AU2006302078B2 - Pyridopyrimidinone inhibitors of PI3Kalpha - Google Patents
Pyridopyrimidinone inhibitors of PI3Kalpha Download PDFInfo
- Publication number
- AU2006302078B2 AU2006302078B2 AU2006302078A AU2006302078A AU2006302078B2 AU 2006302078 B2 AU2006302078 B2 AU 2006302078B2 AU 2006302078 A AU2006302078 A AU 2006302078A AU 2006302078 A AU2006302078 A AU 2006302078A AU 2006302078 B2 AU2006302078 B2 AU 2006302078B2
- Authority
- AU
- Australia
- Prior art keywords
- ethyl
- pyrimidin
- methyl
- pyrido
- 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.)
- Ceased
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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Molecular Biology (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)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2013200931A AU2013200931B2 (en) | 2005-10-07 | 2013-02-20 | Pyridopyrimidinone inhibitors of PI3K alpha |
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 |
|---|---|---|---|
| AU2013200931A Division AU2013200931B2 (en) | 2005-10-07 | 2013-02-20 | Pyridopyrimidinone inhibitors of PI3K alpha |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2006302078A1 AU2006302078A1 (en) | 2007-04-19 |
| AU2006302078B2 true AU2006302078B2 (en) | 2012-11-22 |
Family
ID=45957942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2006302078A Ceased AU2006302078B2 (en) | 2005-10-07 | 2006-10-09 | Pyridopyrimidinone inhibitors of PI3Kalpha |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US8044062B2 (enExample) |
| EP (2) | EP2322523B1 (enExample) |
| JP (1) | JP5461012B2 (enExample) |
| KR (3) | KR101492795B1 (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) | NZ594628A (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 |
|---|---|---|---|---|
| PT1333833E (pt) | 2000-10-23 | 2011-12-09 | Glaxosmithkline Llc | Novo composto 8h-pirido[2,3-d]pirimidin-7-ona trissusbtituída para o tratamento de doenças mediadas por csbp/p38 cinase |
| AR053346A1 (es) * | 2005-03-25 | 2007-05-02 | Glaxo Group Ltd | Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38 |
| US8247408B2 (en) * | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| HRP20130902T1 (hr) * | 2005-10-07 | 2013-11-08 | Exelixis Inc. | PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa |
| NZ608667A (en) * | 2005-10-07 | 2014-08-29 | Exelixis Inc | N-(3-amino-quinoxalin-2-yl)-sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors |
| GB0614471D0 (en) | 2006-07-20 | 2006-08-30 | Syngenta Ltd | Herbicidal Compounds |
| CA2658725A1 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| MY146420A (en) * | 2006-09-15 | 2012-08-15 | Pfizer Prod Inc | Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors |
| DK2139484T3 (da) * | 2007-04-10 | 2013-10-21 | Exelixis Inc | Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa |
| RS53020B (sr) * | 2007-04-11 | 2014-04-30 | Exelixis Inc. | Kombinovane terapije koje sadrže hinoksalin inhibitor pi3k-alfa za upotrebu u lečenju kancera |
| AU2008239655B2 (en) * | 2007-04-11 | 2013-06-20 | Exelixis, Inc. | Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer |
| AU2008239596B2 (en) * | 2007-04-11 | 2013-08-15 | Exelixis, Inc. | Pyrido [2,3-D] pyrimidin-7-one compounds as inhibitors of PI3K-alpha for the treatment of cancer |
| TW201018685A (en) * | 2008-09-30 | 2010-05-16 | 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 |
| WO2010118207A1 (en) | 2009-04-09 | 2010-10-14 | Schering Corporation | 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 |
| HRP20171537T1 (hr) | 2009-11-05 | 2017-12-15 | Rhizen Pharmaceuticals S.A. | Novi modulatori benzopiran kinaze |
| SG183155A1 (en) | 2010-02-03 | 2012-09-27 | Signal Pharm Llc | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| WO2011100319A1 (en) | 2010-02-09 | 2011-08-18 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors |
| NZ606281A (en) * | 2010-08-05 | 2014-09-26 | Univ Temple | 2-substituted-8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitriles and uses thereof |
| CA2812089C (en) | 2010-09-14 | 2020-02-18 | 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 |
| WO2012074869A1 (en) * | 2010-11-24 | 2012-06-07 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| CA2832309A1 (en) * | 2011-04-08 | 2013-03-28 | David Campbell | 8-ethyl-6-(aryl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of nervous system disorders and cancer |
| MX2013012486A (es) | 2011-04-29 | 2014-05-28 | Exelixis Inc | Metodo para tratar linfoma usando inhibidores de piridopirimidinona de fosfonio sitol 3-cinasa/diana de rapalamina en celulas de mamifero (pi3k/mtor). |
| BR112013027774B1 (pt) | 2011-05-04 | 2020-11-17 | Rhizen Pharmaceuticals S.A. | composto e composição farmacêutica |
| 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 |
| CN105039520A (zh) | 2011-08-03 | 2015-11-11 | 西格诺药品有限公司 | 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定 |
| 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 |
| KR20140096083A (ko) | 2011-11-01 | 2014-08-04 | 엑셀리시스, 인코포레이티드 | 림프증식성 악성종양의 치료를 위한 포스파티딜이노시톨 3-키나아제 저해제로서 n(3{[(3{[2클로로5(메톡시)페닐]아미노}퀴녹살린2일)아미노]설포닐}페닐)2메틸알라닌아미드 |
| US9567331B2 (en) | 2011-11-15 | 2017-02-14 | 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 |
| ES2647416T3 (es) | 2012-07-04 | 2017-12-21 | Rhizen Pharmaceuticals S.A. | Inhibidores de PI3K delta selectivos |
| WO2014058947A1 (en) | 2012-10-12 | 2014-04-17 | Sanofi | Compositions and methods for treating cancer using pi3k inhibitor and anti-cd19 maytansinoid immunoconjugate |
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| TW201521792A (zh) * | 2013-03-05 | 2015-06-16 | Sanofi Sa | PI3Kα抑制劑之錠劑調配物 |
| CN105377260B (zh) | 2013-04-17 | 2020-06-12 | 西格诺药品有限公司 | 二氢吡嗪并-吡嗪类化合物在制备治疗癌症的药物中的应用 |
| KR102240356B1 (ko) | 2013-04-17 | 2021-04-14 | 시그날 파마소티칼 엘엘씨 | Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법 |
| JP6382947B2 (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 | 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法 |
| KR102271344B1 (ko) | 2013-04-17 | 2021-07-01 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| BR112015026021A2 (pt) | 2013-04-17 | 2017-07-25 | Signal Pharm Llc | terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer |
| ES2744198T3 (es) | 2013-04-17 | 2020-02-24 | Signal Pharm Llc | Formulaciones farmacéuticas, procesos, formas sólidas y procedimientos de uso relacionados con 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 |
| CN105392499B (zh) | 2013-04-17 | 2018-07-24 | 西格诺药品有限公司 | 用于治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法 |
| WO2014193912A1 (en) | 2013-05-29 | 2014-12-04 | 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 |
| 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 |
| 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 |
| CU24522B1 (es) * | 2016-08-15 | 2021-06-08 | Pfizer | PIRIDO[2,3-d]PIRIMIDIN-7(8H)-ONAS 6-FLUOROALQUIL-2-(ALQUILSULFONILPIPERIDIN-4-IL)AMINO SUSTITUIDAS |
| EA202090103A1 (ru) | 2017-06-22 | 2020-04-24 | Селджин Корпорейшн | Лечение гепатоцеллюлярной карциномы, которая характеризуется вирусной инфекцией гепатита b |
| WO2019157516A1 (en) | 2018-02-12 | 2019-08-15 | resTORbio, Inc. | Combination therapies |
| CA3100448A1 (en) | 2018-05-21 | 2019-11-28 | Nerviano Medical Sciences S.R.L. | Heterocondensed pyridones compounds and their use as idh inhibitors |
| CN117843659A (zh) | 2018-06-15 | 2024-04-09 | 詹森药业有限公司 | 雷帕霉素类似物和其用途 |
| EP4055015B1 (en) | 2019-11-08 | 2025-04-02 | Nerviano Medical Sciences S.r.l. | Gem-disubstituted heterocyclic compounds and their use as idh inhibitors |
| US11819476B2 (en) | 2019-12-05 | 2023-11-21 | Janssen Pharmaceutica Nv | Rapamycin analogs and uses thereof |
| MX2022013417A (es) | 2020-04-29 | 2022-11-14 | Relay Therapeutics Inc | Inhibidores de fosfatidilinositol 3 cinasa (pi3k) alfa y metodos de uso de los mismos. |
| EP4399196A4 (en) * | 2021-09-10 | 2025-08-06 | Relay Therapeutics Inc | PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF |
| 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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