EP1968568A4 - INHIBITEURS D'ACTIVITE Akt - Google Patents

INHIBITEURS D'ACTIVITE Akt

Info

Publication number
EP1968568A4
EP1968568A4 EP06846739A EP06846739A EP1968568A4 EP 1968568 A4 EP1968568 A4 EP 1968568A4 EP 06846739 A EP06846739 A EP 06846739A EP 06846739 A EP06846739 A EP 06846739A EP 1968568 A4 EP1968568 A4 EP 1968568A4
Authority
EP
European Patent Office
Prior art keywords
inhibitors
akt activity
akt
activity
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.)
Withdrawn
Application number
EP06846739A
Other languages
German (de)
English (en)
Other versions
EP1968568A2 (fr
Inventor
Mark Andrew Seefeld
Toshihiro Hamajima
David Kendall Jung
Hiroko Nakamura
Paul R Reid
Michael John Reno
Meagan B Rouse
Dirk A Heerding
Jun Tang
Jizhou Wang
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.)
GlaxoSmithKline LLC
Original Assignee
GlaxoSmithKline 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 GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of EP1968568A2 publication Critical patent/EP1968568A2/fr
Publication of EP1968568A4 publication Critical patent/EP1968568A4/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EP06846739A 2005-12-22 2006-12-21 INHIBITEURS D'ACTIVITE Akt Withdrawn EP1968568A4 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US75303305P 2005-12-22 2005-12-22
US79319806P 2006-04-19 2006-04-19
PCT/US2006/062453 WO2007076423A2 (fr) 2005-12-22 2006-12-21 INHIBITEURS D’ACTIVITE Akt

Publications (2)

Publication Number Publication Date
EP1968568A2 EP1968568A2 (fr) 2008-09-17
EP1968568A4 true EP1968568A4 (fr) 2011-04-13

Family

ID=38218824

Family Applications (1)

Application Number Title Priority Date Filing Date
EP06846739A Withdrawn EP1968568A4 (fr) 2005-12-22 2006-12-21 INHIBITEURS D'ACTIVITE Akt

Country Status (3)

Country Link
EP (1) EP1968568A4 (fr)
JP (1) JP2009521504A (fr)
WO (1) WO2007076423A2 (fr)

Families Citing this family (60)

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US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
HUE030235T2 (en) 2005-12-13 2017-04-28 Incyte Holdings Corp Heteroaryl-substituted pyrrolo [2,3-b] pyridines and pyrrolo [2,3-b] pyrimidines as Janus kinase inhibitors
SI1962830T1 (sl) 2005-12-23 2013-07-31 Glaxosmithkline Llc Azaindolni inhibitorji kinaz Aurora
GB0617161D0 (en) * 2006-08-31 2006-10-11 Vernalis R&D Ltd Enzyme inhibitors
WO2008079965A1 (fr) 2006-12-22 2008-07-03 Incyte Corporation Hétérocycles substitués servant d'inhibiteurs de janus kinases
WO2008098105A1 (fr) * 2007-02-07 2008-08-14 Smithkline Beecham Corporation Inhibiteurs de l'activité de akt
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
EP3070090B1 (fr) 2007-06-13 2018-12-12 Incyte Holdings Corporation Utilisation des sels de l'inhibiteur de janus kinase (r)-3-(4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl)-1h-pyrazol-1-yl) -3-cyclopentylpropanenitrile
EP2215089B1 (fr) 2007-11-02 2012-06-27 Vertex Pharmaceuticals Incorporated Dérivés de [1h-pyrazolo[3,4-b]pyridin-4-yl]-phényle ou -pyridin-2-yle en tant qu'inhibiteurs de la protéine kinase c-thêta
PL2639223T3 (pl) * 2007-12-07 2017-09-29 Vertex Pharmaceuticals Incorporated Sposób wytwarzania kwasów cykloalkilokarboksyamido-pirydyno-benzoesowych
ES2426092T3 (es) * 2008-01-09 2013-10-21 Array Biopharma, Inc. 5H-Ciclopenta[d]pirimidinas como inhibidores de proteínas cinasas AKT
ES2602577T3 (es) 2008-03-11 2017-02-21 Incyte Holdings Corporation Derivados de azetidina y ciclobutano como inhibidores de JAK
EP2303017A4 (fr) * 2008-06-26 2011-06-15 Glaxosmithkline Llc Inhibiteurs d activité akt
PE20120003A1 (es) 2009-01-30 2012-02-12 Glaxosmithkline Llc Hidrocloruro de n-{(1s)-2-amino-1-[(3-fluorofenil)metil)etil}-5-cloro-4-(4-cloro-1-metil-1h-pirazol-5-il)-2-tiofenocarboxamida cristalino
WO2010093885A1 (fr) * 2009-02-12 2010-08-19 Glaxosmithkline Llc Inhibiteurs de l'activité d'akt
US20120065231A1 (en) * 2009-04-30 2012-03-15 Sumitomo Chemical Company Ltd. Thiophene derivative
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
EA020494B1 (ru) 2009-05-22 2014-11-28 Инсайт Корпорейшн 3-[4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ]ОКТАН- ИЛИ ГЕПТАННИТРИЛ КАК JAK-ИНГИБИТОРЫ
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
WO2011044481A1 (fr) 2009-10-09 2011-04-14 Incyte Corporation Dérivés hydroxy, céto et glucuronides de 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3- cyclopentylpropanenitrile
MX347851B (es) 2010-03-10 2017-05-16 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
EP3087972A1 (fr) 2010-05-21 2016-11-02 Incyte Holdings Corporation Formulation topique pour un inhibiteur jak
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2640725B1 (fr) 2010-11-19 2015-01-07 Incyte Corporation Pyrrolopyridines et pyrrolopyrimidines à substitution hétérocyclique utilisées en tant qu'inhibiteurs des jak
KR102024948B1 (ko) 2011-02-18 2019-11-04 노파르티스 파르마 아게 mTOR/JAK 저해제 병용 요법
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
WO2013023119A1 (fr) 2011-08-10 2013-02-14 Novartis Pharma Ag Polythérapie par jak p13k/mtor
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
AP3902A (en) 2012-06-29 2016-11-17 Pfizer Novel 4-(substituted-amino)-7H-pyrrolo[2,3-d]pyrimidines as LRRK2 inhibitors
ES2726833T3 (es) * 2012-08-02 2019-10-09 Nerviano Medical Sciences Srl Pirroles sustituidos activos como inhibidores de cinasas
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
KR20220162825A (ko) 2012-11-15 2022-12-08 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
AU2014225938B2 (en) 2013-03-06 2018-07-19 Incyte Holdings Corporation Processes and intermediates for making a JAK inhibitor
TW201533043A (zh) 2013-04-18 2015-09-01 Lundbeck & Co As H 作爲ｌｒｒｋ２抑制劑的芳基吡咯并吡啶衍生化合物
KR20160045081A (ko) 2013-08-07 2016-04-26 인사이트 코포레이션 Jak1 억제제용 지속 방출 복용 형태
JP6487921B2 (ja) 2013-12-17 2019-03-20 ファイザー・インク ＬＲＲＫ２阻害薬としての新規の３，４−二置換−１Ｈ−ピロロ［２，３−ｂ］ピリジンおよび４，５−二置換−７Ｈ−ピロロ［２，３−ｃ］ピリダジン
CN103833725B (zh) * 2014-03-03 2016-06-08 上海北卡医药技术有限公司 一种合成5-n-叔丁氧羰基-5-n-甲基氨基-2-噻吩甲酸的方法
WO2015184305A1 (fr) 2014-05-30 2015-12-03 Incyte Corporation Traitement de la leucémie neutrophile chronique (cnl) et de la leucémie myéloïde chronique atypique (acml) par des inhibiteurs de jak1
WO2016004305A2 (fr) 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibiteurs de la tyrosine kinase de bruton
MX2018003215A (es) 2015-09-14 2018-06-08 Pfizer Derivados de imidazo[4,5-c]quinolina e imidazo[4,5-c][1,5]naftirid ina novedosos como inhibidores de lrrk2.
US10590084B2 (en) 2016-03-09 2020-03-17 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2018009417A1 (fr) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Modulateurs de calpain et leurs utilisations thérapeutiques
US10934261B2 (en) 2016-09-28 2021-03-02 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CN108948002A (zh) * 2017-05-19 2018-12-07 厦门大学 五元并六元氮杂芳环类化合物、其制备方法、药用组合物及其应用
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
WO2019114741A1 (fr) * 2017-12-13 2019-06-20 南京明德新药研发股份有限公司 Sel servant d'inhibiteur d'akt et cristal de celui-ci
TWI797242B (zh) 2018-01-30 2023-04-01 美商英塞特公司 製備ｊａｋ抑制劑之方法及中間物
MX2022012285A (es) 2018-03-30 2023-08-15 Incyte Corp Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak).
AU2019247842B2 (en) * 2018-04-04 2023-08-31 Epiodyne, Inc. Opioid receptor modulators and products and methods related thereto
EP3866807A1 (fr) 2018-10-16 2021-08-25 F. Hoffmann-La Roche AG Utilisation d'inhibiteurs d'akt en ophtalmologie
WO2020150417A2 (fr) * 2019-01-17 2020-07-23 Ifm Due, Inc. Composés et compositions pour traiter des états pathologiques associés à une activité de sting
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN112266349B (zh) * 2020-11-17 2022-02-15 上海凌凯医药科技有限公司 一种制备2-氨基-4-甲基-1-丙基-1h-吡咯-3-甲腈的方法
CN115073469B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用
WO2022216717A1 (fr) * 2021-04-05 2022-10-13 The Cleveland Clinic Foundation Inhibiteurs de citron kinase

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005103050A2 (fr) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles utiles en tant qu'inhibiteurs de la proteine serine/threonine kinase superhelice de la famille rho (rock) et d'autres proteines kinases
WO2006004984A1 (fr) * 2004-06-30 2006-01-12 Vertex Pharmaceuticals Incorporated Azaindoles utilises comme inhibiteurs de proteine kinases
WO2006058120A1 (fr) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Inhibiteurs bicycliques de rho kinase
WO2006127587A1 (fr) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines utiles en tant qu'inhibiteurs de proteines kinases

Family Cites Families (1)

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Publication number Priority date Publication date Assignee Title
CN102786482A (zh) * 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005103050A2 (fr) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles utiles en tant qu'inhibiteurs de la proteine serine/threonine kinase superhelice de la famille rho (rock) et d'autres proteines kinases
WO2006004984A1 (fr) * 2004-06-30 2006-01-12 Vertex Pharmaceuticals Incorporated Azaindoles utilises comme inhibiteurs de proteine kinases
WO2006058120A1 (fr) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Inhibiteurs bicycliques de rho kinase
WO2006127587A1 (fr) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines utiles en tant qu'inhibiteurs de proteines kinases

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
IUPAC ED - ALAN D MCNAUGHT AND ANDREW WILKINSON: "alkyl groups", 1 January 1997, COMPENDIUM OF CHEMICAL TERMINOLOGY : IUPAC RECOMMENDATIONS; [IUPAC CHEMICAL DATA SERIES], BLACKWELL SCIENCE, OXFORD [U.A.], ISBN: 978-0-86542-684-9, XP002585005 *
IUPAC: "Aryl groups", INTERNET CITATION, 1997, pages 1, XP002582725, Retrieved from the Internet <URL:http://www.iupac.org/goldbook/A00464.pdf> [retrieved on 20100519] *

Also Published As

Publication number Publication date
WO2007076423A3 (fr) 2007-11-29
WO2007076423A2 (fr) 2007-07-05
EP1968568A2 (fr) 2008-09-17
JP2009521504A (ja) 2009-06-04

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