JP2011509252A5 - - Google Patents
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- Publication number
- JP2011509252A5 JP2011509252A5 JP2010541101A JP2010541101A JP2011509252A5 JP 2011509252 A5 JP2011509252 A5 JP 2011509252A5 JP 2010541101 A JP2010541101 A JP 2010541101A JP 2010541101 A JP2010541101 A JP 2010541101A JP 2011509252 A5 JP2011509252 A5 JP 2011509252A5
- Authority
- JP
- Japan
- Prior art keywords
- stereoisomer
- tautomer
- indazol
- aminocarbonyl
- phenyl
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- CXPSLSYYWGMRQH-MZQXSLHISA-N (e)-but-2-enedioate;2-[4-[(3s)-piperidin-1-ium-3-yl]phenyl]indazole-7-carboxamide Chemical compound [O-]C(=O)\C=C\C([O-])=O.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1 CXPSLSYYWGMRQH-MZQXSLHISA-N 0.000 claims 2
- MYGUDASFCHBTGF-XZPBZCASSA-N 2-[4-[(3s)-piperidin-1-ium-3-yl]phenyl]indazole-7-carboxamide;sulfate Chemical compound [O-]S([O-])(=O)=O.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1 MYGUDASFCHBTGF-XZPBZCASSA-N 0.000 claims 2
- ACNPUCQQZDAPJH-FMOMHUKBSA-N 4-methylbenzenesulfonic acid;2-[4-[(3s)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrate Chemical compound O.CC1=CC=C(S([O-])(=O)=O)C=C1.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1 ACNPUCQQZDAPJH-FMOMHUKBSA-N 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 2
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 2
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 2
- PLECLGHOBYKOQA-XZPBZCASSA-N butanedioate;2-[4-[(3s)-piperidin-1-ium-3-yl]phenyl]indazole-7-carboxamide Chemical compound [O-]C(=O)CCC([O-])=O.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1 PLECLGHOBYKOQA-XZPBZCASSA-N 0.000 claims 2
- 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 2
- ORZMSMCZBZARKY-UHFFFAOYSA-N 1,3,2$l^{6}-benzodioxathiole 2,2-dioxide Chemical compound C1=CC=C2OS(=O)(=O)OC2=C1 ORZMSMCZBZARKY-UHFFFAOYSA-N 0.000 claims 1
- LCPFHXWLJMNKNC-PFEQFJNWSA-N 4-methylbenzenesulfonate;2-[4-[(3s)-piperidin-1-ium-3-yl]phenyl]indazole-7-carboxamide Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1.N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCC[NH2+]C1 LCPFHXWLJMNKNC-PFEQFJNWSA-N 0.000 claims 1
- 208000001647 Renal Insufficiency Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010057430 Retinal injury Diseases 0.000 claims 1
- 206010038997 Retroviral infections Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical group O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- SBRRKNDQFQNEJP-FFAASGSZSA-N benzene 2-[4-[(3S)-piperidin-1-ium-3-yl]phenyl]indazole-7-carboxamide sulfate Chemical compound [O-]S([O-])(=O)=O.c1ccccc1.NC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@@H]1CCC[NH2+]C1.NC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@@H]1CCC[NH2+]C1 SBRRKNDQFQNEJP-FFAASGSZSA-N 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000002534 radiation-sensitizing agent Substances 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 230000009759 skin aging Effects 0.000 claims 1
- 230000037380 skin damage Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical group CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1033308P | 2008-01-08 | 2008-01-08 | |
| US61/010,333 | 2008-01-08 | ||
| PCT/GB2009/000041 WO2009087381A1 (en) | 2008-01-08 | 2009-01-08 | Pharmaceutically acceptable salts of 2-{4-[(3s)-piperidin-3- yl]phenyl} -2h-indazole-7-carboxamide |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011509252A JP2011509252A (ja) | 2011-03-24 |
| JP2011509252A5 true JP2011509252A5 (enExample) | 2012-02-16 |
| JP5989965B2 JP5989965B2 (ja) | 2016-09-07 |
Family
ID=40404013
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010541101A Active JP5989965B2 (ja) | 2008-01-08 | 2009-01-08 | ２−｛４−［（３ｓ）−ピペリジン−３−イル］フェニル｝−２ｈ−インダゾール−７−カルボキサミドの薬学的に許容される塩 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8436185B2 (enExample) |
| EP (1) | EP2240466B1 (enExample) |
| JP (1) | JP5989965B2 (enExample) |
| KR (1) | KR101653548B1 (enExample) |
| CN (2) | CN106008460B (enExample) |
| AU (1) | AU2009203598B2 (enExample) |
| BR (1) | BRPI0906020A2 (enExample) |
| CA (1) | CA2711491C (enExample) |
| ES (1) | ES2548131T3 (enExample) |
| FR (1) | FR18C1020I2 (enExample) |
| IL (1) | IL206201A (enExample) |
| MX (1) | MX337421B (enExample) |
| NL (1) | NL300938I2 (enExample) |
| NZ (1) | NZ586675A (enExample) |
| WO (1) | WO2009087381A1 (enExample) |
| ZA (1) | ZA201003902B (enExample) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2740746A1 (en) | 2008-10-14 | 2010-04-22 | Ning Xi | Compounds comprising a spiro-ring and and methods of use |
| EP2408300B1 (en) | 2009-03-21 | 2016-05-11 | Sunshine Lake Pharma Co., Ltd. | Amino ester derivatives, salts thereof and methods of use |
| DK3150610T3 (da) | 2010-02-12 | 2019-11-04 | Pfizer | Salte og polymorfer af 8-fluor-2-{4-[(methylamino}methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-on |
| US9580407B2 (en) | 2012-12-07 | 2017-02-28 | Merck Sharp & Dohme Corp. | Regioselective N-2 arylation of indazoles |
| PL3157566T3 (pl) | 2014-06-17 | 2019-10-31 | Vertex Pharma | Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr |
| EP3277321B1 (en) | 2015-04-01 | 2024-08-14 | AnaptysBio, Inc. | Antibodies directed against t cell immunoglobulin and mucin protein 3 (tim-3) |
| DK3358347T3 (da) * | 2015-09-30 | 2020-11-30 | Univ Tohoku | Markør til bestemmelse af diabetisk nefropati |
| KR102678021B1 (ko) | 2015-09-30 | 2024-06-26 | 버텍스 파마슈티칼스 인코포레이티드 | Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물 |
| FI3478286T3 (fi) | 2016-06-29 | 2024-03-14 | Tesaro Inc | Menetelmiä munasarjasyövän hoitamiseksi |
| CN119606965A (zh) | 2016-07-29 | 2025-03-14 | 詹森药业有限公司 | 治疗前列腺癌的方法 |
| CN107663190B (zh) * | 2016-07-29 | 2020-06-09 | 钟桂发 | 一种尼拉帕尼及其中间体的制备方法以及中间体化合物 |
| CN106432057A (zh) * | 2016-09-17 | 2017-02-22 | 青岛云天生物技术有限公司 | 一种制备(3s)‑3‑(4‑氨基苯基)哌啶‑1‑甲酸叔丁酯的方法 |
| SG11201903867YA (en) | 2016-11-01 | 2019-05-30 | Anaptysbio Inc | Antibodies directed against t cell immunoglobulin and mucin protein 3 (tim-3) |
| EP3666794A1 (en) | 2016-11-01 | 2020-06-17 | AnaptysBio, Inc. | Antibodies directed against programmed death- 1 (pd-1) |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| JP7118073B2 (ja) | 2017-01-09 | 2022-08-15 | テサロ， インコーポレイテッド | 抗ｔｉｍ－３抗体を用いてがんを処置する方法 |
| EP3565844B8 (en) | 2017-01-09 | 2023-04-12 | Tesaro, Inc. | Methods of treating cancer with anti-pd-1 antibodies |
| BR112019020191A2 (pt) * | 2017-03-27 | 2020-04-22 | Tesaro Inc | formulações de niraparib |
| EA201992177A1 (ru) * | 2017-03-27 | 2020-02-25 | Тесаро, Инк. | Композиции на основе нирапариба |
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| EA201992430A1 (ru) | 2017-04-13 | 2020-02-28 | Янссен Фармацевтика Нв | Комбинированная терапия рака предстательной железы |
| CN110753684A (zh) | 2017-04-24 | 2020-02-04 | 特沙诺有限公司 | 尼拉帕利的制造方法 |
| SG11201909395TA (en) | 2017-04-27 | 2019-11-28 | Tesaro Inc | Antibody agents directed against lymphocyte activation gene-3 (lag-3) and uses thereof |
| 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 |
| EP3624850A1 (en) | 2017-05-18 | 2020-03-25 | Tesaro, Inc. | Combination therapies for treating cancer |
| 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 |
| CN109081828B (zh) * | 2017-06-14 | 2021-03-26 | 上海时莱生物技术有限公司 | 聚(adp-核糖)聚合酶抑制剂、制备方法及用途 |
| EP3668857B1 (en) | 2017-08-14 | 2023-07-05 | Teva Pharmaceuticals International GmbH | Processes for the preparation of niraparib and intermediates thereof |
| EP3682236A1 (en) * | 2017-09-13 | 2020-07-22 | B.R.A.H.M.S GmbH | Proadrenomedullin as indicator for renal replacement therapy in critically ill patients |
| EP4027145A1 (en) * | 2017-09-13 | 2022-07-13 | B.R.A.H.M.S GmbH | Pro-adm for therapy monitoring of intensive care unit patients |
| EP3682246A1 (en) * | 2017-09-13 | 2020-07-22 | B.R.A.H.M.S GmbH | Method for guidance of fluid therapy based on proadrenomedullin |
| AU2018341479B2 (en) * | 2017-09-26 | 2022-02-17 | Tesaro, Inc. | Niraparib formulations |
| KR20200086664A (ko) | 2017-09-30 | 2020-07-17 | 테사로, 인코포레이티드 | 암을 치료하기 위한 조합 요법 |
| MA50618A (fr) * | 2017-10-06 | 2020-08-12 | Tesaro Inc | Polyrhérapies et leurs utilisations |
| CA3087060A1 (en) | 2017-12-27 | 2019-07-04 | Tesaro, Inc. | Methods of treating cancer |
| EP3749352A1 (en) | 2018-02-05 | 2020-12-16 | Tesaro Inc. | Pediatric niraparib formulations and pediatric treatment methods |
| TWI852940B (zh) | 2018-09-04 | 2024-08-21 | 美商泰沙羅公司 | 治療癌症之方法 |
| CN118994103A (zh) * | 2018-10-03 | 2024-11-22 | 特沙诺有限公司 | 尼拉帕利盐 |
| US20210347758A1 (en) * | 2018-10-03 | 2021-11-11 | Tesaro, Inc. | Crystalline Forms of Niraparib Freebase |
| WO2020072860A1 (en) | 2018-10-05 | 2020-04-09 | Johnson Matthey Public Limited Company | Niraparib solid state form |
| EP3966782A2 (en) | 2019-05-06 | 2022-03-16 | Tesaro, Inc. | Methods for characterizing and treating a cancer type using cancer images |
| CN110407704B (zh) * | 2019-08-19 | 2022-05-17 | 常州沃腾化工科技有限公司 | 一种3-甲酰基-2-硝基苯甲酸甲酯的合成方法 |
| CN114391013B (zh) | 2019-09-24 | 2024-01-26 | 上海美悦生物科技发展有限公司 | 一种irak抑制剂及其制备方法和用途 |
| AU2021269115A1 (en) | 2020-05-08 | 2023-01-19 | Janssen Pharmaceutica Nv | Treatment of prostate cancer with a combination of abiraterone acetate and niraparib |
| EP4373491A1 (en) | 2021-07-19 | 2024-05-29 | JANSSEN Pharmaceutica NV | Treatment of metastatic castration-resistant prostate cancer with niraparib |
| MX2024009626A (es) | 2022-02-04 | 2024-08-09 | Janssen Pharmaceutica Nv | Niraparib y acetato de abiraterona mas prednisona para mejorar los resultados clinicos en pacientes con cancer de prostata resistente a la castracion metastasico y alteraciones del hrr. |
| US20250352534A1 (en) | 2022-02-15 | 2025-11-20 | Tesaro, Inc. | Use of Niraparib for the Treatment of Brain Cancer |
| EP4712976A1 (en) | 2023-05-17 | 2026-03-25 | Tesaro, Inc. | Novel use of an inhibior of the a poly-adp ribose polymerase (parp) in the treatment of cancer |
| WO2025027138A1 (en) | 2023-08-02 | 2025-02-06 | Janssen Pharmaceutica Nv | Combination of niraparib and abiraterone for use in the treatment of metastatic castration-resistant prostate cancer |
| CN117843713A (zh) * | 2023-12-18 | 2024-04-09 | 上海亲合力生物医药科技股份有限公司 | 基于肿瘤微环境激活的激酶抑制剂、组合物及应用 |
| CN119707921B (zh) * | 2024-12-19 | 2026-03-03 | 四川轻化工大学 | 一种尼拉帕尼的合成方法 |
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-
2009
- 2009-01-08 NZ NZ586675A patent/NZ586675A/en unknown
- 2009-01-08 US US12/811,922 patent/US8436185B2/en active Active
- 2009-01-08 KR KR1020107015011A patent/KR101653548B1/ko active Active
- 2009-01-08 MX MX2010006593A patent/MX337421B/es active IP Right Grant
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