KR101492795B1 - PI3Kα의 피리도피리미디논 억제제 - Google Patents
PI3Kα의 피리도피리미디논 억제제 Download PDFInfo
- Publication number
- KR101492795B1 KR101492795B1 KR1020137026515A KR20137026515A KR101492795B1 KR 101492795 B1 KR101492795 B1 KR 101492795B1 KR 1020137026515 A KR1020137026515 A KR 1020137026515A KR 20137026515 A KR20137026515 A KR 20137026515A KR 101492795 B1 KR101492795 B1 KR 101492795B1
- Authority
- KR
- South Korea
- Prior art keywords
- pyrimidin
- optionally substituted
- compound
- ethyl
- methyl
- 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
- UDNXKVJGJYNNDC-UHFFFAOYSA-N CCN(C(C=C1)=O)c2c1c(C)nc(SC)n2 Chemical compound CCN(C(C=C1)=O)c2c1c(C)nc(SC)n2 UDNXKVJGJYNNDC-UHFFFAOYSA-N 0.000 description 1
- RGHYDLZMTYDBDT-UHFFFAOYSA-N CCN(c1c(C=C2c3ccn[nH]3)c(C)nc(N)n1)C2=O Chemical compound CCN(c1c(C=C2c3ccn[nH]3)c(C)nc(N)n1)C2=O RGHYDLZMTYDBDT-UHFFFAOYSA-N 0.000 description 1
- MHBOFFGOGSNRKL-UHFFFAOYSA-N CCNc1cc(C)nc(N)n1 Chemical compound CCNc1cc(C)nc(N)n1 MHBOFFGOGSNRKL-UHFFFAOYSA-N 0.000 description 1
- UQNQWKQCURPNCV-UHFFFAOYSA-N CCNc1cc(C)nc(SC)n1 Chemical compound CCNc1cc(C)nc(SC)n1 UQNQWKQCURPNCV-UHFFFAOYSA-N 0.000 description 1
- NEUWPDLMDVINSN-UHFFFAOYSA-N OB(c1ccn[nH]1)O Chemical compound OB(c1ccn[nH]1)O NEUWPDLMDVINSN-UHFFFAOYSA-N 0.000 description 1
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)
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 Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020087008369A Division KR101538412B1 (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147023011A Division KR20140105621A (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20130140145A KR20130140145A (ko) | 2013-12-23 |
| KR101492795B1 true KR101492795B1 (ko) | 2015-02-13 |
Family
ID=45957942
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147023011A Ceased KR20140105621A (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
| KR1020137026515A Expired - Fee Related KR101492795B1 (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
| KR1020087008369A Expired - Fee Related KR101538412B1 (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147023011A Ceased KR20140105621A (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020087008369A Expired - Fee Related KR101538412B1 (ko) | 2005-10-07 | 2006-10-09 | PI3Kα의 피리도피리미디논 억제제 |
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) | NZ594628A (enExample) |
| PL (1) | PL1940839T3 (enExample) |
| RS (1) | RS52953B (enExample) |
| WO (1) | WO2007044813A1 (enExample) |
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| EP2404603A1 (en) | 2000-10-23 | 2012-01-11 | Glaxosmithkline LLC | Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds for the treatment of CSBP/p38 kinase mediated diseases |
| PE20061351A1 (es) * | 2005-03-25 | 2007-01-14 | Glaxo Group Ltd | COMPUESTOS 8H-PIRIDO[2,3-d]PIRIMIDIN-7-ONA 2,4,8-TRISUSTITUIDOS COMO INHIBIDORES DE LA QUINASA CSBP/RK/p38 |
| EP1931645B1 (en) * | 2005-10-07 | 2014-07-16 | Exelixis, Inc. | N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors |
| US8247408B2 (en) * | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| KR20140105621A (ko) * | 2005-10-07 | 2014-09-01 | 엑셀리시스, 인코포레이티드 | PI3Kα의 피리도피리미디논 억제제 |
| GB0614471D0 (en) | 2006-07-20 | 2006-08-30 | Syngenta Ltd | Herbicidal Compounds |
| AU2007284562B2 (en) * | 2006-08-16 | 2013-05-02 | Exelixis, Inc. | Using PI3K and MEK modulators in treatments of cancer |
| MX2009002927A (es) * | 2006-09-15 | 2009-03-31 | Pfizer Prod Inc | Compuestos de pirido (2,3-d)pirimidinona y su uso como inhibidores de la enzima fosfoinositido 3. |
| KR101626435B1 (ko) * | 2007-04-10 | 2016-06-01 | 엑셀리시스, 인코포레이티드 | Pi3k 알파의 피리도피리미디논 억제제를 이용한 암 치료 방법 |
| WO2008127678A1 (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 |
| US8481001B2 (en) * | 2007-04-11 | 2013-07-09 | Exelixis, Inc. | Combination therapies comprising quinoxaline inhibitors of P13K-alpha for use in the treatment of cancer |
| 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 |
| 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 |
| 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 |
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| MX2012009030A (es) | 2010-02-03 | 2012-09-12 | Signal Pharm Llc | Identificacion de mutacion lkb1 como biomarcador predictivo para sensibilidad a inhibidores de tor cinasa. |
| 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 |
| EA022527B1 (ru) * | 2010-08-05 | 2016-01-29 | Темпл Юниверсити - Оф Дзе Коммонвелт Систем Оф Хайер Эдьюкейшн | 2-ЗАМЕЩЕННЫЕ-8-АЛКИЛ-7-ОКСО-7,8-ДИГИДРОПИРИДО[2,3-d]ПИРИМИДИН-6-КАРБОНИТРИЛЫ И ИХ ПРИМЕНЕНИЕ |
| AU2011302196B2 (en) | 2010-09-14 | 2016-04-28 | 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 |
| 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 |
| 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 |
| DK2705029T3 (en) | 2011-05-04 | 2019-02-18 | Rhizen Pharmaceuticals S A | Hitherto UNKNOWN RELATIONS AS MODULATORS OF PROTEIN KINASES |
| 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 |
| MX2014001246A (es) | 2011-08-03 | 2014-06-11 | Signal Pharm Llc | Identificación del perfil de la expresión génica como biomarcador predictivo del estatus de lkb1. |
| UY34339A (es) | 2011-09-14 | 2013-04-30 | Exelixis Inc | Inhibidores de la fosfatidilinositol 3-quinasa para el tratamiento del cancer |
| WO2013056067A1 (en) | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
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| 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 |
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| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | 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 |
| MX374749B (es) | 2013-04-17 | 2025-03-06 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un analogo de citidina para tratar cancer. |
| EP2986322A1 (en) | 2013-04-17 | 2016-02-24 | Signal Pharmaceuticals, LLC | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| HK1223286A1 (zh) | 2013-05-29 | 2017-07-28 | 西格诺药品有限公司 | 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法 |
| 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 |
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| WO2021089395A1 (en) | 2019-11-08 | 2021-05-14 | Nerviano Medical Sciences S.R.L. | Gem-disubstituted heterocyclic compounds and their use as idh inhibitors |
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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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| EP1277738A1 (en) * | 2000-04-27 | 2003-01-22 | Yamanouchi Pharmaceutical Co. Ltd. | Condensed heteroaryl derivatives |
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