JP2020512350A5 - - Google Patents
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- Publication number
- JP2020512350A5 JP2020512350A5 JP2019553055A JP2019553055A JP2020512350A5 JP 2020512350 A5 JP2020512350 A5 JP 2020512350A5 JP 2019553055 A JP2019553055 A JP 2019553055A JP 2019553055 A JP2019553055 A JP 2019553055A JP 2020512350 A5 JP2020512350 A5 JP 2020512350A5
- Authority
- JP
- Japan
- Prior art keywords
- indazole
- carboxamide
- phenyl
- composition according
- piperidin
- 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
- 239000000203 mixture Substances 0.000 claims 31
- 238000000634 powder X-ray diffraction Methods 0.000 claims 24
- PCHKPVIQAHNQLW-CQSZACIVSA-N niraparib Chemical compound N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCCNC1 PCHKPVIQAHNQLW-CQSZACIVSA-N 0.000 claims 19
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 14
- 239000013078 crystal Substances 0.000 claims 9
- 229950004288 tosilate Drugs 0.000 claims 8
- 150000008064 anhydrides Chemical class 0.000 claims 7
- 150000004682 monohydrates Chemical class 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 239000000126 substance Substances 0.000 claims 6
- 239000003960 organic solvent Substances 0.000 claims 5
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical group CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 2
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims 1
- 238000004566 IR spectroscopy Methods 0.000 claims 1
- 238000001069 Raman spectroscopy Methods 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000002274 desiccant Substances 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 235000019253 formic acid Nutrition 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- -1 monohydrate salt Chemical class 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000001179 sorption measurement Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762477411P | 2017-03-27 | 2017-03-27 | |
| US62/477,411 | 2017-03-27 | ||
| PCT/US2018/024603 WO2018183354A1 (en) | 2017-03-27 | 2018-03-27 | Niraparib compositions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020512350A JP2020512350A (ja) | 2020-04-23 |
| JP2020512350A5 true JP2020512350A5 (https=) | 2021-05-06 |
Family
ID=63676949
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019553055A Pending JP2020512350A (ja) | 2017-03-27 | 2018-03-27 | ニラパリブ組成物 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US11091459B2 (https=) |
| EP (1) | EP3600314A1 (https=) |
| JP (1) | JP2020512350A (https=) |
| KR (1) | KR20200014736A (https=) |
| CN (1) | CN110944638A (https=) |
| AU (2) | AU2018246214B2 (https=) |
| BR (1) | BR112019020211A2 (https=) |
| CA (1) | CA3058375C (https=) |
| EA (1) | EA201992177A1 (https=) |
| IL (1) | IL269630A (https=) |
| MX (1) | MX2019011496A (https=) |
| SG (1) | SG11201909011PA (https=) |
| TW (1) | TWI761476B (https=) |
| WO (1) | WO2018183354A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201811564QA (en) | 2016-06-29 | 2019-01-30 | Tesaro Inc | Methods of treating ovarian cancer |
| CN110944638A (zh) | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| MA48475A (fr) | 2017-04-24 | 2020-03-04 | Tesaro Inc | Procédés de fabrication de niraparib |
| TW202444417A (zh) | 2017-05-09 | 2024-11-16 | 美商提薩羅有限公司 | 治療癌症的組合療法 |
| KR20200005662A (ko) | 2017-05-18 | 2020-01-15 | 테사로, 인코포레이티드 | 암을 치료하기 위한 조합 요법 |
| TWI843707B (zh) | 2017-09-26 | 2024-06-01 | 美商提薩羅有限公司 | 尼拉帕尼（ｎｉｒａｐａｒｉｂ）調配物 |
| MX2020003770A (es) | 2017-09-30 | 2020-07-29 | Tesaro Inc | Terapias de combinacion para tratar cancer. |
| EA202090655A1 (ru) | 2017-10-06 | 2020-12-07 | Тесаро, Инк. | Комбинированные терапевтические средства и их применение |
| CN111918667A (zh) | 2018-02-05 | 2020-11-10 | 特沙诺有限公司 | 儿科尼拉帕尼配制剂和儿科治疗方法 |
| JP2022504228A (ja) | 2018-10-03 | 2022-01-13 | テサロ， インコーポレイテッド | ニラパリブ遊離塩基の結晶形態 |
| WO2020072860A1 (en) | 2018-10-05 | 2020-04-09 | Johnson Matthey Public Limited Company | Niraparib solid state form |
| CA3087392A1 (en) | 2019-07-16 | 2021-01-16 | Apotex Inc. | Crystalline forms of niraparib tosylate |
| TWI905184B (zh) * | 2020-05-08 | 2025-11-21 | 比利時商健生藥品公司 | 用醋酸阿比特龍和尼拉帕尼之組合治療前列腺癌 |
| JP2024525881A (ja) | 2021-07-19 | 2024-07-12 | ヤンセン ファーマシューティカ エヌ．ベー． | ニラパリブ（ｎｉｒａｐａｒｉｂ）による転移性去勢抵抗性前立腺癌の治療 |
| US20250352534A1 (en) | 2022-02-15 | 2025-11-20 | Tesaro, Inc. | Use of Niraparib for the Treatment of Brain Cancer |
| WO2023201338A1 (en) | 2022-04-15 | 2023-10-19 | Ideaya Biosciences, Inc. | Combination therapy comprising a mat2a inhibitor and a parp inhibitor |
| CA3257870A1 (en) | 2022-06-01 | 2023-12-07 | Ideaya Biosciences, Inc. | THIADIAZOLYL DERIVATIVES USED AS DNA POLYMERASE THETA INHIBITORS AND THEIR USES |
| CN121311226A (zh) | 2023-05-17 | 2026-01-09 | 特沙诺有限公司 | 聚adp核糖聚合酶(parp)抑制剂在治疗癌症中的新用途 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0606663D0 (en) | 2006-04-03 | 2006-05-10 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| CA2647545C (en) | 2006-04-03 | 2016-02-23 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Amide substituted indazole and benzotriazole derivatives as poly(adp-ribose)polymerase (parp) inhibitors |
| WO2008043024A2 (en) | 2006-10-04 | 2008-04-10 | Kalypsys, Inc. | Oral pharmaceutical formulation comprising a sulfonyl bicyclic modulator of ppar for the treatment of disease |
| JP4611444B2 (ja) | 2007-01-10 | 2011-01-12 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー | ポリ（ａｄｐ−リボース）ポリメラーゼ（ｐａｒｐ）阻害剤としてのアミド置換インダゾール |
| CA2702429A1 (en) * | 2007-10-17 | 2009-04-23 | Kudos Pharmaceuticals Limited | Crystalline form l 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one |
| KR101653548B1 (ko) * | 2008-01-08 | 2016-09-02 | 머크 샤프 앤드 돔 리미티드 | 2-｛4-［（3ｓ）-피페리딘-3-일］페닐｝-2ｈ-인다졸-7-카복스아미드의 약제학적으로 허용되는 염 |
| US20100278921A1 (en) | 2009-04-30 | 2010-11-04 | Fischer Cristina M | Solid oral formulation of abt-263 |
| MY156873A (en) * | 2009-08-26 | 2016-04-15 | Cephalon Inc | Novel forms of a multicyclic compound |
| CA2779052A1 (en) | 2012-05-31 | 2013-11-30 | Pharmascience Inc. | Pharmaceutical composition of entecavir and process of manufacturing |
| EP2928473B1 (en) | 2012-12-07 | 2017-06-28 | Merck Sharp & Dohme Corp. | Regioselective n-2 arylation of indazoles |
| US9738915B2 (en) | 2012-12-07 | 2017-08-22 | Merck Sharp & Dohme Corp. | Biocatalytic transamination process |
| KR20160061911A (ko) | 2013-04-08 | 2016-06-01 | 데니스 엠. 브라운 | 최적하 투여된 화학 화합물의 치료 효과 |
| US9191894B2 (en) * | 2013-07-23 | 2015-11-17 | Disney Enterprises, Inc. | Power saving for multi-hop communications |
| CA2935857C (en) | 2014-01-05 | 2020-12-15 | Washington University | Radiolabeled tracers for poly (adp-ribose) polymerase-1 (parp-1), methods and uses therefor |
| US20150299219A1 (en) | 2014-04-22 | 2015-10-22 | Calitor Sciences, Llc | Bicyclic pyrazolone compounds and methods of use |
| WO2015184145A1 (en) | 2014-05-28 | 2015-12-03 | Eisai R&D Management Co., Ltd. | Use of eribulin and poly (adp ribose) polymerase (parp) inhibitors as combination therapy for the treatment of cancer |
| AU2015305696B2 (en) | 2014-08-22 | 2019-08-29 | Pharma& Schweiz Gmbh | High dosage strength tablets of rucaparib |
| US20160160294A1 (en) | 2014-12-08 | 2016-06-09 | Tesaro | Methods and materials for predicting response to niraparib |
| HUE062258T2 (hu) | 2015-07-02 | 2023-10-28 | Acerta Pharma Bv | (S)-4-(8-amino-3-(1-(but-2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamid szilárd alakjai és készítményei |
| SG11201811564QA (en) | 2016-06-29 | 2019-01-30 | Tesaro Inc | Methods of treating ovarian cancer |
| CN106496187A (zh) * | 2016-09-14 | 2017-03-15 | 陕西科技大学 | 一种制备PARP抑制剂Niraparib的合成方法 |
| CN106831708A (zh) | 2016-11-22 | 2017-06-13 | 西安泰科迈医药科技股份有限公司 | 一种新型口服抗癌药物Nirapairb的合成方法 |
| CN108201537A (zh) | 2016-12-16 | 2018-06-26 | 苏州苏融生物医药有限公司 | 一种尼拉帕尼缓控释药物组合物及其用途 |
| CN106854176A (zh) | 2016-12-21 | 2017-06-16 | 南京艾德凯腾生物医药有限责任公司 | 一种制备尼拉帕尼对甲苯磺酸盐一水合物的方法 |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| CN110944638A (zh) | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| KR20190130625A (ko) | 2017-03-27 | 2019-11-22 | 테사로, 인코포레이티드 | 니라파립 제제 |
| MA48475A (fr) | 2017-04-24 | 2020-03-04 | Tesaro Inc | Procédés de fabrication de niraparib |
| TW202444417A (zh) | 2017-05-09 | 2024-11-16 | 美商提薩羅有限公司 | 治療癌症的組合療法 |
| KR20200005662A (ko) | 2017-05-18 | 2020-01-15 | 테사로, 인코포레이티드 | 암을 치료하기 위한 조합 요법 |
| CN108530425A (zh) | 2017-05-27 | 2018-09-14 | 广州科锐特生物科技有限公司 | 一种尼拉帕尼对甲苯磺酸盐水合物晶型及其制备方法 |
| TWI843707B (zh) | 2017-09-26 | 2024-06-01 | 美商提薩羅有限公司 | 尼拉帕尼（ｎｉｒａｐａｒｉｂ）調配物 |
| MX2020003770A (es) | 2017-09-30 | 2020-07-29 | Tesaro Inc | Terapias de combinacion para tratar cancer. |
| EA202090655A1 (ru) | 2017-10-06 | 2020-12-07 | Тесаро, Инк. | Комбинированные терапевтические средства и их применение |
| US20210106574A1 (en) | 2017-12-27 | 2021-04-15 | Tesaro, Inc. | Methods of Treating Cancer |
| CN111918667A (zh) | 2018-02-05 | 2020-11-10 | 特沙诺有限公司 | 儿科尼拉帕尼配制剂和儿科治疗方法 |
| JP2022504228A (ja) * | 2018-10-03 | 2022-01-13 | テサロ， インコーポレイテッド | ニラパリブ遊離塩基の結晶形態 |
| CA3087392A1 (en) * | 2019-07-16 | 2021-01-16 | Apotex Inc. | Crystalline forms of niraparib tosylate |
-
2018
- 2018-03-27 CN CN201880033357.6A patent/CN110944638A/zh active Pending
- 2018-03-27 MX MX2019011496A patent/MX2019011496A/es unknown
- 2018-03-27 EP EP18774912.2A patent/EP3600314A1/en not_active Withdrawn
- 2018-03-27 TW TW107110575A patent/TWI761476B/zh active
- 2018-03-27 SG SG11201909011P patent/SG11201909011PA/en unknown
- 2018-03-27 EA EA201992177A patent/EA201992177A1/ru unknown
- 2018-03-27 WO PCT/US2018/024603 patent/WO2018183354A1/en not_active Ceased
- 2018-03-27 AU AU2018246214A patent/AU2018246214B2/en active Active
- 2018-03-27 JP JP2019553055A patent/JP2020512350A/ja active Pending
- 2018-03-27 BR BR112019020211-0A patent/BR112019020211A2/pt not_active Application Discontinuation
- 2018-03-27 KR KR1020197031668A patent/KR20200014736A/ko not_active Ceased
- 2018-03-27 CA CA3058375A patent/CA3058375C/en active Active
-
2019
- 2019-09-25 IL IL26963019A patent/IL269630A/en unknown
- 2019-09-26 US US16/584,401 patent/US11091459B2/en active Active
-
2021
- 2021-06-04 US US17/339,896 patent/US11673877B2/en active Active
- 2021-10-08 AU AU2021245223A patent/AU2021245223A1/en not_active Abandoned
-
2023
- 2023-05-01 US US18/310,238 patent/US20230416223A1/en active Pending
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