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
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.)
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)
  • 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)
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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US20110212977A1 (en) * 2008-11-11 2011-09-01 Eli Lilly And Company P70 s6 kinase inhibitor and mtor inhibitor combination therapy
HRP20141239T1 (xx) 2009-02-11 2015-03-13 Merck Patent Gmbh Novi amino azaheterocikliäśki karboksamidi
US9023847B2 (en) 2009-08-07 2015-05-05 Merck Patent Gmbh Azaheterocyclic compounds
EA020151B1 (ru) * 2009-10-23 2014-09-30 Эли Лилли Энд Компани Ингибиторы akt и фармацевтические составы, их содержащие
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JP6014034B2 (ja) 2010-07-29 2016-10-25 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 環式アミンアザヘテロ環式カルボキサミド
EP2643313B9 (en) 2010-11-24 2017-02-22 Merck Patent GmbH Quinazoline carboxamide azetidines
RS56534B1 (sr) * 2011-09-12 2018-02-28 Merck Patent Gmbh Novi imidazol akmini kao modulatori aktivnosti kinaza
EA028057B1 (ru) 2011-09-12 2017-10-31 Мерк Патент Гмбх Производные аминопиримидина для применения в качестве модуляторов киназной активности
AU2013312477B2 (en) * 2012-09-06 2018-05-31 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
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CN105051043B (zh) 2012-11-16 2017-05-10 默克专利有限公司 用作激酶活性调节剂的新颖的杂环类衍生物
EP2920154B1 (en) * 2012-11-16 2017-10-11 Merck Patent GmbH Novel imidazol-piperidinyl derivatives as modulators of kinase activity
JP6290917B2 (ja) 2012-11-29 2018-03-07 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 アザキナゾリンカルボキサミド誘導体
KR20150124957A (ko) 2013-03-11 2015-11-06 메르크 파텐트 게엠베하 키나아제 활성의 조절인자로서 (6-[4-1h-이미다졸-2-일)피페리딘-1-일]피리미딘-4-아민 유도체
CN105339008A (zh) 2013-04-17 2016-02-17 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)丙烯酰胺的组合疗法
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
EP2986321A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
JP6382945B2 (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
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.
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
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.
NZ629486A (en) 2013-05-29 2017-11-24 Signal Pharm 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
WO2015134536A1 (en) * 2014-03-04 2015-09-11 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
EP3131551A4 (en) 2014-04-16 2017-09-20 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
WO2016164641A1 (en) 2015-04-08 2016-10-13 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
JP2023551408A (ja) 2020-11-16 2023-12-08 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 がん処置のためのキナーゼインヒビター組み合わせ

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Also Published As

Publication number Publication date
IL201564A (en) 2014-08-31
RS53451B (sr) 2014-12-31
CN101679439A (zh) 2010-03-24
JP5503532B2 (ja) 2014-05-28
SI2148880T1 (sl) 2014-07-31
US8093383B2 (en) 2012-01-10
UA99284C2 (ru) 2012-08-10
MX2009012075A (es) 2009-11-19
PT2148880E (pt) 2014-08-28
US20120071490A1 (en) 2012-03-22
CO6241109A2 (es) 2011-01-20
EA200971051A1 (ru) 2010-06-30
JP2010526814A (ja) 2010-08-05
EA016445B1 (ru) 2012-05-30
CR11106A (es) 2010-04-12
ECSP099721A (es) 2009-12-28
CA2687265C (en) 2012-12-04
GT200900292A (es) 2011-06-24
HK1140767A1 (en) 2010-10-22
WO2008140947A1 (en) 2008-11-20
TN2009000446A1 (en) 2011-03-31
EP2148880A1 (en) 2010-02-03
CN101679439B (zh) 2013-09-11
NZ580423A (en) 2012-02-24
CA2687265A1 (en) 2008-11-20
ES2483726T3 (es) 2014-08-07
PE20090887A1 (es) 2009-07-13
DK2148880T3 (da) 2014-06-16
BRPI0811212A2 (pt) 2014-10-29
AU2008251692A1 (en) 2008-11-20
KR20100005710A (ko) 2010-01-15
MY154898A (en) 2015-08-28
US20090163714A1 (en) 2009-06-25
HRP20140611T1 (hr) 2014-08-15
EP2148880B1 (en) 2014-05-28
MA31433B1 (fr) 2010-06-01
PL2148880T3 (pl) 2014-10-31
IL201564A0 (en) 2010-05-31
TWI423805B (zh) 2014-01-21
DOP2009000257A (es) 2010-03-31
AU2008251692B2 (en) 2012-10-11
CL2008001230A1 (es) 2009-05-22
AR066344A1 (es) 2009-08-12
TW200848053A (en) 2008-12-16

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