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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- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000014616 translation Effects 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- GPRLSGONYQIRFK-MNYXATJNSA-N triton Chemical compound [3H+] GPRLSGONYQIRFK-MNYXATJNSA-N 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000005740 tumor formation Effects 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 210000003606 umbilical vein Anatomy 0.000 description 1
- LSGOVYNHVSXFFJ-UHFFFAOYSA-N vanadate(3-) Chemical compound [O-][V]([O-])([O-])=O LSGOVYNHVSXFFJ-UHFFFAOYSA-N 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
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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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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
ID=39765082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| JP2010507532A Expired - Fee Related JP5503532B2 (ja) | 2007-05-11 | 2008-05-01 | Ｐ７０ｓ６キナーゼ阻害剤 |
Country Status (33)
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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 |
| KR20110075015A (ko) * | 2008-11-11 | 2011-07-05 | 일라이 릴리 앤드 캄파니 | Ｐ70 ｓ6 키나제 억제제 및 ｅｇｆｒ 억제제 조합 요법 |
| US20110212977A1 (en) * | 2008-11-11 | 2011-09-01 | Eli Lilly And Company | P70 s6 kinase inhibitor and mtor inhibitor combination therapy |
| HRP20141239T1 (xx) | 2009-02-11 | 2015-03-13 | Merck Patent Gmbh | Novi amino azaheterocikliäśki karboksamidi |
| US9023847B2 (en) | 2009-08-07 | 2015-05-05 | Merck Patent Gmbh | Azaheterocyclic compounds |
| EA020151B1 (ru) * | 2009-10-23 | 2014-09-30 | Эли Лилли Энд Компани | Ингибиторы akt и фармацевтические составы, их содержащие |
| PH12012501581A1 (en) | 2010-02-03 | 2012-10-22 | Signal Pharm Llc | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| UA110113C2 (xx) | 2010-07-29 | 2015-11-25 | Біциклічні азагетероциклічні карбоксаміди | |
| JP6014034B2 (ja) | 2010-07-29 | 2016-10-25 | 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 | 環式アミンアザヘテロ環式カルボキサミド |
| EP2643313B9 (en) | 2010-11-24 | 2017-02-22 | Merck Patent GmbH | Quinazoline carboxamide azetidines |
| RS56534B1 (sr) * | 2011-09-12 | 2018-02-28 | Merck Patent Gmbh | Novi imidazol akmini kao modulatori aktivnosti kinaza |
| EA028057B1 (ru) | 2011-09-12 | 2017-10-31 | Мерк Патент Гмбх | Производные аминопиримидина для применения в качестве модуляторов киназной активности |
| AU2013312477B2 (en) * | 2012-09-06 | 2018-05-31 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| 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 |
| CN105051043B (zh) | 2012-11-16 | 2017-05-10 | 默克专利有限公司 | 用作激酶活性调节剂的新颖的杂环类衍生物 |
| EP2920154B1 (en) * | 2012-11-16 | 2017-10-11 | Merck Patent GmbH | Novel imidazol-piperidinyl derivatives as modulators of kinase activity |
| JP6290917B2 (ja) | 2012-11-29 | 2018-03-07 | 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 | アザキナゾリンカルボキサミド誘導体 |
| KR20150124957A (ko) | 2013-03-11 | 2015-11-06 | 메르크 파텐트 게엠베하 | 키나아제 활성의 조절인자로서 (6-[4-1h-이미다졸-2-일)피페리딘-1-일]피리미딘-4-아민 유도체 |
| CN105339008A (zh) | 2013-04-17 | 2016-02-17 | 西格诺药品有限公司 | 用于治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯酰胺的组合疗法 |
| BR112015026257B1 (pt) | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| EP2986321A1 (en) | 2013-04-17 | 2016-02-24 | Signal Pharmaceuticals, LLC | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| JP6382945B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ，エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| MX368286B (es) | 2013-04-17 | 2019-09-27 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer. |
| HK1221150A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用二氢吡嗪并-吡嗪类对癌症的治疗 |
| 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. |
| 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 |
| NZ725361A (en) | 2014-04-03 | 2022-09-30 | Merck Patent Gmbh | Combinations of cancer therapeutics |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | 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 |
| WO2016164641A1 (en) | 2015-04-08 | 2016-10-13 | 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 |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
| JP2023551408A (ja) | 2020-11-16 | 2023-12-08 | 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 | がん処置のためのキナーゼインヒビター組み合わせ |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| JP5213229B2 (ja) * | 2004-04-23 | 2013-06-19 | エグゼリクシス， インコーポレイテッド | キナーゼ調節因子および使用方法 |
| 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 |
| JP5274842B2 (ja) | 2004-12-28 | 2013-08-28 | エグゼリクシス， インコーポレイテッド | 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物 |
| JP5114395B2 (ja) | 2005-06-30 | 2013-01-09 | プロシディオン・リミテッド | Ｇｐｃｒアゴニスト |
| US20090082370A1 (en) | 2006-04-25 | 2009-03-26 | Neil Thomas Thompson | Pharmaceutical Combinations of PK Inhibitors and Other Active Agents |
| WO2007125321A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| 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
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- 2008-04-29 PE PE2008000756A patent/PE20090887A1/es not_active Application Discontinuation
- 2008-04-29 AR ARP080101808A patent/AR066344A1/es unknown
- 2008-04-29 CL CL2008001230A patent/CL2008001230A1/es unknown
- 2008-05-01 BR BRPI0811212-6A2A patent/BRPI0811212A2/pt not_active IP Right Cessation
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- 2008-05-01 CN CN2008800156864A patent/CN101679439B/zh not_active Expired - Fee Related
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- 2008-05-01 AU AU2008251692A patent/AU2008251692B2/en not_active Ceased
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- 2008-05-01 DK DK08747285.8T patent/DK2148880T3/da active
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- 2008-05-01 KR KR1020097023455A patent/KR101088219B1/ko not_active Expired - Fee Related
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