EA025948B1 - КОМБИНАЦИЯ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТ-3-КИНАЗЫ (PI3K) И ИНГИБИТОРА mTOR - Google Patents
КОМБИНАЦИЯ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТ-3-КИНАЗЫ (PI3K) И ИНГИБИТОРА mTOR Download PDFInfo
- Publication number
- EA025948B1 EA025948B1 EA201391565A EA201391565A EA025948B1 EA 025948 B1 EA025948 B1 EA 025948B1 EA 201391565 A EA201391565 A EA 201391565A EA 201391565 A EA201391565 A EA 201391565A EA 025948 B1 EA025948 B1 EA 025948B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- kinase
- ttok
- rapamycin
- carcinoma
- dependent
- Prior art date
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- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title abstract description 3
- 229940124302 mTOR inhibitor Drugs 0.000 title 1
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 title 1
- 230000001419 dependent effect Effects 0.000 claims abstract description 10
- 150000003839 salts Chemical class 0.000 claims abstract description 10
- 201000010099 disease Diseases 0.000 claims abstract description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 9
- 108091000080 Phosphotransferase Proteins 0.000 claims abstract description 8
- 102000020233 phosphotransferase Human genes 0.000 claims abstract description 8
- 241000124008 Mammalia Species 0.000 claims abstract description 7
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims abstract description 7
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims abstract description 7
- 229960002930 sirolimus Drugs 0.000 claims abstract description 7
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims abstract description 6
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims abstract description 6
- 239000003112 inhibitor Substances 0.000 claims abstract description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 201000003970 colon lymphoma Diseases 0.000 claims 4
- IHGVAVLSTPCCJP-UHFFFAOYSA-N 4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-amine Chemical compound N1=C(N)SC(C=2C=C(N=CC=2)C(C)(C)C(F)(F)F)=C1C IHGVAVLSTPCCJP-UHFFFAOYSA-N 0.000 claims 3
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 229940125904 compound 1 Drugs 0.000 claims 3
- 229960005167 everolimus Drugs 0.000 claims 3
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 claims 3
- 201000005296 lung carcinoma Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 201000009030 Carcinoma Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 108060006633 protein kinase Proteins 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- OAWXZFGKDDFTGS-UHFFFAOYSA-N pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)C1CCCN1C(O)=O OAWXZFGKDDFTGS-UHFFFAOYSA-N 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 abstract description 2
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 abstract description 2
- 230000002062 proliferating effect Effects 0.000 abstract description 2
- 102000038030 PI3Ks Human genes 0.000 abstract 1
- 108091007960 PI3Ks Proteins 0.000 abstract 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
Classifications
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161478572P | 2011-04-25 | 2011-04-25 | |
| PCT/US2012/034647 WO2012148846A1 (en) | 2011-04-25 | 2012-04-23 | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201391565A1 EA201391565A1 (ru) | 2014-02-28 |
| EA025948B1 true EA025948B1 (ru) | 2017-02-28 |
Family
ID=46018130
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391565A EA025948B1 (ru) | 2011-04-25 | 2012-04-23 | КОМБИНАЦИЯ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТ-3-КИНАЗЫ (PI3K) И ИНГИБИТОРА mTOR |
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|---|---|
| US (3) | US20140066474A1 (enExample) |
| EP (1) | EP2701703A1 (enExample) |
| JP (2) | JP6086902B2 (enExample) |
| KR (1) | KR101925656B1 (enExample) |
| CN (1) | CN103491955B (enExample) |
| AR (1) | AR086481A1 (enExample) |
| AU (2) | AU2012250010A1 (enExample) |
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| CL (1) | CL2013003078A1 (enExample) |
| CO (1) | CO6801759A2 (enExample) |
| EA (1) | EA025948B1 (enExample) |
| EC (1) | ECSP13012994A (enExample) |
| GT (1) | GT201300263A (enExample) |
| IL (1) | IL229008A (enExample) |
| MA (1) | MA35038B1 (enExample) |
| MX (1) | MX2013012385A (enExample) |
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| PE (1) | PE20140601A1 (enExample) |
| PH (1) | PH12013502077A1 (enExample) |
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| UA (1) | UA110961C2 (enExample) |
| WO (1) | WO2012148846A1 (enExample) |
| ZA (1) | ZA201306973B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2014005414A (es) * | 2011-11-02 | 2014-09-22 | Novartis Ag | Derivados de 2-carboxamida-cicloamino-urea para su uso en el tratamiento de las enfermedades dependientes del factor de crecimiento endotelial vascular (vegf). |
| HK1219421A1 (zh) * | 2013-03-15 | 2017-04-07 | 因特利凯有限责任公司 | 激酶抑制剂的组合及其用途 |
| EA201690987A1 (ru) * | 2013-11-13 | 2016-10-31 | Новартис Аг | Низкодозовые иммуностимулирующие ингибиторы mtor и их применения |
| AU2015216590A1 (en) * | 2014-02-11 | 2016-06-30 | Novartis Ag | Pharmaceutical combinations comprising a PI3K inhibitor for the treatment of cancer |
| WO2015148626A1 (en) * | 2014-03-26 | 2015-10-01 | Millennium Pharmaceuticals, Inc. | Treatment of fibrotic disorders |
| EP3200772B1 (en) * | 2014-10-03 | 2022-08-03 | Novartis AG | Pharmaceutical compositions comprising alpelisib |
| US20160339030A1 (en) * | 2015-05-19 | 2016-11-24 | University Of Maryland, Baltimore | Treatment agents for inhibiting hiv and cancer in hiv infected patients |
| JP6691337B2 (ja) * | 2016-02-29 | 2020-04-28 | 学校法人北里研究所 | 膀胱癌患者の予後を予測するための方法 |
| GB202010627D0 (en) * | 2020-07-10 | 2020-08-26 | Qbd (Qs-Ip) Ltd | Blocking method |
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