JP6212045B2 - Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス - Google Patents
Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス Download PDFInfo
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- JP6212045B2 JP6212045B2 JP2014533441A JP2014533441A JP6212045B2 JP 6212045 B2 JP6212045 B2 JP 6212045B2 JP 2014533441 A JP2014533441 A JP 2014533441A JP 2014533441 A JP2014533441 A JP 2014533441A JP 6212045 B2 JP6212045 B2 JP 6212045B2
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C251/48—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyrane Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Catalysts (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161541865P | 2011-09-30 | 2011-09-30 | |
| US61/541,865 | 2011-09-30 | ||
| PCT/US2012/058127 WO2013049726A2 (en) | 2011-09-30 | 2012-09-28 | Processes for making compounds useful as inhibitors of atr kinase |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016221714A Division JP6317800B2 (ja) | 2011-09-30 | 2016-11-14 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| JP2017148280A Division JP2017226676A (ja) | 2011-09-30 | 2017-07-31 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014532054A JP2014532054A (ja) | 2014-12-04 |
| JP2014532054A5 JP2014532054A5 (enExample) | 2015-11-12 |
| JP6212045B2 true JP6212045B2 (ja) | 2017-10-11 |
Family
ID=47019163
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014533441A Expired - Fee Related JP6212045B2 (ja) | 2011-09-30 | 2012-09-28 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| JP2016221714A Active JP6317800B2 (ja) | 2011-09-30 | 2016-11-14 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| JP2017148280A Withdrawn JP2017226676A (ja) | 2011-09-30 | 2017-07-31 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| JP2019099224A Pending JP2019172684A (ja) | 2011-09-30 | 2019-05-28 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016221714A Active JP6317800B2 (ja) | 2011-09-30 | 2016-11-14 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| JP2017148280A Withdrawn JP2017226676A (ja) | 2011-09-30 | 2017-07-31 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| JP2019099224A Pending JP2019172684A (ja) | 2011-09-30 | 2019-05-28 | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
Country Status (23)
| Country | Link |
|---|---|
| US (4) | US9035053B2 (enExample) |
| EP (4) | EP2940017B1 (enExample) |
| JP (4) | JP6212045B2 (enExample) |
| KR (2) | KR102013133B1 (enExample) |
| CN (2) | CN103987709B (enExample) |
| AR (1) | AR088092A1 (enExample) |
| AU (3) | AU2012315615A1 (enExample) |
| BR (1) | BR112014007721B1 (enExample) |
| CA (2) | CA2850566C (enExample) |
| ES (1) | ES2751741T3 (enExample) |
| HR (1) | HRP20191641T1 (enExample) |
| HU (1) | HUE046429T2 (enExample) |
| IL (3) | IL231771A0 (enExample) |
| IN (1) | IN2014KN00929A (enExample) |
| MX (1) | MX353461B (enExample) |
| PL (1) | PL2940017T3 (enExample) |
| PT (1) | PT2940017T (enExample) |
| RS (1) | RS59337B1 (enExample) |
| RU (2) | RU2018147217A (enExample) |
| SG (2) | SG10201606774UA (enExample) |
| TW (3) | TWI625328B (enExample) |
| WO (1) | WO2013049726A2 (enExample) |
| ZA (1) | ZA201402625B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017061519A (ja) * | 2011-09-30 | 2017-03-30 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2376485B1 (en) | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| JP2013526540A (ja) | 2010-05-12 | 2013-06-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
| EP2569284B1 (en) | 2010-05-12 | 2015-07-08 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
| KR20130066633A (ko) | 2010-05-12 | 2013-06-20 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물 |
| EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2011143399A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2011163527A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| WO2012138938A1 (en) * | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| US8822469B2 (en) | 2011-06-22 | 2014-09-02 | Vertex Pharmaceuticals Incorporated | Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase |
| US9096602B2 (en) | 2011-06-22 | 2015-08-04 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| IN2014KN00943A (enExample) | 2011-09-30 | 2015-08-21 | Vertex Pharma | |
| EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| BR112014007690B1 (pt) | 2011-09-30 | 2022-10-04 | Vertex Pharmaceuticals Incorporated | Usos de inibidores de atr no tratamento de câncer pancreático e câncer de pulmão de células não pequenas |
| US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071093A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP3311816A1 (en) | 2012-04-05 | 2018-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase for the treatment of cancer |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| PT3157566T (pt) | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| US10570119B2 (en) | 2016-01-11 | 2020-02-25 | Merrimack Pharmaceuticals, Inc. | Inhibiting ataxia telangiectasia and Rad3-related protein (ATR) |
| US10301324B2 (en) | 2016-04-12 | 2019-05-28 | Atrin Pharmaceuticals LLC | Ataxia telengiectasia and rad3-related (ATR) inhibitors and methods of their use |
| EA039513B1 (ru) * | 2017-01-09 | 2022-02-04 | Селатор Фармасьютикалз, Инк. | Ингибитор атаксии-телеангиэкстазии и rad3-родственного белка (atr) и содержащие его липосомные композиции |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| JP2021508700A (ja) * | 2017-12-29 | 2021-03-11 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atr阻害剤を使用するがん処置の方法 |
| IL277071B2 (en) | 2018-03-08 | 2024-07-01 | Incyte Corp | AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| BR112021004935A2 (pt) | 2018-09-26 | 2021-06-01 | Merck Patent Gmbh | combinação de antagonista de pd-1, inibidor de atr e agente de platinação para tratamento de câncer |
| EP3866785A1 (en) | 2018-10-15 | 2021-08-25 | Merck Patent GmbH | Combination therapy utilizing dna alkylating agents and atr inhibitors |
| CA3199472A1 (en) | 2020-10-26 | 2022-05-05 | Merck Patent Gmbh | Atr inhibitors for use in the treatment of viral infections |
| CN117794924A (zh) * | 2021-08-13 | 2024-03-29 | 苏州爱科百发生物医药技术有限公司 | 用作atr激酶抑制剂的化合物 |
| CN115703768B (zh) * | 2021-08-13 | 2024-12-17 | 苏州爱科百发生物医药技术有限公司 | 用作atr激酶抑制剂的化合物 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017061519A (ja) * | 2011-09-30 | 2017-03-30 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
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