JP2006524254A - Ａｋｔ活性の阻害剤 - Google Patents

Ａｋｔ活性の阻害剤 Download PDF

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Publication number
JP2006524254A
JP2006524254A JP2006513159A JP2006513159A JP2006524254A JP 2006524254 A JP2006524254 A JP 2006524254A JP 2006513159 A JP2006513159 A JP 2006513159A JP 2006513159 A JP2006513159 A JP 2006513159A JP 2006524254 A JP2006524254 A JP 2006524254A
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JP
Japan
Prior art keywords
phenyl
methyl
benzimidazol
piperidin
alkyl
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.)
Ceased
Application number
JP2006513159A
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English (en)
Japanese (ja)
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JP2006524254A5 (https=
Inventor
ビロドー，マーク・テイー
ウー，ジカイ
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.)
Merck and Co Inc
Original Assignee
Merck and 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 and Co Inc filed Critical Merck and Co Inc
Publication of JP2006524254A publication Critical patent/JP2006524254A/ja
Publication of JP2006524254A5 publication Critical patent/JP2006524254A5/ja
Ceased 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2006513159A 2003-04-24 2004-04-20 Ａｋｔ活性の阻害剤 Ceased JP2006524254A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46512303P 2003-04-24 2003-04-24
PCT/US2004/012187 WO2004096130A2 (en) 2003-04-24 2004-04-20 Inhibitors of akt activity

Publications (2)

Publication Number Publication Date
JP2006524254A true JP2006524254A (ja) 2006-10-26
JP2006524254A5 JP2006524254A5 (https=) 2007-04-05

Family

ID=33418186

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2006513159A Ceased JP2006524254A (ja) 2003-04-24 2004-04-20 Ａｋｔ活性の阻害剤

Country Status (7)

Country Link
US (1) US7638530B2 (https=)
EP (1) EP1620095A4 (https=)
JP (1) JP2006524254A (https=)
CN (1) CN1809351A (https=)
AU (1) AU2004233827B2 (https=)
CA (1) CA2522430A1 (https=)
WO (1) WO2004096130A2 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009503037A (ja) * 2005-08-04 2009-01-29 アバンテイス・フアルマ・エス・アー ７−置換アザ−インダゾール、これらを含む組成物、これらの製造方法および使用
JP2009298786A (ja) * 2006-12-06 2009-12-24 Merck & Co Inc Ａｋｔ活性の阻害剤
JP2012517963A (ja) * 2009-02-13 2012-08-09 バイエル ファーマ アクチエンゲゼルシャフト 縮合ピリミジン類
JP2017503024A (ja) * 2014-01-06 2017-01-26 アルゴメディクス インコーポレイテッド Ｔｒｐａ１モジュレーター

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US7468376B2 (en) 2003-02-27 2008-12-23 Palau Pharma, S.A. Pyrazolopyridine derivates
AR045582A1 (es) * 2003-09-05 2005-11-02 Neurogen Corp Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1
EP1694686A1 (en) 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
CA2561311A1 (en) * 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
EP1737861A4 (en) * 2004-04-09 2010-04-28 Merck Sharp & Dohme HEMMER OF ACT ACTIVITY
TW200618800A (en) * 2004-08-03 2006-06-16 Uriach Y Compania S A J Heterocyclic compounds
WO2006023931A2 (en) 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
EP1784175A4 (en) 2004-08-23 2009-07-22 Merck & Co Inc INHIBITORS OF ACT ACTIVITY
EP1812439B2 (en) 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Kinase inhibitors
AR051596A1 (es) 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
PE20061119A1 (es) 2005-01-19 2006-11-27 Aventis Pharma Sa PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie
AU2006216998B2 (en) * 2005-02-14 2010-12-23 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
EP1898903B8 (en) * 2005-06-10 2013-05-15 Merck Sharp & Dohme Corp. Inhibitors of akt activity
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
WO2007059219A1 (en) 2005-11-15 2007-05-24 Vertex Pharmaceuticals Incorporated Azaindazoles useful as inhibitors of kinases
EP1978964A4 (en) 2006-01-24 2009-12-09 Merck & Co Inc JAK2 tyrosine kinase Inhibition
CA2656566C (en) 2006-07-06 2014-06-17 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ATE523499T1 (de) 2006-07-06 2011-09-15 Array Biopharma Inc Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
WO2008070823A2 (en) * 2006-12-07 2008-06-12 University Of South Florida Substrate-mimetic akt inhibitor
US20080207659A1 (en) 2007-02-15 2008-08-28 Asit Kumar Chakraborti Inhibitors of phosphodiesterase type 4
US8642067B2 (en) 2007-04-02 2014-02-04 Allergen, Inc. Methods and compositions for intraocular administration to treat ocular conditions
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2009006567A2 (en) 2007-07-05 2009-01-08 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
CN101918373B (zh) 2007-07-05 2013-06-05 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
WO2009038784A1 (en) * 2007-09-21 2009-03-26 Amgen Inc. Triazole fused heteroaryl compounds as p38 kinase inhibitors
ES2422733T3 (es) 2008-01-09 2013-09-13 Array Biopharma Inc Pirimidilciclopentanos hidroxilados como inhibidores de proteínas cinasas AKT
EP2240455B1 (en) 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
US20100048913A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
JP2011522048A (ja) * 2008-06-03 2011-07-28 メルク・シャープ・エンド・ドーム・コーポレイション Ａｋｔ活性の阻害剤
US8536193B2 (en) * 2008-06-03 2013-09-17 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
ES2402087T3 (es) * 2008-07-23 2013-04-26 Vertex Pharmaceuticals Incorporated Inhibidores de la pirazolopiridina quinasa
CN102686600A (zh) 2009-02-05 2012-09-19 托凯药业股份有限公司 甾体cyp17抑制剂/抗雄激素物质的新型药物前体
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
US8846673B2 (en) 2009-08-11 2014-09-30 Bristol-Myers Squibb Company Azaindazoles as kinase inhibitors and use thereof
PE20121172A1 (es) 2009-10-14 2012-09-05 Merck Sharp & Dohme Piperidinas sustituidas con actividad en la hdm2
GB0919380D0 (en) * 2009-11-04 2009-12-23 Almac Discovery Ltd Pharmaceutical compouds
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP3330377A1 (en) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as 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
RU2013148817A (ru) 2011-04-01 2015-05-10 Дженентек, Инк. Комбинации соединений-ингибиторов акт и мек и способы их применения
WO2012135781A1 (en) 2011-04-01 2012-10-04 Genentech, Inc. Combinations of akt inhibitor compounds and chemotherapeutic agents, and methods of use
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US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
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WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
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EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
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US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
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WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
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CN118767143A (zh) 2019-12-12 2024-10-15 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
US12595248B2 (en) 2019-12-17 2026-04-07 Merck Sharp & Dohme Llc PRMT5 inhibitors
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WO2002022608A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009503037A (ja) * 2005-08-04 2009-01-29 アバンテイス・フアルマ・エス・アー ７−置換アザ−インダゾール、これらを含む組成物、これらの製造方法および使用
JP2009298786A (ja) * 2006-12-06 2009-12-24 Merck & Co Inc Ａｋｔ活性の阻害剤
JP2012517963A (ja) * 2009-02-13 2012-08-09 バイエル ファーマ アクチエンゲゼルシャフト 縮合ピリミジン類
JP2017503024A (ja) * 2014-01-06 2017-01-26 アルゴメディクス インコーポレイテッド Ｔｒｐａ１モジュレーター
US10428049B2 (en) 2014-01-06 2019-10-01 Algomedix, Inc. TRPA1 modulators

Also Published As

Publication number Publication date
CA2522430A1 (en) 2004-11-11
AU2004233827A1 (en) 2004-11-11
AU2004233827B2 (en) 2009-05-28
EP1620095A4 (en) 2009-04-01
EP1620095A2 (en) 2006-02-01
US7638530B2 (en) 2009-12-29
US20060205765A1 (en) 2006-09-14
WO2004096130A3 (en) 2005-04-07
WO2004096130A2 (en) 2004-11-11
CN1809351A (zh) 2006-07-26

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