JP2009516653A5 - - Google Patents
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- Publication number
- JP2009516653A5 JP2009516653A5 JP2008540168A JP2008540168A JP2009516653A5 JP 2009516653 A5 JP2009516653 A5 JP 2009516653A5 JP 2008540168 A JP2008540168 A JP 2008540168A JP 2008540168 A JP2008540168 A JP 2008540168A JP 2009516653 A5 JP2009516653 A5 JP 2009516653A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- solvate
- hydrate
- acceptable salt
- 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
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000011780 sodium chloride Substances 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 5
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- -1 4-amino-1,2,5-oxadiazol-3-yl Chemical group 0.000 claims 2
- 206010003246 Arthritis Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- RPUIWNOVQULTTN-LBPRGKRZSA-N 4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(2S)-morpholin-2-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol Chemical compound C=12N(CC)C(C=3C(=NON=3)N)=NC2=C(C#CC(C)(C)O)N=CC=1OC[C@@H]1CNCCO1 RPUIWNOVQULTTN-LBPRGKRZSA-N 0.000 claims 1
- GSKKWSGZKLGDHM-LBPRGKRZSA-N 4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(2S)-thiomorpholin-2-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol Chemical compound C=12N(CC)C(C=3C(=NON=3)N)=NC2=C(C#CC(C)(C)O)N=CC=1OC[C@@H]1CNCCS1 GSKKWSGZKLGDHM-LBPRGKRZSA-N 0.000 claims 1
- KGPGFQWBCSZGEL-ZDUSSCGKSA-N 4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(3S)-piperidin-3-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol Chemical compound C=12N(CC)C(C=3C(=NON=3)N)=NC2=C(C#CC(C)(C)O)N=CC=1OC[C@H]1CCCNC1 KGPGFQWBCSZGEL-ZDUSSCGKSA-N 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 201000007815 Bannayan-Riley-Ruvalcaba syndrome Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 201000002847 Cowden syndrome Diseases 0.000 claims 1
- 208000005017 Glioblastoma Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025650 Malignant melanoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims 1
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940121369 angiogenesis inhibitors Drugs 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 230000001946 anti-microtubular Effects 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 230000022131 cell cycle Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 239000002944 hormone and hormone analog Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Substances [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 1
- 229910052697 platinum Inorganic materials 0.000 claims 1
- 230000000861 pro-apoptotic Effects 0.000 claims 1
- 201000002025 prostate sarcoma Diseases 0.000 claims 1
- 102000027656 receptor tyrosine kinases Human genes 0.000 claims 1
- 108091007921 receptor tyrosine kinases Proteins 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73595505P | 2005-11-10 | 2005-11-10 | |
| US77228906P | 2006-02-10 | 2006-02-10 | |
| US82692806P | 2006-09-26 | 2006-09-26 | |
| PCT/US2006/043513 WO2007058850A2 (en) | 2005-11-10 | 2006-11-09 | Inhibitors of akt activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009516653A JP2009516653A (ja) | 2009-04-23 |
| JP2009516653A5 true JP2009516653A5 (US07794700-20100914-C00152.png) | 2009-12-17 |
Family
ID=38049129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008540168A Pending JP2009516653A (ja) | 2005-11-10 | 2006-11-09 | Ａｋｔ活性の阻害剤 |
Country Status (16)
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090227616A1 (en) * | 2005-11-10 | 2009-09-10 | Smithkline Beecham Corporation, A Corporation | Inhibitors of akt activity |
| KR20180001596A (ko) | 2008-01-18 | 2018-01-04 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 체액 내에서 질병 또는 병태의 시그너쳐의 검출 방법 |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| EP2286232B1 (en) * | 2008-05-16 | 2012-02-29 | Cellzome Ag | Methods for the identification of parp interacting molecules and for purification of parp proteins |
| US20110086834A1 (en) * | 2008-06-26 | 2011-04-14 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| JP5702293B2 (ja) | 2008-11-10 | 2015-04-15 | 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 | Ａｔｒキナーゼの阻害剤として有用な化合物 |
| LT3354650T (lt) | 2008-12-19 | 2022-06-27 | Vertex Pharmaceuticals Incorporated | Junginiai, naudingi kaip atr kinazės inhibitoriai |
| RU2012153675A (ru) | 2010-05-12 | 2014-06-20 | Вертекс Фармасьютикалз Инкорпорейтед | Соединения, пригодные в качестве ингибиторов atr киназы |
| EP2568984A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US9062008B2 (en) | 2010-05-12 | 2015-06-23 | 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 |
| EP2569287B1 (en) | 2010-05-12 | 2014-07-09 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| WO2011143422A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
| NZ605627A (en) | 2010-06-23 | 2015-06-26 | Vertex Pharma | Pyrrolo-pyrazine derivatives useful as inhibitors of atr kinase |
| AU2011280936A1 (en) | 2010-07-23 | 2013-02-28 | President And Fellows Of Harvard College | Methods of detecting prenatal or pregnancy-related diseases or conditions |
| SG10201505724SA (en) * | 2010-07-23 | 2015-09-29 | Harvard College | Methods of detecting diseases or conditions using phagocytic cells |
| WO2012012694A2 (en) | 2010-07-23 | 2012-01-26 | President And Fellows Of Harvard College | Methods of detecting autoimmune or immune-related diseases or conditions |
| TW201247650A (en) * | 2011-03-16 | 2012-12-01 | Hoffmann La Roche | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
| EP2694498B1 (en) | 2011-04-05 | 2016-03-30 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| JP2014517079A (ja) | 2011-06-22 | 2014-07-17 | 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 |
| WO2012178124A1 (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 |
| JP6162126B2 (ja) | 2011-09-30 | 2017-08-23 | 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阻害剤による膵臓癌及び非小細胞肺癌の治療 |
| EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013049722A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| ES2751741T3 (es) | 2011-09-30 | 2020-04-01 | Vertex Pharma | Procedimiento para fabricar compuestos útiles como inhibidores de la quinasa ATR |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | 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 |
| US8841337B2 (en) | 2011-11-09 | 2014-09-23 | 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 |
| EP2776419B1 (en) | 2011-11-09 | 2016-05-11 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| SI2833973T1 (en) | 2012-04-05 | 2018-04-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase and their combination therapy |
| EP2904406B1 (en) | 2012-10-04 | 2018-03-21 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
| US8912198B2 (en) | 2012-10-16 | 2014-12-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CA2892608C (en) | 2012-12-07 | 2021-10-19 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2965077B1 (en) | 2013-03-09 | 2022-07-13 | Harry Stylli | Methods of detecting cancer |
| US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| ES2909438T3 (es) | 2013-06-26 | 2022-05-06 | Helmholtz Zentrum Muenchen Deutsches Forschungszentrum Gesundheit & Umwelt Gmbh | Enantiómero (S) de mepacina como inhibidor de paracaspasa (MALT1) para tratar cáncer |
| KR20160104612A (ko) | 2013-07-26 | 2016-09-05 | 업데이트 파마 인코포레이트 | 비산트렌의 치료 효과 개선용 조성물 |
| TWI704146B (zh) * | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物 |
| TWI627173B (zh) | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物 |
| SG10201804791UA (en) | 2013-12-06 | 2018-07-30 | Vertex Pharma | 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 |
| PT3152212T (pt) | 2014-06-05 | 2020-03-13 | Vertex Pharma | Derivados radiomarcados de um composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor de atr quinase, preparação do dito composto e diferentes formas sólidas do mesmo |
| KR20170016498A (ko) | 2014-06-17 | 2017-02-13 | 버텍스 파마슈티칼스 인코포레이티드 | Chk1 및 atr 저해제의 병용물을 사용하는 암의 치료 방법 |
| CA2960574C (en) | 2014-10-23 | 2023-03-07 | Janssen Pharmaceutica Nv | Pyrazolopyrimidine derivatives as nik inhibitors |
| BR112017008045A2 (pt) | 2014-10-23 | 2017-12-19 | Janssen Pharmaceutica Nv | compostos como inibidores de nik |
| US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives as NIK inhibitors |
| BR112017007715B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de tienopirimidina como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
| JP7187308B2 (ja) | 2015-09-30 | 2022-12-12 | 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 | Ｄｎａ損傷剤とａｔｒ阻害剤との組み合わせを使用する、がんを処置するための方法 |
| JP2022512706A (ja) | 2018-10-16 | 2022-02-07 | エフ．ホフマン－ラ ロシュ アーゲー | 眼科におけるＡｋｔ阻害剤の使用 |
| US11071730B2 (en) | 2018-10-31 | 2021-07-27 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| LT3873903T (lt) | 2018-10-31 | 2024-05-10 | Gilead Sciences, Inc. | Pakeistieji 6-azabenzimidazolo junginiai, kaip hpk1 inhibitoriai |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| WO2023187037A1 (en) | 2022-03-31 | 2023-10-05 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
| WO2024083716A1 (en) | 2022-10-17 | 2024-04-25 | Astrazeneca Ab | Combinations of a serd for the treatment of cancer |
| WO2024100236A1 (en) | 2022-11-11 | 2024-05-16 | Astrazeneca Ab | Combination therapies for the treatment of cancer |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200523262A (en) * | 2003-07-29 | 2005-07-16 | Smithkline Beecham Corp | Inhibitors of AKT activity |
-
2006
- 2006-11-08 AR ARP060104898A patent/AR056786A1/es unknown
- 2006-11-08 TW TW095141228A patent/TW200736260A/zh unknown
- 2006-11-09 KR KR1020087011158A patent/KR20080067646A/ko not_active Application Discontinuation
- 2006-11-09 WO PCT/US2006/043513 patent/WO2007058850A2/en active Application Filing
- 2006-11-09 AP AP2008004442A patent/AP2008004442A0/xx unknown
- 2006-11-09 AU AU2006315805A patent/AU2006315805A1/en not_active Abandoned
- 2006-11-09 JP JP2008540168A patent/JP2009516653A/ja active Pending
- 2006-11-09 US US12/093,032 patent/US20100056523A1/en not_active Abandoned
- 2006-11-09 EP EP06837170A patent/EP1948188A4/en not_active Withdrawn
- 2006-11-09 CA CA002629429A patent/CA2629429A1/en not_active Abandoned
- 2006-11-09 BR BRPI0618309-3A patent/BRPI0618309A2/pt not_active Application Discontinuation
- 2006-11-09 EA EA200801301A patent/EA200801301A1/ru unknown
-
2008
- 2008-04-17 IL IL190968A patent/IL190968A0/en unknown
- 2008-05-05 EC EC2008008425A patent/ECSP088425A/es unknown
- 2008-05-05 MA MA30904A patent/MA29935B1/fr unknown
- 2008-05-28 NO NO20082414A patent/NO20082414L/no unknown
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