CN102834008B - 合成二氢吡啶并酞嗪酮衍生物的方法 - Google Patents
合成二氢吡啶并酞嗪酮衍生物的方法 Download PDFInfo
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- CN102834008B CN102834008B CN201180017690.6A CN201180017690A CN102834008B CN 102834008 B CN102834008 B CN 102834008B CN 201180017690 A CN201180017690 A CN 201180017690A CN 102834008 B CN102834008 B CN 102834008B
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- 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 4
- PVAIIDFKUPYMQA-UHFFFAOYSA-N C[n]1ncnc1C(C(c(cc1)ccc1F)Nc1c2c(C(OC)=O)cc(F)c1)C2=O Chemical compound C[n]1ncnc1C(C(c(cc1)ccc1F)Nc1c2c(C(OC)=O)cc(F)c1)C2=O PVAIIDFKUPYMQA-UHFFFAOYSA-N 0.000 description 1
- NIYWPALNWVTHPJ-UHFFFAOYSA-N C[n]1ncnc1CC(c(c(C(OC)=O)cc(F)c1)c1[N+]([O-])=O)=O Chemical compound C[n]1ncnc1CC(c(c(C(OC)=O)cc(F)c1)c1[N+]([O-])=O)=O NIYWPALNWVTHPJ-UHFFFAOYSA-N 0.000 description 1
- UOQXIWFBQSVDPP-UHFFFAOYSA-N O=Cc(cc1)ccc1F Chemical compound O=Cc(cc1)ccc1F UOQXIWFBQSVDPP-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/06—Peri-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
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 (2)
| Publication Number | Publication Date |
|---|---|
| CN102834008A CN102834008A (zh) | 2012-12-19 |
| CN102834008B true CN102834008B (zh) | 2014-04-23 |
Family
ID=44354222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180017690.6A Active CN102834008B (zh) | 2010-02-08 | 2011-02-08 | 合成二氢吡啶并酞嗪酮衍生物的方法 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US8765945B2 (enExample) |
| EP (1) | EP2533640B1 (enExample) |
| JP (1) | JP5735988B2 (enExample) |
| KR (1) | KR101826652B1 (enExample) |
| CN (1) | CN102834008B (enExample) |
| AU (1) | AU2011213584B2 (enExample) |
| BR (1) | BR112012019648B1 (enExample) |
| CA (1) | CA2788114C (enExample) |
| CY (1) | CY1118575T1 (enExample) |
| DK (1) | DK2533640T3 (enExample) |
| ES (1) | ES2606174T3 (enExample) |
| HU (1) | HUE030794T2 (enExample) |
| IL (1) | IL221170A (enExample) |
| MX (1) | MX340319B (enExample) |
| PL (1) | PL2533640T3 (enExample) |
| PT (1) | PT2533640T (enExample) |
| RU (1) | RU2561732C2 (enExample) |
| SG (1) | SG182784A1 (enExample) |
| SI (1) | SI2533640T1 (enExample) |
| WO (1) | WO2011097602A1 (enExample) |
| ZA (1) | ZA201205538B (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2326650B9 (en) | 2008-08-06 | 2014-09-10 | BioMarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
| CA2787844C (en) | 2010-02-03 | 2019-08-27 | Biomarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose) polymerase (parp) for use in treatment of diseases associated with a pten deficiency |
| PL2533640T3 (pl) | 2010-02-08 | 2017-06-30 | Medivation Technologies, Inc. | Sposób syntezy pochodnych dihydropirydoftalazynonu |
| EP2630146B1 (en) | 2010-10-21 | 2020-07-01 | Medivation Technologies LLC | Crystaline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phtalazin-3(7h)-one tosylate salt |
| EP3038600B1 (en) | 2013-08-27 | 2020-06-03 | 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 |
| JP2017523243A (ja) * | 2014-07-31 | 2017-08-17 | メディヴェイション テクノロジーズ， インコーポレーテッド | （２ｓ，３ｓ）−メチル ７−フルオロ−２−（４−フルオロフェニル）−３−（１−メチル−１ｈ−１，２，４−トリアゾール−５−イル）−４−オキソ−１，２，３，４−テトラヒドロキノリン−５−カルボキシレートの共形成剤塩、およびそれらを製造する方法 |
| 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 |
| BR112020006371A2 (pt) | 2017-10-13 | 2020-09-29 | Merck Patent Gmbh | combinação de um inibidor de parp e um antagonista de ligação de eixo de pd-1 |
| 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 |
| WO2021181233A2 (en) | 2020-03-09 | 2021-09-16 | Pfizer Inc. | Fusion proteins and uses thereof |
| CA3201467A1 (en) | 2020-11-13 | 2022-05-19 | 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 |
| US20240180906A1 (en) | 2021-03-24 | 2024-06-06 | 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 |
| WO2025210510A1 (en) | 2024-04-04 | 2025-10-09 | Pfizer Inc. | Tmprss2-erg and rb1 as predictive biomarkers for treatment with a parp inhibitor |
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| WO2004080976A1 (en) * | 2003-03-12 | 2004-09-23 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
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| 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) |
| PL2533640T3 (pl) | 2010-02-08 | 2017-06-30 | Medivation Technologies, Inc. | Sposób syntezy pochodnych dihydropirydoftalazynonu |
| WO2011130661A1 (en) | 2010-04-16 | 2011-10-20 | Biomarin Pharmaceutical Inc. | Methods of using dihydropyridophthalazinone inhibitors of poly (adp-ribose)polymerase (parp) |
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| EP2630146B1 (en) * | 2010-10-21 | 2020-07-01 | Medivation Technologies LLC | Crystaline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phtalazin-3(7h)-one tosylate salt |
| 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 |
| JP2017523243A (ja) | 2014-07-31 | 2017-08-17 | メディヴェイション テクノロジーズ， インコーポレーテッド | （２ｓ，３ｓ）−メチル ７−フルオロ−２−（４−フルオロフェニル）−３−（１−メチル−１ｈ−１，２，４−トリアゾール−５−イル）−４−オキソ−１，２，３，４−テトラヒドロキノリン−５−カルボキシレートの共形成剤塩、およびそれらを製造する方法 |
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2011
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004080976A1 (en) * | 2003-03-12 | 2004-09-23 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
Non-Patent Citations (1)
| Title |
|---|
| 《Crystal structure of the catalytic domain of human PARP2 in complex with PARP inhibitor ABT-888》;karlberg;《BIOCHEMISTRY》;20100121;1056-1058 * |
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