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)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 |
|---|---|---|---|---|
| KR101712576B1 (ko) | 2008-11-10 | 2017-03-06 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물 |
| PL3354650T3 (pl) | 2008-12-19 | 2022-06-13 | Vertex Pharmaceuticals Incorporated | Związki przydatne jako inhibitory kinazy atr |
| WO2011143423A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds 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 |
| US9096584B2 (en) | 2010-05-12 | 2015-08-04 | Vertex Pharmaceuticals Incorporated | 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 |
| JP2013526538A (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 |
| JP5836367B2 (ja) | 2010-05-12 | 2015-12-24 | 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Vertex Pharmaceuticals Incorporated | Atrキナーゼ阻害剤として有用な化合物 |
| JP2013529643A (ja) | 2010-06-23 | 2013-07-22 | 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ピロロピラジン誘導体 |
| CA2832100A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| JP2014522818A (ja) | 2011-06-22 | 2014-09-08 | 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 |
| WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| RU2018147217A (ru) | 2011-09-30 | 2019-01-18 | Вертекс Фармасьютикалз Инкорпорейтед | Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr |
| IN2014KN00943A (enExample) | 2011-09-30 | 2015-08-21 | Vertex Pharma | |
| AU2012315384B2 (en) | 2011-09-30 | 2017-08-10 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with ATR inhibitors |
| US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | 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 |
| US8841450B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2776421A1 (en) | 2011-11-09 | 2014-09-17 | 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 |
| US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CN104582795B (zh) | 2012-04-05 | 2018-04-20 | 沃泰克斯药物股份有限公司 | 可用作atr激酶抑制剂的化合物及其组合疗法 |
| US8859553B2 (en) * | 2012-07-30 | 2014-10-14 | Astar Biotech Llc | Protein kinase inhibitors |
| DK2904406T3 (en) | 2012-10-04 | 2018-06-18 | Vertex Pharma | METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE |
| US8912198B2 (en) | 2012-10-16 | 2014-12-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| LT3418281T (lt) | 2012-12-07 | 2021-01-11 | Vertex Pharmaceuticals Inc. | Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui |
| MX2015008010A (es) * | 2012-12-20 | 2016-04-26 | qing-bin Lu | Compuestos radiosensabilizadores para usarse en combinacion con radiacion. |
| WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| HUE046727T2 (hu) | 2013-12-06 | 2020-03-30 | Vertex Pharma | Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai |
| ES2777608T3 (es) | 2014-06-05 | 2020-08-05 | Vertex Pharma | Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo |
| US11179394B2 (en) | 2014-06-17 | 2021-11-23 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of Chk1 and ATR inhibitors |
| 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 |
| US11464774B2 (en) | 2015-09-30 | 2022-10-11 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| EP3936153B1 (en) | 2016-01-11 | 2024-08-21 | 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 |
| WO2018153969A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with radium-223 salt |
| 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 |
| WO2018218197A2 (en) * | 2017-05-26 | 2018-11-29 | 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 |
| HRP20240368T1 (hr) | 2017-07-13 | 2024-08-30 | Board Of Regents, The University Of Texas System | Heterociklički inhibitori atr kinaze |
| EP3661560B1 (en) | 2017-08-04 | 2025-02-26 | Bayer Pharma 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 |
| BR112020008727A2 (pt) | 2017-10-30 | 2020-10-20 | Neuropore Therapies, Inc. | fenil sulfonil fenil triazol tionas substituídas e usos destas |
| WO2019110586A1 (en) | 2017-12-08 | 2019-06-13 | Bayer Aktiengesellschaft | Predictive markers for atr kinase inhibitors |
| JP7341156B2 (ja) | 2018-03-16 | 2023-09-08 | ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム | Atrキナーゼの複素環式阻害剤 |
| CA3114024A1 (en) | 2018-09-26 | 2020-04-02 | Merck Patent Gmbh | Combination of a pd-1 antagonist, an atr inhibitor and a platinating agent for the treatment of cancer |
| JP2022505041A (ja) | 2018-10-15 | 2022-01-14 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | Dnaアルキル化剤及びatr阻害剤を使用する併用療法 |
| EP3866805A1 (en) | 2018-10-16 | 2021-08-25 | 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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| EP2569289A1 (en) | 2013-03-20 |
| US8962631B2 (en) | 2015-02-24 |
| US20120035407A1 (en) | 2012-02-09 |
| WO2011143419A1 (en) | 2011-11-17 |
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