JP5503532B2 - Ｐ７０ｓ６キナーゼ阻害剤 - Google Patents
Ｐ７０ｓ６キナーゼ阻害剤 Download PDFInfo
- Publication number
- JP5503532B2 JP5503532B2 JP2010507532A JP2010507532A JP5503532B2 JP 5503532 B2 JP5503532 B2 JP 5503532B2 JP 2010507532 A JP2010507532 A JP 2010507532A JP 2010507532 A JP2010507532 A JP 2010507532A JP 5503532 B2 JP5503532 B2 JP 5503532B2
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- mmol
- added
- trifluoromethyl
- imidazol
- 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.)
- Expired - Fee Related
Links
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 14
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91733107P | 2007-05-11 | 2007-05-11 | |
| US60/917,331 | 2007-05-11 | ||
| PCT/US2008/062143 WO2008140947A1 (en) | 2007-05-11 | 2008-05-01 | P70 s6 kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010526814A JP2010526814A (ja) | 2010-08-05 |
| JP2010526814A5 JP2010526814A5 (enExample) | 2011-06-16 |
| JP5503532B2 true JP5503532B2 (ja) | 2014-05-28 |
Family
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| JP2010507532A Expired - Fee Related JP5503532B2 (ja) | 2007-05-11 | 2008-05-01 | Ｐ７０ｓ６キナーゼ阻害剤 |
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| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
| US8252791B2 (en) * | 2008-08-13 | 2012-08-28 | Jenrin Discovery, Inc. | Purine compounds as cannabinoid receptor blockers |
| AR074072A1 (es) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
| BRPI0921888A2 (pt) * | 2008-11-11 | 2015-12-29 | Lilly Co Eli | terapia de combinação de inibidor de egfr inibidor da p70 s6 quinase |
| EA018824B1 (ru) * | 2008-11-11 | 2013-10-30 | Эли Лилли Энд Компани | КОМБИНИРОВАННАЯ ТЕРАПИЯ ИНГИБИТОРОМ КИНАЗЫ p70 S6 И ИНГИБИТОРОМ mTOR |
| PT2396307E (pt) | 2009-02-11 | 2015-02-04 | Merck Patent Gmbh | Novas carboxamidas azaheterocíclicas de amino |
| ES2654332T3 (es) | 2009-08-07 | 2018-02-13 | Merck Patent Gmbh | Nuevos compuestos azaheterocíclicos |
| AU2010310786B2 (en) * | 2009-10-23 | 2014-03-27 | Eli Lilly And Company | AKT inhibitors |
| ES2670659T3 (es) | 2010-02-03 | 2018-05-31 | Signal Pharmaceuticals, Llc | Identificación de mutación en LKB1 como un biomarcador predictivo para la sensibilidad a inhibidores de la quinasa TOR |
| EA028012B1 (ru) | 2010-07-29 | 2017-09-29 | Мерк Патент Гмбх | Циклический амин-азагетероциклический карбоксамид |
| UA110113C2 (xx) | 2010-07-29 | 2015-11-25 | Біциклічні азагетероциклічні карбоксаміди | |
| US8946247B2 (en) | 2010-11-24 | 2015-02-03 | Merck Patent Gmbh | Quinazoline carboxamide azetidines |
| HRP20171655T1 (hr) | 2011-09-12 | 2017-12-15 | Merck Patent Gmbh | Derivati aminopirimidina za upotrebu kao modulatori aktivnosti kinaze |
| PL2755965T3 (pl) | 2011-09-12 | 2018-01-31 | Merck Patent Gmbh | Nowe aminy imidazolowe jako modulatory aktywności kinazowej |
| MX2015002887A (es) * | 2012-09-06 | 2015-07-06 | Plexxikon Inc | Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello. |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| JP6280130B2 (ja) | 2012-11-16 | 2018-02-14 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | キナーゼ活性のモジュレーターとしての新規イミダゾール−ピペリジニル誘導体 |
| CA2890288A1 (en) | 2012-11-16 | 2014-05-22 | Merck Patent Gmbh | Novel heterocyclic derivatives as modulators of kinase activity |
| KR20150090044A (ko) | 2012-11-29 | 2015-08-05 | 메르크 파텐트 게엠베하 | 아자퀴나졸린 카복사미드 유도체 |
| SG11201505999VA (en) * | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| KR102240356B1 (ko) | 2013-04-17 | 2021-04-14 | 시그날 파마소티칼 엘엘씨 | Ｔｏｒ 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법 |
| MX393164B (es) | 2013-04-17 | 2025-03-21 | Signal Pharm Llc | Formulaciones farmacéuticas, proceso, formas sólidas y métodos de uso relacionados con 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-ii)piridin-3-ii)-3,4-dihidropirazino[2,3-b]pirazin-2(1h)-ona. |
| US9937169B2 (en) | 2013-04-17 | 2018-04-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy |
| AU2014254057A1 (en) | 2013-04-17 | 2015-11-05 | Signal Pharmaceuticals, Llc | Combination therapy comprising a TOR kinase inhibitor and N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| BR112015026247B1 (pt) | 2013-04-17 | 2022-08-23 | Signal Pharmaceuticals, Llc | Uso de compostos em combinação com um análogo de citidina, composição farmacêutica que os compreende, e kit |
| WO2014172426A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| BR112015026238A8 (pt) | 2013-04-17 | 2019-12-24 | Signal Pharm Llc | composto dihidropirazino-pirazina, composição farmacêutica que o compreende, uso do composto, métodos para inibir ou medir a fosforilação e para inibir a atividade da proteína quinase, bem como kit |
| NZ629486A (en) | 2013-05-29 | 2017-11-24 | Signal Pharm Llc | Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| WO2015134536A1 (en) * | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN106456752B (zh) | 2014-04-03 | 2020-11-20 | 默克专利股份公司 | 癌症治疗剂的组合 |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| WO2016040078A1 (en) * | 2014-09-10 | 2016-03-17 | Eli Lilly And Company | Substituted phenyl imidazolyl piperidyl compounds as p70s6k1 inhibitors |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN106187899B (zh) * | 2016-06-28 | 2019-07-16 | 绍兴文理学院 | 一种氟代氮杂芳烃的合成方法 |
| CN110996955A (zh) | 2017-06-22 | 2020-04-10 | 细胞基因公司 | 以乙型肝炎病毒感染为特征的肝细胞癌的治疗 |
| US20240024324A1 (en) | 2020-11-16 | 2024-01-25 | Merck Patent Gmbh | Kinase inhibitor combinations for cancer treatment |
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| NL1004346C2 (nl) | 1996-10-23 | 1998-04-24 | Dsm Nv | Werkwijze voor het scheiden van een mengsel van enantiomeren in een geschikt oplosmiddel. |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| CA2563699C (en) * | 2004-04-23 | 2014-03-25 | Exelixis, Inc. | Kinase modulators and method of use |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| EP1848719B1 (en) | 2004-12-28 | 2012-02-01 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| WO2007003960A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| EP2043655A2 (en) | 2006-04-25 | 2009-04-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| EP2037931A2 (en) | 2006-04-25 | 2009-03-25 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
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- 2008-04-29 PE PE2008000756A patent/PE20090887A1/es not_active Application Discontinuation
- 2008-05-01 RS RS20140385A patent/RS53451B/sr unknown
- 2008-05-01 WO PCT/US2008/062143 patent/WO2008140947A1/en not_active Ceased
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- 2008-05-01 KR KR1020097023455A patent/KR101088219B1/ko not_active Expired - Fee Related
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