CN101711249A - 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 - Google Patents
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 Download PDFInfo
- Publication number
- CN101711249A CN101711249A CN200880018758A CN200880018758A CN101711249A CN 101711249 A CN101711249 A CN 101711249A CN 200880018758 A CN200880018758 A CN 200880018758A CN 200880018758 A CN200880018758 A CN 200880018758A CN 101711249 A CN101711249 A CN 101711249A
- Authority
- CN
- China
- Prior art keywords
- compound
- methyl
- formula
- amino
- pyrido
- 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
- 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
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/025—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus inorganic Tc complexes or compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
- A61N5/1001—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy using radiation sources introduced into or applied onto the body; brachytherapy
-
- 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)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Mycology (AREA)
- Immunology (AREA)
- Radiology & Medical Imaging (AREA)
- Microbiology (AREA)
- Inorganic Chemistry (AREA)
- Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Pathology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91116007P | 2007-04-11 | 2007-04-11 | |
| US60/911,160 | 2007-04-11 | ||
| PCT/US2008/004807 WO2008127712A1 (en) | 2007-04-11 | 2008-04-11 | Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101711249A true CN101711249A (zh) | 2010-05-19 |
Family
ID=39642739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200880018758A Pending CN101711249A (zh) | 2007-04-11 | 2008-04-11 | 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 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20100209340A1 (enExample) |
| EP (1) | EP2142544B8 (enExample) |
| JP (1) | JP2010523681A (enExample) |
| KR (1) | KR20090130104A (enExample) |
| CN (1) | CN101711249A (enExample) |
| AU (1) | AU2008239596B2 (enExample) |
| BR (1) | BRPI0810175A2 (enExample) |
| CA (1) | CA2683820A1 (enExample) |
| CO (1) | CO6241119A2 (enExample) |
| CR (1) | CR11098A (enExample) |
| DO (1) | DOP2009000242A (enExample) |
| EA (1) | EA018964B1 (enExample) |
| EC (1) | ECSP099722A (enExample) |
| ES (1) | ES2425068T3 (enExample) |
| IL (1) | IL201209A0 (enExample) |
| MA (1) | MA31336B1 (enExample) |
| MX (1) | MX2009010815A (enExample) |
| MY (1) | MY150747A (enExample) |
| NI (1) | NI200900183A (enExample) |
| NZ (1) | NZ579945A (enExample) |
| SV (1) | SV2009003389A (enExample) |
| TN (1) | TN2009000389A1 (enExample) |
| UA (1) | UA101315C2 (enExample) |
| WO (1) | WO2008127712A1 (enExample) |
| ZA (1) | ZA200906648B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5111113B2 (ja) * | 2004-12-13 | 2012-12-26 | サネシス ファーマシューティカルズ, インコーポレイテッド | Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン |
| EP2364974A1 (en) * | 2005-10-07 | 2011-09-14 | Exelixis, Inc. | N-(3-Phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors |
| HRP20130902T1 (hr) * | 2005-10-07 | 2013-11-08 | Exelixis Inc. | PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa |
| JP2010500994A (ja) | 2006-08-16 | 2010-01-14 | エグゼリクシス, インコーポレイテッド | Pi3kおよびmekモジュレーターを使用する方法 |
| HRP20110621T2 (hr) | 2006-09-15 | 2013-12-06 | Pfizer Products Inc. | SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3 |
| ES2430614T3 (es) | 2007-04-10 | 2013-11-21 | Exelixis, Inc. | Métodos de tratamiento del cáncer usando inhibidores de piridopirimidinona de PI3K alfa |
| US20100150827A1 (en) * | 2007-04-11 | 2010-06-17 | Exelixis, Inc | Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of p13k-alpha for the treatment of cancer |
| US8101622B2 (en) * | 2008-09-30 | 2012-01-24 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα and mTOR |
| AU2010341573B2 (en) * | 2009-12-22 | 2016-10-13 | Vertex Pharmaceuticals Incorporated | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| 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 |
| AR082985A1 (es) | 2010-09-14 | 2013-01-23 | Exelixis Inc | INHIBIDORES DE PI3K-d Y METODOS DE SU USO Y PREPARACION |
| WO2013056067A1 (en) * | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| MX2014005249A (es) | 2011-11-01 | 2015-03-05 | Exelixis Inc | N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]s ulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-cinasa para el tratamiento de neoplasias malignas linfoproliferativas. |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1183099A (zh) * | 1995-05-03 | 1998-05-27 | 沃尼尔·朗伯公司 | 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3-d]嘧啶 |
| WO2007044813A1 (en) * | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2937284A (en) * | 1958-05-01 | 1960-05-17 | Burroughs Wellcome Co | 2, 4-diamino-5, 6-dialkylpyrido (2, 3-d) pyrimidines and method |
| US7019002B2 (en) * | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| DE602005002562T2 (de) * | 2004-05-04 | 2008-01-31 | Warner-Lambert Company Llc | Pyrrolylsubstituierte pyridoä2,3-düpyrimidin-7-one und derivate davon als therapeutische mittel |
| JP5480503B2 (ja) * | 2005-10-07 | 2014-04-23 | 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 |
| JP2010500994A (ja) * | 2006-08-16 | 2010-01-14 | エグゼリクシス, インコーポレイテッド | Pi3kおよびmekモジュレーターを使用する方法 |
| HRP20110621T2 (hr) * | 2006-09-15 | 2013-12-06 | Pfizer Products Inc. | SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3 |
-
2008
- 2008-04-11 WO PCT/US2008/004807 patent/WO2008127712A1/en not_active Ceased
- 2008-04-11 CN CN200880018758A patent/CN101711249A/zh active Pending
- 2008-04-11 KR KR1020097023146A patent/KR20090130104A/ko not_active Ceased
- 2008-04-11 CA CA002683820A patent/CA2683820A1/en not_active Abandoned
- 2008-04-11 JP JP2010503085A patent/JP2010523681A/ja active Pending
- 2008-04-11 BR BRPI0810175-2A2A patent/BRPI0810175A2/pt not_active IP Right Cessation
- 2008-04-11 US US12/595,233 patent/US20100209340A1/en not_active Abandoned
- 2008-04-11 NZ NZ579945A patent/NZ579945A/en not_active IP Right Cessation
- 2008-04-11 MY MYPI20094194 patent/MY150747A/en unknown
- 2008-04-11 UA UAA200911451A patent/UA101315C2/ru unknown
- 2008-04-11 EA EA200970936A patent/EA018964B1/ru not_active IP Right Cessation
- 2008-04-11 EP EP08742864.5A patent/EP2142544B8/en active Active
- 2008-04-11 MX MX2009010815A patent/MX2009010815A/es active IP Right Grant
- 2008-04-11 ES ES08742864T patent/ES2425068T3/es active Active
- 2008-04-11 AU AU2008239596A patent/AU2008239596B2/en not_active Ceased
-
2009
- 2009-09-23 ZA ZA200906648A patent/ZA200906648B/xx unknown
- 2009-09-24 TN TNP2009000389A patent/TN2009000389A1/fr unknown
- 2009-09-29 IL IL201209A patent/IL201209A0/en unknown
- 2009-10-09 NI NI200900183A patent/NI200900183A/es unknown
- 2009-10-09 SV SV2009003389A patent/SV2009003389A/es not_active Application Discontinuation
- 2009-10-09 DO DO2009000242A patent/DOP2009000242A/es unknown
- 2009-10-30 MA MA32314A patent/MA31336B1/fr unknown
- 2009-11-09 CO CO09126919A patent/CO6241119A2/es not_active Application Discontinuation
- 2009-11-09 EC EC2009009722A patent/ECSP099722A/es unknown
- 2009-11-09 CR CR11098A patent/CR11098A/es unknown
-
2013
- 2013-01-03 US US13/694,772 patent/US20130343988A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1183099A (zh) * | 1995-05-03 | 1998-05-27 | 沃尼尔·朗伯公司 | 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3-d]嘧啶 |
| WO2007044813A1 (en) * | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2142544B1 (en) | 2013-05-22 |
| MY150747A (en) | 2014-02-28 |
| DOP2009000242A (es) | 2010-04-30 |
| CA2683820A1 (en) | 2008-10-23 |
| MA31336B1 (fr) | 2010-04-01 |
| EP2142544A1 (en) | 2010-01-13 |
| CO6241119A2 (es) | 2011-01-20 |
| ECSP099722A (es) | 2009-12-28 |
| KR20090130104A (ko) | 2009-12-17 |
| ZA200906648B (en) | 2010-04-28 |
| AU2008239596B2 (en) | 2013-08-15 |
| BRPI0810175A2 (pt) | 2014-12-30 |
| NZ579945A (en) | 2012-05-25 |
| EP2142544B8 (en) | 2013-07-03 |
| HK1139941A1 (en) | 2010-09-30 |
| TN2009000389A1 (en) | 2010-12-31 |
| ES2425068T3 (es) | 2013-10-11 |
| CR11098A (es) | 2010-01-27 |
| AU2008239596A1 (en) | 2008-10-23 |
| JP2010523681A (ja) | 2010-07-15 |
| US20130343988A1 (en) | 2013-12-26 |
| MX2009010815A (es) | 2009-10-29 |
| SV2009003389A (es) | 2010-04-27 |
| NI200900183A (es) | 2010-10-05 |
| EA200970936A1 (ru) | 2010-02-26 |
| US20100209340A1 (en) | 2010-08-19 |
| IL201209A0 (en) | 2010-05-31 |
| WO2008127712A1 (en) | 2008-10-23 |
| UA101315C2 (ru) | 2013-03-25 |
| EA018964B1 (ru) | 2013-12-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20100519 |