EP1968568A4 - INHIBITORS OF Akt ACTIVITY - Google Patents

INHIBITORS OF Akt ACTIVITY

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Withdrawn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)
French (fr)
Other versions
EP1968568A2 (en
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/en
Publication of EP1968568A4 publication Critical patent/EP1968568A4/en
Withdrawn legal-status Critical Current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
EP06846739A 2005-12-22 2006-12-21 INHIBITORS OF Akt ACTIVITY Withdrawn EP1968568A4 (en)

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 (en) 2005-12-22 2006-12-21 INHIBITORS OF Akt ACTIVITY

Publications (2)

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

Family

ID=38218824

Family Applications (1)

Application Number Title Priority Date Filing Date
EP06846739A Withdrawn EP1968568A4 (en) 2005-12-22 2006-12-21 INHIBITORS OF Akt ACTIVITY

Country Status (3)

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

Families Citing this family (60)

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MX2008008320A (en) 2005-12-23 2008-09-03 Smithkline Beecham Corp Azaindole inhibitors of aurora kinases.
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US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
UY30892A1 (en) * 2007-02-07 2008-09-02 Smithkline Beckman Corp AKT ACTIVITY INHIBITORS
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SG10201509887UA (en) 2007-06-13 2016-01-28 Incyte Corp Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
TW200924762A (en) 2007-11-02 2009-06-16 Vertex Pharma Kinase inhibitors
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JP5635910B2 (en) * 2008-01-09 2014-12-03 アレイ バイオファーマ、インコーポレイテッド 5H-cyclopenta [d] pyrimidine as an AKT protein kinase inhibitor
ES2602577T3 (en) 2008-03-11 2017-02-21 Incyte Holdings Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
JP2011525929A (en) * 2008-06-26 2011-09-29 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Inhibitor of Akt activity
SG172926A1 (en) 2009-01-30 2011-08-29 Glaxosmithkline Llc Crystalline n-{(1-s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
WO2010093885A1 (en) * 2009-02-12 2010-08-19 Glaxosmithkline Llc Inhibitors of akt activity
AU2010242307A1 (en) * 2009-04-30 2011-11-24 Sumitomo Chemical Company, Limited Thiophene derivative
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
EA025520B1 (en) 2009-05-22 2017-01-30 Инсайт Холдингс Корпорейшн N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
US8486902B2 (en) 2009-10-09 2013-07-16 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
MX347851B (en) 2010-03-10 2017-05-16 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors.
EP2574168B9 (en) 2010-05-21 2016-10-05 Incyte Holdings Corporation Topical formulation for a jak inhibitor
WO2012068450A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
AU2012219395B2 (en) 2011-02-18 2017-05-25 Incyte Corporation mTOR/JAK inhibitor combination therapy
CA2839767A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (en) 2011-08-18 2013-04-01 Incyte Corp Cyclohexyl azetidine derivatives as JAK inhibitors
UA111854C2 (en) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
NZ702571A (en) 2012-06-29 2017-02-24 Pfizer 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors
BR112015002152B1 (en) * 2012-08-02 2021-04-27 Nerviano Medical Sciences S.R.L. COMPOUNDS OF REPLACED PYRROILS ACTIVE AS KINASE INHIBITORS, PROCESS FOR THE PREPARATION OF SUCH COMPOUNDS, PHARMACEUTICAL COMPOSITION, IN VITRO METHOD FOR INHIBITION OF THE ACTIVITY OF KINASE PROTEINS OF THE JAK FAMILY
DE102012019369A1 (en) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
BR112015010663B1 (en) 2012-11-15 2022-12-06 Incyte Holdings Corporation SUSTAINED RELEASE ORAL DOSAGE FORMS AND USE OF RUXOLITINIB OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
CN105189509B (en) 2013-03-06 2017-12-19 因赛特公司 For preparing the method and intermediate of JAK inhibitor
TW201533043A (en) 2013-04-18 2015-09-01 Lundbeck & Co As H Arylpyrrolopyridine derived compounds as LRRK2 inhibitors
RS60469B1 (en) 2013-08-07 2020-07-31 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
JP6487921B2 (en) 2013-12-17 2019-03-20 ファイザー・インク Novel 3,4-disubstituted-1H-pyrrolo [2,3-b] pyridines and 4,5-disubstituted-7H-pyrrolo [2,3-c] pyridazines as LRRK2 inhibitors
CN103833725B (en) * 2014-03-03 2016-06-08 上海北卡医药技术有限公司 A kind of method synthesizing 5-N-tertiary butoxy carbonyl-5-N-methylamino-2-thiophenic acid
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2016004272A1 (en) 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
CN108137586B (en) 2015-09-14 2021-04-13 辉瑞大药厂 Novel imidazo [4,5-c ] quinoline and imidazo [4,5-c ] [1,5] naphthyridine derivatives as LRRK2 inhibitors
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
US11292801B2 (en) 2016-07-05 2022-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CA3038331A1 (en) 2016-09-28 2018-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CN108948002A (en) * 2017-05-19 2018-12-07 厦门大学 Five yuan and hexa-atomic nitrogen heteroaromatic rings class compound, preparation method, Pharmaceutical composition and its application
JOP20180094A1 (en) 2017-10-18 2019-04-18 Hk Inno N Corp Heterocyclic compound as a protein kinase inhibito
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
KR102394934B1 (en) * 2017-12-13 2022-05-04 하얼빈 젠바오 파마슈티컬 컴퍼니, 리미티드 Salt form and crystal form thereof as Akt inhibitor
WO2019152374A1 (en) 2018-01-30 2019-08-08 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
MX2022012285A (en) 2018-03-30 2023-08-15 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors.
AU2019247842B2 (en) * 2018-04-04 2023-08-31 Epiodyne, Inc. Opioid receptor modulators and products and methods related thereto
JP2022512706A (en) 2018-10-16 2022-02-07 エフ．ホフマン－ラ ロシュ アーゲー Use of Akt inhibitors in ophthalmology
WO2020150417A2 (en) * 2019-01-17 2020-07-23 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN112266349B (en) * 2020-11-17 2022-02-15 上海凌凯医药科技有限公司 Method for preparing 2-amino-4-methyl-1-propyl-1H-pyrrole-3-carbonitrile
CN115073469B (en) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 Preparation and application of pyrrolopyrimidine compound as kinase inhibitor
WO2022216717A1 (en) * 2021-04-05 2022-10-13 The Cleveland Clinic Foundation Citron kinase inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005103050A2 (en) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
WO2006004984A1 (en) * 2004-06-30 2006-01-12 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
WO2006058120A1 (en) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
WO2006127587A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase

Family Cites Families (1)

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Publication number Priority date Publication date Assignee Title
RU2006121990A (en) * 2003-11-21 2007-12-27 Эррэй Биофарма Инк. (Us) ACT PROTEINKINASE INHIBITORS

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005103050A2 (en) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
WO2006004984A1 (en) * 2004-06-30 2006-01-12 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
WO2006058120A1 (en) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
WO2006127587A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase

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
EP1968568A2 (en) 2008-09-17
JP2009521504A (en) 2009-06-04
WO2007076423A3 (en) 2007-11-29
WO2007076423A2 (en) 2007-07-05

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Legal Events

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PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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Effective date: 20080704

AK Designated contracting states

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Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR

AX Request for extension of the european patent

Extension state: HR

RAP1 Party data changed (applicant data changed or rights of an application transferred)

Owner name: GLAXOSMITHKLINE LLC

A4 Supplementary search report drawn up and despatched

Effective date: 20110311

RIC1 Information provided on ipc code assigned before grant

Ipc: A61P 19/02 20060101ALI20110307BHEP

Ipc: A61P 35/00 20060101ALI20110307BHEP

Ipc: A61K 31/33 20060101AFI20080722BHEP

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Effective date: 20110609