KR101088219B1 - P70 s6 키나제 억제제 - Google Patents

P70 s6 키나제 억제제 Download PDF

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Publication number
KR101088219B1
KR101088219B1 KR1020097023455A KR20097023455A KR101088219B1 KR 101088219 B1 KR101088219 B1 KR 101088219B1 KR 1020097023455 A KR1020097023455 A KR 1020097023455A KR 20097023455 A KR20097023455 A KR 20097023455A KR 101088219 B1 KR101088219 B1 KR 101088219B1
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KR
South Korea
Prior art keywords
phenyl
mmol
trifluoromethyl
equiv
added
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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.)
Expired - Fee Related
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KR1020097023455A
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English (en)
Korean (ko)
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KR20100005710A (ko
Inventor
로버트 딘 달리
지안핑 후앙
사잔 죠셉
티모시 알란 세퍼드
크리스티안 엘. 홀스트
Original Assignee
일라이 릴리 앤드 캄파니
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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  • 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)
KR1020097023455A 2007-05-11 2008-05-01 P70 s6 키나제 억제제 Expired - Fee Related KR101088219B1 (ko)

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 (2)

Publication Number Publication Date
KR20100005710A KR20100005710A (ko) 2010-01-15
KR101088219B1 true KR101088219B1 (ko) 2011-11-30

Family

ID=39765082

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020097023455A Expired - Fee Related KR101088219B1 (ko) 2007-05-11 2008-05-01 P70 s6 키나제 억제제

Country Status (33)

Country Link
US (2) US8093383B2 (enExample)
EP (1) EP2148880B1 (enExample)
JP (1) JP5503532B2 (enExample)
KR (1) KR101088219B1 (enExample)
CN (1) CN101679439B (enExample)
AR (1) AR066344A1 (enExample)
AU (1) AU2008251692B2 (enExample)
BR (1) BRPI0811212A2 (enExample)
CA (1) CA2687265C (enExample)
CL (1) CL2008001230A1 (enExample)
CO (1) CO6241109A2 (enExample)
CR (1) CR11106A (enExample)
DK (1) DK2148880T3 (enExample)
DO (1) DOP2009000257A (enExample)
EA (1) EA016445B1 (enExample)
EC (1) ECSP099721A (enExample)
ES (1) ES2483726T3 (enExample)
GT (1) GT200900292A (enExample)
HR (1) HRP20140611T1 (enExample)
IL (1) IL201564A (enExample)
MA (1) MA31433B1 (enExample)
MX (1) MX2009012075A (enExample)
MY (1) MY154898A (enExample)
NZ (1) NZ580423A (enExample)
PE (1) PE20090887A1 (enExample)
PL (1) PL2148880T3 (enExample)
PT (1) PT2148880E (enExample)
RS (1) RS53451B (enExample)
SI (1) SI2148880T1 (enExample)
TN (1) TN2009000446A1 (enExample)
TW (1) TWI423805B (enExample)
UA (1) UA99284C2 (enExample)
WO (1) WO2008140947A1 (enExample)

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BRPI0921888A2 (pt) * 2008-11-11 2015-12-29 Lilly Co Eli terapia de combinação de inibidor de egfr inibidor da p70 s6 quinase
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CN102317269B (zh) 2009-02-11 2015-06-17 默克专利有限公司 新氨基氮杂杂环甲酰胺类
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KR101398268B1 (ko) 2009-10-23 2014-05-23 일라이 릴리 앤드 캄파니 Akt 억제제
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
WO2012016001A1 (en) 2010-07-29 2012-02-02 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
CA2818706C (en) 2010-11-24 2019-07-23 Merck Patent Gmbh Quinazoline carboxamide azetidines
JP6082011B2 (ja) 2011-09-12 2017-02-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung キナーゼ活性のモジュレーターとして使用するためのアミノピリミジン誘導体
ES2644536T3 (es) * 2011-09-12 2017-11-29 Merck Patent Gmbh Imidazol-aminas novedosas como moduladores de la actividad cinasa
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
ES2807539T3 (es) 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
ES2620119T3 (es) 2012-11-16 2017-06-27 Merck Patent Gmbh Derivados heterocíclicos novedosos como moduladores de la actividad de quinasa
ES2821102T3 (es) 2012-11-29 2021-04-23 Merck Patent Gmbh Derivados de azaquinazolincarboxamida
AR095202A1 (es) 2013-03-11 2015-09-30 Merck Patent Gmbh Heterociclos como moduladores de la actividad quinasa
EA030808B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ПРИМЕНЕНИЕ 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1Н-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1Н)-ОНА В ЛЕЧЕНИИ МУЛЬТИФОРМНОЙ ГЛИОБЛАСТОМЫ
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
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
WO2014172432A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
CA2909579A1 (en) 2013-04-17 2014-10-23 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
HK1221174A1 (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5-取代喹唑啉酮化合物的组合疗法
MX364101B (es) 2013-04-17 2019-04-12 Signal Pharm Llc Terapia de combinación que comprende un compuesto de dihidropirazino-pirazina y un antagonista de receptor de andrógenos para tratar cáncer de próstata.
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WO2015134536A1 (en) * 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
KR102410696B1 (ko) 2014-04-03 2022-06-17 메르크 파텐트 게엠베하 암 치료법의 조합
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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
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Publication number Publication date
US20120071490A1 (en) 2012-03-22
US20090163714A1 (en) 2009-06-25
IL201564A0 (en) 2010-05-31
AU2008251692B2 (en) 2012-10-11
AR066344A1 (es) 2009-08-12
WO2008140947A1 (en) 2008-11-20
CL2008001230A1 (es) 2009-05-22
CN101679439B (zh) 2013-09-11
RS53451B (sr) 2014-12-31
ECSP099721A (es) 2009-12-28
IL201564A (en) 2014-08-31
DOP2009000257A (es) 2010-03-31
KR20100005710A (ko) 2010-01-15
JP5503532B2 (ja) 2014-05-28
PT2148880E (pt) 2014-08-28
BRPI0811212A2 (pt) 2014-10-29
SI2148880T1 (sl) 2014-07-31
CA2687265A1 (en) 2008-11-20
CA2687265C (en) 2012-12-04
MX2009012075A (es) 2009-11-19
HRP20140611T1 (hr) 2014-08-15
UA99284C2 (ru) 2012-08-10
EP2148880A1 (en) 2010-02-03
MA31433B1 (fr) 2010-06-01
US8093383B2 (en) 2012-01-10
AU2008251692A1 (en) 2008-11-20
CN101679439A (zh) 2010-03-24
EP2148880B1 (en) 2014-05-28
NZ580423A (en) 2012-02-24
TN2009000446A1 (en) 2011-03-31
JP2010526814A (ja) 2010-08-05
PL2148880T3 (pl) 2014-10-31
TWI423805B (zh) 2014-01-21
PE20090887A1 (es) 2009-07-13
DK2148880T3 (da) 2014-06-16
EA016445B1 (ru) 2012-05-30
TW200848053A (en) 2008-12-16
CO6241109A2 (es) 2011-01-20
HK1140767A1 (en) 2010-10-22
EA200971051A1 (ru) 2010-06-30
MY154898A (en) 2015-08-28
ES2483726T3 (es) 2014-08-07
CR11106A (es) 2010-04-12
GT200900292A (es) 2011-06-24

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