PE20090887A1 - DERIVADOS DE 1H-PIRAZOL-[3,4-d]-PIRIMIDINA, 9H-PURINA Y 7H-PIRROL-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASA P70 S6 - Google Patents
DERIVADOS DE 1H-PIRAZOL-[3,4-d]-PIRIMIDINA, 9H-PURINA Y 7H-PIRROL-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASA P70 S6Info
- Publication number
- PE20090887A1 PE20090887A1 PE2008000756A PE2008000756A PE20090887A1 PE 20090887 A1 PE20090887 A1 PE 20090887A1 PE 2008000756 A PE2008000756 A PE 2008000756A PE 2008000756 A PE2008000756 A PE 2008000756A PE 20090887 A1 PE20090887 A1 PE 20090887A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrimidine
- imidazol
- piperidin
- phenyl
- pyrrol
- Prior art date
Links
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 2
- -1 4-FLUORO-3-TRIFLUOROMETHYL-PHENYL Chemical class 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- GEAXLHPORCRESC-UHFFFAOYSA-N chlorocyclohexatriene Chemical class ClC1=CC=C=C[CH]1 GEAXLHPORCRESC-UHFFFAOYSA-N 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91733107P | 2007-05-11 | 2007-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090887A1 true PE20090887A1 (es) | 2009-07-13 |
Family
ID=39765082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008000756A PE20090887A1 (es) | 2007-05-11 | 2008-04-29 | DERIVADOS DE 1H-PIRAZOL-[3,4-d]-PIRIMIDINA, 9H-PURINA Y 7H-PIRROL-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASA P70 S6 |
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 |
| WO2010019762A1 (en) * | 2008-08-13 | 2010-02-18 | Jenrin Discovery | Purine compounds as cannabinoid receptor blockers |
| 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 |
| CA2743242A1 (en) * | 2008-11-11 | 2010-05-20 | Eli Lilly And Company | P70 s6 kinase inhibitor and mtor inhibitor combination therapy |
| KR101699991B1 (ko) | 2009-02-11 | 2017-01-26 | 메르크 파텐트 게엠베하 | 신규의 아미노 아자헤테로시클릭 카르복사미드 |
| ES2654332T3 (es) | 2009-08-07 | 2018-02-13 | Merck Patent Gmbh | Nuevos compuestos azaheterocíclicos |
| BR112012011328A2 (pt) * | 2009-10-23 | 2016-11-22 | Lilly Co Eli | inibidores de akt |
| BR112012019459A2 (pt) | 2010-02-03 | 2017-10-17 | Signal Pharm Llc | identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase. |
| US9586938B2 (en) | 2010-07-29 | 2017-03-07 | Merck Patent Gmbh | Cyclic amine azaheterocyclic carboxamides |
| UA110113C2 (xx) | 2010-07-29 | 2015-11-25 | Біциклічні азагетероциклічні карбоксаміди | |
| EA023821B1 (ru) | 2010-11-24 | 2016-07-29 | Мерк Патент Гмбх | Хиназолинкарбоксамидазетидины, их применение в лечении гиперпролиферативных заболеваний и содержащие их композиции |
| HRP20171554T1 (hr) * | 2011-09-12 | 2017-11-17 | Merck Patent Gmbh | Novi imidazol amini kao modulatori aktivnosti kinaze |
| ES2646759T3 (es) | 2011-09-12 | 2017-12-15 | Merck Patent Gmbh | Derivados de aminopirimidina para uso como moduladores de la actividad de la quinasa |
| JP6318156B2 (ja) * | 2012-09-06 | 2018-04-25 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
| 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 |
| AR093511A1 (es) | 2012-11-16 | 2015-06-10 | Merck Patent Gmbh | Derivados de imidazol-piperidinilo como moduladores de la actividad de cinasas |
| AR093512A1 (es) | 2012-11-16 | 2015-06-10 | Merck Patent Gmbh | Derivados heterociclicos como moduladores de la actividad de cinasas |
| EA033655B1 (ru) | 2012-11-29 | 2019-11-13 | Merck Patent Gmbh | Производные азахиназолин карбоксамида |
| MX370448B (es) | 2013-03-11 | 2019-12-13 | Merck Patent Gmbh | Derivados de 6- [4- (1h-imidazol-2-il) piperidin-1-il] pirimidin-4-amina como moduladores de la actividad de cinasa. |
| WO2014172425A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| HK1221168A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法 |
| 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 |
| MY189663A (en) | 2013-04-17 | 2022-02-23 | Signal Pharm Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| 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 |
| 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 |
| EP3549940A1 (en) | 2013-04-17 | 2019-10-09 | Signal Pharmaceuticals, LLC | Pharmaceutical formulations, 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 |
| CN107474051B (zh) | 2013-05-29 | 2020-10-30 | 西格诺药品有限公司 | 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 |
| 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 |
| 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 |
| 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 |
| 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 |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
| IL302951A (en) | 2020-11-16 | 2023-07-01 | 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 |
| 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 |
| AU2005322085B2 (en) | 2004-12-28 | 2012-07-19 | Exelixis, Inc. | [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| US20090325924A1 (en) | 2005-06-30 | 2009-12-31 | Stuart Edward | GPCR Agonists |
| WO2007125321A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| EP2037931A2 (en) | 2006-04-25 | 2009-03-25 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| 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 CL CL2008001230A patent/CL2008001230A1/es unknown
- 2008-04-29 AR ARP080101808A patent/AR066344A1/es unknown
- 2008-05-01 KR KR1020097023455A patent/KR101088219B1/ko not_active Expired - Fee Related
- 2008-05-01 MY MYPI20094763A patent/MY154898A/en unknown
- 2008-05-01 AU AU2008251692A patent/AU2008251692B2/en not_active Ceased
- 2008-05-01 ES ES08747285.8T patent/ES2483726T3/es active Active
- 2008-05-01 RS RS20140385A patent/RS53451B/sr unknown
- 2008-05-01 BR BRPI0811212-6A2A patent/BRPI0811212A2/pt not_active IP Right Cessation
- 2008-05-01 JP JP2010507532A patent/JP5503532B2/ja not_active Expired - Fee Related
- 2008-05-01 MX MX2009012075A patent/MX2009012075A/es active IP Right Grant
- 2008-05-01 PL PL08747285T patent/PL2148880T3/pl unknown
- 2008-05-01 CN CN2008800156864A patent/CN101679439B/zh not_active Expired - Fee Related
- 2008-05-01 DK DK08747285.8T patent/DK2148880T3/da active
- 2008-05-01 SI SI200831223T patent/SI2148880T1/sl unknown
- 2008-05-01 EA EA200971051A patent/EA016445B1/ru not_active IP Right Cessation
- 2008-05-01 PT PT87472858T patent/PT2148880E/pt unknown
- 2008-05-01 HR HRP20140611AT patent/HRP20140611T1/hr unknown
- 2008-05-01 NZ NZ580423A patent/NZ580423A/en not_active IP Right Cessation
- 2008-05-01 WO PCT/US2008/062143 patent/WO2008140947A1/en not_active Ceased
- 2008-05-01 EP EP08747285.8A patent/EP2148880B1/en active Active
- 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 CO CO09127778A patent/CO6241109A2/es active IP Right Grant
- 2009-11-10 CR CR11106A patent/CR11106A/es unknown
- 2009-11-10 DO DO2009000257A patent/DOP2009000257A/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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |