RU2019113160A - Соединения пригодные для использования в качестве ингибиторов atr киназы - Google Patents
Соединения пригодные для использования в качестве ингибиторов atr киназы Download PDFInfo
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- RU2019113160A RU2019113160A RU2019113160A RU2019113160A RU2019113160A RU 2019113160 A RU2019113160 A RU 2019113160A RU 2019113160 A RU2019113160 A RU 2019113160A RU 2019113160 A RU2019113160 A RU 2019113160A RU 2019113160 A RU2019113160 A RU 2019113160A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
- C07D487/04—Ortho-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
- C07C45/63—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Condensed Matter Physics & Semiconductors (AREA)
- Crystallography & Structural Chemistry (AREA)
- General Physics & Mathematics (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Claims (49)
1. Способ получения соединения формулы I-1
включающий стадию
a) взаимодействия соединения формулы 6a*
с соединением формулы 27:
при соответствующих условиях образования амидной связи с образованием соединения формулы 28
b) очистку соединения формулы 28 с использованием соответствующего хелатирующего агента для палладия;
c) взаимодействия соединения формулы 28 при соответствующих условиях снятия защиты с образованием соединения формулы 30
d) взаимодействия соединения формулы 30 с соединением формулы 25:
при соответствующих условиях образования амидной связи с образованием соединения формулы I-1.
2. Способ по п.1, в котором соответствующие условия для образования амидной связи включают взаимодействие соединения формулы 30 с соединением формулы 25 в присутствии партнера для образования амидной связи, апротонного растворителя и основания.
3. Соединение по п.2, где апротонный растворитель независимо выбирают из NMP, DMF или тетрагидрофурана.
4. Способ по п.3, в котором апротонный растворитель представляет собой тетрагидрофуран.
5. Способ по п.2, в котором основание представляет собой алифатический амин.
6. Способ по п.5, в котором основание представляет собой DIPEA.
7. Способ по любому из пп.2-6, в котором партнер для образования амидной связи независимо выбирают из CDI, TBTU, или TCTU.
8. Способ по п.7, в котором партнер для образования амидной связи представляет собой TCTU.
9. Способ по п.7, в котором партнер для образования амидной связи представляет собой CDI.
10. Способ по п.1, в котором соответствующие условия снятия защиты включают взаимодействие соединения формулы 28 с кислотой в присутствии растворителя.
11. Способ по п.10, в котором кислота представляет собой HCl.
12. Способ по п.10, в котором растворитель представляет собой 1,4-диоксан.
13. Способ по п.1, в котором соответствующие условия для образования амидной связи включают взаимодействие соединения формулы 6a* с соединением формулы 27 в апротонном растворителе при нагреве.
14. Способ по п.13, в котором апротонный растворитель независимо выбирается из NMP, пиридин или DMF.
15. Способ по п.14, в котором апротонный растворитель представляет собой пиридин.
16. Способ по п.15, в котором реакцию осуществляют при температуре, по меньшей мере, 80°C.
17. Способ по п.1, в котором хелатирующий агент для палладия независимо выбирается из пропан-1,2-диамина; этан-1,2-диамина; этан-1,2-диамина; пропан-1,3-диамина; тетраметилэтилендиамина; этиленгликоля; 1,3-бис(дифенилфосфанил)пропана; 1,4-бис(дифенилфосфанил)бутана; и 1,2-бис(дифенилфосфанил)этан/Pr-1,2-диамина.
18. Способ по п.17, в котором хелатирующий агент для палладия представляет собой пропан-1,2-диамин.
19. Способ получения соединения формулы I-1
включающий стадии
a) взаимодействия соединения формулы 5a
при соответствующих условиях галогенирования с образованием соединения формулы 34
где X представляет собой галоген;
b) взаимодействия соединения формулы 34 с соединением формулы 27
при соответствующих условиях образования амидной связи с образованием соединения формулы 28.
c) взаимодействия соединения формулы 28 при соответствующих условиях снятия защиты с образованием соединения формулы 30
d) взаимодействия соединения формулы 30 с соединением формулы 25
при соответствующих условиях образования амидной связи с образованием соединения формулы I-1.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
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US201361912636P | 2013-12-06 | 2013-12-06 | |
US61/912,636 | 2013-12-06 | ||
US201462008220P | 2014-06-05 | 2014-06-05 | |
US62/008,220 | 2014-06-05 | ||
US201462058819P | 2014-10-02 | 2014-10-02 | |
US62/058,819 | 2014-10-02 |
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RU2016126919A Division RU2687276C2 (ru) | 2013-12-06 | 2014-12-05 | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
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RU2020114516A Division RU2750148C1 (ru) | 2013-12-06 | 2020-04-23 | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
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RU2019113160A true RU2019113160A (ru) | 2019-06-17 |
RU2019113160A3 RU2019113160A3 (ru) | 2019-11-19 |
RU2720408C2 RU2720408C2 (ru) | 2020-04-29 |
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RU2019113160A RU2720408C2 (ru) | 2013-12-06 | 2014-12-05 | Способ получения ингибиторов atr киназы (варианты) |
RU2016126919A RU2687276C2 (ru) | 2013-12-06 | 2014-12-05 | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
RU2020114516A RU2750148C1 (ru) | 2013-12-06 | 2020-04-23 | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
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RU2016126919A RU2687276C2 (ru) | 2013-12-06 | 2014-12-05 | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
RU2020114516A RU2750148C1 (ru) | 2013-12-06 | 2020-04-23 | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
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US (3) | US10160760B2 (ru) |
EP (1) | EP3077397B1 (ru) |
JP (1) | JP6543252B2 (ru) |
KR (1) | KR102153886B1 (ru) |
CN (1) | CN105934435B (ru) |
AU (2) | AU2014360380B2 (ru) |
BR (1) | BR112016012734B1 (ru) |
CA (1) | CA2932757C (ru) |
DK (1) | DK3077397T3 (ru) |
ES (1) | ES2768678T3 (ru) |
HR (1) | HRP20192183T1 (ru) |
HU (1) | HUE046727T2 (ru) |
IL (1) | IL246028B (ru) |
LT (1) | LT3077397T (ru) |
MX (1) | MX370390B (ru) |
PL (1) | PL3077397T3 (ru) |
PT (1) | PT3077397T (ru) |
RS (1) | RS59679B1 (ru) |
RU (3) | RU2720408C2 (ru) |
SG (2) | SG10201804791UA (ru) |
SI (1) | SI3077397T1 (ru) |
WO (1) | WO2015085132A1 (ru) |
ZA (1) | ZA201603893B (ru) |
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