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
Authority
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)
Other versions
JP2006524254A5 (enExample
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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (enExample) 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 (enExample)
EP (1) EP1620095A4 (enExample)
JP (1) JP2006524254A (enExample)
CN (1) CN1809351A (enExample)
AU (1) AU2004233827B2 (enExample)
CA (1) CA2522430A1 (enExample)
WO (1) WO2004096130A2 (enExample)

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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NZ541836A (en) 2003-02-27 2008-12-24 Palau Pharma Sa Pyrazolopyridine derivatives
AU2004270713A1 (en) * 2003-09-05 2005-03-17 Aventis Pharmaceuticals Inc. Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands
JP2007514759A (ja) 2003-12-19 2007-06-07 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
ATE499364T1 (de) * 2004-04-09 2011-03-15 Merck Sharp & Dohme Hemmer der akt aktivität
CN1942470A (zh) * 2004-04-09 2007-04-04 默克公司 Akt活性抑制剂
TW200618800A (en) * 2004-08-03 2006-06-16 Uriach Y Compania S A J Heterocyclic compounds
JP2008510734A (ja) 2004-08-18 2008-04-10 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
CA2576172A1 (en) 2004-08-23 2006-04-06 Merck & Co., Inc. Inhibitors of akt activity
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
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
CA2597456A1 (en) * 2005-02-14 2006-08-31 Merck & Co., Inc. Inhibitors of akt activity
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
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1948657A1 (en) 2005-11-15 2008-07-30 Vertex Pharmaceuticals Incorporated Azaindazoles useful as inhibitors of kinases
US20090062302A1 (en) 2006-01-24 2009-03-05 Buser-Doepner Carolyn A Jak2 Tyrosine Kinase Inhibition
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
JP5231411B2 (ja) 2006-07-06 2013-07-10 アレイ バイオファーマ、インコーポレイテッド Ａｋｔプロテインキナーゼ阻害剤としてのジヒドロチエノピリミジン
ES2372955T3 (es) 2006-07-06 2012-01-30 Array Biopharma, Inc. Ciclopenta[d]pirimidinas como inhibidores de la proteína cinasa akt.
ATE493418T1 (de) 2006-07-06 2011-01-15 Array Biopharma Inc Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren
BRPI0719883A2 (pt) 2006-10-09 2015-05-05 Takeda Pharmaceutical Inibidores de quinase
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
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
NZ582692A (en) 2007-07-05 2012-05-25 Array Biopharma Inc Pyrimidyl cyclopentanes as akt protein kinase inhibitors
US8377937B2 (en) 2007-07-05 2013-02-19 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
US8314131B2 (en) 2007-09-21 2012-11-20 Amgen Inc. Triazole fused heteroaryl compounds and methods of use thereof
CA2711692A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
WO2009089459A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
US20100048912A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
AU2009255329A1 (en) * 2008-06-03 2009-12-10 Msd K.K. Inhibitors of Akt activity
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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
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 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CN107090456B (zh) 2010-08-02 2022-01-18 瑟纳治疗公司 使用短干扰核酸的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1基因表达的抑制
LT2606134T (lt) 2010-08-17 2019-07-25 Sirna Therapeutics, Inc. Hepatito b viruso (hbv) geno raiškos slopinimas, tarpininkaujant rnr interferencijai naudojant mažą interferuojančią nukleorūgštį (sina)
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ES2663009T3 (es) 2010-10-29 2018-04-10 Sirna Therapeutics, Inc. Inhibición de la expresión génica mediada por interferencia por ARN utilizando ácidos nucleicos de interferencia cortos (ANic)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
RS56759B2 (sr) 2011-04-01 2024-10-31 Genentech Inc Kombinacija akt inhibitor jedinjenja i abiraterona za upotrebu pri terapeutskim tretiranjima
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JP2019521189A (ja) * 2016-07-06 2019-07-25 アルゴメディックス，インク． ドライアイ、眼痛および炎症の処置のためのｔｒｐａ１アンタゴニスト
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CN118267470A (zh) 2017-04-13 2024-07-02 赛罗帕私人有限公司 抗SIRPα抗体
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019094312A1 (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
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
MA53287A (fr) 2018-08-07 2022-05-11 Merck Sharp & Dohme Inhibiteurs de prmt5
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2021118924A2 (en) 2019-12-12 2021-06-17 Ting Therapeutics Llc Compositions and methods for the prevention and treatment of hearing loss
US12441730B2 (en) 2019-12-17 2025-10-14 Merck Sharp & Dohme Llc PRMT5 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
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Also Published As

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

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