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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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Filing date
Publication date
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
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
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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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 (OSRAM)
EP (1) EP2148880B1 (OSRAM)
JP (1) JP5503532B2 (OSRAM)
KR (1) KR101088219B1 (OSRAM)
CN (1) CN101679439B (OSRAM)
AR (1) AR066344A1 (OSRAM)
AU (1) AU2008251692B2 (OSRAM)
BR (1) BRPI0811212A2 (OSRAM)
CA (1) CA2687265C (OSRAM)
CL (1) CL2008001230A1 (OSRAM)
CO (1) CO6241109A2 (OSRAM)
CR (1) CR11106A (OSRAM)
DK (1) DK2148880T3 (OSRAM)
DO (1) DOP2009000257A (OSRAM)
EA (1) EA016445B1 (OSRAM)
EC (1) ECSP099721A (OSRAM)
ES (1) ES2483726T3 (OSRAM)
GT (1) GT200900292A (OSRAM)
HR (1) HRP20140611T1 (OSRAM)
IL (1) IL201564A (OSRAM)
MA (1) MA31433B1 (OSRAM)
MX (1) MX2009012075A (OSRAM)
MY (1) MY154898A (OSRAM)
NZ (1) NZ580423A (OSRAM)
PE (1) PE20090887A1 (OSRAM)
PL (1) PL2148880T3 (OSRAM)
PT (1) PT2148880E (OSRAM)
RS (1) RS53451B (OSRAM)
SI (1) SI2148880T1 (OSRAM)
TN (1) TN2009000446A1 (OSRAM)
TW (1) TWI423805B (OSRAM)
UA (1) UA99284C2 (OSRAM)
WO (1) WO2008140947A1 (OSRAM)

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US8252791B2 (en) * 2008-08-13 2012-08-28 Jenrin Discovery, Inc. Purine compounds as cannabinoid receptor blockers
EP2355821A1 (en) * 2008-11-11 2011-08-17 Eli Lilly and Company P70 s6 kinase inhibitor and egfr inhibitor combination therapy
EA018824B1 (ru) * 2008-11-11 2013-10-30 Эли Лилли Энд Компани КОМБИНИРОВАННАЯ ТЕРАПИЯ ИНГИБИТОРОМ КИНАЗЫ p70 S6 И ИНГИБИТОРОМ mTOR
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
WO2010093419A1 (en) 2009-02-11 2010-08-19 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides
AU2010281503B2 (en) 2009-08-07 2016-01-28 Merck Patent Gmbh Novel azaheterocyclic compounds
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
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
ES2729754T3 (es) 2010-07-29 2019-11-06 Merck Patent Gmbh Carboxamidas azaheterocíclicas de aminas cíclicas
PL2643313T3 (pl) 2010-11-24 2017-03-31 Merck Patent Gmbh Azetydyny chinazolino-karboksyamidowe
SI2755958T1 (sl) 2011-09-12 2017-12-29 Merck Patent Gmbh Aminopirimidinski derivati za uporabo kot modulatorji kinazne aktivnosti
SG10201606301YA (en) * 2011-09-12 2016-09-29 Merck Patent Gmbh Novel imidazole amines as modulators of kinase activity
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
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
ES2807539T3 (es) * 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
ES2821102T3 (es) 2012-11-29 2021-04-23 Merck Patent Gmbh Derivados de azaquinazolincarboxamida
US9458134B2 (en) * 2013-03-11 2016-10-04 Merck Patent Gmbh Heterocycles as modulators of kinase activity
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
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
WO2014172431A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate 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
TWI654979B (zh) 2013-04-17 2019-04-01 美商標誌製藥公司 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
KR102459285B1 (ko) 2013-04-17 2022-10-27 시그날 파마소티칼 엘엘씨 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법
CN113831345A (zh) 2013-05-29 2021-12-24 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
WO2015134536A1 (en) * 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG11201608189WA (en) 2014-04-03 2016-10-28 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
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
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
SG11201912403SA (en) 2017-06-22 2020-01-30 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
AU2021376892A1 (en) 2020-11-16 2023-06-29 Merck Patent Gmbh Kinase inhibitor combinations for cancer treatment

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Also Published As

Publication number Publication date
EP2148880B1 (en) 2014-05-28
AR066344A1 (es) 2009-08-12
US20090163714A1 (en) 2009-06-25
RS53451B (sr) 2014-12-31
US8093383B2 (en) 2012-01-10
MA31433B1 (fr) 2010-06-01
CA2687265A1 (en) 2008-11-20
TW200848053A (en) 2008-12-16
EP2148880A1 (en) 2010-02-03
EA200971051A1 (ru) 2010-06-30
MX2009012075A (es) 2009-11-19
HK1140767A1 (en) 2010-10-22
CO6241109A2 (es) 2011-01-20
ES2483726T3 (es) 2014-08-07
KR20100005710A (ko) 2010-01-15
KR101088219B1 (ko) 2011-11-30
CR11106A (es) 2010-04-12
IL201564A (en) 2014-08-31
EA016445B1 (ru) 2012-05-30
ECSP099721A (es) 2009-12-28
IL201564A0 (en) 2010-05-31
WO2008140947A1 (en) 2008-11-20
UA99284C2 (ru) 2012-08-10
PE20090887A1 (es) 2009-07-13
AU2008251692A1 (en) 2008-11-20
CA2687265C (en) 2012-12-04
MY154898A (en) 2015-08-28
DOP2009000257A (es) 2010-03-31
BRPI0811212A2 (pt) 2014-10-29
CL2008001230A1 (es) 2009-05-22
CN101679439A (zh) 2010-03-24
DK2148880T3 (da) 2014-06-16
AU2008251692B2 (en) 2012-10-11
HRP20140611T1 (hr) 2014-08-15
TN2009000446A1 (en) 2011-03-31
JP5503532B2 (ja) 2014-05-28
TWI423805B (zh) 2014-01-21
US20120071490A1 (en) 2012-03-22
PT2148880E (pt) 2014-08-28
PL2148880T3 (pl) 2014-10-31
JP2010526814A (ja) 2010-08-05
NZ580423A (en) 2012-02-24
SI2148880T1 (sl) 2014-07-31
GT200900292A (es) 2011-06-24

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Granted publication date: 20130911

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CF01 Termination of patent right due to non-payment of annual fee