NZ594628A - PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka - Google Patents
PYRIDOPYRIMIDINONE INHIBITORS OF PI3KaInfo
- Publication number
- NZ594628A NZ594628A NZ594628A NZ59462806A NZ594628A NZ 594628 A NZ594628 A NZ 594628A NZ 594628 A NZ594628 A NZ 594628A NZ 59462806 A NZ59462806 A NZ 59462806A NZ 594628 A NZ594628 A NZ 594628A
- Authority
- NZ
- New Zealand
- Prior art keywords
- formula
- ethyl
- methyl
- pyrimidin
- methylthio
- 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Dispersion Chemistry (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72457105P | 2005-10-07 | 2005-10-07 | |
| US74371906P | 2006-03-23 | 2006-03-23 | |
| PCT/US2006/039734 WO2007044813A1 (en) | 2005-10-07 | 2006-10-09 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ594628A true NZ594628A (en) | 2013-04-26 |
Family
ID=45957942
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ566903A NZ566903A (en) | 2005-10-07 | 2006-10-09 | Pyrido (2,3-D) pyrimidinone compounds and their use as PI3 inhibitors |
| NZ594628A NZ594628A (en) | 2005-10-07 | 2006-10-09 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ566903A NZ566903A (en) | 2005-10-07 | 2006-10-09 | Pyrido (2,3-D) pyrimidinone compounds and their use as PI3 inhibitors |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US8044062B2 (enExample) |
| EP (2) | EP1940839B1 (enExample) |
| JP (1) | JP5461012B2 (enExample) |
| KR (3) | KR20140105621A (enExample) |
| CN (1) | CN101395155A (enExample) |
| AU (1) | AU2006302078B2 (enExample) |
| BR (1) | BRPI0617159B8 (enExample) |
| CA (1) | CA2623770C (enExample) |
| DK (1) | DK1940839T3 (enExample) |
| EA (1) | EA016945B1 (enExample) |
| ES (1) | ES2432046T3 (enExample) |
| GE (1) | GEP20115304B (enExample) |
| HR (1) | HRP20130902T1 (enExample) |
| IL (1) | IL190292A (enExample) |
| NO (1) | NO343136B1 (enExample) |
| NZ (2) | NZ566903A (enExample) |
| PL (1) | PL1940839T3 (enExample) |
| RS (1) | RS52953B (enExample) |
| WO (1) | WO2007044813A1 (enExample) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2426654C (en) | 2000-10-23 | 2010-12-21 | Smithkline Beecham Corporation | 2,4,8-trisubstituted-8h-pyrido[2,3-d}pyrimidin-7-one compounds |
| MY145343A (en) * | 2005-03-25 | 2012-01-31 | Glaxo Group Ltd | Novel compounds |
| CN101282948A (zh) * | 2005-10-07 | 2008-10-08 | 埃克塞里艾克西斯公司 | N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途 |
| EP1931670B1 (en) * | 2005-10-07 | 2012-09-12 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k |
| JP5461012B2 (ja) * | 2005-10-07 | 2014-04-02 | エクセリクシス, インク. | PI3Kαのピリドピリミジノン型阻害剤 |
| GB0614471D0 (en) | 2006-07-20 | 2006-08-30 | Syngenta Ltd | Herbicidal Compounds |
| WO2008021389A2 (en) * | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| ATE514695T1 (de) | 2006-09-15 | 2011-07-15 | Pfizer Prod Inc | Pyrido(2,3-d)pyrimidinonverbindungen und ihre verwendung als pi3-inhibitoren |
| DK2139484T3 (da) * | 2007-04-10 | 2013-10-21 | Exelixis Inc | Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa |
| JP2010523681A (ja) * | 2007-04-11 | 2010-07-15 | エクセリクシス, インク. | 癌の治療のためのPI3K−αの阻害剤としてのピリド[2,3−D]ピリミジン−7−オン化合物 |
| CA2683784A1 (en) * | 2007-04-11 | 2008-10-23 | Exelixis, Inc. | Pyrido[2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| NZ580009A (en) * | 2007-04-11 | 2012-06-29 | Exelixis Inc | Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer |
| EP2350070A1 (en) * | 2008-09-30 | 2011-08-03 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k and mtor |
| TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
| JP2010111702A (ja) | 2009-02-16 | 2010-05-20 | Tetsuya Nishio | 複素環化合物、その製造法および用途 |
| US8591943B2 (en) | 2009-04-09 | 2013-11-26 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors |
| WO2011049625A1 (en) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Method for aflatoxin screening of products |
| PT2496567T (pt) | 2009-11-05 | 2017-11-15 | Rhizen Pharmaceuticals S A | Novos moduladores de quinase benzopiran |
| 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 |
| AR080151A1 (es) * | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| KR101434841B1 (ko) * | 2010-08-05 | 2014-08-29 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 2-치환-8-알킬-7-옥소-7,8-디하이드로피리도[2,3-d] 피리미딘-6-카르보니트릴 및 이의 용도 |
| TWI642670B (zh) | 2010-09-14 | 2018-12-01 | 伊塞利克斯公司 | Pi3k-德爾塔抑制劑以及其應用和生產方法 |
| WO2012065019A2 (en) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of p13k alpha |
| AU2011336882A1 (en) * | 2010-11-24 | 2013-06-20 | Exelixis, Inc. | Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture |
| RU2013149800A (ru) * | 2011-04-08 | 2015-05-20 | Афраксис Холдингз, Инк. | 8-этил-6-(арил)пиридо[2,3-d]пиримидин-7(8h)-оны для лечения расстройств нервной системы и рака |
| TW201311683A (zh) * | 2011-04-29 | 2013-03-16 | Exelixis Inc | 使用吡啶并嘧啶酮pi3k/mtor抑制劑治療淋巴瘤之方法 |
| KR101992311B1 (ko) | 2011-05-04 | 2019-09-27 | 리젠 파마슈티컬스 소시에떼 아노님 | 단백질 키나아제의 조절제로서 신규한 화합물 |
| TW201306842A (zh) * | 2011-06-15 | 2013-02-16 | Exelixis Inc | 使用pi3k/mtor吡啶並嘧啶酮抑制劑及苯達莫司汀及/或利妥昔單抗治療惡性血液疾病之組合療法 |
| WO2013019927A1 (en) | 2011-08-03 | 2013-02-07 | Signal Pharmaceuticals, Llc | Identification of gene expression profile as a predictive biomarker for lkb1 status |
| TW201325592A (zh) | 2011-09-14 | 2013-07-01 | Exelixis Inc | 用於治療癌症之磷脂醯肌醇-3激酶抑制劑 |
| WO2013056067A1 (en) | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| CN104302294A (zh) | 2011-11-01 | 2015-01-21 | 埃克塞利希斯股份有限公司 | 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺 |
| US9567331B2 (en) | 2011-11-15 | 2017-02-14 | Trustees Of Boston University | Pyridopyrimidinone inhibitors of viruses |
| CN104334192A (zh) | 2012-04-06 | 2015-02-04 | 赛诺菲 | 使用pi3k抑制剂和mek抑制剂治疗癌症的方法 |
| KR101988079B1 (ko) | 2012-07-04 | 2019-06-11 | 리젠 파마슈티컬스 소시에떼 아노님 | 선택적 pi3k 델타 억제제 |
| WO2014058947A1 (en) | 2012-10-12 | 2014-04-17 | Sanofi | Compositions and methods for treating cancer using pi3k inhibitor and anti-cd19 maytansinoid immunoconjugate |
| 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 |
| TW201521792A (zh) * | 2013-03-05 | 2015-06-16 | Sanofi Sa | PI3Kα抑制劑之錠劑調配物 |
| KR102221029B1 (ko) | 2013-04-17 | 2021-02-26 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| WO2014172436A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| NZ631082A (en) | 2013-04-17 | 2017-06-30 | Signal Pharm Llc | Methods for treating cancer using tor kinase inhibitor combination therapy |
| EA037683B1 (ru) | 2013-04-17 | 2021-04-29 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Фармацевтические составы, способы, твердые формы и способы применения, относящиеся к 1-этил-7-(2-метил-6-(1h-1,2,4-триазол-3-ил)пиридин-3-ил)-3,4-дигидропиразино[2,3-b] пиразин-2(1h)-ону |
| UA115805C2 (uk) | 2013-04-17 | 2017-12-26 | Сігнал Фармасьютікалз, Елелсі | Комбінована терапія, яка включає сполуку дигідропіразинопіразину й антагоніст рецептора андрогену, для лікування раку простати |
| PH12021552945B1 (en) | 2013-04-17 | 2024-02-28 | Signal Pharm Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| US9358232B2 (en) | 2013-04-17 | 2016-06-07 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy |
| CN105407892B (zh) | 2013-05-29 | 2019-05-07 | 西格诺药品有限公司 | 一种化合物的药物组合物、其固体形式及它们的使用方法 |
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| 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 |
| RS61934B1 (sr) * | 2016-08-15 | 2021-07-30 | Pfizer | Inhibitori piridopirimdinona cdk2/ 4/6 |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
| WO2019157516A1 (en) | 2018-02-12 | 2019-08-15 | resTORbio, Inc. | Combination therapies |
| BR112020023736A2 (pt) | 2018-05-21 | 2021-02-09 | Nerviano Medical Sciences, S.R.L. | compostos de piridonas heterocondensados e seu uso como inibidores de idh |
| EA202092692A1 (ru) | 2018-06-15 | 2021-04-21 | Навитор Фармасьютикалз, Инк. | Аналоги рапамицина и их применения |
| CN115038700B (zh) | 2019-11-08 | 2025-07-25 | 内尔维亚诺医疗科学公司 | 偕二取代的杂环化合物及其作为idh抑制剂的用途 |
| KR20220128345A (ko) | 2019-12-05 | 2022-09-20 | 아나쿠리아 테라퓨틱스, 인코포레이티드 | 라파마이신 유사체 및 이의 용도 |
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| CN117430597A (zh) * | 2022-07-14 | 2024-01-23 | 浙江同源康医药股份有限公司 | 用作cdk4激酶抑制剂的化合物及其应用 |
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- 2006-10-09 CN CNA2006800370996A patent/CN101395155A/zh active Pending
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