CN101679439B - P70 s6激酶抑制剂 - Google Patents

P70 s6激酶抑制剂 Download PDF

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Publication number
CN101679439B
CN101679439B CN2008800156864A CN200880015686A CN101679439B CN 101679439 B CN101679439 B CN 101679439B CN 2008800156864 A CN2008800156864 A CN 2008800156864A CN 200880015686 A CN200880015686 A CN 200880015686A CN 101679439 B CN101679439 B CN 101679439B
Authority
CN
China
Prior art keywords
phenyl
imidazol
trifluoromethyl
piperidine
mmol
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
Application number
CN2008800156864A
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English (en)
Chinese (zh)
Other versions
CN101679439A (zh
Inventor
R·D·达利
黄建平
S·约瑟夫
T·A·谢泼德
C·L·霍尔斯特
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Eli Lilly and Co
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Eli Lilly and Co
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Publication date
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Publication of CN101679439A publication Critical patent/CN101679439A/zh
Application granted granted Critical
Publication of CN101679439B publication Critical patent/CN101679439B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • 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

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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)
CN2008800156864A 2007-05-11 2008-05-01 P70 s6激酶抑制剂 Expired - Fee Related CN101679439B (zh)

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
CN101679439A CN101679439A (zh) 2010-03-24
CN101679439B true CN101679439B (zh) 2013-09-11

Family

ID=39765082

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2008800156864A Expired - Fee Related CN101679439B (zh) 2007-05-11 2008-05-01 P70 s6激酶抑制剂

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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UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
BR112013002212A2 (pt) 2010-07-29 2017-09-26 Merck Patent Gmbh carboxamidas aza-heterocíclicas de aminas cíclicas
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SG2014009260A (en) 2011-09-12 2014-09-26 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
SI2755965T1 (sl) * 2011-09-12 2017-12-29 Merck Patent Gmbh Novi imidazolni amidi kot modulatorji kinazne aktivnosti
CN104981247A (zh) 2012-09-06 2015-10-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
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
JP6386467B2 (ja) 2012-11-16 2018-09-05 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の新規複素環式誘導体
WO2014085528A1 (en) 2012-11-29 2014-06-05 Merck Patent Gmbh Azaquinazoline carboxamide derivatives
SG11201505999VA (en) * 2013-03-11 2015-08-28 Merck Patent Gmbh 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
AU2014254059B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and a cytidine analog for treating cancer
CA2908353C (en) 2013-04-17 2021-11-02 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
US9505764B2 (en) 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
CA2908957C (en) 2013-04-17 2021-05-18 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
EA030726B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ, СПОСОБЫ, ТВЕРДЫЕ ФОРМЫ И СПОСОБЫ ПРИМЕНЕНИЯ, ОТНОСЯЩИЕСЯ К 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1H-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1H)-ОНУ
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.
HK1223286A1 (zh) 2013-05-29 2017-07-28 西格诺药品有限公司 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3，4-二氢吡嗪并[2，3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法
WO2015134536A1 (en) * 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AU2015240094B2 (en) 2014-04-03 2020-07-30 Merck Patent Gmbh Combinations of cancer therapeutics
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
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
ES2959860T3 (es) 2017-06-22 2024-02-28 Celgene Corp Tratamiento del carcinoma hepatocelular caracterizado por la infección por el virus de la hepatitis B
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
NZ580423A (en) 2012-02-24
IL201564A (en) 2014-08-31
CL2008001230A1 (es) 2009-05-22
ES2483726T3 (es) 2014-08-07
JP2010526814A (ja) 2010-08-05
RS53451B (sr) 2014-12-31
EA016445B1 (ru) 2012-05-30
TWI423805B (zh) 2014-01-21
HRP20140611T1 (hr) 2014-08-15
PL2148880T3 (pl) 2014-10-31
CN101679439A (zh) 2010-03-24
US20090163714A1 (en) 2009-06-25
GT200900292A (es) 2011-06-24
IL201564A0 (en) 2010-05-31
CO6241109A2 (es) 2011-01-20
SI2148880T1 (sl) 2014-07-31
JP5503532B2 (ja) 2014-05-28
CA2687265A1 (en) 2008-11-20
WO2008140947A1 (en) 2008-11-20
KR101088219B1 (ko) 2011-11-30
US8093383B2 (en) 2012-01-10
AU2008251692A1 (en) 2008-11-20
HK1140767A1 (en) 2010-10-22
CA2687265C (en) 2012-12-04
EP2148880A1 (en) 2010-02-03
TN2009000446A1 (en) 2011-03-31
BRPI0811212A2 (pt) 2014-10-29
ECSP099721A (es) 2009-12-28
MA31433B1 (fr) 2010-06-01
KR20100005710A (ko) 2010-01-15
DK2148880T3 (da) 2014-06-16
AR066344A1 (es) 2009-08-12
DOP2009000257A (es) 2010-03-31
EA200971051A1 (ru) 2010-06-30
PT2148880E (pt) 2014-08-28
US20120071490A1 (en) 2012-03-22
EP2148880B1 (en) 2014-05-28
UA99284C2 (ru) 2012-08-10
CR11106A (es) 2010-04-12
PE20090887A1 (es) 2009-07-13
MX2009012075A (es) 2009-11-19
MY154898A (en) 2015-08-28
AU2008251692B2 (en) 2012-10-11
TW200848053A (en) 2008-12-16

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