JP2010526814A5 - - Google Patents
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- Publication number
- JP2010526814A5 JP2010526814A5 JP2010507532A JP2010507532A JP2010526814A5 JP 2010526814 A5 JP2010526814 A5 JP 2010526814A5 JP 2010507532 A JP2010507532 A JP 2010507532A JP 2010507532 A JP2010507532 A JP 2010507532A JP 2010526814 A5 JP2010526814 A5 JP 2010526814A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- halo
- trifluoromethyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- -1 4-Fluoro-3-trifluoromethyl-phenyl Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- UEGFNRZYLNKXAD-UHFFFAOYSA-N 4-methylbenzenesulfonic acid;pyrimidine Chemical compound C1=CN=CN=C1.CC1=CC=C(S(O)(=O)=O)C=C1 UEGFNRZYLNKXAD-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000000112 colonic effect Effects 0.000 claims 1
- 210000004907 gland Anatomy 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91733107P | 2007-05-11 | 2007-05-11 | |
| US60/917,331 | 2007-05-11 | ||
| PCT/US2008/062143 WO2008140947A1 (en) | 2007-05-11 | 2008-05-01 | P70 s6 kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010526814A JP2010526814A (ja) | 2010-08-05 |
| JP2010526814A5 true JP2010526814A5 (enExample) | 2011-06-16 |
| JP5503532B2 JP5503532B2 (ja) | 2014-05-28 |
Family
ID=39765082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010507532A Expired - Fee Related JP5503532B2 (ja) | 2007-05-11 | 2008-05-01 | Ｐ７０ｓ６キナーゼ阻害剤 |
Country Status (33)
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
| US8252791B2 (en) * | 2008-08-13 | 2012-08-28 | Jenrin Discovery, Inc. | Purine compounds as cannabinoid receptor blockers |
| MX2011005003A (es) * | 2008-11-11 | 2011-05-25 | Lilly Co Eli | Inhibidor de p70 s6 quinasa y terapia de combinacion de inhibidor de mtor. |
| CN102209538B (zh) * | 2008-11-11 | 2013-06-12 | 伊莱利利公司 | P70 s6激酶抑制剂和egfr抑制剂的组合治疗剂 |
| AR074072A1 (es) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
| KR101699991B1 (ko) | 2009-02-11 | 2017-01-26 | 메르크 파텐트 게엠베하 | 신규의 아미노 아자헤테로시클릭 카르복사미드 |
| EA020302B1 (ru) | 2009-08-07 | 2014-10-30 | Мерк Патент Гмбх | Новые азагетероциклические соединения |
| MX2012004780A (es) * | 2009-10-23 | 2012-08-23 | Lilly Co Eli | Inhibidores de akt. |
| EP2531194B1 (en) | 2010-02-03 | 2018-04-18 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| ES2729754T3 (es) | 2010-07-29 | 2019-11-06 | Merck Patent Gmbh | Carboxamidas azaheterocíclicas de aminas cíclicas |
| UA110113C2 (xx) | 2010-07-29 | 2015-11-25 | Біциклічні азагетероциклічні карбоксаміди | |
| SI2643313T1 (sl) | 2010-11-24 | 2016-11-30 | Merck Patent Gmbh | Kinazolin-karboksamidni azetidini |
| LT2755965T (lt) * | 2011-09-12 | 2017-11-10 | Merck Patent Gmbh | Naujieji imidazolo aminai kaip kinazės aktyvumo moduliatoriai |
| KR101992505B1 (ko) | 2011-09-12 | 2019-06-24 | 메르크 파텐트 게엠베하 | 키나아제 활성의 조절제로서 용도를 위한 아미노피리미딘 유도체 |
| MX2015002887A (es) * | 2012-09-06 | 2015-07-06 | Plexxikon Inc | Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello. |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US9580443B2 (en) | 2012-11-16 | 2017-02-28 | Merck Patent Gmbh | Heterocyclic derivatives as modulators of kinase activity |
| CN110078743A (zh) * | 2012-11-16 | 2019-08-02 | 默克专利有限公司 | 用作激酶活性调节剂的新颖的咪唑-哌啶基衍生物 |
| MX2015006516A (es) | 2012-11-29 | 2015-08-14 | Merck Patent Gmbh | Derivados de azaquinolin-carboxamida. |
| EP2970201B1 (en) * | 2013-03-11 | 2019-06-19 | Merck Patent GmbH | 6-[4-(1h-imidazol-2-yl)piperidin-1-yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| HK1221150A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用二氢吡嗪并-吡嗪类对癌症的治疗 |
| BR112015026021A2 (pt) | 2013-04-17 | 2017-07-25 | Signal Pharm Llc | terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer |
| WO2014172436A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| JP2016516815A (ja) | 2013-04-17 | 2016-06-09 | シグナル ファーマシューティカルズ，エルエルシー | １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オンに関する医薬製剤、プロセス、固形形態、及び使用方法 |
| WO2014172431A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| BR112015026238A8 (pt) | 2013-04-17 | 2019-12-24 | Signal Pharm Llc | composto dihidropirazino-pirazina, composição farmacêutica que o compreende, uso do composto, métodos para inibir ou medir a fosforilação e para inibir a atividade da proteína quinase, bem como kit |
| TWI631949B (zh) | 2013-04-17 | 2018-08-11 | 標誌製藥公司 | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| WO2014193912A1 (en) | 2013-05-29 | 2014-12-04 | Signal Pharmaceuticals, Llc | Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| WO2015134536A1 (en) * | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US9980966B2 (en) | 2014-04-03 | 2018-05-29 | Merck Patent Gmbh | Combinations of cancer therapeutics |
| US9512129B2 (en) | 2014-04-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| WO2016040078A1 (en) * | 2014-09-10 | 2016-03-17 | Eli Lilly And Company | Substituted phenyl imidazolyl piperidyl compounds as p70s6k1 inhibitors |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN106187899B (zh) * | 2016-06-28 | 2019-07-16 | 绍兴文理学院 | 一种氟代氮杂芳烃的合成方法 |
| AU2018289539B2 (en) | 2017-06-22 | 2024-07-04 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis B virus infection |
| KR20230110296A (ko) | 2020-11-16 | 2023-07-21 | 메르크 파텐트 게엠베하 | 암 치료를 위한 키나제 억제제 조합 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL1004346C2 (nl) | 1996-10-23 | 1998-04-24 | Dsm Nv | Werkwijze voor het scheiden van een mengsel van enantiomeren in een geschikt oplosmiddel. |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| WO2006071819A1 (en) | 2004-12-28 | 2006-07-06 | Exelixis, Inc. | [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| JP5114395B2 (ja) | 2005-06-30 | 2013-01-09 | プロシディオン・リミテッド | Ｇｐｃｒアゴニスト |
| WO2007125310A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| ES2878130T3 (es) | 2006-04-25 | 2021-11-18 | Astex Therapeutics Ltd | Derivados de purina y deazapurina como compuestos farmacéuticos |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
-
2008
- 2008-01-05 UA UAA200911422A patent/UA99284C2/ru unknown
- 2008-04-23 TW TW097114908A patent/TWI423805B/zh not_active IP Right Cessation
- 2008-04-29 AR ARP080101808A patent/AR066344A1/es unknown
- 2008-04-29 CL CL2008001230A patent/CL2008001230A1/es unknown
- 2008-04-29 PE PE2008000756A patent/PE20090887A1/es not_active Application Discontinuation
- 2008-05-01 KR KR1020097023455A patent/KR101088219B1/ko not_active Expired - Fee Related
- 2008-05-01 CN CN2008800156864A patent/CN101679439B/zh not_active Expired - Fee Related
- 2008-05-01 MX MX2009012075A patent/MX2009012075A/es active IP Right Grant
- 2008-05-01 HR HRP20140611AT patent/HRP20140611T1/hr unknown
- 2008-05-01 MY MYPI20094763A patent/MY154898A/en unknown
- 2008-05-01 BR BRPI0811212-6A2A patent/BRPI0811212A2/pt not_active IP Right Cessation
- 2008-05-01 ES ES08747285.8T patent/ES2483726T3/es active Active
- 2008-05-01 EA EA200971051A patent/EA016445B1/ru not_active IP Right Cessation
- 2008-05-01 DK DK08747285.8T patent/DK2148880T3/da active
- 2008-05-01 AU AU2008251692A patent/AU2008251692B2/en not_active Ceased
- 2008-05-01 EP EP08747285.8A patent/EP2148880B1/en active Active
- 2008-05-01 WO PCT/US2008/062143 patent/WO2008140947A1/en not_active Ceased
- 2008-05-01 SI SI200831223T patent/SI2148880T1/sl unknown
- 2008-05-01 JP JP2010507532A patent/JP5503532B2/ja not_active Expired - Fee Related
- 2008-05-01 PT PT87472858T patent/PT2148880E/pt unknown
- 2008-05-01 RS RS20140385A patent/RS53451B/sr unknown
- 2008-05-01 PL PL08747285T patent/PL2148880T3/pl unknown
- 2008-05-01 CA CA2687265A patent/CA2687265C/en not_active Expired - Fee Related
- 2008-05-01 NZ NZ580423A patent/NZ580423A/en not_active IP Right Cessation
-
2009
- 2009-03-02 US US12/396,103 patent/US8093383B2/en not_active Expired - Fee Related
- 2009-10-15 IL IL201564A patent/IL201564A/en not_active IP Right Cessation
- 2009-10-28 TN TNP2009000446A patent/TN2009000446A1/fr unknown
- 2009-11-09 EC EC2009009721A patent/ECSP099721A/es unknown
- 2009-11-10 GT GT200900292A patent/GT200900292A/es unknown
- 2009-11-10 CR CR11106A patent/CR11106A/es unknown
- 2009-11-10 DO DO2009000257A patent/DOP2009000257A/es unknown
- 2009-11-10 CO CO09127778A patent/CO6241109A2/es active IP Right Grant
- 2009-12-07 MA MA32404A patent/MA31433B1/fr unknown
-
2011
- 2011-11-30 US US13/307,560 patent/US20120071490A1/en not_active Abandoned
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