DK2533640T3 - Fremgangsmåder til syntese af dihydropyridophthalazinonderivater - Google Patents
Fremgangsmåder til syntese af dihydropyridophthalazinonderivater Download PDFInfo
- Publication number
- DK2533640T3 DK2533640T3 DK11740513.4T DK11740513T DK2533640T3 DK 2533640 T3 DK2533640 T3 DK 2533640T3 DK 11740513 T DK11740513 T DK 11740513T DK 2533640 T3 DK2533640 T3 DK 2533640T3
- Authority
- DK
- Denmark
- Prior art keywords
- compound
- formula
- salt
- acid
- optionally
- Prior art date
Links
Classifications
-
- 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
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)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (23)
1. Fremgangsmåde til fremstilling af en forbindelse med formlen (1):
eller et salt deraf, hvilken fremgangsmåde omfatter: omsætning af en forbindelse med formlen (5),
eller et salt deraf, med hydrazinmonohydrat; hvor R er Cj-Ce-alkyl, hvor forbindelsen med formlen (5), eller salt deraf, fremstilles ved omsætning af en forbindelse med formlen (4):
eller et salt deraf, med 4-fluorbenzaldehyd i nærvær af et reduktionsreagens og en syre eller en Lewis-syre; hvor R er Ci-Ce alkyl.
2. Fremgangsmåde ifølge krav 1, hvor reduktionsmidlet er a) et metalhalogenid, eventuelt hvor metalhalogenidet er T1CI3 eller SnCh: eller b) pulverform!gt Fe; eller c) hydrogen i nærvær af en metalkatalysator, eventuelt hvor metalkatalysatoren er udvalgt fra gruppen bestående af palladium, nikkel, og platin; eller d) MCNBH3, hvor M er udvalgt fra gruppen bestående af Li, Na, K og BtuN.
3. Fremgangsmåde ifølge krav 1, hvor syren er en uorganisk syre udvalgt fra gruppen bestående af HCi, HBr, HI, H2SO4 og H3PQ4.
4. Fremgangsmåde ifølge krav 1, a), hvor syren er en organisk syre udvalgt fra gruppen bestående af myresyre, eddikesyre, propionsyre, smørsyre, trifmoreddikesyre, p-toluensulfonsyre og methylsulfonsyre; eller b) hvor Lewis-syren er udvalgt fra gruppen bestående af AlCb, TiCH, SnCLt og ZnCb.
5. Fremgangsmåde ifølge krav 1, hvor forbindelsen med formlen (4), eller salt deraf, fremstilles ved behandling af en forbindelse med formlen (3):
eller et salt deraf, med R-OH i nærvær af en syre; hvor R er udvalgt fra gruppen bestående af methyl, ethyl, propyl, isopropyl, butyl, og isobutyl; og syren er udvalgt fra gruppen bestående af HCI, eddikesyre, p-toluensulfonsyre og trifluoreddikesyre.
6. Fremgangsmåde ifølge krav 5, hvor forbindelsen med formlen (3), eller salt deraf, fremstilles ved omsætning af en forbindelse med formlen (2):
med l-methyl-li/-l,2,4-triazol-5-carbaldehyd under en kondenseringstilstand.
7. Fremgangsmåde ifølge krav 6, hvor kondenseringstilstand en omfatter anvendelse af en base i nærvær af en vand-scavenger ved en temperatur på ca, 80 til ca. 90 °C; eventuelt hvor basen er triethylamin og vand-scavengeren er eddikesyreanhydrid.
8. Fremgangsmåde til fremstilling af en forbindelse med formlen (1):
eller et salt deraf, hvilken fremgangsmåde omfatter: omsætning af en forbindelse med formlen (8):
eller et salt deraf, med. en base.
9. Fremgangsmåde ifølge krav 8, hvor basen er et metalcarbonat eller et metalhydrid a) eventuelt hvor metalcarbonatet er udvalgt fra gruppen bestående af Na2C03, Kog Cs ’C '0·: eller b) eventuelt hvor metalhydridet er NaH eller KH.
10. Fremgangsmåde ifølge krav 8, hvor forbindelsen (8), eller salt deraf, fremstilles ved omsætning af en forbindelse med formlen (7):
eller et salt deraf, med 4-fluorbenzaldehyd.
11. Fremgangsmåde ifølge krav 10, hvor forbindelsen med formlen (7), eller salt deraf, fremstilles ved omsætning af en forbindelse med formlen (3):
eller et salt deraf, med hydrazinmonohydrat i nærvær af en syre; eventuelt hvor syren er udvalgt fra gruppen bestående af eddikesyre, trifluoreddikesyre, HC1 og p-toluensudfonsym.
12. Fremgangsmåde til fremstil ling af en forbindelse med forml en (1):
eller et salt deraf, hvilken fremgangsmåde omfatter: omsætning af en forbindelse med formlen (5),
eller et salt deraf, med hydrazinmonohydrat; hvor R er Ci-Ce-alkyl; hvor forbindelsen med formlen (5), eller salt deraf, fremstilles ved omsætning af en forbindelse med formlen (9):
eller et salt deraf, med et reduktionsreagens i et inert opløsningsmiddel ved en temperatur på ca, 0 til ca. 140 °C i ca. 1 til ca. 48 timer; hvor R er Ci-Cé-alkyl.
13. Fremgangsmåde ifølge krav 12, hvor reduktiønsmidlet er a) et metalborhydrid, eventuelt hvor metalborhydridet er NaBFU eller NaCJNBH?,; eller b) pulverformigt Fe; eller c) TiCb eller Sni 1-·; eller d) hydrogen i nærvær af et overgangsmetal, eventuelt hvor overgangsmetallet er udvalgt fra gruppen bestående af palladium, nikkel, og platin.
14. Fremgangsmåde til fremstilling af en forbindelse med formlen (1):
eller et salt deraf, hvilken fremgangsmåde omfatter: omsætning af en forbindelse med formlen (5),
eller et salt deraf, med hydrazinmonohydrat; hvor R er Ci-Cé-alkyl; hvor forbindelsen med formlen (5), eller salt deraf, fremstilles ved omsætning af en forbindelse med formlen (10):
eller et salt deraf, med et reduktionsreagens; hvor R er Ci-Cé-alkyl.
15. Fremgangsmåde ifølge krav 14, hvor reduktiønsmidlet er a) pulverformigt Fe; eller b) et metalborhydrid, eventuelt metalborhydridet er NaBH4; eller c) hydrogen i nærvær af et overgangsmetal, eventuelt hvor overgangsmetallet er udvalgt fra gruppen bestående af palladium, nikkel og platin.
16. Fremgangsmåde ifølge krav 14, hvor forbindelsen med formlen (10), eller salt deraf, fremstilles ved omsætning afen forbindelse med formlen (9):
eller et salt deraf, med et reduktionsreagens; hvor R er Ci-Cé-alkyl.
17. Fremgangsmåde ifølge krav 16, hvor reduktionsmidlet er hydrogen under atmosfærisk tryk ved omgivende temperatur.
18. Fremgangsmåde til fremstilling af en forbindelse med formlen (la) eller (lb):
eller et salt deraf, omfattende chiral kromatografiopløsning af en forbindelse med formlen (1):
hvor den chirale opløsning opnås med en SFC-, Supercritical Fluid Chromatography, enhed; og endvidere omfatter anvendelse af en chiral stationær fase, hvor den chirale stationære fase er en CHIRALPAK® søjle, hvor CHIRALPAK^’ søjlen er udvalgt fra gruppen bestående af AD-, OJ-, og OD-søjler; og hvilken fremgangsmåde eventuelt endvidere omfatter anvendelse af en mobil fase, hvor den mobile fase omfatter CO2 og en alkohol, hvor alkoholen er MeOFT eller EtOH.
19. Fremgangsmåde til fremstilling af en forbindelse med formlen (la) eller (Ib):
eller et salt deraf, omfattende omsætning af en forbindelse med formlen (6a) eller (6b):
eller et salt deraf, med hydrazinmonohydrat i en alkohol; hvor R er Ci-Cé-alkyl.
20. Fremgangsmåde ifølge krav 19, hvor forbindelsen med formlen (6a) eller (6b) fremstilles ved udførelse af chiral kromatografi opløsning af en forbindelse med formlen (5):
21. Fremgangsmåde ifølge krav 19, hvor den ehirale opløsning opnås med en SFC-, Supercritical Fluid Chromatography, enhed, a) hvilken fremgangsmåde eventuelt endvidere omfatter anvendelse af en chiral stationær fase, hvor den ehirale stationære fase er en CHIRALPAK® søjle, eventuelt hvor CHIRALPAK® søjlen er en IC-eller AY-søjle; eller b) hvilken fremgangsmåde eventuelt endvidere omfatter anvendelse af en mobil fase, hvor den mobile fase omfatter CO;? og MeOH.
22. Fremgangsmåde ifølge krav 19, hvor den ehirale opløsning opnås med en SMB-, Simulated Moving Bed, kromatografienhed, a) hvilken fremgangsmåde eventuelt endvidere omfatter anvendelse af en chiral stationær fase, hvor den ehirale stationære fase er en CHIRALPAK® søjle, eventuelt hvor CHIRALPAK®søjlen er en IC-søjle; eller b) hvilken fremgangsmåde eventuelt endvidere omfatter anvendelse af en mobil fase, hvor den mobile fase er acetonitril.
23. Forbindelse udvalgt fra gruppen bestående af:
hvor R er Ci-Ce-alkyl.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30245710P | 2010-02-08 | 2010-02-08 | |
PCT/US2011/023965 WO2011097602A1 (en) | 2010-02-08 | 2011-02-08 | Processes of synthesizing dihydropyridophthalazinone derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2533640T3 true DK2533640T3 (da) | 2017-01-23 |
Family
ID=44354222
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK11740513.4T DK2533640T3 (da) | 2010-02-08 | 2011-02-08 | Fremgangsmåder til syntese af dihydropyridophthalazinonderivater |
Country Status (21)
Country | Link |
---|---|
US (2) | US8765945B2 (da) |
EP (1) | EP2533640B1 (da) |
JP (1) | JP5735988B2 (da) |
KR (1) | KR101826652B1 (da) |
CN (1) | CN102834008B (da) |
AU (1) | AU2011213584B2 (da) |
BR (1) | BR112012019648B1 (da) |
CA (1) | CA2788114C (da) |
CY (1) | CY1118575T1 (da) |
DK (1) | DK2533640T3 (da) |
ES (1) | ES2606174T3 (da) |
HU (1) | HUE030794T2 (da) |
IL (1) | IL221170A (da) |
MX (1) | MX340319B (da) |
PL (1) | PL2533640T3 (da) |
PT (1) | PT2533640T (da) |
RU (1) | RU2561732C2 (da) |
SG (1) | SG182784A1 (da) |
SI (1) | SI2533640T1 (da) |
WO (1) | WO2011097602A1 (da) |
ZA (1) | ZA201205538B (da) |
Families Citing this family (21)
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) |
AU2011212928B2 (en) | 2010-02-03 | 2016-06-23 | Medivation Technologies Llc | Dihydropyridophthalazinone inhibitors of poly(ADP-ribose) polymerase (PARP) for use in treatment of diseases associated with a PTEN deficiency |
WO2011097602A1 (en) | 2010-02-08 | 2011-08-11 | Biomarin Pharmaceutical Inc. | Processes of synthesizing dihydropyridophthalazinone derivatives |
SG189939A1 (en) | 2010-10-21 | 2013-06-28 | Biomarin Pharm Inc | Crystalline (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]phthalazin-3(7h)-one tosylate salt |
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 |
WO2015069851A1 (en) | 2013-11-07 | 2015-05-14 | Biomarin Pharmaceutical Inc. | Triazole intermediates useful in the synthesis of protected n-alkyltriazolecarbaldehydes |
EP3174855B1 (en) * | 2014-07-31 | 2023-05-10 | Medivation Technologies LLC | Coformer salts of (2s,3s)-methyl 7-fluoro-2-(4-fluorophenyl)-3-(1-methyl-1h-1,2,4-triazol-5-yl)-4-oxo-1,2,3,4-tetrahydroquinoline-5-carboxylate and methods of preparing them |
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 |
EP3876940A1 (en) | 2018-11-05 | 2021-09-15 | Pfizer Inc. | Combinations for treating cancer |
EP4118105A2 (en) | 2020-03-09 | 2023-01-18 | Pfizer Inc. | Cd80-fc fusion protein and uses thereof |
EP4243785A1 (en) | 2020-11-13 | 2023-09-20 | Pfizer Inc. | Talazoparib soft gelatin capsule dosage form |
WO2022123427A1 (en) | 2020-12-07 | 2022-06-16 | Pfizer Inc. | Methods of identifying a tumor that is sensitive to treatment with talazoparib and methods of treatment thereof |
JP2024510666A (ja) | 2021-03-24 | 2024-03-08 | ファイザー・インク | Ddr遺伝子変異転移性去勢感受性前立腺がんを処置するためのタラゾパリブおよび抗アンドロゲンの組合せ |
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 |
WO2024074959A1 (en) | 2022-10-02 | 2024-04-11 | Pfizer Inc. | Combination of talazoparib and enzalutamide in the treatment of metastatic castration-resistant prostate cancer |
WO2024127140A1 (en) | 2022-12-17 | 2024-06-20 | Pfizer Inc. | Combination of talazoparib and enzalutamide in the treatment of metastatic castration-resistant prostate cancer |
Family Cites Families (43)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
WO1999059975A1 (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 |
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 |
DE60336890D1 (de) * | 2002-02-19 | 2011-06-09 | Ono Pharmaceutical Co | Kondensierte pyridazinderivat-verbindungen und die verbindungen als wirkstoff enthaltende arzneimittel |
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 |
CA2505876A1 (en) | 2002-11-12 | 2004-05-27 | Mochida Pharmaceutical Co., Ltd. | Novel parp inhibitors |
GB2415430B (en) | 2003-03-12 | 2006-07-12 | Kudos Pharm Ltd | Phthalazinone derivatives |
CA2527420C (en) | 2003-05-28 | 2013-01-08 | Guilford Pharmaceuticals, Inc. | Compounds, methods and pharmaceutical compositions for inhibiting parp |
US7269138B2 (en) * | 2003-06-04 | 2007-09-11 | Motorola, Inc. | Distributed MAC protocol facilitating collaborative ranging in communications networks |
TW200533664A (en) | 2004-02-18 | 2005-10-16 | Astrazeneca Ab | Tetrazole compounds and their use as metabotropic glutamate receptor antagonists |
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 |
MX2009011816A (es) | 2007-05-03 | 2009-11-19 | Pfizer Ltd | Derivados de piridina. |
JP2010536807A (ja) | 2007-08-22 | 2010-12-02 | 4エスツェー アクチェンゲゼルシャフト | キネシンスピンドルタンパク質(eg5)の阻害剤としてのインドロピリジン |
KR101596526B1 (ko) * | 2007-10-03 | 2016-02-22 | 에이자이 아이엔씨. | Parp 억제제 화합물, 조성물 및 사용 방법 |
CN101998959B (zh) | 2008-02-06 | 2013-08-28 | 生物马林药物股份有限公司 | 聚(adp-核糖)聚合酶(parp)的苯并噁唑甲酰胺抑制剂 |
US8012976B2 (en) | 2008-08-06 | 2011-09-06 | Biomarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP) |
BRPI0914556A2 (pt) | 2008-08-12 | 2015-08-04 | Boehringer Ingelheim Int | Processo para a preparação de compostos de piperazina substituídos por cicloalquila |
AU2011212928B2 (en) * | 2010-02-03 | 2016-06-23 | Medivation Technologies Llc | Dihydropyridophthalazinone inhibitors of poly(ADP-ribose) polymerase (PARP) for use in treatment of diseases associated with a PTEN deficiency |
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) |
WO2011097602A1 (en) | 2010-02-08 | 2011-08-11 | Biomarin Pharmaceutical Inc. | Processes of synthesizing dihydropyridophthalazinone derivatives |
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 |
SG189939A1 (en) | 2010-10-21 | 2013-06-28 | Biomarin Pharm Inc | Crystalline (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]phthalazin-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) |
WO2015069851A1 (en) | 2013-11-07 | 2015-05-14 | Biomarin Pharmaceutical Inc. | Triazole intermediates useful in the synthesis of protected n-alkyltriazolecarbaldehydes |
EP3174855B1 (en) | 2014-07-31 | 2023-05-10 | Medivation Technologies LLC | Coformer salts of (2s,3s)-methyl 7-fluoro-2-(4-fluorophenyl)-3-(1-methyl-1h-1,2,4-triazol-5-yl)-4-oxo-1,2,3,4-tetrahydroquinoline-5-carboxylate and methods of preparing them |
-
2011
- 2011-02-08 WO PCT/US2011/023965 patent/WO2011097602A1/en active Application Filing
- 2011-02-08 MX MX2012008903A patent/MX340319B/es active IP Right Grant
- 2011-02-08 PT PT117405134T patent/PT2533640T/pt unknown
- 2011-02-08 CN CN201180017690.6A patent/CN102834008B/zh active Active
- 2011-02-08 DK DK11740513.4T patent/DK2533640T3/da active
- 2011-02-08 SI SI201131061T patent/SI2533640T1/sl unknown
- 2011-02-08 PL PL11740513T patent/PL2533640T3/pl unknown
- 2011-02-08 AU AU2011213584A patent/AU2011213584B2/en active Active
- 2011-02-08 RU RU2012138345/04A patent/RU2561732C2/ru active
- 2011-02-08 SG SG2012056123A patent/SG182784A1/en unknown
- 2011-02-08 HU HUE11740513A patent/HUE030794T2/en unknown
- 2011-02-08 EP EP11740513.4A patent/EP2533640B1/en active Active
- 2011-02-08 KR KR1020127021601A patent/KR101826652B1/ko active IP Right Grant
- 2011-02-08 CA CA2788114A patent/CA2788114C/en active Active
- 2011-02-08 US US13/023,140 patent/US8765945B2/en active Active
- 2011-02-08 JP JP2012552143A patent/JP5735988B2/ja active Active
- 2011-02-08 BR BR112012019648-0A patent/BR112012019648B1/pt active IP Right Grant
- 2011-02-08 ES ES11740513.4T patent/ES2606174T3/es 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
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
DK2533640T3 (da) | Fremgangsmåder til syntese af dihydropyridophthalazinonderivater | |
US20120041205A1 (en) | Preparation of dihydropyrrol derivatives as intermediates | |
CN107915720B (zh) | 沃诺拉赞的新制备方法 | |
CN107200741B (zh) | 一种间变性淋巴瘤激酶抑制剂的制备方法 | |
JP7347852B2 (ja) | 重水素化大環状化合物の調製方法 | |
JP2021517573A (ja) | 二つの4−{[(2s)−2−{4−[5−クロロ−2−(1h−1,2,3−トリアゾール−1−イル)フェニル]−5−メトキシ−2−オキソピリジン−1(2h)−イル}ブタノイル]アミノ}−2−フルオロベンズアミド誘導体の調製方法 | |
JP5518088B2 (ja) | 四置換ピリダジンヘッジホッグ経路アンタゴニスト | |
EP2687518B1 (en) | Nitrogen-containing saturated heterocyclic compound | |
WO2010004198A2 (fr) | Derives anticancereux, leur preparation et leur application en therapeutique | |
JP2020518573A (ja) | 2−([1,2,3]トリアゾール−2−イル)−安息香酸誘導体の製造 | |
EP3794001B1 (en) | Intermediates and processes for the preparation of linagliptin and its salts | |
EP3741744B1 (en) | A pharmaceutical intermediate for preparing pimavanserin | |
WO2020171073A1 (ja) | ベンゾアゼピン誘導体の製造方法及びその中間体 | |
US20090270417A1 (en) | Organic Compounds | |
KR101116754B1 (ko) | 히스톤 디아세틸라제 저해활성을 갖는 6-아미노-ν-하이드록시헥산아마이드 화합물 및 이의 제조방법 | |
CN116367832A (zh) | 取代的杂芳基化合物及其用途 |