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
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 (63)

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JP2008510823A (ja) * 2004-08-23 2008-04-10 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性阻害剤
US20100047338A1 (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
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
AU2006264966B2 (en) 2005-07-04 2013-02-21 High Point Pharmaceuticals, Llc Histamine H3 receptor antagonists
RU2416609C2 (ru) * 2005-12-07 2011-04-20 Сумитомо Кемикал Компани, Лимитед Соединение пиридазина и его применение
US20090062302A1 (en) 2006-01-24 2009-03-05 Buser-Doepner Carolyn A Jak2 Tyrosine Kinase Inhibition
JP5467862B2 (ja) 2006-03-31 2014-04-09 ノバルティス アーゲー 新規化合物
SI2079732T1 (sl) 2006-05-29 2012-03-30 High Point Pharmaceuticals Llc benzodioksol il ciklopropilpiperazin il piridazin njegove soli in solvati in njegova uporaba kot antagonist histaminskega receptorja H
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
EP2014656A3 (de) 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC Neue heterocyclische H3-Antagonisten
EA201000297A1 (ru) 2007-08-14 2010-08-30 Байер Шеринг Фарма Акциенгезельшафт Конденсированные бициклические имидазолы
TWI439272B (zh) * 2007-08-14 2014-06-01 拜耳知識產權公司 稠合雙環嘧啶
EP2062893A1 (de) * 2007-10-18 2009-05-27 Bayer Schering Pharma AG Fusionierte Imidazole zur Behandlung von Krebs
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
WO2009148887A1 (en) * 2008-06-03 2009-12-10 Merck & Co., Inc. Inhibitors of akt activity
CA2761389A1 (en) 2009-02-05 2010-08-12 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
CA2752114C (en) 2009-02-13 2017-06-20 Bayer Pharma Aktiengesellschaft Fused pyrimidines as akt inhibitors
MX2011008583A (es) 2009-02-13 2011-12-12 Bayer Pharma AG Pirimidinas fusionadas.
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
CN102638981B (zh) 2009-10-14 2015-07-22 默沙东公司 提高p53活性的取代的哌啶和其用途
AU2010338011B2 (en) * 2009-12-28 2015-04-02 Development Center For Biotechnology Novel pyrimidine compounds as mTOR and P13K inhibitors
US9315491B2 (en) 2009-12-28 2016-04-19 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
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)
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)
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2632472B1 (de) 2010-10-29 2017-12-13 Sirna Therapeutics, Inc. Durch rna-interferenz vermittelte inhibition einer genexpression unter verwendung von short-interfering-nukleinsäuren (sina)
EP2654748B1 (de) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
US8703767B2 (en) 2011-04-01 2014-04-22 University Of Utah Research Foundation Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
JP6118794B2 (ja) * 2011-04-01 2017-04-19 ザ ユニバーシティ オブ ユタ リサーチ ファウンデイション Ａｘｌキナーゼの阻害剤としての置換ｎ−フェニルピリミジン−２−アミン類似体
EP2698372B1 (de) * 2011-04-06 2016-02-03 Taiho Pharmaceutical Co., Ltd. Neue imidazo-oxazin-verbindungen oder salze davon
AP3597A (en) 2011-04-07 2016-02-19 Bayer Ip Gmbh Imidazopyridazines as akt kinase inhibitors
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
EP3453762B1 (de) 2012-05-02 2021-04-21 Sirna Therapeutics, Inc. Sina-zusammensetzungen
US9233979B2 (en) 2012-09-28 2016-01-12 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP2903972B1 (de) 2012-10-04 2019-12-04 University of Utah Research Foundation Substituierte n-(3-(pyrimidin-4-yl-)phenyl-)acrylamid-analoga als tyrosinrezeptorkinase-btk-hemmer
US9296703B2 (en) 2012-10-04 2016-03-29 University Of Utah Research Foundation Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
RU2660349C2 (ru) 2012-11-28 2018-07-05 Мерк Шарп И Доум Корп. Композиции и способы для лечения злокачественной опухоли
BR112015013611A2 (pt) 2012-12-20 2017-11-14 Merck Sharp & Dohme composto, e, composição farmacêutica
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
ES2738493T3 (es) 2013-03-14 2020-01-23 Tolero Pharmaceuticals Inc Inhibidores de JAK2 y ALK2 y métodos para su uso
EP4066841A1 (de) 2013-03-14 2022-10-05 University of Maryland, Baltimore Mittel zur androgenrezeptor-abwärtsregelung und verwendungen davon
AU2014306698A1 (en) 2013-08-12 2016-01-28 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
JP6787899B2 (ja) * 2014-12-23 2020-11-18 ベルゲンビオ アーエスアー 医薬的活性化合物
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
KR20190140454A (ko) 2017-04-13 2019-12-19 아두로 바이오테크 홀딩스, 유럽 비.브이. 항-sirp 알파 항체
EP3706742B1 (de) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5-inhibitoren
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
US11013741B1 (en) 2018-04-05 2021-05-25 Sumitomo Dainippon Pharma Oncology, Inc. AXL kinase inhibitors and use of the same
CA3103995A1 (en) 2018-07-26 2020-01-30 Sumitomo Dainippon Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP4077282A4 (de) 2019-12-17 2023-11-08 Merck Sharp & Dohme LLC Prmt5-inhibitoren

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AU2002252614B2 (en) * 2001-04-10 2006-09-14 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US20050130977A1 (en) * 2002-04-08 2005-06-16 Lindsley Craig W. Inhibitors of akt activity
AU2003226271B2 (en) * 2002-04-08 2007-10-18 Merck Sharp & Dohme Corp. Fused quinoxaline derivatives as inhibitors of Akt activity
AU2003226250B2 (en) * 2002-04-08 2007-08-16 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US7223738B2 (en) * 2002-04-08 2007-05-29 Merck & Co., Inc. Inhibitors of Akt activity
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DE60336576D1 (de) * 2002-10-30 2011-05-12 Merck Sharp & Dohme Hemmer der akt aktivität
WO2004096130A2 (en) * 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
CA2522431A1 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
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Also Published As

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

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