MX338150B - Imidazolonilquinolinas [4, 5-c] como inhibidores de proteina cinasa dependiente de adn (adn-pk). - Google Patents
Imidazolonilquinolinas [4, 5-c] como inhibidores de proteina cinasa dependiente de adn (adn-pk).Info
- Publication number
- MX338150B MX338150B MX2013002259A MX2013002259A MX338150B MX 338150 B MX338150 B MX 338150B MX 2013002259 A MX2013002259 A MX 2013002259A MX 2013002259 A MX2013002259 A MX 2013002259A MX 338150 B MX338150 B MX 338150B
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- formula
- quinolines
- imidazo
- inhibitors
- Prior art date
Links
Classifications
-
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/46—Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/11—Protein-serine/threonine kinases (2.7.11)
- C12Y207/11001—Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Zoology (AREA)
- General Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invención se refiere a compuestos de las fórmulas (I) y (II) (Ver Formulas) en donde R1, R2, R3, R4, R5, R8, X y m presentan el significado en las reivindicaciones, y/o sus sales, tautómeros y estereoisómeros fisiológicamente inocuos, incluyendo sus mezclas en todas las proporciones. Los compuestos de la fórmula (I) se pueden usar para la inhibición de las serina-treonina-prote ína cinasas, así como para la sensibilización de células cancerosas a los agentes anticáncer y/o radiación ionizante. También es objeto de la invención el uso de los compuestos de la fórmula (I) en la prevención, la terapia o el control del curso de cáncer, tumores, metástasis o trastornos de la angiogénesis, en combinación con radioterapia y/o un agente anticáncer. La invención también se refiere a un proceso para la preparación de los compuestos de la fórmula (I) por reacción de los compuestos de las fórmulas (II) eventualmente conversión de una base o un ácido de los compuestos de la fórmula (I) en una de sus sales.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102010035744A DE102010035744A1 (de) | 2010-08-28 | 2010-08-28 | Imidazolonylchinoline |
PCT/EP2011/003744 WO2012028233A1 (de) | 2010-08-28 | 2011-07-26 | Imidazo [4,5-c]chinoline als dna-pk-inhibitoren |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2013002259A MX2013002259A (es) | 2013-05-09 |
MX338150B true MX338150B (es) | 2016-04-05 |
Family
ID=44509164
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2013002259A MX338150B (es) | 2010-08-28 | 2011-07-26 | Imidazolonilquinolinas [4, 5-c] como inhibidores de proteina cinasa dependiente de adn (adn-pk). |
Country Status (25)
Country | Link |
---|---|
US (3) | US9000153B2 (es) |
EP (1) | EP2609082B1 (es) |
JP (1) | JP5882329B2 (es) |
KR (1) | KR101912475B1 (es) |
CN (1) | CN103068803B (es) |
AR (1) | AR082728A1 (es) |
AU (1) | AU2011298013B9 (es) |
BR (1) | BR112013004613B1 (es) |
CA (1) | CA2809553C (es) |
CY (1) | CY1116281T1 (es) |
DE (1) | DE102010035744A1 (es) |
DK (1) | DK2609082T3 (es) |
EA (1) | EA022095B1 (es) |
ES (1) | ES2536313T3 (es) |
HK (1) | HK1184154A1 (es) |
HR (1) | HRP20150489T1 (es) |
HU (1) | HUE025692T2 (es) |
IL (1) | IL224903A (es) |
MX (1) | MX338150B (es) |
PL (1) | PL2609082T3 (es) |
PT (1) | PT2609082E (es) |
RS (1) | RS54038B1 (es) |
SG (1) | SG187954A1 (es) |
SI (1) | SI2609082T1 (es) |
WO (1) | WO2012028233A1 (es) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RS61664B1 (sr) | 2012-04-24 | 2021-04-29 | Vertex Pharma | Inhibitori dna-pk |
HUE041544T2 (hu) * | 2013-03-12 | 2019-05-28 | Vertex Pharma | DNS-PK inhibitorok |
PT3424920T (pt) | 2013-10-17 | 2020-07-07 | Vertex Pharma | Co-cristais de (s)-n-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolina-4-carboxamida e derivados deuterados dos mesmos como inibidores de adn-pk |
NO2714752T3 (es) | 2014-05-08 | 2018-04-21 | ||
RU2743343C2 (ru) * | 2015-04-02 | 2021-02-17 | Мерк Патент Гмбх | Имидазолонилхинолины и их применение в качестве ингибиторов киназы атм |
GB201516504D0 (en) | 2015-09-17 | 2015-11-04 | Astrazeneca Ab | Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer |
CA3038657A1 (en) | 2016-09-27 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors |
US20200101080A1 (en) * | 2017-03-31 | 2020-04-02 | Bioventures, Llc | Inhibitors of dna pk and uses thereof |
IL272352B2 (en) * | 2017-08-11 | 2023-10-01 | Merck Patent Gmbh | A pharmaceutical preparation containing 3-fluoro-4-[7-methoxy-3-methyl-8-(1-methyl-1 H-pyrazol-4-yl)-2-oxo-2,3-dihydro-imidazo[5,4 -C]quinolin-1-yl]-benzonitrile |
WO2019177971A1 (en) * | 2018-03-12 | 2019-09-19 | Mavupharma, Inc. | Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitors and uses thereof |
RU2020133020A (ru) * | 2018-03-14 | 2022-04-14 | Мерк Патент Гмбх | Соединения и их применения для лечения опухолей у субъекта |
TWI820146B (zh) | 2018-06-15 | 2023-11-01 | 瑞典商阿斯特捷利康公司 | 嘌呤酮化合物及其在治療癌症中之用途 |
CN111909144A (zh) * | 2019-05-10 | 2020-11-10 | 山东轩竹医药科技有限公司 | 喹唑啉类dna-pk抑制剂 |
HRP20231548T1 (hr) | 2019-07-10 | 2024-03-15 | Merck Patent Gmbh | Farmaceutski pripravak |
US20230014730A1 (en) | 2019-09-23 | 2023-01-19 | Nanjing Zhengxiang Pharmaceuticals Co., Ltd. | Phosphodiesterase inhibitors and use |
CN114615995A (zh) | 2019-11-01 | 2022-06-10 | 阿雷斯贸易股份有限公司 | PD-1、TGFβ和ATM联合抑制与放疗联合用于癌症治疗 |
CN115916203A (zh) | 2020-06-18 | 2023-04-04 | 默克专利股份公司 | 用于治疗病毒感染的化合物 |
EP4171651A1 (en) | 2020-06-24 | 2023-05-03 | AstraZeneca UK Limited | Combination of antibody-drug conjugate and atm inhibitor |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SK400992A3 (en) | 1990-11-06 | 1995-08-09 | Pfizer | Quinazolines derivatives for enhancing antitumor activity |
EP1187633A4 (en) | 1999-04-08 | 2005-05-11 | Arch Dev Corp | USE OF ANTI-VEGF ANTIBODY FOR INCREASING IRRADIATION IN CANCER THERAPY |
GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
EP1590348A1 (en) * | 2002-12-20 | 2005-11-02 | 3M Innovative Properties Company | Aryl / hetaryl substituted imidazoquinolines |
CA2536136C (en) * | 2003-08-27 | 2012-10-30 | 3M Innovative Properties Company | Aryloxy and arylalkyleneoxy substituted imidazoquinolines |
SG149828A1 (en) * | 2003-10-03 | 2009-02-27 | 3M Innovative Properties Co | Alkoxy substituted imidazoquinolines |
AR046845A1 (es) * | 2003-11-21 | 2005-12-28 | Novartis Ag | Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas |
CN1830964B (zh) * | 2005-03-11 | 2011-06-15 | 中国科学院上海药物研究所 | 4-取代苯氨基-3-硝基喹啉类化合物及其制备方法和用途 |
AR053358A1 (es) | 2005-04-15 | 2007-05-02 | Cancer Rec Tech Ltd | Inhibidores de adn - pk |
GB0510390D0 (en) * | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
WO2007056112A2 (en) * | 2005-11-04 | 2007-05-18 | Coley Pharmaceutical Group, Inc. | Hydroxy and alkoxy substituted 1h-imidazoquinolines and methods |
CN101541793A (zh) * | 2006-11-20 | 2009-09-23 | 诺瓦提斯公司 | 2-甲基-2-[4-(3-甲基-2-氧代-8-喹啉-3-基-2,3-二氢-咪唑并[4,5-c]喹啉-1-基)-苯基]-丙腈的盐和晶型 |
US20110130386A1 (en) | 2008-04-25 | 2011-06-02 | Mark Frigerio | Dna-pk inhibitors |
EP2303890A4 (en) | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
JP5347628B2 (ja) * | 2009-03-26 | 2013-11-20 | 富士通株式会社 | マイクロ構造体 |
WO2010139731A1 (en) * | 2009-06-04 | 2010-12-09 | Novartis Ag | 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES |
EP2438063A1 (en) * | 2009-06-04 | 2012-04-11 | Novartis AG | 1h-imidazo[4,5-c]quinolinone compounds, useful for the treatment of proliferative diseases |
EP2448937B1 (en) * | 2009-06-30 | 2014-04-09 | Piramal Enterprises Limited | Imidazo[4,5-c]quinoline derivatives and their use in the treatment of tumours and/or inflammations |
-
2010
- 2010-08-28 DE DE102010035744A patent/DE102010035744A1/de not_active Withdrawn
-
2011
- 2011-07-26 SI SI201130493T patent/SI2609082T1/sl unknown
- 2011-07-26 US US13/819,488 patent/US9000153B2/en active Active
- 2011-07-26 SG SG2013013966A patent/SG187954A1/en unknown
- 2011-07-26 WO PCT/EP2011/003744 patent/WO2012028233A1/de active Application Filing
- 2011-07-26 MX MX2013002259A patent/MX338150B/es active IP Right Grant
- 2011-07-26 CA CA2809553A patent/CA2809553C/en active Active
- 2011-07-26 DK DK11748260.4T patent/DK2609082T3/en active
- 2011-07-26 KR KR1020137006794A patent/KR101912475B1/ko active IP Right Grant
- 2011-07-26 PL PL11748260T patent/PL2609082T3/pl unknown
- 2011-07-26 RS RS20150330A patent/RS54038B1/en unknown
- 2011-07-26 PT PT117482604T patent/PT2609082E/pt unknown
- 2011-07-26 CN CN201180041966.4A patent/CN103068803B/zh active Active
- 2011-07-26 JP JP2013526334A patent/JP5882329B2/ja active Active
- 2011-07-26 HU HUE11748260A patent/HUE025692T2/en unknown
- 2011-07-26 BR BR112013004613-9A patent/BR112013004613B1/pt active IP Right Grant
- 2011-07-26 EP EP11748260.4A patent/EP2609082B1/de active Active
- 2011-07-26 EA EA201300288A patent/EA022095B1/ru not_active IP Right Cessation
- 2011-07-26 ES ES11748260.4T patent/ES2536313T3/es active Active
- 2011-07-26 AU AU2011298013A patent/AU2011298013B9/en active Active
- 2011-08-26 AR ARP110103113A patent/AR082728A1/es active IP Right Grant
-
2013
- 2013-02-25 IL IL224903A patent/IL224903A/en active IP Right Grant
- 2013-10-17 HK HK13111720.9A patent/HK1184154A1/zh unknown
-
2015
- 2015-04-01 US US14/676,125 patent/US9598408B2/en active Active
- 2015-05-07 HR HRP20150489TT patent/HRP20150489T1/hr unknown
- 2015-05-14 CY CY20151100429T patent/CY1116281T1/el unknown
-
2017
- 2017-02-27 US US15/443,349 patent/US20170166567A1/en not_active Abandoned
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