JP2014532751A5 - - Google Patents
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- Publication number
- JP2014532751A5 JP2014532751A5 JP2014540552A JP2014540552A JP2014532751A5 JP 2014532751 A5 JP2014532751 A5 JP 2014532751A5 JP 2014540552 A JP2014540552 A JP 2014540552A JP 2014540552 A JP2014540552 A JP 2014540552A JP 2014532751 A5 JP2014532751 A5 JP 2014532751A5
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- JP
- Japan
- Prior art keywords
- compound according
- cancer
- der
- independently
- compound
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 147
- 150000003839 salts Chemical class 0.000 claims description 25
- 239000011780 sodium chloride Substances 0.000 claims description 25
- 239000012453 solvate Substances 0.000 claims description 25
- -1 hydrate Substances 0.000 claims description 21
- 201000011510 cancer Diseases 0.000 claims description 20
- 230000002401 inhibitory effect Effects 0.000 claims description 15
- 125000001931 aliphatic group Chemical group 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 11
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 101710015564 CHEK1 Proteins 0.000 claims description 9
- 102100019702 CHEK1 Human genes 0.000 claims description 9
- 102000005497 Thymidylate Synthase Human genes 0.000 claims description 8
- 108010067449 Thymidylate Synthase Proteins 0.000 claims description 8
- 239000003112 inhibitor Substances 0.000 claims description 8
- 206010006187 Breast cancer Diseases 0.000 claims description 7
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 7
- 206010025650 Malignant melanoma Diseases 0.000 claims description 7
- 206010029260 Neuroblastoma Diseases 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 201000005202 lung cancer Diseases 0.000 claims description 7
- 201000001441 melanoma Diseases 0.000 claims description 7
- 206010033128 Ovarian cancer Diseases 0.000 claims description 6
- 201000011231 colorectal cancer Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 102000003915 DNA Topoisomerases Human genes 0.000 claims description 4
- 108090000323 DNA Topoisomerases Proteins 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- 210000004688 Microtubules Anatomy 0.000 claims description 4
- 102000028664 Microtubules Human genes 0.000 claims description 4
- 108091022031 Microtubules Proteins 0.000 claims description 4
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 claims description 4
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 claims description 4
- 230000000340 anti-metabolite Effects 0.000 claims description 4
- 239000002256 antimetabolite Substances 0.000 claims description 4
- 229920003013 deoxyribonucleic acid Polymers 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 230000001404 mediated Effects 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 3
- 206010017758 Gastric cancer Diseases 0.000 claims description 3
- 206010020243 Hodgkin's disease Diseases 0.000 claims description 3
- 206010024324 Leukaemias Diseases 0.000 claims description 3
- 206010027476 Metastasis Diseases 0.000 claims description 3
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims description 3
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 3
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims description 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 3
- 206010039491 Sarcoma Diseases 0.000 claims description 3
- 201000005188 adrenal gland cancer Diseases 0.000 claims description 3
- 125000002947 alkylene group Chemical group 0.000 claims description 3
- 201000009036 biliary tract cancer Diseases 0.000 claims description 3
- 201000004101 esophageal cancer Diseases 0.000 claims description 3
- 201000007270 liver cancer Diseases 0.000 claims description 3
- 230000036210 malignancy Effects 0.000 claims description 3
- 201000000349 mediastinal cancer Diseases 0.000 claims description 3
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 3
- 201000011682 nervous system cancer Diseases 0.000 claims description 3
- 201000008968 osteosarcoma Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 201000000849 skin cancer Diseases 0.000 claims description 3
- 201000002314 small intestine cancer Diseases 0.000 claims description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 201000002510 thyroid cancer Diseases 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 210000001072 Colon Anatomy 0.000 claims 1
- 206010038038 Rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 description 9
- 238000004519 manufacturing process Methods 0.000 description 6
- 210000004027 cells Anatomy 0.000 description 5
- 229940079593 drugs Drugs 0.000 description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 3
- 230000002950 deficient Effects 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 230000002062 proliferating Effects 0.000 description 3
- 0 C*(CC1)CC1C(C)=C Chemical compound C*(CC1)CC1C(C)=C 0.000 description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
- 206010059512 Apoptosis Diseases 0.000 description 1
- 210000001672 Ovary Anatomy 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000022131 cell cycle Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 201000011061 large intestine cancer Diseases 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006011 modification reaction Methods 0.000 description 1
- 230000001737 promoting Effects 0.000 description 1
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2014532751A JP2014532751A (ja) | 2014-12-08 |
| JP2014532751A5 true JP2014532751A5 (US20040106767A1-20040603-C00005.png) | 2015-12-10 |
| JP6073910B2 JP6073910B2 (ja) | 2017-02-01 |
Family
ID=47178213
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014540552A Active JP6073910B2 (ja) | 2011-11-09 | 2012-11-09 | ５−（ピリジン−２−イル−アミノ）−ピラジン−２−カルボニトリル化合物及びその治療使用 |
Country Status (10)
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2641693C2 (ru) | 2011-11-09 | 2018-01-22 | Кансер Ресёрч Текнолоджи Лимитед | Соединения 5-(пиридин-2-иламино)-пиразин-2-карбонитрила и их терапевтическое применение |
| RU2659786C2 (ru) | 2012-05-15 | 2018-07-04 | Кансер Ресёрч Текнолоджи Лимитед | 5-[[4-[[морфолин-2-ил]метиламино]-5-(трифторметил)-2-пиридил]амино]пиразин-2-карбонитрил, его терапевтические применения |
| 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 |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| 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 |
Family Cites Families (30)
| 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 |
| DK0836605T3 (da) | 1995-07-06 | 2002-05-13 | Novartis Ag | Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling |
| BR0206161A (pt) | 2001-10-19 | 2005-02-01 | Ortho Mcneil Pharm Inc | 2-fenil benzimidazóis e imidazo-[4,5]-piridinas como inibidores de cds1/chk2 e adjuvantes para quimioterapia ou terapia por radiação no tratamento de câncer |
| IL161576A0 (en) | 2001-10-26 | 2004-09-27 | Aventis Pharma Inc | Benzimidazoles and analogues and their use as protein kinases inhibitors |
| WO2003037898A1 (en) | 2001-10-31 | 2003-05-08 | Bayer Healthcare Ag | Pyrimido [4,5-b] indole derivatives |
| CA2484209C (en) | 2002-05-03 | 2013-06-11 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| WO2003101444A1 (en) | 2002-05-29 | 2003-12-11 | Millennium Pharmaceuticals, Inc. | Diarylurea compounds and derivatives as chk-1 inhibitors for the treatment of cancer |
| EP1651648A4 (en) | 2003-07-29 | 2009-09-02 | Irm Llc | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS |
| CA2542105C (en) | 2003-10-08 | 2011-08-02 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| PT1678166E (pt) | 2003-10-14 | 2009-10-30 | Supergen Inc | Inibidores de proteína-quinase |
| MXPA06003607A (es) | 2003-10-16 | 2006-06-05 | Chiron Corp | Quinazolinas, quinoxalinas, quinolinas e isoquinolinas 2.6-disubstituidas como inhibidores de la cinasa raf para el tratamiento del 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 |
| BRPI0609956A2 (pt) | 2005-04-28 | 2010-05-18 | Supergen Inc | inibidores de proteìna quinase |
| CN101213187B (zh) | 2005-06-28 | 2012-06-06 | 塞诺菲-安万特股份有限公司 | 作为rho-激酶抑制剂的异喹啉衍生物 |
| TWI387592B (zh) * | 2005-08-30 | 2013-03-01 | Novartis Ag | 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法 |
| US7776865B2 (en) | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| CA2673920C (en) | 2006-12-27 | 2015-03-24 | Sanofi-Aventis | Cycloalkylamine substituted isoquinoline derivatives |
| JP5569956B2 (ja) | 2007-03-16 | 2014-08-13 | ザ スクリプス リサーチ インスティテュート | 接着斑キナーゼのインヒビター |
| 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 |
| GB0719644D0 (en) | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB0803018D0 (en) | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| JP5599784B2 (ja) * | 2008-06-11 | 2014-10-01 | ジェネンテック， インコーポレイテッド | ジアザカルバゾール類と使用方法 |
| RU2641693C2 (ru) | 2011-11-09 | 2018-01-22 | Кансер Ресёрч Текнолоджи Лимитед | Соединения 5-(пиридин-2-иламино)-пиразин-2-карбонитрила и их терапевтическое применение |
| RU2659786C2 (ru) | 2012-05-15 | 2018-07-04 | Кансер Ресёрч Текнолоджи Лимитед | 5-[[4-[[морфолин-2-ил]метиламино]-5-(трифторметил)-2-пиридил]амино]пиразин-2-карбонитрил, его терапевтические применения |
-
2012
- 2012-11-09 RU RU2014121334A patent/RU2641693C2/ru active
- 2012-11-09 CA CA2849566A patent/CA2849566C/en active Active
- 2012-11-09 AU AU2012335409A patent/AU2012335409B2/en active Active
- 2012-11-09 BR BR112014010938A patent/BR112014010938A2/pt not_active IP Right Cessation
- 2012-11-09 CN CN201280055367.2A patent/CN104105696B/zh active Active
- 2012-11-09 JP JP2014540552A patent/JP6073910B2/ja active Active
- 2012-11-09 US US14/356,626 patent/US9040540B2/en active Active
- 2012-11-09 ES ES12784666T patent/ES2709003T3/es active Active
- 2012-11-09 WO PCT/GB2012/052786 patent/WO2013068755A1/en active Application Filing
- 2012-11-09 EP EP12784666.5A patent/EP2776417B1/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 active Active
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