ATE503483T1 - Hemmer der akt aktivität - Google Patents

Hemmer der akt aktivität

Info

Publication number
ATE503483T1
ATE503483T1 AT03779301T AT03779301T ATE503483T1 AT E503483 T1 ATE503483 T1 AT E503483T1 AT 03779301 T AT03779301 T AT 03779301T AT 03779301 T AT03779301 T AT 03779301T AT E503483 T1 ATE503483 T1 AT E503483T1
Authority
AT
Austria
Prior art keywords
compounds
activity inhibitor
act activity
directed
act
Prior art date
Application number
AT03779301T
Other languages
English (en)
Inventor
Mark Duggan
Craig Lindsley
Zhijian Zhao
Original Assignee
Merck Sharp & Dohme
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 Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of ATE503483T1 publication Critical patent/ATE503483T1/de

Links

Classifications

    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AT03779301T 2002-10-30 2003-10-24 Hemmer der akt aktivität ATE503483T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42230702P 2002-10-30 2002-10-30
PCT/US2003/034007 WO2004041162A2 (en) 2002-10-30 2003-10-24 Inhibitors of akt activity

Publications (1)

Publication Number Publication Date
ATE503483T1 true ATE503483T1 (de) 2011-04-15

Family

ID=32312489

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03779301T ATE503483T1 (de) 2002-10-30 2003-10-24 Hemmer der akt aktivität

Country Status (8)

Country Link
US (1) US7399764B2 (de)
EP (1) EP1558586B1 (de)
JP (1) JP2006507299A (de)
AT (1) ATE503483T1 (de)
AU (1) AU2003284981B2 (de)
CA (1) CA2501365C (de)
DE (1) DE60336576D1 (de)
WO (1) WO2004041162A2 (de)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
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WO2004096131A2 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
CN1809351A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
DE602004026047D1 (de) * 2003-04-24 2010-04-29 Merck Sharp & Dohme Hemmer der akt aktivität
EP1737843B1 (de) * 2004-04-09 2011-02-23 Merck Sharp & Dohme Corp. Hemmer der akt aktivität
CN1942470A (zh) * 2004-04-09 2007-04-04 默克公司 Akt活性抑制剂
AU2005290081B2 (en) * 2004-08-23 2010-12-02 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
ZA200704888B (en) * 2004-11-22 2009-02-25 Vertex Pharma Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
AU2006258124B8 (en) 2005-06-10 2010-01-07 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
EP1978964A4 (de) 2006-01-24 2009-12-09 Merck & Co Inc Jak2-tyrosinkinase-hemmung
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ATE532789T1 (de) * 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
WO2008006032A1 (en) 2006-07-06 2008-01-10 Array Biopharma Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
CN101511842B (zh) * 2006-07-06 2012-10-31 阵列生物制药公司 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶
CA2670767A1 (en) * 2006-12-06 2008-06-12 Merck & Co., Inc. Inhibitors of akt activity
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
WO2008070823A2 (en) * 2006-12-07 2008-06-12 University Of South Florida Substrate-mimetic akt inhibitor
SI2173723T1 (sl) 2007-07-05 2011-12-30 Array Biopharma Inc Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze
US8618097B2 (en) 2007-07-05 2013-12-31 Array Biopharma, Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
JP5346345B2 (ja) 2008-01-09 2013-11-20 アレイ バイオファーマ、インコーポレイテッド Aktタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン類
EP2240455B1 (de) 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylierte pyrimidyl-cyclopentane als akt-proteinkinasehemmer
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EP2405756B1 (de) 2009-03-12 2013-07-03 Merck Sharp & Dohme Corp. Hemmer der akt-aktivität
WO2010114780A1 (en) * 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JP5099731B1 (ja) 2009-10-14 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション p53活性を増大する置換ピペリジン及びその使用
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EP2584903B1 (de) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Neue heterozyklische verbindungen als erk-hemmer
ES2539257T3 (es) * 2010-07-28 2015-06-29 Bayer Intellectual Property Gmbh Imidazo[1,2-b]piridazinas sustituidas
AU2011285909B2 (en) 2010-08-02 2016-11-10 Sirna Therapeutics, Inc. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP2606134B1 (de) 2010-08-17 2019-04-10 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte hemmung der hepatitis b-virus (hbv)-genexpression mittels kurzer interferierender nukleinsäure (sina)
EP2613782B1 (de) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
EP3766975A1 (de) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte inhibition von genexpression unter verwendung kurzer interferierender nukleinsäure (sina)
EP2654748B1 (de) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
KR20140022053A (ko) 2011-04-01 2014-02-21 제넨테크, 인크. Akt 및 mek 억제제 화합물의 조합물, 및 사용 방법
ES2620644T3 (es) 2011-04-01 2017-06-29 Genentech, Inc. Combinaciones de compuestos inhibidores de AKT y agentes quimioterapéuticos, y métodos de uso
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
EP3358013B1 (de) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Sina-zusammensetzungen
KR20150060724A (ko) 2012-09-28 2015-06-03 머크 샤프 앤드 돔 코포레이션 Erk 억제제인 신규 화합물
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EP2935263B1 (de) 2012-12-20 2018-12-05 Merck Sharp & Dohme Corp. Substituierte imidazopyridine als hdm2 inhibitoren
KR101470115B1 (ko) * 2013-01-09 2014-12-05 동국대학교 산학협력단 2-(페닐에티닐)티에노[3,4-b]피라진 유도체 및 이를 포함하는 암의 예방 또는 치료용 약학적 조성물
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
EP2968370A4 (de) 2013-03-14 2016-09-21 Univ Maryland Mittel zur androgenrezeptor-abwärtsregelung und verwendungen davon
EP3033088A4 (de) 2013-08-12 2017-03-08 Tokai Pharmaceuticals, Inc. Biomarker zur behandlung neoplastischer störungen mit androgen-anzielenden therapien
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
WO2018190719A2 (en) 2017-04-13 2018-10-18 Aduro Biotech Holdings, Europe B.V. Anti-sirp alpha antibodies
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
WO2020033285A1 (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
BR112021002267A8 (pt) 2018-08-07 2023-02-07 Merck Sharp & Dohme Inibidores de prmt5
EP3833668B1 (de) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5-inhibitoren
CN114981298B (zh) 2019-12-12 2024-08-20 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
EP4076459B1 (de) 2019-12-17 2026-04-29 Merck Sharp & Dohme LLC Prmt5-inhibitoren
CA3160153A1 (en) 2019-12-17 2021-06-24 Michelle Machacek Prmt5 inhibitors
BR112022012015A2 (pt) 2019-12-17 2022-08-30 Merck Sharp & Dohme Llc Inibidores de prmt5
EP4076460B1 (de) 2019-12-17 2026-01-21 Merck Sharp & Dohme LLC 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidin]-derivate als prmt5 inhibitoren zur behandlung von krebs
WO2026027944A1 (en) 2024-07-30 2026-02-05 Sairopa B.V. Anti-sirp alpha antibody formulations and uses thereof

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Also Published As

Publication number Publication date
CA2501365A1 (en) 2004-05-21
WO2004041162A2 (en) 2004-05-21
DE60336576D1 (de) 2011-05-12
JP2006507299A (ja) 2006-03-02
CA2501365C (en) 2011-05-31
AU2003284981B2 (en) 2009-05-28
US7399764B2 (en) 2008-07-15
US20050288294A1 (en) 2005-12-29
EP1558586A4 (de) 2007-06-27
EP1558586A2 (de) 2005-08-03
EP1558586B1 (de) 2011-03-30
AU2003284981A1 (en) 2004-06-07
WO2004041162A3 (en) 2004-07-29

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