ES2439793T3 - Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis - Google Patents
Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis Download PDFInfo
- Publication number
- ES2439793T3 ES2439793T3 ES10716162.2T ES10716162T ES2439793T3 ES 2439793 T3 ES2439793 T3 ES 2439793T3 ES 10716162 T ES10716162 T ES 10716162T ES 2439793 T3 ES2439793 T3 ES 2439793T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- heteroaryl
- kinase
- inhibitors
- synthesis
- 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.)
- Active
Links
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 title 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- -1 amino- Chemical class 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000003368 amide group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 229910052757 nitrogen Chemical group 0.000 abstract 2
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17013809P | 2009-04-17 | 2009-04-17 | |
| US170138P | 2009-04-17 | ||
| PCT/US2010/031191 WO2010120998A1 (en) | 2009-04-17 | 2010-04-15 | Pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2439793T3 true ES2439793T3 (es) | 2014-01-24 |
| ES2439793T9 ES2439793T9 (es) | 2016-03-10 |
Family
ID=42269326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10716162.2T Active ES2439793T3 (es) | 2009-04-17 | 2010-04-15 | Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8835429B2 (OSRAM) |
| EP (1) | EP2419432B9 (OSRAM) |
| JP (1) | JP5649643B2 (OSRAM) |
| CA (1) | CA2755554C (OSRAM) |
| ES (1) | ES2439793T3 (OSRAM) |
| WO (1) | WO2010120998A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9249129B2 (en) | 2010-03-04 | 2016-02-02 | Cellzome Limited | Morpholino substituted urea derivatives as mTOR inhibitors |
| CN103501610A (zh) * | 2011-03-09 | 2014-01-08 | 西建阿维拉米斯研究公司 | Pi3激酶抑制剂和其用途 |
| JP2014510122A (ja) * | 2011-04-04 | 2014-04-24 | セルゾーム リミテッド | ｍＴＯＲ阻害剤としてのジヒドロピロロピリミジン誘導体 |
| CN103917530B (zh) | 2011-09-21 | 2016-08-24 | 塞尔佐姆有限公司 | 作为mtor抑制剂的吗啉代取代的脲或氨基甲酸衍生物 |
| AU2012320465B2 (en) | 2011-10-07 | 2016-03-03 | Cellzome Limited | Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mTOR inhibitors |
| 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 |
| CN104230952B (zh) * | 2014-08-16 | 2017-02-01 | 沈阳药科大学 | 含有嘧啶骨架的化合物及其制备方法和用途 |
| CN107001348B (zh) * | 2014-12-17 | 2019-10-11 | 上海海雁医药科技有限公司 | 2-吗啉-4,6-二取代的嘧啶衍生物、其制法与医药上的用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9009A (en) * | 1852-06-08 | Bat-trap | ||
| CA2528032A1 (en) * | 2003-06-03 | 2004-12-16 | Beth Israel Deaconess Medical Center | Methods and compounds for the treatment of vascular stenosis |
| GB0520657D0 (en) * | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| GB0525083D0 (en) * | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| MX2009002046A (es) * | 2006-08-24 | 2009-03-06 | Astrazeneca Ab | Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos. |
| AU2008255005B2 (en) * | 2007-05-18 | 2013-05-02 | Merck Sharp & Dohme Corp. | OXO bridged diazepan orexin receptor antagonists |
| MX2010004260A (es) * | 2007-10-16 | 2010-04-30 | Wyeth Llc | Compuestos de tienopirimidina y pirazolopirimidina y su uso como inhibidores de mtor cinasa y pi3 cinasa. |
-
2010
- 2010-04-15 JP JP2012506209A patent/JP5649643B2/ja not_active Expired - Fee Related
- 2010-04-15 US US13/264,776 patent/US8835429B2/en not_active Expired - Fee Related
- 2010-04-15 CA CA2755554A patent/CA2755554C/en not_active Expired - Fee Related
- 2010-04-15 WO PCT/US2010/031191 patent/WO2010120998A1/en not_active Ceased
- 2010-04-15 ES ES10716162.2T patent/ES2439793T3/es active Active
- 2010-04-15 EP EP10716162.2A patent/EP2419432B9/en not_active Not-in-force
Also Published As
| Publication number | Publication date |
|---|---|
| US8835429B2 (en) | 2014-09-16 |
| JP5649643B2 (ja) | 2015-01-07 |
| EP2419432A1 (en) | 2012-02-22 |
| ES2439793T9 (es) | 2016-03-10 |
| WO2010120998A1 (en) | 2010-10-21 |
| EP2419432B9 (en) | 2016-02-17 |
| US20120134959A1 (en) | 2012-05-31 |
| CA2755554C (en) | 2013-09-24 |
| JP2012524103A (ja) | 2012-10-11 |
| EP2419432B1 (en) | 2013-11-20 |
| CA2755554A1 (en) | 2010-10-21 |
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