CA2852921C - Treatment of cancer with tor kinase inhibitors - Google Patents

Treatment of cancer with tor kinase inhibitors Download PDF

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Publication number
CA2852921C
CA2852921C CA2852921A CA2852921A CA2852921C CA 2852921 C CA2852921 C CA 2852921C CA 2852921 A CA2852921 A CA 2852921A CA 2852921 A CA2852921 A CA 2852921A CA 2852921 C CA2852921 C CA 2852921C
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CA
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Prior art keywords
substituted
pyrazin
unsubstituted
tor kinase
dihydropyrazino
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Active
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CA2852921A
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English (en)
French (fr)
Other versions
CA2852921A1 (en
Inventor
Shuichan Xu
Kristen Mae Hege
Antonia Lopez-Girona
Heather Raymon
Rama K. Narla
Rajesh Chopra
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Signal Pharmaceuticals LLC
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Signal Pharmaceuticals LLC
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Publication of CA2852921A1 publication Critical patent/CA2852921A1/en
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2852921A 2011-10-19 2012-10-18 Treatment of cancer with tor kinase inhibitors Active CA2852921C (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161549034P 2011-10-19 2011-10-19
US61/549,034 2011-10-19
US201261591401P 2012-01-27 2012-01-27
US61/591,401 2012-01-27
US201261647233P 2012-05-15 2012-05-15
US61/647,233 2012-05-15
US201261653436P 2012-05-31 2012-05-31
US61/653,436 2012-05-31
PCT/US2012/060723 WO2013059396A2 (en) 2011-10-19 2012-10-18 Treatment of cancer with tor kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2852921A1 CA2852921A1 (en) 2013-04-25
CA2852921C true CA2852921C (en) 2023-10-10

Family

ID=47116477

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2852921A Active CA2852921C (en) 2011-10-19 2012-10-18 Treatment of cancer with tor kinase inhibitors

Country Status (19)

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US (4) US9493466B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (3) EP2768500B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (5) JP2014530861A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR101978537B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (2) CN103998036B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR112014009755B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2852921C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EA (2) EA034512B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (2) ES2751921T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (3) IL232128B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2014CN02887A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (4) MX357833B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MY (1) MY183661A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PH (1) PH12014500869A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (3) SG10201912850WA (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TW (4) TWI708605B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
UA (1) UA115319C2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2013059396A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (2) ZA201402771B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8299248B2 (en) 2006-08-02 2012-10-30 Cytokinetics, Incorporated Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols and methods for their use
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
SG11201505446WA (en) 2013-01-16 2015-08-28 Signal Pharm Llc Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
US20160008356A1 (en) * 2013-02-28 2016-01-14 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
WO2014172429A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and an imid compound for treating cancer
EP2986322A1 (en) * 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
MX393164B (es) 2013-04-17 2025-03-21 Signal Pharm Llc Formulaciones farmacéuticas, proceso, formas sólidas y métodos de uso relacionados con 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-ii)piridin-3-ii)-3,4-dihidropirazino[2,3-b]pirazin-2(1h)-ona.
SG11201508223YA (en) * 2013-04-17 2015-11-27 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
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
SG10201708111YA (en) 2013-04-17 2017-11-29 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
HK1221144A1 (zh) * 2013-04-17 2017-05-26 西格诺药品有限公司 用於治療癌症的包含tor激酶抑制劑和胞苷類似物的組合療法
EP3003313A1 (en) 2013-05-29 2016-04-13 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
WO2015051251A1 (en) * 2013-10-04 2015-04-09 Signal Pharmaceuticals, Llc A tor kinase inhibitor in the prevention or treatment of cancer characterized by gene mutations
JP2017511367A (ja) 2014-04-16 2017-04-20 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）−オン及び共形成物を含む固体形態、その組成物及び使用方法
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-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
ES2823756T3 (es) 2014-04-16 2021-05-10 Signal Pharm Llc Métodos para tratar el cáncer usando terapia de combinación de inhibidores de quinasa TOR
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
SG11201804098TA (en) 2015-11-20 2018-06-28 Forma Therapeutics Inc Purinones as ubiquitin-specific protease 1 inhibitors
US10765681B2 (en) 2016-02-05 2020-09-08 Academia Sinica Purine compounds possessing anticancer activity
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
BR112019012217B1 (pt) 2016-12-20 2021-08-10 Astrazeneca Ab Compostos, formas cristalinas, composição farmacêutica e uso de um composto ou seu sal farmaceuticamente aceitável
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
MX2020004239A (es) * 2017-11-01 2020-09-09 Juno Therapeutics Inc Proceso para producir una composicion de celulas t.
AU2019231551B2 (en) 2018-03-09 2023-08-03 Recurium Ip Holdings, Llc Substituted 1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-ones
CN110526907B (zh) * 2018-05-23 2021-04-23 四川大学 苯并噁嗪酮类衍生物及其应用
EP4003980A1 (en) 2019-07-31 2022-06-01 Ribon Therapeutics Inc. Heterobicyclic amides as inhibitors of cd38
WO2021098813A1 (zh) * 2019-11-22 2021-05-27 南京明德新药研发有限公司 作为dna-pk抑制剂的嘧啶并吡咯类螺环化合物及其衍生物
IL293318A (en) * 2019-11-25 2022-07-01 Medshine Discovery Inc Pyrimidoimidazole compounds used as dna-pk inhibitors

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE262026C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4317909A (en) 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4294837A (en) 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4294836A (en) 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4309537A (en) 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk ２−アミノイミダゾ〔４，５−ｂ〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US4963561A (en) 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 1992-09-26 1996-04-21 Hoechst Ag
DE19601627A1 (de) 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US6031105A (en) 1996-04-09 2000-02-29 Pfizer Inc Substituted pyridines
ATE281834T1 (de) 1997-09-26 2004-11-15 Zentaris Gmbh Azabenzimidazol-verbindungen zur modulation der serin/threonin protein-kinase funktion
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd ２−アリールプリン−９−アセトアミド誘導体
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 ２−アリール−８−オキソジヒドロプリン誘導体からなる医薬
JP2002100363A (ja) 2000-09-25 2002-04-05 Mitsubishi Chemicals Corp リチウム二次電池用正極材料、リチウム二次電池用正極及びリチウム二次電池
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd ２−（７，８−ジヒドロ−８−オキソ−９ｈ−プリン−９−イル）酢酸誘導体
US6566367B2 (en) 2000-12-12 2003-05-20 Pfizer Inc. Spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
ES2268093T3 (es) 2001-09-04 2007-03-16 BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG Nuevas dihidropteridinonas, procedimiento para su preparacion y su uso como medicamentos.
JP2005506350A (ja) 2001-10-18 2005-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害薬としての１，４−二置換ベンゾ−縮合尿素化合物
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
AU2003232071A1 (en) 2002-05-06 2003-11-17 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection
AU2003299531A1 (en) 2002-08-05 2004-06-07 University Of Massachusetts Compounds for modulating rna interference
JP2006512313A (ja) 2002-10-31 2006-04-13 アムジェン インコーポレイテッド 抗炎症剤
CA2512646A1 (en) 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
EA008778B1 (ru) 2003-02-26 2007-08-31 Бёрингер Ингельхайм Фарма Гмбх Унд Ко. Кг Дигидроптеридиноны, способ их получения и их применение в качестве лекарственных средств
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
JP2006524289A (ja) 2003-04-23 2006-10-26 ワイス・ホールディングズ・コーポレイション Ｐｅｇ−ワートマニンコンジュゲート
PL3521297T3 (pl) 2003-05-30 2022-04-04 Gilead Pharmasset Llc Zmodyfikowane fluorowane analogi nukleozydów
ATE461196T1 (de) 2003-06-26 2010-04-15 Merck Sharp & Dohme Benzodiazepin-cgrp-rezeptor-antagonisten
JP2008501707A (ja) 2004-06-04 2008-01-24 アイコス、コーポレーション マスト細胞障害を処置するための方法
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. ２－アリールプリン誘導体の製造方法
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
CN101065016A (zh) * 2004-09-24 2007-10-31 詹森药业有限公司 蛋白激酶的抑制剂咪唑并[4,5－b]吡嗪酮
US7855205B2 (en) 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
JP5118972B2 (ja) 2004-10-29 2013-01-16 テイボテク・フアーマシユーチカルズ Ｈｉｖ阻害性二環式ピリミジン誘導体
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New compounds
AU2005316668B2 (en) 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
RU2405780C2 (ru) 2005-02-16 2010-12-10 Астразенека Аб Химические соединения
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
WO2006108103A1 (en) 2005-04-05 2006-10-12 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
US9006224B2 (en) 2005-11-21 2015-04-14 Novartis Ag Neuroendocrine tumor treatment
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
MX2009001170A (es) 2006-08-02 2009-05-21 Cytokinetics Inc Determinadas entidades quimicas, composiciones y metodos.
WO2008030744A2 (en) 2006-09-05 2008-03-13 Board Of Regents, The University Of Texas System Inhibitors of c-met and uses thereof
AU2007338601C1 (en) 2006-09-05 2014-07-24 Emory University Tyrosine kinase inhibitors for prevention or treatment of infection
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
TW200831104A (en) 2006-10-04 2008-08-01 Pharmacopeia Inc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
BRPI0717773A2 (pt) 2006-10-19 2013-11-05 Signal Pharm Llc Composto, composição farmacêutica, e, métodos para tratar ou prevenir câncer, uma condição inflamatória, uma condição imunológica ou uma condição metabólica, e para inibir uma quinase em uma célula que expressa a dita quinase
KR101504669B1 (ko) * 2006-10-19 2015-03-20 시그날 파마소티칼 엘엘씨 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도
JP2011507910A (ja) 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
US8846664B2 (en) 2008-11-12 2014-09-30 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
CN102264743B (zh) * 2008-11-25 2015-02-11 罗彻斯特大学 Mlk抑制剂及其使用方法
MY177695A (en) * 2009-10-26 2020-09-23 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
CN102821767A (zh) * 2010-02-03 2012-12-12 西格诺药品有限公司 Lkb1突变作为对tor激酶抑制剂的敏感性的预测生物标记的鉴定
US20120028972A1 (en) 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
EP2739751A1 (en) 2011-08-03 2014-06-11 Signal Pharmaceuticals, LLC Identification of gene expression profile as a predictive biomarker for lkb1 status
BR112014013332B1 (pt) 2011-12-02 2022-09-06 Signal Pharmaceuticals, Llc Composições farmacêuticas de 7-(6-(2-hidroxi-propan-2-il)piridin-3-il)-1-((trans)-4- metoxicicloexil)-3,4-diidropirazino [2,3-b]pirazin-2(1h)-ona, uma forma sólida dessa e métodos de seu uso

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