ATE400274T1 - Hemmstoffe der akt aktivität - Google Patents

Hemmstoffe der akt aktivität

Info

Publication number
ATE400274T1
ATE400274T1 AT02721697T AT02721697T ATE400274T1 AT E400274 T1 ATE400274 T1 AT E400274T1 AT 02721697 T AT02721697 T AT 02721697T AT 02721697 T AT02721697 T AT 02721697T AT E400274 T1 ATE400274 T1 AT E400274T1
Authority
AT
Austria
Prior art keywords
compounds
activity inhibitors
act activity
act
directed
Prior art date
Application number
AT02721697T
Other languages
English (en)
Inventor
Stanley Barnett
Samuel Graham
David Remy
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of ATE400274T1 publication Critical patent/ATE400274T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/42Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Seeds, Soups, And Other Foods (AREA)
  • General Preparation And Processing Of Foods (AREA)
AT02721697T 2001-04-10 2002-04-08 Hemmstoffe der akt aktivität ATE400274T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US28278101P 2001-04-10 2001-04-10

Publications (1)

Publication Number Publication Date
ATE400274T1 true ATE400274T1 (de) 2008-07-15

Family

ID=23083087

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02721697T ATE400274T1 (de) 2001-04-10 2002-04-08 Hemmstoffe der akt aktivität

Country Status (8)

Country Link
US (1) US7034026B2 (de)
EP (1) EP1379251B1 (de)
JP (1) JP4361276B2 (de)
AT (1) ATE400274T1 (de)
AU (1) AU2002252614B2 (de)
CA (1) CA2442270C (de)
DE (1) DE60227492D1 (de)
WO (1) WO2002083138A1 (de)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL144583A0 (en) * 2001-07-26 2002-05-23 Peptor Ltd Chimeric protein kinase inhibitors
CA2480880C (en) 2002-04-08 2011-03-22 Merck & Co., Inc. Inhibitors of akt activity
WO2003086394A1 (en) * 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
CA2501365C (en) * 2002-10-30 2011-05-31 Merck & Co., Inc. Inhibitors of akt activity
KR101251624B1 (ko) 2003-04-18 2013-04-08 가부시키가이샤 한도오따이 에네루기 켄큐쇼 퀴녹살린 유도체, 그것을 이용한 유기 반도체 소자 및 전계 발광 소자
CN1809351A (zh) 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
CA2522431A1 (en) * 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
AU2004233826B2 (en) 2003-04-24 2009-08-13 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US7414055B2 (en) 2003-04-24 2008-08-19 Merck & Co., Inc. Inhibitors of Akt activity
IL156429A0 (en) * 2003-06-12 2004-01-04 Peptor Ltd Cell permeable conjugates of peptides for inhibition of protein kinases
JP2007532551A (ja) * 2004-04-09 2007-11-15 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害剤
CA2561311A1 (en) * 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
EP1784175A4 (de) * 2004-08-23 2009-07-22 Merck & Co Inc Inhibitoren von akt-aktivität
CN101242834A (zh) 2004-12-15 2008-08-13 默克公司 Akt活性抑制剂
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
PT1898903E (pt) 2005-06-10 2013-06-28 Merck Sharp & Dohme Inibidores da atividade de akt
WO2007032258A1 (en) * 2005-09-12 2007-03-22 Semiconductor Energy Laboratory Co., Ltd. Quinoxaline derivative, and light emitting element, light emitting device, and electronic appliance using the same
EP1978964A4 (de) 2006-01-24 2009-12-09 Merck & Co Inc Jak2-tyrosinkinase-hemmung
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2007108403A1 (en) * 2006-03-21 2007-09-27 Semiconductor Energy Laboratory Co., Ltd. Quinoxaline derivative, and light-emitting element, light-emitting device, electronic device using the quinoxaline derivative
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
US20100022573A1 (en) * 2006-12-06 2010-01-28 Layton Mark E Inhibitors of akt activity
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
AU2007340129B2 (en) 2006-12-26 2012-02-02 Pharmacyclics Llc Method of using histone deacetylase inhibitors and monitoring biomarkers in combination therapy
PL2805945T3 (pl) 2007-01-10 2019-09-30 Msd Italia S.R.L. Indazole podstawione grupą amidową jako inhibitory polimerazy poli(adp-rybozy) - (parp)
US8178216B2 (en) * 2007-02-28 2012-05-15 Semiconductor Energy Laboratory Co., Ltd. Quinoxaline derivative, and light-emitting element, light-emitting device, and electronic device including quinoxaline derivative
KR101514853B1 (ko) 2007-03-01 2015-04-24 노파르티스 아게 Pim 키나제 억제제 및 이들의 사용 방법
ES2452349T3 (es) 2007-05-21 2014-04-01 Novartis Ag Inhibidores de CSF-1R, composiciones, y métodos de uso
AR066879A1 (es) * 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
WO2009002495A1 (en) 2007-06-27 2008-12-31 Merck & Co., Inc. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
EP2067778B1 (de) * 2007-12-03 2016-08-17 Semiconductor Energy Laboratory Co., Ltd. Quinoxalin-Derivat und lichtemittierendes Element, lichtemittierende Vorrichtung und elektronische Vorrichtung damit
JP5574598B2 (ja) * 2007-12-03 2014-08-20 株式会社半導体エネルギー研究所 キノキサリン誘導体、およびキノキサリン誘導体を用いた発光素子、発光装置、電子機器
WO2009148916A1 (en) * 2008-06-03 2009-12-10 Merck & Co., Inc. Inhibitors of akt activity
MX2010013224A (es) * 2008-06-03 2010-12-21 Merck Sharp & Dohme Inhibidores de la actividad de la serina/treonina cinasa.
CA2750051A1 (en) * 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CA2752150A1 (en) * 2009-02-11 2010-08-19 Reaction Biology Corp. Selective kinase inhibitors
US8168652B2 (en) 2009-03-12 2012-05-01 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
UA109417C2 (uk) 2009-10-14 2015-08-25 Мерк Шарп Енд Доме Корп. ЗАМІЩЕНІ ПІПЕРИДИНИ, ЯКІ ПІДВИЩУЮТЬ АКТИВНІСТЬ p53, І ЇХ ЗАСТОСУВАННЯ
WO2011075515A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP4079856A1 (de) 2010-08-17 2022-10-26 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte hemmung der hepatitis b-virus (hbv)-genexpression mittels kurzer interferierender nukleinsäure (sina)
EP2608669B1 (de) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. Neue pyrazolo-[1,5-a-]pyrimidinderivate als mtor-hemmer
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
CA2833009A1 (en) 2011-04-21 2012-10-26 Merck Sharp & Dohme Corp. Insulin-like growth factor-1 receptor inhibitors
EP2548877A1 (de) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Gliedrige kondensierte Pyridinyl)benzamide als BTK-Inhibitoren
ES2725790T3 (es) 2011-08-26 2019-09-27 Neupharma Inc Algunas entidades químicas, composiciones, y métodos
JP6093768B2 (ja) 2011-09-14 2017-03-08 ニューファーマ, インコーポレイテッド 特定の化学的実体、組成物、および方法
US9249110B2 (en) 2011-09-21 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
US9249111B2 (en) 2011-09-30 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-RAF kinase inhibitors
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
US9670180B2 (en) 2012-01-25 2017-06-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2013192088A1 (en) 2012-06-22 2013-12-27 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2863916B1 (de) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituierte pyridin-milz-tyrosinkinaseinhibitoren
US9688635B2 (en) 2012-09-24 2017-06-27 Neupharma, Inc. Certain chemical entities, compositions, and methods
MX2015004041A (es) 2012-09-28 2015-07-06 Merck Sharp & Dohme Compuestos novedosos que son inhibidores de erk.
WO2014075077A1 (en) 2012-11-12 2014-05-15 Neupharma, Inc. Certain chemical entities, compositions, and methods
CA2892361A1 (en) 2012-11-28 2014-06-05 Merck Sharp & Dohme Corp. Use of a wee1 inhibitor for treating a cancer characterized by low pkmyt1 expression levels
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
US20140206681A1 (en) 2013-01-23 2014-07-24 Ronald M. Kim Btk inhibitors
WO2014113942A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
AU2014214326B2 (en) 2013-02-07 2018-07-05 Prexton Therapeutics Sa Substituted quinoxaline derivatives and their use as positive allosteric modulators of mGluR4
EP2988749B1 (de) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazolsubstituierte aminopyridine als milztyrosinkinasehemmer
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015095102A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
EP3083560B1 (de) 2013-12-20 2021-10-27 Merck Sharp & Dohme Corp. Thiazolsubstituierte aminoheteroaryle als milztyrosinkinasehemmer
US9637486B2 (en) 2013-12-20 2017-05-02 Merck Sharp & Dohme Corp. Btk inhibitors
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
WO2016106624A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Tertiary alcohol imidazopyrazine btk inhibitors
WO2016106626A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors
WO2016106623A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Benzamide imidazopyrazine btk inhibitors
WO2016106629A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016106628A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
US10045981B2 (en) 2015-11-24 2018-08-14 Jakpharm, Llc Selective kinase inhibitors
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
SG11201908813QA (en) 2017-04-13 2019-10-30 Aduro Biotech Holdings Europe B V Anti-sirp alpha antibodies
EP3706742B1 (de) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5-inhibitoren
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
JP7162372B2 (ja) 2018-07-02 2022-10-28 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのアルキニル(ヘテロ)芳香族化合物
CN110272426B (zh) 2018-07-17 2022-05-31 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白激酶活性的炔基(杂)芳环类化合物
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833667B1 (de) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5-inhibitoren
CN109518211B (zh) * 2019-01-08 2020-11-06 合肥工业大学 一种芳香偶酰类化合物的电化学合成方法
CN115087638B (zh) 2019-12-17 2023-11-24 默沙东公司 Prmt5抑制剂

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1384713A (fr) * 1962-11-24 1965-01-08 Kalle Ag Matériel d'électrophotographie
NL300539A (de) * 1962-11-24
DE3420039A1 (de) 1984-05-29 1985-12-12 Hoechst Ag, 6230 Frankfurt 2,3-bis(dialkylaminophenyl)chinoxaline und ihre verwendung in elektrophotographischen aufzeichnungsmaterialien
IN166761B (de) 1987-04-10 1990-07-14 Hoechst India
JPS6457261A (en) * 1987-08-28 1989-03-03 Alps Electric Co Ltd Photoconductive film and electrophotographic sensitive body using same
EP0397859A4 (en) 1987-11-12 1990-12-19 Terumo Kabushiki Kaisha Pyrazine derivatives and medicinal preparation containing same
GB2293380A (en) 1994-09-22 1996-03-27 Zeneca Ltd Pesticidal heterocyclic and phenyl compounds
US6060491A (en) 1997-06-19 2000-05-09 Dupont Pharmaceuticals 6-membered aromatics as factor Xa inhibitors
WO1999042461A1 (en) 1998-02-23 1999-08-26 Warner-Lambert Company Substituted quinoxaline derivatives as interleukin-8 receptor antagonists
JP2000309578A (ja) 1999-04-27 2000-11-07 Kyowa Hakko Kogyo Co Ltd キノキサリン誘導体
IL156369A0 (en) 2000-12-21 2004-01-04 Vertex Pharma Pyrazole derivatives and pharmaceutical compositions containing the same
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors

Also Published As

Publication number Publication date
EP1379251A4 (de) 2005-05-25
US20040143117A1 (en) 2004-07-22
JP4361276B2 (ja) 2009-11-11
WO2002083138A1 (en) 2002-10-24
JP2004525961A (ja) 2004-08-26
EP1379251A1 (de) 2004-01-14
CA2442270A1 (en) 2002-10-24
EP1379251B1 (de) 2008-07-09
US7034026B2 (en) 2006-04-25
DE60227492D1 (de) 2008-08-21
CA2442270C (en) 2009-09-08
AU2002252614B2 (en) 2006-09-14

Similar Documents

Publication Publication Date Title
ATE400274T1 (de) Hemmstoffe der akt aktivität
CA2480800A1 (en) Inhibitors of akt activity
ATE446752T1 (de) Hemmer der akt aktivität
ATE512957T1 (de) Hemmer der akt aktivität
WO2003086279A3 (en) Inhibitors of akt activity
ATE461179T1 (de) Hemmer der akt aktivität
ATE503483T1 (de) Hemmer der akt aktivität
WO2006036395A3 (en) Inhibitors of akt activity
ATE499364T1 (de) Hemmer der akt aktivität
WO2004096130A3 (en) Inhibitors of akt activity
MXPA03010961A (es) Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
WO2002083675A3 (en) Inhibitors of akt activity
DE60214703D1 (de) Thiazolverbindungen, die sich als inhibitoren von proteinkinasen eignen
BG106585A (en) Kinase inhibitors as therapeutic agents
MY141739A (en) Substituted quinazoline derivatives as inhibitors of aurora kinases
MXPA03010207A (es) Nuevas 4-anilinoquinolin-3-carboxamidas.
ATE437872T1 (de) Proteinkinaseinhibitoren
BG106020A (en) Inhibitors of impdh enzyme
NO20034204L (no) Farmasöytiske kombinasjoner til behandling av kreft
YU21404A (sh) Supstituisana jedinjenja benzimidazola i njihova primena u lečenju raka
MXPA04005809A (es) Inhibidores de proteinas quinasas.
ZA200400824B (en) Pyridin-2-yl-methlyamine derivatives for treating opioid dependence.
DE60231646D1 (de) Durch c-verbundene imidazole substituierte 1,8-annellierten chinolon-derivate als farnesyl transferase inhibitoren

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties