-24 | 2020-11-06 | Ｎ－［５－（３，５－ジフルオロ－ベンジル）－１ｈ－インダゾール－３－イル］－４－（４－メチル－ピペラジン－１－イル）－２－（テトラヒドロ－ピラン－４－イルアミノ）－ベンズアミドの新規結晶形 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019516749A JP2019516749A (ja) | 2019-06-20 |
| JP2019516749A5 true JP2019516749A5 (OSRAM) | 2020-04-23 |
| JP7094228B2 JP7094228B2 (ja) | 2022-07-01 |
Family
ID=58709993
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018561474A Active JP7094228B2 (ja) | 2016-05-24 | 2017-05-18 | Ｎ－［５－（３，５－ジフルオロ－ベンジル）－１ｈ－インダゾール－３－イル］－４－（４－メチル－ピペラジン－１－イル）－２－（テトラヒドロ－ピラン－４－イルアミノ）－ベンズアミドの新規結晶形 |
| JP2020185594A Active JP7154271B2 (ja) | 2016-05-24 | 2020-11-06 | Ｎ－［５－（３，５－ジフルオロ－ベンジル）－１ｈ－インダゾール－３－イル］－４－（４－メチル－ピペラジン－１－イル）－２－（テトラヒドロ－ピラン－４－イルアミノ）－ベンズアミドの新規結晶形 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020185594A Active JP7154271B2 (ja) | 2016-05-24 | 2020-11-06 | Ｎ－［５－（３，５－ジフルオロ－ベンジル）－１ｈ－インダゾール－３－イル］－４－（４－メチル－ピペラジン－１－イル）－２－（テトラヒドロ－ピラン－４－イルアミノ）－ベンズアミドの新規結晶形 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10738037B2 (OSRAM) |
| EP (2) | EP3967689A1 (OSRAM) |
| JP (2) | JP7094228B2 (OSRAM) |
| KR (1) | KR102441736B1 (OSRAM) |
| CN (1) | CN109153669B (OSRAM) |
| AU (1) | AU2017271458B2 (OSRAM) |
| CA (1) | CA3024208C (OSRAM) |
| ES (1) | ES2899953T3 (OSRAM) |
| IL (1) | IL263004B (OSRAM) |
| MX (1) | MX379558B (OSRAM) |
| PL (1) | PL3464276T3 (OSRAM) |
| WO (1) | WO2017202674A1 (OSRAM) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017202674A1 (en) | 2016-05-24 | 2017-11-30 | Nerviano Medical Sciences S.R.L. | New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
| CN119909073A (zh) | 2019-07-31 | 2025-05-02 | 豪夫迈·罗氏有限公司 | 新型药物制剂 |
| US20220372024A1 (en) * | 2019-11-01 | 2022-11-24 | Johnson Matthey Public Limited Company | Crystalline forms of entrectinib |
| CN113024521B (zh) * | 2019-12-09 | 2023-01-17 | 武汉九州钰民医药科技有限公司 | 一种制备恩曲替尼的方法 |
| CN111171009B (zh) * | 2020-01-10 | 2022-07-12 | 安礼特（上海）医药科技有限公司 | 恩曲替尼晶型及其制备方法 |
| CN113354626B (zh) * | 2020-03-04 | 2025-06-03 | 罗欣药业(上海)有限公司 | 恩曲替尼的晶型及其制备方法 |
| CN113801062B (zh) * | 2020-06-15 | 2023-05-26 | 沈阳药科大学 | 3-氨基-5-(3,5-二氟苄基)-1h-吲唑的制备方法 |
| CN112336723B (zh) * | 2020-12-11 | 2023-09-26 | 江南大学 | 制备用于降低trpv4与nox2耦联度的药物的方法 |
| CN116669735A (zh) * | 2021-02-03 | 2023-08-29 | 齐鲁制药有限公司 | 恩曲替尼晶型及其制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2176231T3 (pl) * | 2007-07-20 | 2017-04-28 | Nerviano Medical Sciences S.R.L. | Podstawione pochodne indazolu aktywne jako inhibitory kinazy |
| ES2751944T3 (es) * | 2012-05-23 | 2020-04-02 | Nerviano Medical Sciences Srl | Proceso para la preparación de N-[5-(3,5-difluoro-bencil)-1H-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida |
| US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
| WO2017202674A1 (en) | 2016-05-24 | 2017-11-30 | Nerviano Medical Sciences S.R.L. | New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide |
-
2017
- 2017-05-18 WO PCT/EP2017/061919 patent/WO2017202674A1/en not_active Ceased
- 2017-05-18 US US16/301,826 patent/US10738037B2/en active Active
- 2017-05-18 CN CN201780031576.6A patent/CN109153669B/zh active Active
- 2017-05-18 PL PL17724052T patent/PL3464276T3/pl unknown
- 2017-05-18 KR KR1020187037182A patent/KR102441736B1/ko active Active
- 2017-05-18 MX MX2018014298A patent/MX379558B/es unknown
- 2017-05-18 AU AU2017271458A patent/AU2017271458B2/en active Active
- 2017-05-18 EP EP21188238.6A patent/EP3967689A1/en not_active Withdrawn
- 2017-05-18 JP JP2018561474A patent/JP7094228B2/ja active Active
- 2017-05-18 EP EP17724052.0A patent/EP3464276B1/en active Active
- 2017-05-18 ES ES17724052T patent/ES2899953T3/es active Active
- 2017-05-18 CA CA3024208A patent/CA3024208C/en active Active
-
2018
- 2018-11-14 IL IL263004A patent/IL263004B/en unknown
-
2020
- 2020-06-26 US US16/912,965 patent/US11091469B2/en active Active
- 2020-11-06 JP JP2020185594A patent/JP7154271B2/ja active Active
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