KR102148681B1 - Pi3 키나제 모듈레이터로서의 헤테로방향족 화합물 - Google Patents
Pi3 키나제 모듈레이터로서의 헤테로방향족 화합물 Download PDFInfo
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- KR102148681B1 KR102148681B1 KR1020157019069A KR20157019069A KR102148681B1 KR 102148681 B1 KR102148681 B1 KR 102148681B1 KR 1020157019069 A KR1020157019069 A KR 1020157019069A KR 20157019069 A KR20157019069 A KR 20157019069A KR 102148681 B1 KR102148681 B1 KR 102148681B1
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- Prior art keywords
- cancer
- alkylene
- compound
- cycloalkyl
- alkyl
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- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title abstract description 60
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- 238000000034 method Methods 0.000 claims abstract description 66
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- 150000003839 salts Chemical class 0.000 claims abstract description 44
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims abstract description 32
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims abstract description 32
- 230000000694 effects Effects 0.000 claims abstract description 23
- 102000001253 Protein Kinase Human genes 0.000 claims abstract description 11
- 108060006633 protein kinase Proteins 0.000 claims abstract description 11
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 8
- -1 5-10 membered heteroaryl Compound Chemical class 0.000 claims description 158
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- 125000001424 substituent group Chemical group 0.000 claims description 49
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- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 34
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 28
- 229940124597 therapeutic agent Drugs 0.000 claims description 28
- 229910052731 fluorine Inorganic materials 0.000 claims description 27
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- 125000005842 heteroatom Chemical group 0.000 claims description 24
- 229910052717 sulfur Inorganic materials 0.000 claims description 24
- 239000003795 chemical substances by application Substances 0.000 claims description 22
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- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 20
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Classifications
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- A—HUMAN NECESSITIES
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/33—Heterocyclic compounds
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
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- C—CHEMISTRY; METALLURGY
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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| RU2018122089A (ru) * | 2015-11-19 | 2019-12-25 | Блюпринт Медсинс Корпорейшн | Соединения и композиции, подходящие для лечения расстройств, связанных с ntrk |
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| MX393780B (es) | 2017-01-17 | 2025-03-24 | Heparegenix Gmbh | Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos |
| WO2018169700A1 (en) * | 2017-03-14 | 2018-09-20 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| CN109867671B (zh) * | 2017-12-02 | 2020-07-07 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途 |
| CN109867668B (zh) * | 2017-12-02 | 2021-03-26 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途 |
| CN109867669B (zh) * | 2017-12-02 | 2021-02-26 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途 |
| CN109867672B (zh) * | 2017-12-02 | 2020-07-07 | 广东东阳光药业有限公司 | 吡唑[1,5-a]吡啶衍生物的盐及其用途 |
| CN109867670B (zh) * | 2017-12-02 | 2020-07-07 | 广东东阳光药业有限公司 | 一种吡唑[1,5-a]吡啶化合物的单钠盐及其医药用途 |
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| EP2958564A1 (en) | 2015-12-30 |
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| MY182036A (en) | 2021-01-18 |
| JP6389829B2 (ja) | 2018-09-12 |
| MX2015010700A (es) | 2017-01-23 |
| RU2015131467A (ru) | 2017-03-24 |
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