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 (OSRAM) | 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)
| Country | Link |
|---|---|
| US (2) | US8093383B2 (OSRAM) |
| EP (1) | EP2148880B1 (OSRAM) |
| JP (1) | JP5503532B2 (OSRAM) |
| KR (1) | KR101088219B1 (OSRAM) |
| CN (1) | CN101679439B (OSRAM) |
| AR (1) | AR066344A1 (OSRAM) |
| AU (1) | AU2008251692B2 (OSRAM) |
| BR (1) | BRPI0811212A2 (OSRAM) |
| CA (1) | CA2687265C (OSRAM) |
| CL (1) | CL2008001230A1 (OSRAM) |
| CO (1) | CO6241109A2 (OSRAM) |
| CR (1) | CR11106A (OSRAM) |
| DK (1) | DK2148880T3 (OSRAM) |
| DO (1) | DOP2009000257A (OSRAM) |
| EA (1) | EA016445B1 (OSRAM) |
| EC (1) | ECSP099721A (OSRAM) |
| ES (1) | ES2483726T3 (OSRAM) |
| GT (1) | GT200900292A (OSRAM) |
| HR (1) | HRP20140611T1 (OSRAM) |
| IL (1) | IL201564A (OSRAM) |
| MA (1) | MA31433B1 (OSRAM) |
| MX (1) | MX2009012075A (OSRAM) |
| MY (1) | MY154898A (OSRAM) |
| NZ (1) | NZ580423A (OSRAM) |
| PE (1) | PE20090887A1 (OSRAM) |
| PL (1) | PL2148880T3 (OSRAM) |
| PT (1) | PT2148880E (OSRAM) |
| RS (1) | RS53451B (OSRAM) |
| SI (1) | SI2148880T1 (OSRAM) |
| TN (1) | TN2009000446A1 (OSRAM) |
| TW (1) | TWI423805B (OSRAM) |
| UA (1) | UA99284C2 (OSRAM) |
| WO (1) | WO2008140947A1 (OSRAM) |
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 |
| WO2010019762A1 (en) * | 2008-08-13 | 2010-02-18 | Jenrin Discovery | Purine compounds as cannabinoid receptor blockers |
| CN102209539B (zh) * | 2008-11-11 | 2013-06-12 | 伊莱利利公司 | P70 s6激酶抑制剂和mtor抑制剂的组合治疗剂 |
| BRPI0921888A2 (pt) | 2008-11-11 | 2015-12-29 | Lilly Co Eli | terapia de combinação de inibidor de egfr inibidor da p70 s6 quinase |
| 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 |
| EP2396307B1 (en) | 2009-02-11 | 2014-10-15 | Merck Patent GmbH | Novel amino azaheterocyclic carboxamides |
| EP2462141B1 (en) | 2009-08-07 | 2017-09-27 | Merck Patent GmbH | Novel azaheterocyclic compounds |
| CN102574852B (zh) * | 2009-10-23 | 2014-06-25 | 伊莱利利公司 | Akt抑制剂 |
| UA110697C2 (uk) | 2010-02-03 | 2016-02-10 | Сігнал Фармасьютікалз, Елелсі | ЗАСТОСУВАННЯ ІНГІБІТОРІВ TOR-КІНАЗИ ДЛЯ ЛІКУВАННЯ ПУХЛИННИХ ЗАХВОРЮВАНЬ У ПАЦІЄНТА ЗІ ЗНИЖЕНИМ РІВНЕМ БІЛКА pAMPK ТА/АБО АКТИВНОСТІ AMPK |
| 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 | |
| EP2643313B9 (en) | 2010-11-24 | 2017-02-22 | Merck Patent GmbH | Quinazoline carboxamide azetidines |
| US9145392B2 (en) * | 2011-09-12 | 2015-09-29 | Merck Patent Gmbh | Imidazole amines as modulators of kinase activity |
| DK2755958T3 (en) | 2011-09-12 | 2017-09-25 | Merck Patent Gmbh | AMINOPYRIMIDINE DERIVATIVES USED AS MODULATORS OF KINASE ACTIVITY |
| WO2014039714A2 (en) * | 2012-09-06 | 2014-03-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| 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 |
| CA2890288A1 (en) | 2012-11-16 | 2014-05-22 | Merck Patent Gmbh | Novel heterocyclic derivatives as modulators of kinase activity |
| CN105102435A (zh) | 2012-11-16 | 2015-11-25 | 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 |
| CN105793254B (zh) | 2012-11-29 | 2020-10-23 | 默克专利有限公司 | 氮杂喹唑啉羧酰胺衍生物 |
| HK1218756A1 (zh) * | 2013-03-11 | 2017-03-10 | 默克专利有限公司 | 用作激酶活性调节剂的6-[4-(1h-咪唑-2-基)哌啶-1-基]嘧啶-4-胺衍生物 |
| SG11201508527VA (en) | 2013-04-17 | 2015-11-27 | Signal Pharm Llc | Pharmaceutical formulations, processes, solid forms and methods of use relating to 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 |
| KR102242505B1 (ko) | 2013-04-17 | 2021-04-20 | 시그날 파마소티칼 엘엘씨 | 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법 |
| AU2014254057A1 (en) | 2013-04-17 | 2015-11-05 | Signal Pharmaceuticals, Llc | Combination therapy comprising a TOR kinase inhibitor and N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| NZ629411A (en) | 2013-04-17 | 2017-06-30 | Signal Pharm Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| BR112015026257B1 (pt) | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| MX368286B (es) | 2013-04-17 | 2019-09-27 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer. |
| ES2944478T3 (es) | 2013-04-17 | 2023-06-21 | Signal Pharm Llc | 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-ona para tratar el glioblastoma multiforme |
| JP6401250B2 (ja) | 2013-05-29 | 2018-10-10 | シグナル ファーマシューティカルズ，エルエルシー | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（ｔｒａｎｓ）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン、その固体形態の医薬組成物、及びその使用方法 |
| WO2015134536A1 (en) * | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| RU2733401C2 (ru) | 2014-04-03 | 2020-10-01 | Мерк Патент Гмбх | Комбинации противораковых лекарств |
| 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 |
| EP3641772B1 (en) | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| WO2022101459A1 (en) | 2020-11-16 | 2022-05-19 | Merck Patent Gmbh | Kinase inhibitor combinations for cancer treatment |
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 |
| JP5213229B2 (ja) * | 2004-04-23 | 2013-06-19 | エグゼリクシス， インコーポレイテッド | キナーゼ調節因子および使用方法 |
| 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 |
| US7994172B2 (en) | 2004-12-28 | 2011-08-09 | 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 |
| EP2043655A2 (en) | 2006-04-25 | 2009-04-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| 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 PE PE2008000756A patent/PE20090887A1/es not_active Application Discontinuation
- 2008-04-29 AR ARP080101808A patent/AR066344A1/es unknown
- 2008-04-29 CL CL2008001230A patent/CL2008001230A1/es unknown
- 2008-05-01 KR KR1020097023455A patent/KR101088219B1/ko not_active Expired - Fee Related
- 2008-05-01 BR BRPI0811212-6A2A patent/BRPI0811212A2/pt not_active IP Right Cessation
- 2008-05-01 AU AU2008251692A patent/AU2008251692B2/en not_active Ceased
- 2008-05-01 NZ NZ580423A patent/NZ580423A/en not_active IP Right Cessation
- 2008-05-01 MX MX2009012075A patent/MX2009012075A/es active IP Right Grant
- 2008-05-01 CN CN2008800156864A patent/CN101679439B/zh not_active Expired - Fee Related
- 2008-05-01 WO PCT/US2008/062143 patent/WO2008140947A1/en not_active Ceased
- 2008-05-01 PL PL08747285T patent/PL2148880T3/pl unknown
- 2008-05-01 RS RS20140385A patent/RS53451B/sr unknown
- 2008-05-01 ES ES08747285.8T patent/ES2483726T3/es active Active
- 2008-05-01 DK DK08747285.8T patent/DK2148880T3/da active
- 2008-05-01 HR HRP20140611AT patent/HRP20140611T1/hr unknown
- 2008-05-01 EP EP08747285.8A patent/EP2148880B1/en active Active
- 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 MY MYPI20094763A patent/MY154898A/en unknown
- 2008-05-01 PT PT87472858T patent/PT2148880E/pt unknown
- 2008-05-01 EA EA200971051A patent/EA016445B1/ru not_active IP Right Cessation
- 2008-05-01 CA CA2687265A patent/CA2687265C/en not_active Expired - Fee Related
-
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 DO DO2009000257A patent/DOP2009000257A/es unknown
- 2009-11-10 CO CO09127778A patent/CO6241109A2/es active IP Right Grant
- 2009-11-10 CR CR11106A patent/CR11106A/es unknown
- 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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