CA2788114C - Processes of synthesizing dihydropyridophthalazinone derivatives - Google Patents
Processes of synthesizing dihydropyridophthalazinone derivatives Download PDFInfo
- Publication number
- CA2788114C CA2788114C CA2788114A CA2788114A CA2788114C CA 2788114 C CA2788114 C CA 2788114C CA 2788114 A CA2788114 A CA 2788114A CA 2788114 A CA2788114 A CA 2788114A CA 2788114 C CA2788114 C CA 2788114C
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- Prior art keywords
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- salt
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Classifications
-
- 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
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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 |
|---|---|
| CA2788114A1 CA2788114A1 (en) | 2011-08-11 |
| CA2788114C true CA2788114C (en) | 2018-11-06 |
Family
ID=44354222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2788114A Active CA2788114C (en) | 2010-02-08 | 2011-02-08 | Processes of synthesizing dihydropyridophthalazinone derivatives |
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 (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8012976B2 (en) | 2008-08-06 | 2011-09-06 | Biomarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP) |
| US8541403B2 (en) | 2010-02-03 | 2013-09-24 | Biomarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP) for use in treatment of diseases associated with a PTEN deficiency |
| DK2533640T3 (en) | 2010-02-08 | 2017-01-23 | Medivation Technologies Inc | METHODS OF SYNTHESIS OF DIHYDROPYRIDOPHTHALAZINE DERIVATIVES |
| PL2630146T3 (pl) | 2010-10-21 | 2020-11-02 | Medivation Technologies Llc | Krystaliczna sól tosylanowa (8S,9R)-5-fluoro-8-(4-fluorofenylo)-9-(1-metylo-1H-1,2,4-triazol-5-ilo)-8,9-dihydro-2H-pirydo[4,3,2-de]ftalazyno-3(7H)-onu |
| JP2016529284A (ja) | 2013-08-27 | 2016-09-23 | ノースイースタン ユニバーシティ | ナノ粒子薬物デリバリシステムおよび、癌および神経外傷の治療方法 |
| EP3066084A1 (en) * | 2013-11-07 | 2016-09-14 | Medivation Technologies, Inc. | Triazole intermediates useful in the synthesis of protected n-alkyltriazolecarbaldehydes |
| 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 |
| EP3694551A1 (en) | 2017-10-13 | 2020-08-19 | 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 |
| JP2023517044A (ja) | 2020-03-09 | 2023-04-21 | ファイザー・インク | 融合タンパク質およびその使用 |
| EP4243785B1 (en) | 2020-11-13 | 2026-04-08 | 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 |
| KR20230159510A (ko) | 2021-03-24 | 2023-11-21 | 화이자 인코포레이티드 | Ddr 유전자 돌연변이된 전이성 거세-감수성 전립선암의 치료를 위한 탈라조파립과 항안드로겐의 조합 |
| 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 |
| 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 |
| SK278998B6 (sk) * | 1991-02-01 | 1998-05-06 | Merck Sharp & Dohme Limited | Deriváty imidazolu, triazolu a tetrazolu, spôsob i |
| 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 |
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| CA2332239A1 (en) | 1998-05-15 | 1999-11-25 | Guilford Pharmaceuticals Inc. | Fused tricyclic compounds which inhibit parp activity |
| DE19921567A1 (de) | 1999-05-11 | 2000-11-16 | Basf Ag | Verwendung von Phthalazine-Derivaten |
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| JP2002284699A (ja) | 2001-03-28 | 2002-10-03 | Sumitomo Pharmaceut Co Ltd | 視細胞変性疾患治療剤 |
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| SE0102315D0 (sv) | 2001-06-28 | 2001-06-28 | Astrazeneca Ab | Compounds |
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| 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 |
| AU2004220321B2 (en) | 2003-03-12 | 2010-02-25 | Kudos Pharmaceuticals Ltd | Phthalazinone derivatives |
| WO2004105700A2 (en) | 2003-05-28 | 2004-12-09 | Guildford Pharmaceuticals, Inc. | Compounds, methods and pharmaceutical compositions for inhibiting parp |
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| GB0612971D0 (en) | 2006-06-30 | 2006-08-09 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
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| BRPI0721950A2 (pt) | 2007-08-22 | 2015-09-29 | 4Sc Ag | indolopiridinas como inibidores da proteína de fuso de cinesina |
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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) |
| DK2533640T3 (en) | 2010-02-08 | 2017-01-23 | Medivation Technologies Inc | METHODS OF SYNTHESIS OF DIHYDROPYRIDOPHTHALAZINE DERIVATIVES |
| 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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| PL2630146T3 (pl) | 2010-10-21 | 2020-11-02 | Medivation Technologies Llc | Krystaliczna sól tosylanowa (8S,9R)-5-fluoro-8-(4-fluorofenylo)-9-(1-metylo-1H-1,2,4-triazol-5-ilo)-8,9-dihydro-2H-pirydo[4,3,2-de]ftalazyno-3(7H)-onu |
| 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) |
| EP3066084A1 (en) | 2013-11-07 | 2016-09-14 | Medivation Technologies, Inc. | Triazole intermediates useful in the synthesis of protected n-alkyltriazolecarbaldehydes |
| 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 DK DK11740513.4T patent/DK2533640T3/en active
- 2011-02-08 RU RU2012138345/04A patent/RU2561732C2/ru active
- 2011-02-08 CN CN201180017690.6A patent/CN102834008B/zh active Active
- 2011-02-08 BR BR112012019648-0A patent/BR112012019648B1/pt not_active IP Right Cessation
- 2011-02-08 SG SG2012056123A patent/SG182784A1/en unknown
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