CN101395155A - PI3Kα的吡啶并嘧啶酮抑制剂 - Google Patents
PI3Kα的吡啶并嘧啶酮抑制剂 Download PDFInfo
- Publication number
- CN101395155A CN101395155A CNA2006800370996A CN200680037099A CN101395155A CN 101395155 A CN101395155 A CN 101395155A CN A2006800370996 A CNA2006800370996 A CN A2006800370996A CN 200680037099 A CN200680037099 A CN 200680037099A CN 101395155 A CN101395155 A CN 101395155A
- Authority
- CN
- China
- Prior art keywords
- pyrimidin
- ethyl
- methyl
- optionally substituted
- ethylamino
- 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.)
- Pending
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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Dispersion Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72457105P | 2005-10-07 | 2005-10-07 | |
| US60/724,571 | 2005-10-07 | ||
| US74371906P | 2006-03-23 | 2006-03-23 | |
| US60/743,719 | 2006-03-23 | ||
| PCT/US2006/039734 WO2007044813A1 (en) | 2005-10-07 | 2006-10-09 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012102106887A Division CN102746298A (zh) | 2005-10-07 | 2006-10-09 | PI3Kα的吡啶并嘧啶酮抑制剂 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101395155A true CN101395155A (zh) | 2009-03-25 |
Family
ID=45957942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2006800370996A Pending CN101395155A (zh) | 2005-10-07 | 2006-10-09 | PI3Kα的吡啶并嘧啶酮抑制剂 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US8044062B2 (https=) |
| EP (2) | EP1940839B1 (https=) |
| JP (1) | JP5461012B2 (https=) |
| KR (3) | KR101492795B1 (https=) |
| CN (1) | CN101395155A (https=) |
| AU (1) | AU2006302078B2 (https=) |
| BR (1) | BRPI0617159B8 (https=) |
| CA (1) | CA2623770C (https=) |
| DK (1) | DK1940839T3 (https=) |
| EA (1) | EA016945B1 (https=) |
| ES (1) | ES2432046T3 (https=) |
| GE (1) | GEP20115304B (https=) |
| HR (1) | HRP20130902T1 (https=) |
| IL (1) | IL190292A (https=) |
| NO (1) | NO343136B1 (https=) |
| NZ (2) | NZ594628A (https=) |
| PL (1) | PL1940839T3 (https=) |
| RS (1) | RS52953B (https=) |
| WO (1) | WO2007044813A1 (https=) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103402999A (zh) * | 2010-11-24 | 2013-11-20 | 埃克塞里艾克西斯公司 | 作为PI3K/mTOR抑制剂的苯并氧氮杂卓及其使用和生产方法 |
| CN103596951A (zh) * | 2011-04-08 | 2014-02-19 | 阿弗拉克西斯控股股份有限公司 | 用于治疗神经系统障碍和癌症的8-乙基-6-(芳基)吡啶并[2,3-d]嘧啶-7(8h)-酮 |
| CN103635183A (zh) * | 2011-04-29 | 2014-03-12 | 埃克塞利希斯股份有限公司 | 使用pi3k/mtor的吡啶并嘧啶抑制剂来治疗淋巴瘤的方法 |
| CN114394966A (zh) * | 2016-08-15 | 2022-04-26 | 辉瑞公司 | 吡啶并嘧啶酮cdk2/4/6抑制剂 |
| WO2024012543A1 (zh) * | 2022-07-14 | 2024-01-18 | 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 |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE521353T1 (de) | 2000-10-23 | 2011-09-15 | Glaxosmithkline Llc | Neues trisubstitutiertes 8h-pyridoä2,3- düpyrimidin-7-onderivat zur behandlung von durch csbp/p38kinase vermittelten krankheiten |
| UY29440A1 (es) * | 2005-03-25 | 2006-10-02 | Glaxo Group Ltd | Nuevos compuestos |
| CN101395155A (zh) * | 2005-10-07 | 2009-03-25 | 埃克塞里艾克西斯公司 | PI3Kα的吡啶并嘧啶酮抑制剂 |
| US8247408B2 (en) * | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| BRPI0617162B8 (pt) * | 2005-10-07 | 2021-05-25 | Exelixis Inc | compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos |
| GB0614471D0 (en) | 2006-07-20 | 2006-08-30 | Syngenta Ltd | Herbicidal Compounds |
| CN101528231A (zh) | 2006-08-16 | 2009-09-09 | 埃克塞利希斯股份有限公司 | 在癌症的治疗中使用pi3k和mek调控剂 |
| DK2074122T5 (da) | 2006-09-15 | 2014-03-17 | Pfizer Prod Inc | Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer |
| JP2010523670A (ja) * | 2007-04-10 | 2010-07-15 | エクセリクシス, インク. | Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法 |
| EP2142543B8 (en) * | 2007-04-11 | 2013-07-03 | Exelixis, Inc. | Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| BRPI0810208A2 (pt) * | 2007-04-11 | 2014-10-21 | Exelixis Inc | Combinação de terapias compreendendo inibidores p13k-alpha à base de quinoxalina para uso no tratamento do câncer. |
| CN101711249A (zh) * | 2007-04-11 | 2010-05-19 | 埃克塞里艾克西斯公司 | 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 |
| WO2010039740A1 (en) * | 2008-09-30 | 2010-04-08 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα 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 |
| PH12012500901A1 (en) | 2009-11-05 | 2016-08-05 | Rhizen Pharmaceuticals Sa | Novel benzopyran kinase modulators |
| EP2531194B1 (en) | 2010-02-03 | 2018-04-18 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
| CA2807498C (en) * | 2010-08-05 | 2017-02-07 | Temple University-Of The Commonwealth System Of Higher Education | 2-substituted-8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitriles and uses thereof |
| EP2616442B8 (en) | 2010-09-14 | 2018-10-17 | Exelixis, Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| WO2012065019A2 (en) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of p13k alpha |
| HRP20190128T1 (hr) | 2011-05-04 | 2019-03-08 | Rhizen Pharmaceuticals S.A. | Novi spojevi kao modulatori protein kinaza |
| 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 |
| CA2843887A1 (en) | 2011-08-03 | 2013-02-07 | Signal Pharmaceuticals, Llc | Identification of gene expression profile as a predictive biomarker for lkb1 status |
| KR20140077911A (ko) | 2011-09-14 | 2014-06-24 | 엑셀리시스, 인코포레이티드 | 암의 치료를 위한 포스파티딜이노시톨 3-키나아제 저해제 |
| 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 |
| WO2013115884A2 (en) | 2011-11-15 | 2013-08-08 | Trustees Of Boston University | Pyridopyrimidinone inhibitors of viruses |
| AU2013243429A1 (en) * | 2012-04-06 | 2014-10-23 | Merck Patent Gmbh | Methods for treating cancer using PI3K inhibitor and MEK inhibitor |
| CN109970742A (zh) | 2012-07-04 | 2019-07-05 | 理森制药股份公司 | 选择性PI3Kδ抑制剂 |
| 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 |
| TW201527300A (zh) | 2013-04-17 | 2015-07-16 | Signal Pharm Llc | 關於1-乙基-7-(2-甲基-6-(1H-1,2,4-三唑-3-基)吡啶-3-基)-3,4-二氫吡并[2,3-b]吡-2(1H)-酮之醫藥調配物、方法、固態型式及使用方法 |
| US9782427B2 (en) | 2013-04-17 | 2017-10-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy |
| BR112015026292B1 (pt) | 2013-04-17 | 2022-04-12 | Signal Pharmaceuticals, Llc | Uso de 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino [2,3-b]pirazin-2(1h)- ona e métodos in vitro |
| AU2014254052B2 (en) | 2013-04-17 | 2019-06-06 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| US9937169B2 (en) | 2013-04-17 | 2018-04-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy |
| BR112015026297B1 (pt) | 2013-04-17 | 2022-08-23 | Signal Pharmaceuticals, Llc | Uso de um inibidor da quinase tor e quinazolinona 5-substituída, composição farmacêutica que os compreende, e kit |
| TW201521725A (zh) | 2013-04-17 | 2015-06-16 | Signal Pharm Llc | 使用tor激酶抑制劑組合療法以治療癌症之方法 |
| EP3003313A1 (en) | 2013-05-29 | 2016-04-13 | Signal Pharmaceuticals, 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 |
| US9512129B2 (en) | 2014-04-16 | 2016-12-06 | 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 |
| 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 |
| EP3641772B1 (en) | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
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2006
- 2006-10-09 CN CNA2006800370996A patent/CN101395155A/zh active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103402999A (zh) * | 2010-11-24 | 2013-11-20 | 埃克塞里艾克西斯公司 | 作为PI3K/mTOR抑制剂的苯并氧氮杂卓及其使用和生产方法 |
| CN103596951A (zh) * | 2011-04-08 | 2014-02-19 | 阿弗拉克西斯控股股份有限公司 | 用于治疗神经系统障碍和癌症的8-乙基-6-(芳基)吡啶并[2,3-d]嘧啶-7(8h)-酮 |
| CN103635183A (zh) * | 2011-04-29 | 2014-03-12 | 埃克塞利希斯股份有限公司 | 使用pi3k/mtor的吡啶并嘧啶抑制剂来治疗淋巴瘤的方法 |
| CN114394966A (zh) * | 2016-08-15 | 2022-04-26 | 辉瑞公司 | 吡啶并嘧啶酮cdk2/4/6抑制剂 |
| WO2024012543A1 (zh) * | 2022-07-14 | 2024-01-18 | 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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