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DE602005026509D1 - Hemmer der akt aktivität - Google Patents

Hemmer der akt aktivität

Info

Publication number
DE602005026509D1
DE602005026509D1 DE602005026509T DE602005026509T DE602005026509D1 DE 602005026509 D1 DE602005026509 D1 DE 602005026509D1 DE 602005026509 T DE602005026509 T DE 602005026509T DE 602005026509 T DE602005026509 T DE 602005026509T DE 602005026509 D1 DE602005026509 D1 DE 602005026509D1
Authority
DE
Germany
Prior art keywords
compounds
hemmer
activity
act activity
directed
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.)
Active
Application number
DE602005026509T
Other languages
English (en)
Inventor
Mark T Bilodeau
Peter C Chua
Nicholas D P Cosford
Jacob M Hoffman
Johnny Yasuo Nagasawa
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 Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
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 and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of DE602005026509D1 publication Critical patent/DE602005026509D1/de
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
DE602005026509T 2004-04-09 2005-04-05 Hemmer der akt aktivität Active DE602005026509D1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56116704P 2004-04-09 2004-04-09
PCT/US2005/011687 WO2005100344A1 (en) 2004-04-09 2005-04-05 Inhibitors of akt activity

Publications (1)

Publication Number Publication Date
DE602005026509D1 true DE602005026509D1 (de) 2011-04-07

Family

ID=35149934

Family Applications (1)

Application Number Title Priority Date Filing Date
DE602005026509T Active DE602005026509D1 (de) 2004-04-09 2005-04-05 Hemmer der akt aktivität

Country Status (9)

Country Link
US (2) US7655649B2 (de)
EP (1) EP1737843B1 (de)
JP (1) JP2007532558A (de)
CN (1) CN1942465A (de)
AT (1) ATE499364T1 (de)
AU (1) AU2005233584B2 (de)
CA (1) CA2561311A1 (de)
DE (1) DE602005026509D1 (de)
WO (1) WO2005100344A1 (de)

Families Citing this family (66)

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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
JP4803034B2 (ja) 2004-06-30 2011-10-26 Ｍｓｄ株式会社 ビアリール誘導体
WO2006036395A2 (en) * 2004-08-23 2006-04-06 Merck & Co., Inc. Inhibitors of akt activity
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
EP2386554A1 (de) 2005-07-04 2011-11-16 High Point Pharmaceuticals, LLC Histamine H3 Rezeptor aktive Verbindungen
RU2416609C2 (ru) 2005-12-07 2011-04-20 Сумитомо Кемикал Компани, Лимитед Соединение пиридазина и его применение
EP1978964A4 (de) 2006-01-24 2009-12-09 Merck & Co Inc Jak2-tyrosinkinase-hemmung
UA97474C2 (ru) 2006-03-31 2012-02-27 Новартис Аг Соединения для лечения нарушений, связанных с активностью dgat1
NZ571972A (en) 2006-05-29 2011-09-30 High Point Pharmaceuticals Llc 3- (1, 3-benz0di0x0l-5-yl) -6- (4-cyclopropylpiperazin-1-yl) -pyridazine, its salts and solvates and its use as histamine h3 receptor antagonist
EP2120951A4 (de) * 2006-12-06 2012-02-15 Merck Sharp & Dohme Hemmer der akt-aktivität
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
EP2014656A3 (de) 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC Neue heterocyclische H3-Antagonisten
MX2010001745A (es) 2007-08-14 2010-03-10 Bayer Schering Pharma Ag Imidazoles fusionados para el tratamiento del cancer.
BRPI0815207A2 (pt) * 2007-08-14 2017-03-28 Bayer Schering Pharma Ag pirimidinas bicíclicas fundidas
EP2062893A1 (de) * 2007-10-18 2009-05-27 Bayer Schering Pharma AG Fusionierte Imidazole zur Behandlung von Krebs
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
CA2726317A1 (en) * 2008-06-03 2009-12-10 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2299825B1 (de) * 2008-06-03 2013-07-31 Merck Sharp & Dohme Corp. Hemmer der akt-aktivität
JP2012516900A (ja) 2009-02-05 2012-07-26 トーカイ ファーマシューティカルズ，インク． ステロイド性ｃｙｐ１７阻害剤／抗アンドロゲン剤の新しいプロドラッグ
US8957064B2 (en) 2009-02-13 2015-02-17 Bayer Intellectual Property Gmbh Fused pyrimidines
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US8168652B2 (en) 2009-03-12 2012-05-01 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
CN104945382B (zh) 2009-10-14 2020-02-07 默沙东公司 提高p53活性的取代的哌啶和其用途
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
CA2785618C (en) * 2009-12-28 2015-03-17 Development Center For Biotechnology Pyrimidine compounds as mtor and pi3k inhibitors
WO2011130921A1 (en) * 2010-04-23 2011-10-27 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2584903B1 (de) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Neue heterozyklische verbindungen als erk-hemmer
JP6043285B2 (ja) 2010-08-02 2016-12-14 サーナ・セラピューティクス・インコーポレイテッドＳｉｒｎａ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． 低分子干渉核酸（ｓｉＮＡ）を用いたカテニン（カドヘリン結合型タンパク質）β１（ＣＴＮＮＢ１）遺伝子発現のＲＮＡ干渉媒介性阻害
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)
EP2613782B1 (de) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. 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
EP2694486B1 (de) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituierte n-(3-(pyrimidin-4-yl-)phenyl-)acrylamid-analoga als tyrosinrezeptorkinase-btk-hemmer
PL2693881T3 (pl) * 2011-04-01 2020-03-31 University Of Utah Research Foundation Podstawione analogi N-fenylopirymidyno-2-aminy jako inhibitory kinazy AXL
EP2698372B1 (de) * 2011-04-06 2016-02-03 Taiho Pharmaceutical Co., Ltd. Neue imidazo-oxazin-verbindungen oder salze davon
EA024890B1 (ru) 2011-04-07 2016-10-31 Байер Интеллектчуал Проперти Гмбх Имидазопиридазины в качестве ингибиторов akt киназы
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
EP3919620A1 (de) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Zusammensetzungen mit kurzer interferierender nukleinsäure (sina)
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
KR20150067298A (ko) 2012-10-04 2015-06-17 유니버시티 오브 유타 리서치 파운데이션 티로신 수용체 키나아제 btk 억제제로서의 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체
WO2014055928A2 (en) 2012-10-04 2014-04-10 University Of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
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
BR112015013611A2 (pt) 2012-12-20 2017-11-14 Merck Sharp & Dohme composto, e, composição farmacêutica
EP2951180B1 (de) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8-substituierte purine als hdm2-inhibitoren
RU2019119893A (ru) 2013-03-14 2019-08-09 Толеро Фармасьютикалз, Инк. Ингибиторы jak2 и alk2 и способы их использования
EP2968370A4 (de) 2013-03-14 2016-09-21 Univ Maryland Mittel zur androgenrezeptor-abwärtsregelung und verwendungen davon
MX2016001901A (es) 2013-08-12 2016-10-13 Tokai Pharmaceuticals Inc Biomarcadores para tratamiento de trastornos neoplasicos usando terapias dirigidas con andrógeno.
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EP3240784A2 (de) * 2014-12-23 2017-11-08 BerGenBio ASA Inhibitoren der akt-kinase
WO2016136928A1 (ja) 2015-02-27 2016-09-01 大鵬薬品工業株式会社 イミダゾオキサジンの結晶、当該結晶を含む医薬組成物、及び当該結晶の製造方法
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
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
JP7160833B2 (ja) 2017-04-13 2022-10-25 サイロパ ビー．ブイ． 抗ｓｉｒｐアルファ抗体
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
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AU2002952121A0 (en) 2002-10-17 2002-10-31 Alchemia Limited Novel carbohydrate based anti-bacterials
EP1558586B1 (de) 2002-10-30 2011-03-30 Merck Sharp & Dohme Corp. Hemmer der akt aktivität
DE602004023838D1 (de) 2003-04-24 2009-12-10 Merck & Co Inc Hemmer der akt aktivität
AU2004233828B2 (en) 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2522262A1 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
US7638530B2 (en) 2003-04-24 2009-12-29 Merck & Co., Inc. Inhibitors of Akt activity
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
US20080103123A1 (en) * 2006-08-30 2008-05-01 Biovitrum New compounds

Also Published As

Publication number Publication date
JP2007532558A (ja) 2007-11-15
CA2561311A1 (en) 2005-10-27
ATE499364T1 (de) 2011-03-15
AU2005233584B2 (en) 2010-12-09
WO2005100344A1 (en) 2005-10-27
AU2005233584A1 (en) 2005-10-27
US7655649B2 (en) 2010-02-02
US20100075970A1 (en) 2010-03-25
EP1737843A1 (de) 2007-01-03
CN1942465A (zh) 2007-04-04
US20080280889A1 (en) 2008-11-13
EP1737843A4 (de) 2009-01-28
US8003643B2 (en) 2011-08-23
EP1737843B1 (de) 2011-02-23

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