CO6241109A2 - Inhibidores de cinasa p70 s6 - Google Patents
Inhibidores de cinasa p70 s6Info
- Publication number
- CO6241109A2 CO6241109A2 CO09127778A CO09127778A CO6241109A2 CO 6241109 A2 CO6241109 A2 CO 6241109A2 CO 09127778 A CO09127778 A CO 09127778A CO 09127778 A CO09127778 A CO 09127778A CO 6241109 A2 CO6241109 A2 CO 6241109A2
- Authority
- CO
- Colombia
- Prior art keywords
- halo
- hydrogen
- alkyl
- substituent selected
- independently
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
1.- Un compuesto de la fórmula I:caracterizado porque: Y es N o CR6; Z1 y Z2 son independientemente CR3 o N, siempre que Z1 y Z2 no sean ambos N;R1 es H o alquilo C1-C4; R2 es fenilo opcionalmente sustituido con un primer sustituyente seleccionado a partir de alcoxi C1-C4, ciano, NO2, halo, y trifluorometilo, trifluorometoxi y opcionalmente, además sustituido con un segundo sustituyente seleccionado del grupo que consiste de halo;R3 es hidrógeno, halo, alquilo C1-C4, cicloalquilo C3-C6, o alquinilo C2-C6, en donde alquinilo C2-C6 es opcionalmente sustituido con hidroxi; R4 y R5 son independientemente hidrógeno o alquilo C1-C4; R6 es hidrógeno; o una sal del mismo farmacéuticamente aceptable. 2.- El compuesto de conformidad con la reivindicación 1, de la fórmula: caracterizado porque:Y es N o CR6; Z1 y Z2 son independientemente CR3 o N, siempre que Z1 y Z2 no sean ambos N; R1 es H o alquilo C1-C4; R2 es fenilo opcionalmente sustituido con un primer sustituyente seleccionado a partir de alcoxi C1-C4, ciano, NO2, halo, trifluorometilo, y trifluorometoxi y opcionalmente, además sustituido con un segundo sustituyente seleccionado del grupo que consiste de halo; R3 es hidrógeno, halo o cicloalquilo C3-C6;R4 y R5 son independientemente hidrógeno o alquilo C1-C4; R6 es hidrógeno, o una sal del mismo farmacéuticamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91733107P | 2007-05-11 | 2007-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6241109A2 true CO6241109A2 (es) | 2011-01-20 |
Family
ID=39765082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO09127778A CO6241109A2 (es) | 2007-05-11 | 2009-11-10 | Inhibidores de cinasa p70 s6 |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US8093383B2 (es) |
| EP (1) | EP2148880B1 (es) |
| JP (1) | JP5503532B2 (es) |
| KR (1) | KR101088219B1 (es) |
| CN (1) | CN101679439B (es) |
| AR (1) | AR066344A1 (es) |
| AU (1) | AU2008251692B2 (es) |
| BR (1) | BRPI0811212A2 (es) |
| CA (1) | CA2687265C (es) |
| CL (1) | CL2008001230A1 (es) |
| CO (1) | CO6241109A2 (es) |
| CR (1) | CR11106A (es) |
| DK (1) | DK2148880T3 (es) |
| DO (1) | DOP2009000257A (es) |
| EA (1) | EA016445B1 (es) |
| EC (1) | ECSP099721A (es) |
| ES (1) | ES2483726T3 (es) |
| GT (1) | GT200900292A (es) |
| HK (1) | HK1140767A1 (es) |
| HR (1) | HRP20140611T1 (es) |
| IL (1) | IL201564A (es) |
| MA (1) | MA31433B1 (es) |
| MX (1) | MX2009012075A (es) |
| MY (1) | MY154898A (es) |
| NZ (1) | NZ580423A (es) |
| PE (1) | PE20090887A1 (es) |
| PL (1) | PL2148880T3 (es) |
| PT (1) | PT2148880E (es) |
| RS (1) | RS53451B (es) |
| SI (1) | SI2148880T1 (es) |
| TN (1) | TN2009000446A1 (es) |
| TW (1) | TWI423805B (es) |
| UA (1) | UA99284C2 (es) |
| WO (1) | WO2008140947A1 (es) |
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 |
| US8334293B2 (en) | 2008-11-11 | 2012-12-18 | Eli Lilly And Company | P70 S6 kinase inhibitor and EGFR inhibitor combination therapy |
| KR20110075014A (ko) * | 2008-11-11 | 2011-07-05 | 일라이 릴리 앤드 캄파니 | Ｐ70 ｓ6 키나제 억제제 및 ｍｔｏｒ 억제제 조합 요법 |
| 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 |
| BRPI1008325A2 (pt) | 2009-02-11 | 2020-08-25 | Merck Patent Gmbh | carboxamidas azaeterocíclicas de amino |
| US9023847B2 (en) | 2009-08-07 | 2015-05-05 | Merck Patent Gmbh | Azaheterocyclic compounds |
| EP2491032B1 (en) | 2009-10-23 | 2014-04-16 | Eli Lilly and Company | Akt inhibitors |
| EP2992878A1 (en) | 2010-02-03 | 2016-03-09 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| KR101945061B1 (ko) | 2010-07-29 | 2019-02-01 | 메르크 파텐트 게엠베하 | 시클릭 아민 아자헤테로시클릭 카르복사미드 |
| UA110113C2 (xx) | 2010-07-29 | 2015-11-25 | Біциклічні азагетероциклічні карбоксаміди | |
| CN103228649B (zh) | 2010-11-24 | 2015-11-25 | 默克专利股份公司 | 喹唑啉甲酰胺氮杂环丁烷 |
| ES2644536T3 (es) * | 2011-09-12 | 2017-11-29 | Merck Patent Gmbh | Imidazol-aminas novedosas como moduladores de la actividad cinasa |
| RS56486B1 (sr) | 2011-09-12 | 2018-01-31 | Merck Patent Gmbh | Aminopirimidin derivati za upotrebu kao modulatori aktivnosti kinaza |
| 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 |
| WO2014078634A1 (en) * | 2012-11-16 | 2014-05-22 | Merck Patent Gmbh | Novel imidazol-piperidinyl derivatives as modulators of kinase activity |
| US9580443B2 (en) | 2012-11-16 | 2017-02-28 | Merck Patent Gmbh | Heterocyclic derivatives as modulators of kinase activity |
| CA2887539C (en) | 2012-11-29 | 2021-10-26 | Merck Patent Gmbh | Azaquinazoline carboxamide derivatives |
| AR095202A1 (es) | 2013-03-11 | 2015-09-30 | Merck Patent Gmbh | Heterociclos como moduladores de la actividad quinasa |
| JP6382946B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ，エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| KR102271344B1 (ko) | 2013-04-17 | 2021-07-01 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| CA2908742C (en) | 2013-04-17 | 2021-06-01 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| 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 |
| AU2014254058B2 (en) | 2013-04-17 | 2019-06-06 | Signal Pharmaceuticals, Llc | Combination therapy comprising a Dihydropyrazino-Pyrazine Compound and an androgen receptor antagonist for treating prostate cancer |
| EP2986319A1 (en) | 2013-04-17 | 2016-02-24 | 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 |
| CN105339009B (zh) | 2013-04-17 | 2018-08-28 | 西格诺药品有限公司 | 用于治疗癌症的包括tor激酶抑制剂和5-取代喹唑啉酮化合物的组合疗法 |
| 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 |
| US9771369B2 (en) | 2014-03-04 | 2017-09-26 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| NZ725361A (en) | 2014-04-03 | 2022-09-30 | Merck Patent Gmbh | Combinations of cancer therapeutics |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | 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, COMPOSITIONS AND METHODS OF USE THEREOF |
| 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 |
| TWI787284B (zh) | 2017-06-22 | 2022-12-21 | 美商西建公司 | 以b型肝炎病毒感染表徵之肝細胞癌之治療 |
| US20240024324A1 (en) | 2020-11-16 | 2024-01-25 | 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 |
| EP1750727A2 (en) * | 2004-04-23 | 2007-02-14 | 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 |
| EP1907383A1 (en) | 2005-06-30 | 2008-04-09 | Prosidion Limited | Gpcr agonists |
| WO2007125310A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| EP3421471B1 (en) | 2006-04-25 | 2021-05-26 | 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 CL CL2008001230A patent/CL2008001230A1/es unknown
- 2008-04-29 AR ARP080101808A patent/AR066344A1/es unknown
- 2008-04-29 PE PE2008000756A patent/PE20090887A1/es not_active Application Discontinuation
- 2008-05-01 AU AU2008251692A patent/AU2008251692B2/en not_active Ceased
- 2008-05-01 CA CA2687265A patent/CA2687265C/en not_active Expired - Fee Related
- 2008-05-01 MY MYPI20094763A patent/MY154898A/en unknown
- 2008-05-01 JP JP2010507532A patent/JP5503532B2/ja not_active Expired - Fee Related
- 2008-05-01 KR KR1020097023455A patent/KR101088219B1/ko not_active IP Right Cessation
- 2008-05-01 BR BRPI0811212-6A2A patent/BRPI0811212A2/pt not_active IP Right Cessation
- 2008-05-01 NZ NZ580423A patent/NZ580423A/en not_active IP Right Cessation
- 2008-05-01 EA EA200971051A patent/EA016445B1/ru not_active IP Right Cessation
- 2008-05-01 PL PL08747285T patent/PL2148880T3/pl unknown
- 2008-05-01 DK DK08747285.8T patent/DK2148880T3/da active
- 2008-05-01 MX MX2009012075A patent/MX2009012075A/es active IP Right Grant
- 2008-05-01 WO PCT/US2008/062143 patent/WO2008140947A1/en active Application Filing
- 2008-05-01 PT PT87472858T patent/PT2148880E/pt unknown
- 2008-05-01 RS RS20140385A patent/RS53451B/en unknown
- 2008-05-01 EP EP08747285.8A patent/EP2148880B1/en active Active
- 2008-05-01 ES ES08747285.8T patent/ES2483726T3/es active Active
- 2008-05-01 CN CN2008800156864A patent/CN101679439B/zh not_active Expired - Fee Related
- 2008-05-01 SI SI200831223T patent/SI2148880T1/sl unknown
-
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
-
2010
- 2010-07-29 HK HK10107283.9A patent/HK1140767A1/xx not_active IP Right Cessation
-
2011
- 2011-11-30 US US13/307,560 patent/US20120071490A1/en not_active Abandoned
-
2014
- 2014-06-26 HR HRP20140611AT patent/HRP20140611T1/hr unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused | ||
| FG | Application granted |