CN101679439B - P70 s6激酶抑制剂 - Google Patents

P70 s6激酶抑制剂 Download PDF

Info

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
Other languages
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
Priority date (The priority date 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 date listed.)
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
Anticipated expiration legal-status Critical

Links

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

Landscapes

  • 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)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA99284C2 (ru) * 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
WO2010019762A1 (en) * 2008-08-13 2010-02-18 Jenrin Discovery Purine compounds as cannabinoid receptor blockers
BRPI0921888A2 (pt) 2008-11-11 2015-12-29 Lilly Co Eli terapia de combinação de inibidor de egfr inibidor da p70 s6 quinase
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
CA2743242A1 (en) * 2008-11-11 2010-05-20 Eli Lilly And Company P70 s6 kinase inhibitor and mtor inhibitor combination therapy
KR101699991B1 (ko) 2009-02-11 2017-01-26 메르크 파텐트 게엠베하 신규의 아미노 아자헤테로시클릭 카르복사미드
ES2654332T3 (es) 2009-08-07 2018-02-13 Merck Patent Gmbh Nuevos compuestos azaheterocíclicos
BR112012011328A2 (pt) * 2009-10-23 2016-11-22 Lilly Co Eli inibidores de akt
BR112012019459A2 (pt) 2010-02-03 2017-10-17 Signal Pharm Llc identificação de mutação de lkb1 como um biomarcador preditivo para sensibilidade para inibidores de tor quinase.
US9586938B2 (en) 2010-07-29 2017-03-07 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
EA023821B1 (ru) 2010-11-24 2016-07-29 Мерк Патент Гмбх Хиназолинкарбоксамидазетидины, их применение в лечении гиперпролиферативных заболеваний и содержащие их композиции
HRP20171554T1 (hr) * 2011-09-12 2017-11-17 Merck Patent Gmbh Novi imidazol amini kao modulatori aktivnosti kinaze
ES2646759T3 (es) 2011-09-12 2017-12-15 Merck Patent Gmbh Derivados de aminopirimidina para uso como moduladores de la actividad de la quinasa
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
AR093511A1 (es) 2012-11-16 2015-06-10 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de cinasas
AR093512A1 (es) 2012-11-16 2015-06-10 Merck Patent Gmbh Derivados heterociclicos como moduladores de la actividad de cinasas
EA033655B1 (ru) 2012-11-29 2019-11-13 Merck Patent Gmbh Производные азахиназолин карбоксамида
MX370448B (es) 2013-03-11 2019-12-13 Merck Patent Gmbh Derivados de 6- [4- (1h-imidazol-2-il) piperidin-1-il] pirimidin-4-amina como moduladores de la actividad de cinasa.
WO2014172425A1 (en) 2013-04-17 2014-10-23 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
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
MY189663A (en) 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
JP6382946B2 (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
EP3549940A1 (en) 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, 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
CN107474051B (zh) 2013-05-29 2020-10-30 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
US9771369B2 (en) 2014-03-04 2017-09-26 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
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
WO2015160880A1 (en) 2014-04-16 2015-10-22 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
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
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
IL302951A (en) 2020-11-16 2023-07-01 Merck Patent Gmbh Kinase inhibitor combinations for cancer treatment

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL1004346C2 (nl) 1996-10-23 1998-04-24 Dsm Nv Werkwijze voor het scheiden van een mengsel van enantiomeren in een geschikt oplosmiddel.
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
AU2005322085B2 (en) 2004-12-28 2012-07-19 Exelixis, Inc. [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
US20090325924A1 (en) 2005-06-30 2009-12-31 Stuart Edward GPCR Agonists
WO2007125321A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
AR064416A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
UA99284C2 (ru) * 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
刘奕等.mTOR/P70S6激酶信号通路在腮腺腺癌发生中的作用.《中国医科大学学报》.2004,第33卷(第3期),229-231. *

Also Published As

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

Similar Documents

Publication Publication Date Title
US8093383B2 (en) P70 S6 kinase inhibitors
AU2020228799B2 (en) JAK inhibitor compound and use thereof
EP2545045B1 (en) Piperidin-4-yl azetidine derivatives as jak1 inhibitors
WO2020239103A1 (zh) 一种btk抑制剂环衍生物及其制备方法和药学上的应用
CN112707893A (zh) 作为usp30抑制剂的1-氰基吡咯烷化合物
JP2021515767A (ja) Ｅｒｋ５阻害剤の同定及び使用
WO2021147952A1 (zh) 嘧啶并吡咯类化合物
JP2026507654A (ja) Ｅｇｆｒ阻害剤としての大環状アミノピリジン化合物
HK1140767B (en) P70 s6 kinase inhibitors
HK40043421A (en) 1-cyano-pyrrolidine compounds as usp30 inhibitors
HK40077703A (en) Piperidin-4-yl azetidine derivatives as jak1 inhibitors
CN120025352A (zh) 稠合杂环化合物、药物组合物及其应用
HK1207374A1 (en) Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors
HK1207374B (en) Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors
HK1230164A (en) Piperidin-4-yl azetidine derivatives as jak1 inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20130911

Termination date: 20170501

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