JP2013526539A - Atrキナーゼ阻害剤として有用なピラジン - Google Patents
Atrキナーゼ阻害剤として有用なピラジン Download PDFInfo
- Publication number
- JP2013526539A JP2013526539A JP2013510296A JP2013510296A JP2013526539A JP 2013526539 A JP2013526539 A JP 2013526539A JP 2013510296 A JP2013510296 A JP 2013510296A JP 2013510296 A JP2013510296 A JP 2013510296A JP 2013526539 A JP2013526539 A JP 2013526539A
- Authority
- JP
- Japan
- Prior art keywords
- aliphatic
- compound
- cancer
- compound according
- alkyl
- 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.)
- Pending
Links
- 0 *c1ncc(N)nc1C(Nc1ccccc1)=O Chemical compound *c1ncc(N)nc1C(Nc1ccccc1)=O 0.000 description 1
- FBYUCYIVLCKFGO-ONEGZZNKSA-N C/C=C/c(nc1-c2nc(ccc(C)c3)c3[nH]2)cnc1N Chemical compound C/C=C/c(nc1-c2nc(ccc(C)c3)c3[nH]2)cnc1N FBYUCYIVLCKFGO-ONEGZZNKSA-N 0.000 description 1
- ATRCFFDRJPZWFK-UHFFFAOYSA-N CN(CC1)CCN1c1cc(Nc2nc(C(Nc3ccccc3)=O)c(N)nc2)ccc1 Chemical compound CN(CC1)CCN1c1cc(Nc2nc(C(Nc3ccccc3)=O)c(N)nc2)ccc1 ATRCFFDRJPZWFK-UHFFFAOYSA-N 0.000 description 1
- INCSQLZZXBPATR-UHFFFAOYSA-N COC(c1c(N)nccn1)=O Chemical compound COC(c1c(N)nccn1)=O INCSQLZZXBPATR-UHFFFAOYSA-N 0.000 description 1
- CNXSIRHOIFRMOB-UHFFFAOYSA-N COC(c1nc(Br)cnc1N)=O Chemical compound COC(c1nc(Br)cnc1N)=O CNXSIRHOIFRMOB-UHFFFAOYSA-N 0.000 description 1
- UWHOUQGLFIVGKW-UHFFFAOYSA-N Cc(cc1)cc2c1nc(-c1nc(NC(CC#N)=O)cnc1N)[nH]2 Chemical compound Cc(cc1)cc2c1nc(-c1nc(NC(CC#N)=O)cnc1N)[nH]2 UWHOUQGLFIVGKW-UHFFFAOYSA-N 0.000 description 1
- CAELIUDQACEMGX-UHFFFAOYSA-N Cc(nc1)c(C(Nc(cccc2)c2OC)=O)nc1N Chemical compound Cc(nc1)c(C(Nc(cccc2)c2OC)=O)nc1N CAELIUDQACEMGX-UHFFFAOYSA-N 0.000 description 1
- XWCYVCRFSFOMDJ-UHFFFAOYSA-N Cc1ccc2nc(-c3nc(Br)cnc3N)[nH]c2c1 Chemical compound Cc1ccc2nc(-c3nc(Br)cnc3N)[nH]c2c1 XWCYVCRFSFOMDJ-UHFFFAOYSA-N 0.000 description 1
- JZNWUXZWEPEKHO-UHFFFAOYSA-N Nc(c(-c1nc2ccccc2[nH]1)n1)ncc1Sc1cccc(F)c1 Chemical compound Nc(c(-c1nc2ccccc2[nH]1)n1)ncc1Sc1cccc(F)c1 JZNWUXZWEPEKHO-UHFFFAOYSA-N 0.000 description 1
- RSFJAMFLTSNZHU-UHFFFAOYSA-N Nc(c(C(NNC(c1ccccc1)=O)=O)n1)ncc1Br Chemical compound Nc(c(C(NNC(c1ccccc1)=O)=O)n1)ncc1Br RSFJAMFLTSNZHU-UHFFFAOYSA-N 0.000 description 1
- ICSNLGPSRYBMBD-UHFFFAOYSA-N Nc1ccccn1 Chemical compound Nc1ccccn1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33385210P | 2010-05-12 | 2010-05-12 | |
| US61/333,852 | 2010-05-12 | ||
| PCT/US2011/036239 WO2011143419A1 (en) | 2010-05-12 | 2011-05-12 | Pyrazines useful as inhibitors of atr kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013526539A true JP2013526539A (ja) | 2013-06-24 |
| JP2013526539A5 JP2013526539A5 (enExample) | 2014-06-26 |
Family
ID=44628457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013510296A Pending JP2013526539A (ja) | 2010-05-12 | 2011-05-12 | Atrキナーゼ阻害剤として有用なピラジン |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US8962631B2 (enExample) |
| EP (1) | EP2569289A1 (enExample) |
| JP (1) | JP2013526539A (enExample) |
| WO (1) | WO2011143419A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2020217733A1 (enExample) * | 2019-04-26 | 2020-10-29 |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011004953A (es) | 2008-11-10 | 2011-12-14 | Vertex Pharma | Compuestos utiles como inhibidores de cinasa atr. |
| ES2921576T3 (es) | 2008-12-19 | 2022-08-29 | Vertex Pharma | Compuestos útiles como inhibidores de la quinasa ATR |
| EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| EP2569313A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8969356B2 (en) | 2010-05-12 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2011143419A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
| US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| NZ603478A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
| EP2585468A1 (en) | 2010-06-23 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| AU2012240030A1 (en) | 2011-04-05 | 2013-10-24 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of TRA kinase |
| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| RU2018108589A (ru) | 2011-09-30 | 2019-02-25 | Вертекс Фармасьютикалз Инкорпорейтед | Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr |
| CA2850564A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013049720A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP3878851A1 (en) | 2011-09-30 | 2021-09-15 | Vertex Pharmaceuticals Incorporated | Process for making 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 |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| EP2776429A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2015502925A (ja) | 2011-11-09 | 2015-01-29 | 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ピラジン化合物 |
| PT2833973T (pt) | 2012-04-05 | 2017-12-21 | Vertex Pharma | Compostos úteis como inibidores da cinase atr e terapias de combinação dos mesmos |
| US8859553B2 (en) * | 2012-07-30 | 2014-10-14 | Astar Biotech Llc | Protein kinase inhibitors |
| WO2014055756A1 (en) | 2012-10-04 | 2014-04-10 | 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 |
| WO2014089379A1 (en) | 2012-12-07 | 2014-06-12 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| BR112015014855A2 (pt) * | 2012-12-20 | 2017-07-11 | Qing Bin Lu | compostos radiossensibilizadores para uso em combinação com radiação |
| US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2015085132A1 (en) | 2013-12-06 | 2015-06-11 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| HRP20200186T1 (hr) | 2014-06-05 | 2020-05-29 | Vertex Pharmaceuticals Inc. | Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici |
| JP6936007B2 (ja) | 2014-06-17 | 2021-09-15 | 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 | Chk1阻害剤とatr阻害剤との組み合わせを使用してがんを処置する方法 |
| TWI656121B (zh) | 2014-08-04 | 2019-04-11 | 德商拜耳製藥公司 | 2-(嗎啉-4-基)-1,7-萘啶 |
| WO2016207345A1 (en) * | 2015-06-24 | 2016-12-29 | Pierre Fabre Medicament | 3-amino-pyrazin-2-yl carboxamide and 2-amino-pyridin-3-yl carboxamide derivatives as polo-like kinase 1 (plk-1) inhibitors for the treatment of cancer |
| EP3355926B1 (en) | 2015-09-30 | 2025-12-24 | Vertex Pharmaceuticals Inc. | Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using |
| ES2997263T3 (en) | 2016-01-11 | 2025-02-14 | Celator Pharmaceuticals Inc | Inhibiting ataxia telangiectasia and rad3-related protein (atr) |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| TW201840319A (zh) | 2017-02-24 | 2018-11-16 | 德商拜耳廠股份有限公司 | Atr激酶抑制劑與鐳-223鹽之組合 |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| US10421765B2 (en) | 2017-05-26 | 2019-09-24 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of ATR kinase |
| US10377591B2 (en) | 2017-07-07 | 2019-08-13 | Zebra Technologies Corporation | Input handling for media processing devices |
| DK3651768T3 (da) | 2017-07-13 | 2024-03-18 | Univ Texas | Heterocykliske inhibitorer af atr-kinase |
| US11690911B2 (en) | 2017-08-04 | 2023-07-04 | Bayer Aktiengesellschaft | Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| AU2018359224B2 (en) | 2017-10-30 | 2023-10-05 | Neuropore Therapies, Inc. | Substituted phenyl sulfonyl phenyl triazole thiones and uses thereof |
| US11712440B2 (en) | 2017-12-08 | 2023-08-01 | Bayer Aktiengesellschaft | Predictive markers for ATR kinase inhibitors |
| CN112218631B (zh) | 2018-03-16 | 2023-12-22 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| 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 |
| US20210369724A1 (en) | 2018-10-16 | 2021-12-02 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| CA3181279A1 (en) | 2022-03-24 | 2023-09-24 | Bloom Energy Corporation | Fuel cell stack assembly including heat sink inserts |
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Also Published As
| Publication number | Publication date |
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| EP2569289A1 (en) | 2013-03-20 |
| WO2011143419A1 (en) | 2011-11-17 |
| US8962631B2 (en) | 2015-02-24 |
| US20120035407A1 (en) | 2012-02-09 |
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