JP2021181446A5 - - Google Patents
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- JP2021181446A5 JP2021181446A5 JP2021118355A JP2021118355A JP2021181446A5 JP 2021181446 A5 JP2021181446 A5 JP 2021181446A5 JP 2021118355 A JP2021118355 A JP 2021118355A JP 2021118355 A JP2021118355 A JP 2021118355A JP 2021181446 A5 JP2021181446 A5 JP 2021181446A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutical composition
- effective amount
- therapeutically effective
- crystalline
- 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.)
- Pending
Links
- 239000003814 drug Substances 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 101000605639 Homo sapiens Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Proteins 0.000 claims 3
- 238000005481 NMR spectroscopy Methods 0.000 claims 3
- 102100038332 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Human genes 0.000 claims 3
- 150000008064 anhydrides Chemical class 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 229960000575 trastuzumab Drugs 0.000 claims 3
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 229960004390 palbociclib Drugs 0.000 claims 2
- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- 238000001228 spectrum Methods 0.000 claims 2
- GRZXWCHAXNAUHY-NSISKUIASA-N (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl]-3-(propan-2-ylamino)-1-propanone Chemical compound C1([C@H](C(=O)N2CCN(CC2)C=2C=3[C@H](C)C[C@@H](O)C=3N=CN=2)CNC(C)C)=CC=C(Cl)C=C1 GRZXWCHAXNAUHY-NSISKUIASA-N 0.000 claims 1
- BURHGPHDEVGCEZ-KJGLQBJMSA-N (e)-3-[4-[(e)-2-(2-chloro-4-fluorophenyl)-1-(1h-indazol-5-yl)but-1-enyl]phenyl]prop-2-enoic acid Chemical compound C=1C=C(F)C=C(Cl)C=1C(/CC)=C(C=1C=C2C=NNC2=CC=1)\C1=CC=C(\C=C\C(O)=O)C=C1 BURHGPHDEVGCEZ-KJGLQBJMSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 229960002271 cobimetinib Drugs 0.000 claims 1
- RESIMIUSNACMNW-BXRWSSRYSA-N cobimetinib fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F RESIMIUSNACMNW-BXRWSSRYSA-N 0.000 claims 1
- 229960003957 dexamethasone Drugs 0.000 claims 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003623 enhancer Substances 0.000 claims 1
- UFNVPOGXISZXJD-XJPMSQCNSA-N eribulin Chemical compound C([C@H]1CC[C@@H]2O[C@@H]3[C@H]4O[C@H]5C[C@](O[C@H]4[C@H]2O1)(O[C@@H]53)CC[C@@H]1O[C@H](C(C1)=C)CC1)C(=O)C[C@@H]2[C@@H](OC)[C@@H](C[C@H](O)CN)O[C@H]2C[C@@H]2C(=C)[C@H](C)C[C@H]1O2 UFNVPOGXISZXJD-XJPMSQCNSA-N 0.000 claims 1
- 229960003649 eribulin Drugs 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- -1 fullbestland Chemical compound 0.000 claims 1
- 229960002258 fulvestrant Drugs 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 108091008039 hormone receptors Proteins 0.000 claims 1
- 150000002460 imidazoles Chemical class 0.000 claims 1
- 229950006331 ipatasertib Drugs 0.000 claims 1
- 229960003881 letrozole Drugs 0.000 claims 1
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 229960002087 pertuzumab Drugs 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 1
- 102200085639 rs104886003 Human genes 0.000 claims 1
- 102200085641 rs121913273 Human genes 0.000 claims 1
- 102200085788 rs121913279 Human genes 0.000 claims 1
- 102200085789 rs121913279 Human genes 0.000 claims 1
- 102200085808 rs397517201 Human genes 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762491812P | 2017-04-28 | 2017-04-28 | |
| US62/491,812 | 2017-04-28 | ||
| JP2019558502A JP6998969B2 (ja) | 2017-04-28 | 2018-04-26 | （ｓ）－２－（（２－（（ｓ）－４－（ジフルオロメチル）－２－オキソオキサゾリジン－３－イル）－５，６－ジヒドロベンゾ［ｆ］イミダゾ［１，２－ｄ］［１，４］オキサゼピン－９－イル）アミノ）プロパンアミドの多形体及び固体形態と、生産方法 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019558502A Division JP6998969B2 (ja) | 2017-04-28 | 2018-04-26 | （ｓ）－２－（（２－（（ｓ）－４－（ジフルオロメチル）－２－オキソオキサゾリジン－３－イル）－５，６－ジヒドロベンゾ［ｆ］イミダゾ［１，２－ｄ］［１，４］オキサゼピン－９－イル）アミノ）プロパンアミドの多形体及び固体形態と、生産方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021181446A JP2021181446A (ja) | 2021-11-25 |
| JP2021181446A5 true JP2021181446A5 (enExample) | 2022-05-20 |
Family
ID=62492573
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019558502A Active JP6998969B2 (ja) | 2017-04-28 | 2018-04-26 | （ｓ）－２－（（２－（（ｓ）－４－（ジフルオロメチル）－２－オキソオキサゾリジン－３－イル）－５，６－ジヒドロベンゾ［ｆ］イミダゾ［１，２－ｄ］［１，４］オキサゼピン－９－イル）アミノ）プロパンアミドの多形体及び固体形態と、生産方法 |
| JP2021118355A Pending JP2021181446A (ja) | 2017-04-28 | 2021-07-19 | （ｓ）−２−（（２−（（ｓ）−４−（ジフルオロメチル）−２−オキソオキサゾリジン−３−イル）−５，６−ジヒドロベンゾ［ｆ］イミダゾ［１，２−ｄ］［１，４］オキサゼピン−９−イル）アミノ）プロパンアミドの多形体及び固体形態と、生産方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019558502A Active JP6998969B2 (ja) | 2017-04-28 | 2018-04-26 | （ｓ）－２－（（２－（（ｓ）－４－（ジフルオロメチル）－２－オキソオキサゾリジン－３－イル）－５，６－ジヒドロベンゾ［ｆ］イミダゾ［１，２－ｄ］［１，４］オキサゼピン－９－イル）アミノ）プロパンアミドの多形体及び固体形態と、生産方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US20180339997A1 (enExample) |
| EP (2) | EP3615541B1 (enExample) |
| JP (2) | JP6998969B2 (enExample) |
| KR (1) | KR102342776B1 (enExample) |
| CN (1) | CN110650963B (enExample) |
| AU (1) | AU2018259089B2 (enExample) |
| CA (1) | CA3048591A1 (enExample) |
| ES (1) | ES3027566T3 (enExample) |
| IL (3) | IL298518B2 (enExample) |
| MX (1) | MX394540B (enExample) |
| PL (1) | PL3615541T3 (enExample) |
| TW (1) | TWI826373B (enExample) |
| WO (1) | WO2018197653A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111909173B (zh) | 2015-07-02 | 2025-03-04 | 豪夫迈·罗氏有限公司 | 苯并氧氮杂䓬噁唑烷酮化合物及其使用方法 |
| PL3851441T3 (pl) | 2016-12-15 | 2023-11-06 | F. Hoffmann-La Roche Ag | Proces otrzymywania (S)-2-((2-((S)-4-(difluorometylo)-2-oksooksazolidyn-3-ylo)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oksazepin-9-ylo)amino)propanamidu |
| IL298518B2 (en) * | 2017-04-28 | 2025-05-01 | Hoffmann La Roche | Polymorphs and solid forms of (S)–2–((2–((S–4–(difluoromethyl)–2–oxoxazolidin-3–yl)–5,6–dihydrobenzo[F]imidazo[1,2–D][1,4]oxazepin-9–yl)amino)propanamide and methods of preparation |
| JP7365073B2 (ja) * | 2019-05-21 | 2023-10-19 | ジァンスー フォアフロント ファーマシューティカル カンパニー，リミテッド | トレプロスチニルナトリウムの新規な結晶形および製造方法 |
| CA3144791A1 (en) * | 2019-07-07 | 2021-01-14 | Olema Pharmaceuticals, Inc. | Regimens of estrogen receptor antagonists |
| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| CN112830935B (zh) * | 2019-11-25 | 2023-12-22 | 上海翰森生物医药科技有限公司 | 含三并环类衍生物自由碱的晶型及其药物组合物 |
| CN113227101B (zh) * | 2019-11-25 | 2024-10-11 | 上海翰森生物医药科技有限公司 | 含三并环类衍生物的盐或晶型及其药物组合物 |
| TWI801730B (zh) * | 2020-04-07 | 2023-05-11 | 神雲科技股份有限公司 | 具系統設定資料同步功能的伺服器 |
| WO2022161347A1 (zh) * | 2021-01-29 | 2022-08-04 | 南京明德新药研发有限公司 | 三并环类化合物及其应用 |
| TW202440096A (zh) | 2023-03-24 | 2024-10-16 | 美商亞文納營運公司 | 雌激素受體降解劑之給藥方案 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6274327B1 (en) | 1992-04-13 | 2001-08-14 | Ludwig Institute For Cancer Research | Polypeptides having kinase activity, their preparation and use |
| US5846824A (en) | 1994-02-07 | 1998-12-08 | Ludwig Institute For Cancer Research | Polypeptides having kinase activity, their preparation and use |
| GB9208135D0 (en) | 1992-04-13 | 1992-05-27 | Ludwig Inst Cancer Res | Polypeptides having kinase activity,their preparation and use |
| TWI423980B (zh) | 2009-09-28 | 2014-01-21 | Hoffmann La Roche | 苯并氧氮呯ｐｉ３ｋ抑制劑化合物及使用方法 |
| JP5808818B2 (ja) | 2010-11-25 | 2015-11-10 | ラツィオファーム・ゲーエムベーハー | アファチニブの新規塩及び多形形態 |
| US9266903B2 (en) | 2013-12-16 | 2016-02-23 | Genentech, Inc. | Polymorphs of 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazole-5-yl)-5,6-dihydrobenzo[F]imidazo [1,2-D][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide, methods of production, and pharmaceutical uses thereof |
| CN111909173B (zh) | 2015-07-02 | 2025-03-04 | 豪夫迈·罗氏有限公司 | 苯并氧氮杂䓬噁唑烷酮化合物及其使用方法 |
| PL3851441T3 (pl) | 2016-12-15 | 2023-11-06 | F. Hoffmann-La Roche Ag | Proces otrzymywania (S)-2-((2-((S)-4-(difluorometylo)-2-oksooksazolidyn-3-ylo)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oksazepin-9-ylo)amino)propanamidu |
| IL298518B2 (en) | 2017-04-28 | 2025-05-01 | Hoffmann La Roche | Polymorphs and solid forms of (S)–2–((2–((S–4–(difluoromethyl)–2–oxoxazolidin-3–yl)–5,6–dihydrobenzo[F]imidazo[1,2–D][1,4]oxazepin-9–yl)amino)propanamide and methods of preparation |
-
2018
- 2018-04-26 IL IL298518A patent/IL298518B2/en unknown
- 2018-04-26 MX MX2019012507A patent/MX394540B/es unknown
- 2018-04-26 KR KR1020197031575A patent/KR102342776B1/ko active Active
- 2018-04-26 CN CN201880028227.3A patent/CN110650963B/zh active Active
- 2018-04-26 CA CA3048591A patent/CA3048591A1/en active Pending
- 2018-04-26 ES ES18728514T patent/ES3027566T3/es active Active
- 2018-04-26 US US15/963,876 patent/US20180339997A1/en not_active Abandoned
- 2018-04-26 EP EP18728514.3A patent/EP3615541B1/en active Active
- 2018-04-26 JP JP2019558502A patent/JP6998969B2/ja active Active
- 2018-04-26 EP EP25158128.6A patent/EP4534148A3/en active Pending
- 2018-04-26 TW TW107114314A patent/TWI826373B/zh active
- 2018-04-26 AU AU2018259089A patent/AU2018259089B2/en active Active
- 2018-04-26 PL PL18728514.3T patent/PL3615541T3/pl unknown
- 2018-04-26 IL IL317762A patent/IL317762A/en unknown
- 2018-04-26 WO PCT/EP2018/060820 patent/WO2018197653A1/en not_active Ceased
-
2019
- 2019-06-18 IL IL267464A patent/IL267464B2/en unknown
-
2020
- 2020-05-15 US US16/875,537 patent/US11028100B2/en active Active
- 2020-05-15 US US16/875,545 patent/US11591345B2/en active Active
-
2021
- 2021-07-19 JP JP2021118355A patent/JP2021181446A/ja active Pending
-
2023
- 2023-01-26 US US18/101,951 patent/US12410189B2/en active Active
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