CN104105696B - 5‑(吡啶‑2‑基‑氨基)‑吡嗪‑2‑腈化合物及其治疗用途 - Google Patents
5‑(吡啶‑2‑基‑氨基)‑吡嗪‑2‑腈化合物及其治疗用途 Download PDFInfo
- Publication number
- CN104105696B CN104105696B CN201280055367.2A CN201280055367A CN104105696B CN 104105696 B CN104105696 B CN 104105696B CN 201280055367 A CN201280055367 A CN 201280055367A CN 104105696 B CN104105696 B CN 104105696B
- Authority
- CN
- China
- Prior art keywords
- compound
- compound according
- papc
- inhibitor
- following formula
- 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.)
- Expired - Fee Related
Links
- 0 C[C@](CN(C)*)Oc1c(C#N)ncc(N(C)c(nc2)cc(*)c2-c2c[n](C)nc2)n1 Chemical compound C[C@](CN(C)*)Oc1c(C#N)ncc(N(C)c(nc2)cc(*)c2-c2c[n](C)nc2)n1 0.000 description 15
- BRNWLHZAXFTSIC-CQSZACIVSA-N CC(C)(C#Cc(c(NC)c1)cnc1Nc1nc(O[C@H]2CNCC2)c(C#N)nc1)O Chemical compound CC(C)(C#Cc(c(NC)c1)cnc1Nc1nc(O[C@H]2CNCC2)c(C#N)nc1)O BRNWLHZAXFTSIC-CQSZACIVSA-N 0.000 description 1
- DRSMNQZNUICKHG-UHFFFAOYSA-N CC(CN(C)C)Oc1c(C#N)ncc(N(C)c(nc2)cc3c2c(Cl)ccc3)n1 Chemical compound CC(CN(C)C)Oc1c(C#N)ncc(N(C)c(nc2)cc3c2c(Cl)ccc3)n1 DRSMNQZNUICKHG-UHFFFAOYSA-N 0.000 description 1
- UCNGGGYMLHAMJG-UHFFFAOYSA-N CC1(C)OB(c2c[n](C)nc2)OC1(C)C Chemical compound CC1(C)OB(c2c[n](C)nc2)OC1(C)C UCNGGGYMLHAMJG-UHFFFAOYSA-N 0.000 description 1
- SIXBNTXJJILJTJ-UHFFFAOYSA-N CNc1cc(Nc2nc(OC3CN(C)CC3)c(C#N)nc2)ncc1[AlH2] Chemical compound CNc1cc(Nc2nc(OC3CN(C)CC3)c(C#N)nc2)ncc1[AlH2] SIXBNTXJJILJTJ-UHFFFAOYSA-N 0.000 description 1
- SULISRUYVHVEAK-UHFFFAOYSA-N C[n]1ncc(-c(c(OC)c2)cnc2Cl)c1 Chemical compound C[n]1ncc(-c(c(OC)c2)cnc2Cl)c1 SULISRUYVHVEAK-UHFFFAOYSA-N 0.000 description 1
- DEJUUKULVAIMNF-UHFFFAOYSA-N Nc1cc(Cl)ncc1I Chemical compound Nc1cc(Cl)ncc1I DEJUUKULVAIMNF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D401/00—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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
- A61N2005/1092—Details
- A61N2005/1098—Enhancing the effect of the particle by an injected agent or implanted device
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Pathology (AREA)
- Radiology & Medical Imaging (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (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 |
|---|---|---|---|
| US201161557457P | 2011-11-09 | 2011-11-09 | |
| US61/557,457 | 2011-11-09 | ||
| PCT/GB2012/052786 WO2013068755A1 (en) | 2011-11-09 | 2012-11-09 | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104105696A CN104105696A (zh) | 2014-10-15 |
| CN104105696B true CN104105696B (zh) | 2017-11-14 |
Family
ID=47178213
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280055367.2A Expired - Fee Related CN104105696B (zh) | 2011-11-09 | 2012-11-09 | 5‑(吡啶‑2‑基‑氨基)‑吡嗪‑2‑腈化合物及其治疗用途 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US9040540B2 (enExample) |
| EP (1) | EP2776417B1 (enExample) |
| JP (1) | JP6073910B2 (enExample) |
| CN (1) | CN104105696B (enExample) |
| AU (1) | AU2012335409B2 (enExample) |
| BR (1) | BR112014010938A2 (enExample) |
| CA (1) | CA2849566C (enExample) |
| ES (1) | ES2709003T3 (enExample) |
| RU (1) | RU2641693C2 (enExample) |
| WO (1) | WO2013068755A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013068755A1 (en) | 2011-11-09 | 2013-05-16 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| JP6027230B2 (ja) | 2012-05-15 | 2016-11-16 | キャンサー・リサーチ・テクノロジー・リミテッド | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
| CZ306322B6 (cs) | 2014-12-17 | 2016-11-30 | Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové | Substituovaný 2-(2-fenylhydrazinyl)pyrazin, způsob jeho přípravy, jeho použití a farmaceutický přípravek ho obsahující |
| TW202340194A (zh) | 2017-02-16 | 2023-10-16 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| TWI721483B (zh) | 2018-07-13 | 2021-03-11 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| CN110872277B (zh) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-取代芳环-2-氨基嘧啶类化合物及用途 |
| CN120441567A (zh) | 2020-04-07 | 2025-08-08 | Crt先锋基金有限公司 | Chk1抑制剂的合成方法 |
| US12245355B2 (en) | 2021-02-19 | 2025-03-04 | Mevion Medical Systems, Inc. | Gantry for a particle therapy system |
| WO2026108771A2 (en) * | 2024-11-19 | 2026-05-28 | Groovy Medicine (Hangzhou) Ltd. | Substituted heteroaromatic compounds as inhibitors of checkpoint kinase 1 and notch signaling pathway and uses thereof |
| WO2026108769A1 (en) | 2024-11-19 | 2026-05-28 | Groovy Medicine (Hangzhou) Ltd. | Substituted 2- [ (5-cyanopyrazin-2-yl) amino] pyridines, their prodrugs and uses thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009044162A1 (en) * | 2007-10-05 | 2009-04-09 | Cancer Research Technology Limited | Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine compounds and their use |
| WO2009103966A1 (en) * | 2008-02-19 | 2009-08-27 | Cancer Research Technology Limited | Bicyclylaryl-aryl-amine compounds and their use |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773778A (en) | 1972-01-24 | 1973-11-20 | Squibb & Sons Inc | Sulfur derivatives of pyrazolo (3,4-b)pyridines |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| PL188959B1 (pl) | 1995-07-06 | 2005-05-31 | Novartis Ag | Pirolopirymidyny i sposoby ich wytwarzania |
| JP4637481B2 (ja) | 2001-10-19 | 2011-02-23 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | Ｃｄｓ１／ｃｈｋ２阻害剤および癌治療における化学療法または放射線療法の補助剤としての２−フェニルベンズイミダゾールおよびイミダゾ−［４，５］−ピリジン |
| IL161576A0 (en) | 2001-10-26 | 2004-09-27 | Aventis Pharma Inc | Benzimidazoles and analogues and their use as protein kinases inhibitors |
| CA2464934A1 (en) | 2001-10-31 | 2003-05-08 | Bayer Healthcare Ag | Pyrimido [4,5-b] indole derivatives |
| AU2003234464B2 (en) | 2002-05-03 | 2009-06-04 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| AU2003243318A1 (en) | 2002-05-29 | 2003-12-19 | Millennium Pharmaceuticals, Inc. | Diarylurea compounds and derivatives as chk-1 inhibitors for the treatment of cancer |
| AU2004260689B8 (en) | 2003-07-29 | 2008-05-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| WO2005034869A2 (en) | 2003-10-08 | 2005-04-21 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| WO2005037825A2 (en) | 2003-10-14 | 2005-04-28 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein kinase inhibitors |
| WO2005037285A1 (en) | 2003-10-16 | 2005-04-28 | Chiron Corporation | 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines as inhibitors of raf kinase for treatment of cancer |
| US20050096324A1 (en) | 2003-11-05 | 2005-05-05 | Zhi-Fu Tao | Macrocyclic kinase inhibitors |
| US7163939B2 (en) | 2003-11-05 | 2007-01-16 | Abbott Laboratories | Macrocyclic kinase inhibitors |
| US7642354B2 (en) | 2004-04-13 | 2010-01-05 | Icagen, Inc. | Polycyclic pyrazines as potassium ion channel modulators |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| CN101189239A (zh) | 2005-04-28 | 2008-05-28 | 休普基因公司 | 蛋白激酶抑制剂 |
| EP1899322B1 (en) | 2005-06-28 | 2009-09-02 | Sanofi-Aventis | Isoquinoline derivatives as inhibitors of rho-kinase |
| PE20070335A1 (es) * | 2005-08-30 | 2007-04-21 | Novartis Ag | Benzimidazoles sustituidos y metodos para su preparacion |
| PE20070543A1 (es) | 2005-10-06 | 2007-06-14 | Schering Corp | Pirazolopirimidinas como inhibidores de protein quinasas |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| AU2007338410B2 (en) | 2006-12-27 | 2012-08-16 | Sanofi-Aventis | Cycloalkylamine substituted isoquinoline derivatives |
| EP2134689B1 (en) | 2007-03-16 | 2014-04-23 | The Scripps Research Institute | Inhibitors of focal adhesion kinase |
| WO2008117050A1 (en) | 2007-03-27 | 2008-10-02 | Astrazeneca Ab | Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer |
| US8618121B2 (en) | 2007-07-02 | 2013-12-31 | Cancer Research Technology Limited | 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors |
| PE20110365A1 (es) * | 2008-06-11 | 2011-07-11 | Genentech Inc | Diazacarbazoles como inhibidores de checkpoint quinasa 1 (chk1) |
| WO2013068755A1 (en) | 2011-11-09 | 2013-05-16 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| JP6027230B2 (ja) | 2012-05-15 | 2016-11-16 | キャンサー・リサーチ・テクノロジー・リミテッド | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
-
2012
- 2012-11-09 WO PCT/GB2012/052786 patent/WO2013068755A1/en not_active Ceased
- 2012-11-09 AU AU2012335409A patent/AU2012335409B2/en not_active Ceased
- 2012-11-09 CN CN201280055367.2A patent/CN104105696B/zh not_active Expired - Fee Related
- 2012-11-09 US US14/356,626 patent/US9040540B2/en active Active
- 2012-11-09 RU RU2014121334A patent/RU2641693C2/ru active
- 2012-11-09 JP JP2014540552A patent/JP6073910B2/ja active Active
- 2012-11-09 ES ES12784666T patent/ES2709003T3/es active Active
- 2012-11-09 BR BR112014010938A patent/BR112014010938A2/pt not_active IP Right Cessation
- 2012-11-09 EP EP12784666.5A patent/EP2776417B1/en active Active
- 2012-11-09 CA CA2849566A patent/CA2849566C/en active Active
-
2015
- 2015-04-22 US US14/693,307 patent/US9403797B2/en active Active
-
2016
- 2016-06-24 US US15/191,967 patent/US9765059B2/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009044162A1 (en) * | 2007-10-05 | 2009-04-09 | Cancer Research Technology Limited | Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine compounds and their use |
| WO2009103966A1 (en) * | 2008-02-19 | 2009-08-27 | Cancer Research Technology Limited | Bicyclylaryl-aryl-amine compounds and their use |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2641693C2 (ru) | 2018-01-22 |
| US20160304493A1 (en) | 2016-10-20 |
| EP2776417A1 (en) | 2014-09-17 |
| JP6073910B2 (ja) | 2017-02-01 |
| US9403797B2 (en) | 2016-08-02 |
| CA2849566A1 (en) | 2013-05-16 |
| RU2014121334A (ru) | 2015-12-20 |
| CN104105696A (zh) | 2014-10-15 |
| EP2776417B1 (en) | 2018-10-31 |
| AU2012335409B2 (en) | 2017-07-13 |
| US20140315925A1 (en) | 2014-10-23 |
| BR112014010938A2 (pt) | 2017-05-16 |
| CA2849566C (en) | 2021-02-09 |
| WO2013068755A1 (en) | 2013-05-16 |
| JP2014532751A (ja) | 2014-12-08 |
| AU2012335409A1 (en) | 2014-04-17 |
| ES2709003T3 (es) | 2019-04-12 |
| US9765059B2 (en) | 2017-09-19 |
| US9040540B2 (en) | 2015-05-26 |
| US20150225372A1 (en) | 2015-08-13 |
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| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20171114 |
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| CF01 | Termination of patent right due to non-payment of annual fee |