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)
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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)
  • 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 (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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KR101312736B1 (ko) 2003-02-27 2013-09-27 팔라우 파르마 에스에이 피라졸로피리딘 유도체
US20050113379A1 (en) * 2003-09-05 2005-05-26 Ping Ge Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands
WO2005061519A1 (en) 2003-12-19 2005-07-07 Takeda San Diego, Inc. Kinase inhibitors
AU2005233584B2 (en) * 2004-04-09 2010-12-09 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
AU2005233569B2 (en) * 2004-04-09 2010-08-19 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
TW200618800A (en) * 2004-08-03 2006-06-16 Uriach Y Compania S A J Heterocyclic compounds
EP1778669A2 (en) 2004-08-18 2007-05-02 Takeda San Diego, Inc. Kinase inhibitors
US7544677B2 (en) 2004-08-23 2009-06-09 Merck & Co., Inc. Inhibitors of Akt activity
ATE479687T1 (de) 2004-10-15 2010-09-15 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
CN101115479A (zh) * 2005-02-14 2008-01-30 默克公司 Akt活性抑制剂
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
US8008317B2 (en) * 2005-06-10 2011-08-30 Merck Sharp & Dohme Corp. Inhibitors of akt activtiy
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
US8017781B2 (en) 2005-11-15 2011-09-13 Vertex Pharmaceuticals Incorporated Azaindazoles useful as inhibitors of kinases
WO2007087246A2 (en) 2006-01-24 2007-08-02 Merck & Co., Inc. 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
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
EP2049500B1 (en) 2006-07-06 2011-09-07 Array Biopharma, Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
US8329701B2 (en) 2006-07-06 2012-12-11 Array Biopharma Inc. Dihydrofuro pyrimidines as AKT protein kinase inhibitors
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
EP1958947A1 (en) 2007-02-15 2008-08-20 Ranbaxy Laboratories Limited 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
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
CN103396409B (zh) 2007-07-05 2015-03-11 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
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
WO2009038784A1 (en) * 2007-09-21 2009-03-26 Amgen Inc. Triazole fused heteroaryl compounds as p38 kinase inhibitors
US8853216B2 (en) 2008-01-09 2014-10-07 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor
NZ586346A (en) 2008-01-09 2012-02-24 Array Biopharma Inc Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
US20100048524A1 (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
CA2726317A1 (en) * 2008-06-03 2009-12-10 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2299825B1 (en) * 2008-06-03 2013-07-31 Merck Sharp & Dohme Corp. Inhibitors of akt activity
ES2402087T3 (es) * 2008-07-23 2013-04-26 Vertex Pharmaceuticals Incorporated Inhibidores de la pirazolopiridina quinasa
WO2010091306A1 (en) 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
WO2010104705A1 (en) 2009-03-12 2010-09-16 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
US8859776B2 (en) 2009-10-14 2014-10-14 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
GB0919380D0 (en) * 2009-11-04 2009-12-23 Almac Discovery Ltd Pharmaceutical compouds
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation 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)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
KR102021157B1 (ko) 2011-04-01 2019-09-11 제넨테크, 인크. Ａｋｔ 억제제 화합물 및 아비라테론의 조합물, 및 사용 방법
TR201815685T4 (tr) 2011-04-01 2018-11-21 Genentech Inc Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları.
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TW201429969A (zh) 2012-12-20 2014-08-01 Merck Sharp & Dohme 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
KR20150127720A (ko) 2013-03-14 2015-11-17 유니버시티 오브 매릴랜드, 발티모어 안드로겐 수용체 하향 조절제 및 그의 용도
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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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WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
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EP3833669A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
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
CN115003303B (zh) 2019-12-17 2024-03-08 默沙东公司 Prmt5抑制剂
EP4076460B1 (en) 2019-12-17 2026-01-21 Merck Sharp & Dohme LLC 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer
JP7589247B2 (ja) 2019-12-17 2024-11-25 メルク・シャープ・アンド・ドーム・エルエルシー Ｐｒｍｔ５阻害剤
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WO2026027944A1 (en) 2024-07-30 2026-02-05 Sairopa B.V. Anti-sirp alpha antibody formulations and uses thereof

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WO1999020624A1 (en) * 1997-10-20 1999-04-29 F.Hoffmann-La Roche Ag Bicyclic kinase inhibitors
WO2002022608A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors

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

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