JP2013518910A5 - - Google Patents
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- JP2013518910A5 JP2013518910A5 JP2012552143A JP2012552143A JP2013518910A5 JP 2013518910 A5 JP2013518910 A5 JP 2013518910A5 JP 2012552143 A JP2012552143 A JP 2012552143A JP 2012552143 A JP2012552143 A JP 2012552143A JP 2013518910 A5 JP2013518910 A5 JP 2013518910A5
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- JP
- Japan
- Prior art keywords
- compound
- formula
- salt
- acid
- reducing reagent
- 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
- 0 C[n]1ncnc1C(C(c(cc1)ccc1F)Nc1c2c(C(O*)=O)cc(F)c1)C2=O Chemical compound C[n]1ncnc1C(C(c(cc1)ccc1F)Nc1c2c(C(O*)=O)cc(F)c1)C2=O 0.000 description 14
- HWGQMRYQVZSGDQ-UHFFFAOYSA-N C[n]1ncnc1C(C(c(cc1)ccc1F)Nc1c2c3cc(F)c1)C2=NNC3=O Chemical compound C[n]1ncnc1C(C(c(cc1)ccc1F)Nc1c2c3cc(F)c1)C2=NNC3=O HWGQMRYQVZSGDQ-UHFFFAOYSA-N 0.000 description 4
- IHYDPJKFRHSULT-WTKPLQERSA-N C[n]1ncnc1/C=C(/c(c1cc(F)c2)c2[N+]([O-])=O)\OC1=O Chemical compound C[n]1ncnc1/C=C(/c(c1cc(F)c2)c2[N+]([O-])=O)\OC1=O IHYDPJKFRHSULT-WTKPLQERSA-N 0.000 description 2
- RFNLRJMPADAXDJ-LSFURLLWSA-N C[n]1ncnc1CC(c(c1cc(F)c2)c2/N=C/c(cc2)ccc2F)=NNC1=O Chemical compound C[n]1ncnc1CC(c(c1cc(F)c2)c2/N=C/c(cc2)ccc2F)=NNC1=O RFNLRJMPADAXDJ-LSFURLLWSA-N 0.000 description 2
- RUJPELCBXQXIFP-UHFFFAOYSA-N CN/C(/CC(c(c1cc(F)c2)c2N)=NNC1=O)=N\C=N Chemical compound CN/C(/CC(c(c1cc(F)c2)c2N)=NNC1=O)=N\C=N RUJPELCBXQXIFP-UHFFFAOYSA-N 0.000 description 1
- PAJDMXUECFRDFU-UHFFFAOYSA-N C[n]1ncnc1CC(c(c1cc(F)c2)c2N)=NNC1=O Chemical compound C[n]1ncnc1CC(c(c1cc(F)c2)c2N)=NNC1=O PAJDMXUECFRDFU-UHFFFAOYSA-N 0.000 description 1
- HWGQMRYQVZSGDQ-HOTGVXAUSA-N C[n]1ncnc1[C@@H]([C@H](c(cc1)ccc1F)Nc1cc(F)cc2c11)C1=NNC2=O Chemical compound C[n]1ncnc1[C@@H]([C@H](c(cc1)ccc1F)Nc1cc(F)cc2c11)C1=NNC2=O HWGQMRYQVZSGDQ-HOTGVXAUSA-N 0.000 description 1
- HWGQMRYQVZSGDQ-HZPDHXFCSA-N C[n]1ncnc1[C@H]([C@@H](c(cc1)ccc1F)Nc1c2c3cc(F)c1)C2=NNC3=O Chemical compound C[n]1ncnc1[C@H]([C@@H](c(cc1)ccc1F)Nc1c2c3cc(F)c1)C2=NNC3=O HWGQMRYQVZSGDQ-HZPDHXFCSA-N 0.000 description 1
- JBLFHMWQMPVDDL-UHFFFAOYSA-N [O-][N+](c1cc(F)cc2c1COC2=O)=O Chemical compound [O-][N+](c1cc(F)cc2c1COC2=O)=O JBLFHMWQMPVDDL-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30245710P | 2010-02-08 | 2010-02-08 | |
| US61/302,457 | 2010-02-08 | ||
| PCT/US2011/023965 WO2011097602A1 (en) | 2010-02-08 | 2011-02-08 | Processes of synthesizing dihydropyridophthalazinone derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013518910A JP2013518910A (ja) | 2013-05-23 |
| JP2013518910A5 true JP2013518910A5 (https=) | 2014-03-27 |
| JP5735988B2 JP5735988B2 (ja) | 2015-06-17 |
Family
ID=44354222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012552143A Active JP5735988B2 (ja) | 2010-02-08 | 2011-02-08 | ジヒドロピリドフタラジノン誘導体を合成する方法 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US8765945B2 (https=) |
| EP (1) | EP2533640B1 (https=) |
| JP (1) | JP5735988B2 (https=) |
| KR (1) | KR101826652B1 (https=) |
| CN (1) | CN102834008B (https=) |
| AU (1) | AU2011213584B2 (https=) |
| BR (1) | BR112012019648B1 (https=) |
| CA (1) | CA2788114C (https=) |
| CY (1) | CY1118575T1 (https=) |
| DK (1) | DK2533640T3 (https=) |
| ES (1) | ES2606174T3 (https=) |
| HU (1) | HUE030794T2 (https=) |
| IL (1) | IL221170A (https=) |
| MX (1) | MX340319B (https=) |
| PL (1) | PL2533640T3 (https=) |
| PT (1) | PT2533640T (https=) |
| RU (1) | RU2561732C2 (https=) |
| SG (1) | SG182784A1 (https=) |
| SI (1) | SI2533640T1 (https=) |
| WO (1) | WO2011097602A1 (https=) |
| ZA (1) | ZA201205538B (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104478875B (zh) | 2008-08-06 | 2017-04-12 | 麦迪韦逊科技有限公司 | 聚(adp‑核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂 |
| EP2531033A4 (en) | 2010-02-03 | 2013-07-31 | Biomarin Pharm Inc | POLY (ADP-RIBOSE) POLYMERASE (PARP) DIHYDROPYRIDOPHTHALAZINE HEMMER FOR USE IN THE TREATMENT OF PTEN-LACK ASSOCIATED DISEASES |
| KR101826652B1 (ko) | 2010-02-08 | 2018-02-07 | 메디베이션 테크놀로지즈, 인크. | 디히드로피리도프탈라지논 유도체의 합성 방법 |
| KR20190120458A (ko) | 2010-10-21 | 2019-10-23 | 메디베이션 테크놀로지즈 엘엘씨 | 결정질의 (8s,9r)-5-플루오로-8-(4-플루오로페닐)-9-(1-메틸-1h-1,2,4-트리아졸-5-일)-8,9-디하이드로-2h-피리도[4,3,2-de]프탈라진-3(7h)-온 토실레이트 염 |
| US10111871B2 (en) | 2013-08-27 | 2018-10-30 | Northeastern University | Nanoparticle drug delivery system and method of treating cancer and neurotrauma |
| CN105916846A (zh) * | 2013-11-07 | 2016-08-31 | 麦迪韦逊科技有限公司 | 用于合成经保护的n-烷基三唑甲醛的三唑中间体 |
| EA201790290A1 (ru) * | 2014-07-31 | 2017-07-31 | Медивэйшн Текнолоджиз, Инк. | Формерные соли (2s,3s)-метил 7-фтор-2-(4-фторфенил)-3-(1-метил-1h-1,2,4-триазол-5-ил)-4-оксо-1,2,3,4-тетрагидрохинолин-5-карбоксилата и способы их получения |
| CN104557917A (zh) * | 2014-12-12 | 2015-04-29 | 重庆博腾制药科技股份有限公司 | 一种5-卤代氮杂环吲哚的制备方法 |
| JP6786761B2 (ja) * | 2015-05-26 | 2020-11-18 | ディーエスエム アイピー アセッツ ビー．ブイ．Ｄｓｍ Ｉｐ Ａｓｓｅｔｓ Ｂ．Ｖ． | Ｓｆｃによるキラル異性体の分離 |
| US9708319B1 (en) * | 2016-06-13 | 2017-07-18 | Yong Xu | Synthesis of PARP inhibitor talazoparib |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| CA3078806A1 (en) | 2017-10-13 | 2019-04-18 | Merck Patent Gmbh | Combination of a parp inhibitor and a pd-1 axis binding antagonist |
| TW201938165A (zh) | 2017-12-18 | 2019-10-01 | 美商輝瑞股份有限公司 | 治療癌症的方法及組合療法 |
| US20210355223A1 (en) | 2018-11-05 | 2021-11-18 | Pfizer Inc. | Combinations for Treating Cancer |
| EP4118105A2 (en) | 2020-03-09 | 2023-01-18 | Pfizer Inc. | Cd80-fc fusion protein and uses thereof |
| US20230414522A1 (en) | 2020-11-13 | 2023-12-28 | Pfizer Inc. | Talazoparib soft gelatin capsule dosage form |
| EP4256088A1 (en) | 2020-12-07 | 2023-10-11 | Pfizer Inc. | Methods of identifying a tumor that is sensitive to treatment with talazoparib and methods of treatment thereof |
| WO2022200982A1 (en) | 2021-03-24 | 2022-09-29 | Pfizer Inc. | Combination of talazoparib and an anti-androgen for the treatment of ddr gene mutated metastatic castration-sensitive prostate cancer |
| WO2023131894A1 (en) | 2022-01-08 | 2023-07-13 | Pfizer Inc. | Genomic loss of heterozygosity as a predictive biomarker for treatment with talazoparib and methods of treatment thereof |
| TWI883565B (zh) | 2022-10-02 | 2025-05-11 | 美商輝瑞大藥廠 | 用於治療轉移性去勢抵抗性前列腺癌之他拉唑帕尼及恩雜魯胺之組合 |
| TW202425976A (zh) | 2022-12-17 | 2024-07-01 | 美商輝瑞大藥廠 | 用於治療轉移性去勢抵抗性前列腺癌之他拉唑帕尼及恩雜魯胺之組合 |
| TW202600137A (zh) | 2024-04-04 | 2026-01-01 | 美商輝瑞股份有限公司 | 於使用ｐａｒｐ抑制劑的治療作為預測性生物標記之ｔｍｐｒｓｓ２－ｅｒｇ和ｒｂｉ及使用ｐａｒｐ抑制劑之治療方法 |
| WO2026078615A1 (en) | 2024-10-09 | 2026-04-16 | Pfizer Inc. | Combination of talazoparib and enzalutamide in the treatment of metastatic castration-resistant prostate cancer |
| WO2026078619A1 (en) | 2024-10-09 | 2026-04-16 | Pfizer Inc. | Combination of talazoparib and enzalutamide in the treatment of metastatic castration-resistant prostate cancer |
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| US4415504A (en) | 1981-09-21 | 1983-11-15 | Tanabe Seiyaku Co., Ltd. | p-Hydroxyphenylglycine.α-phenylethanesulfonate, process for production thereof and utilization thereof in resolution of p-hydroxyphenylglycine |
| JPS58225065A (ja) | 1982-06-21 | 1983-12-27 | Nippon Shinyaku Co Ltd | ２−キノロン誘導体 |
| US5328905A (en) | 1987-07-20 | 1994-07-12 | Duphar International Research B.V. | 8,9-anellated-1,2,3,4-tetrahydro-β-carboline derivatives |
| CZ283018B6 (cs) * | 1991-02-01 | 1997-12-17 | Merck Sharp And Dohme Limited | Deriváty imidazolu, triazolu a tetrazolu a farmaceutické přípravky na jejich bázi |
| GB9505538D0 (en) | 1995-03-18 | 1995-05-03 | Ciba Geigy Ag | New compounds |
| ID19155A (id) | 1996-12-13 | 1998-06-18 | Tanabe Seiyaku Co | Turunan-turunan piridin, pembuatannya dan intermediet untuk pembuatannya |
| DE19727410A1 (de) | 1997-06-27 | 1999-01-07 | Hoechst Schering Agrevo Gmbh | 3-(5-Tetrazolylcarbonyl)-2-chinolone und diese enthaltende nutzpflanzenschützende Mittel |
| US6514983B1 (en) | 1997-09-03 | 2003-02-04 | Guilford Pharmaceuticals Inc. | Compounds, methods and pharmaceutical compositions for treating neural or cardiovascular tissue damage |
| TW430656B (en) | 1997-12-03 | 2001-04-21 | Dainippon Ink & Chemicals | Quinolinone derivative, method for preparing the same, and anti-allergic agent |
| AU9298798A (en) | 1998-05-15 | 1999-12-06 | Guilford Pharmaceuticals Inc. | Fused tricyclic compounds which inhibit parp activity |
| DE19921567A1 (de) | 1999-05-11 | 2000-11-16 | Basf Ag | Verwendung von Phthalazine-Derivaten |
| JP2001302669A (ja) * | 2000-04-18 | 2001-10-31 | Meiji Seika Kaisha Ltd | 三環性フタラジノン誘導体 |
| JP2002284699A (ja) | 2001-03-28 | 2002-10-03 | Sumitomo Pharmaceut Co Ltd | 視細胞変性疾患治療剤 |
| AR036081A1 (es) | 2001-06-07 | 2004-08-11 | Smithkline Beecham Corp | Compuesto de 1,2-dihidroquinolina, su uso para preparar una composicion farmaceutica, metodos para prepararlo y compuestos del acido 2-aminobenzoico n-alquilado de utilidad como intermediarios en dichos metodos |
| SE0102315D0 (sv) | 2001-06-28 | 2001-06-28 | Astrazeneca Ab | Compounds |
| AU2003211381B9 (en) | 2002-02-19 | 2009-07-30 | Ono Pharmaceutical Co., Ltd. | Fused pyridazine derivative compounds and drugs containing the compounds as the active ingredient |
| EP1340819A1 (en) | 2002-02-28 | 2003-09-03 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Microsatellite markers |
| GB0221443D0 (en) | 2002-09-16 | 2002-10-23 | Glaxo Group Ltd | Pyridine derivates |
| EP1400244A1 (en) | 2002-09-17 | 2004-03-24 | Warner-Lambert Company LLC | New spirocondensed quinazolinones and their use as phosphodiesterase inhibitors |
| JPWO2004043959A1 (ja) * | 2002-11-12 | 2006-03-09 | 持田製薬株式会社 | 新規ｐａｒｐ阻害剤 |
| PL1633724T3 (pl) * | 2003-03-12 | 2011-10-31 | Kudos Pharm Ltd | Pochodne ftalazynonu |
| ES2396334T3 (es) | 2003-05-28 | 2013-02-20 | Eisai Inc. | Compuestos, métodos y composiciones farmacéuticas para la inhibición de PARP |
| US7269138B2 (en) * | 2003-06-04 | 2007-09-11 | Motorola, Inc. | Distributed MAC protocol facilitating collaborative ranging in communications networks |
| WO2005080356A1 (en) | 2004-02-18 | 2005-09-01 | Astrazeneca Ab | Tetrazole compounds and their use as metabotropic glutamate receptor antagonits |
| GB0612971D0 (en) | 2006-06-30 | 2006-08-09 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| US8198448B2 (en) | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| CA2684105C (en) | 2007-05-03 | 2011-09-06 | Pfizer Limited | Pyridine derivatives |
| WO2009024190A1 (en) | 2007-08-22 | 2009-02-26 | 4Sc Ag | Indolopyridines as inhibitors of the kinesin spindle protein (eg5 ) |
| ES2504690T3 (es) * | 2007-10-03 | 2014-10-08 | Eisai Inc. | Compuestos inhibidores de PARP, composiciones y métodos de uso |
| WO2009099736A2 (en) | 2008-02-06 | 2009-08-13 | Lead Therapeutics, Inc. | Benzoxazole carboxamide inhibitors of poly(adp-ribose)polymerase (parp) |
| CN104478875B (zh) | 2008-08-06 | 2017-04-12 | 麦迪韦逊科技有限公司 | 聚(adp‑核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂 |
| KR20110053424A (ko) | 2008-08-12 | 2011-05-23 | 베링거 인겔하임 인터내셔날 게엠베하 | 사이클로알킬-치환된 피페라진 화합물의 제조 방법 |
| EP2531033A4 (en) * | 2010-02-03 | 2013-07-31 | Biomarin Pharm Inc | POLY (ADP-RIBOSE) POLYMERASE (PARP) DIHYDROPYRIDOPHTHALAZINE HEMMER FOR USE IN THE TREATMENT OF PTEN-LACK ASSOCIATED DISEASES |
| US20110190266A1 (en) | 2010-02-04 | 2011-08-04 | Daniel Chu | 5,6,6a,7,8,9-HEXAHYDRO-2H-PYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) |
| KR101826652B1 (ko) | 2010-02-08 | 2018-02-07 | 메디베이션 테크놀로지즈, 인크. | 디히드로피리도프탈라지논 유도체의 합성 방법 |
| WO2011130661A1 (en) | 2010-04-16 | 2011-10-20 | Biomarin Pharmaceutical Inc. | Methods of using dihydropyridophthalazinone inhibitors of poly (adp-ribose)polymerase (parp) |
| WO2011140009A1 (en) | 2010-05-04 | 2011-11-10 | Biomarin Pharmaceutical Inc. | Methods of using semi-synthetic glycopeptides as antibacterial agents |
| KR20190120458A (ko) | 2010-10-21 | 2019-10-23 | 메디베이션 테크놀로지즈 엘엘씨 | 결정질의 (8s,9r)-5-플루오로-8-(4-플루오로페닐)-9-(1-메틸-1h-1,2,4-트리아졸-5-일)-8,9-디하이드로-2h-피리도[4,3,2-de]프탈라진-3(7h)-온 토실레이트 염 |
| WO2012166151A1 (en) | 2011-06-03 | 2012-12-06 | Biomarin Pharmaceutical Inc. | Use of dihydropyridophthalazinone inhibitors of poly (adp-ribose) polymerase (parp) in the treatment of myelodysplastic syndrome (mds) and acute myeloid leukaemia (aml) |
| WO2013028495A1 (en) | 2011-08-19 | 2013-02-28 | Biomarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly (adp-ribose) polymerase (parp) for the treatment of multiple myeloma |
| US20130053365A1 (en) | 2011-08-30 | 2013-02-28 | Biomarin Pharmaceutical, Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
| CN105916846A (zh) | 2013-11-07 | 2016-08-31 | 麦迪韦逊科技有限公司 | 用于合成经保护的n-烷基三唑甲醛的三唑中间体 |
| EA201790290A1 (ru) | 2014-07-31 | 2017-07-31 | Медивэйшн Текнолоджиз, Инк. | Формерные соли (2s,3s)-метил 7-фтор-2-(4-фторфенил)-3-(1-метил-1h-1,2,4-триазол-5-ил)-4-оксо-1,2,3,4-тетрагидрохинолин-5-карбоксилата и способы их получения |
-
2011
- 2011-02-08 KR KR1020127021601A patent/KR101826652B1/ko not_active Expired - Fee Related
- 2011-02-08 CA CA2788114A patent/CA2788114C/en active Active
- 2011-02-08 PL PL11740513T patent/PL2533640T3/pl unknown
- 2011-02-08 HU HUE11740513A patent/HUE030794T2/en unknown
- 2011-02-08 MX MX2012008903A patent/MX340319B/es active IP Right Grant
- 2011-02-08 RU RU2012138345/04A patent/RU2561732C2/ru active
- 2011-02-08 ES ES11740513.4T patent/ES2606174T3/es active Active
- 2011-02-08 SI SI201131061T patent/SI2533640T1/sl unknown
- 2011-02-08 JP JP2012552143A patent/JP5735988B2/ja active Active
- 2011-02-08 DK DK11740513.4T patent/DK2533640T3/en active
- 2011-02-08 PT PT117405134T patent/PT2533640T/pt unknown
- 2011-02-08 AU AU2011213584A patent/AU2011213584B2/en not_active Ceased
- 2011-02-08 WO PCT/US2011/023965 patent/WO2011097602A1/en not_active Ceased
- 2011-02-08 BR BR112012019648-0A patent/BR112012019648B1/pt not_active IP Right Cessation
- 2011-02-08 SG SG2012056123A patent/SG182784A1/en unknown
- 2011-02-08 US US13/023,140 patent/US8765945B2/en active Active
- 2011-02-08 CN CN201180017690.6A patent/CN102834008B/zh active Active
- 2011-02-08 EP EP11740513.4A patent/EP2533640B1/en active Active
-
2012
- 2012-07-23 ZA ZA2012/05538A patent/ZA201205538B/en unknown
- 2012-07-29 IL IL221170A patent/IL221170A/en active IP Right Grant
-
2014
- 2014-06-02 US US14/293,642 patent/US9926303B2/en active Active
-
2016
- 2016-12-28 CY CY20161101354T patent/CY1118575T1/el unknown
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