WO2007076423A3 - INHIBITORS OF Akt ACTIVITY - Google Patents

INHIBITORS OF Akt ACTIVITY Download PDF

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Publication number
WO2007076423A3
WO2007076423A3 PCT/US2006/062453 US2006062453W WO2007076423A3 WO 2007076423 A3 WO2007076423 A3 WO 2007076423A3 US 2006062453 W US2006062453 W US 2006062453W WO 2007076423 A3 WO2007076423 A3 WO 2007076423A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
akt activity
activity
compounds
akt
Prior art date
Application number
PCT/US2006/062453
Other languages
French (fr)
Other versions
WO2007076423A2 (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
Original Assignee
Smithkline Beecham Corp
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
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 Smithkline Beecham Corp, 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 filed Critical Smithkline Beecham Corp
Priority to EP06846739A priority Critical patent/EP1968568A4/en
Priority to JP2008547763A priority patent/JP2009521504A/en
Publication of WO2007076423A2 publication Critical patent/WO2007076423A2/en
Publication of WO2007076423A3 publication Critical patent/WO2007076423A3/en

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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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)

Abstract

Invented are novel thiophene compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
PCT/US2006/062453 2005-12-22 2006-12-21 INHIBITORS OF Akt ACTIVITY WO2007076423A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP06846739A EP1968568A4 (en) 2005-12-22 2006-12-21 INHIBITORS OF Akt ACTIVITY
JP2008547763A JP2009521504A (en) 2005-12-22 2006-12-21 Akt activity inhibitor

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US75303305P 2005-12-22 2005-12-22
US60/753,033 2005-12-22
US79319806P 2006-04-19 2006-04-19
US60/793,198 2006-04-19

Publications (2)

Publication Number Publication Date
WO2007076423A2 WO2007076423A2 (en) 2007-07-05
WO2007076423A3 true WO2007076423A3 (en) 2007-11-29

Family

ID=38218824

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/062453 WO2007076423A2 (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)

Cited By (15)

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US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
US8933085B2 (en) 2010-11-19 2015-01-13 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US8933086B2 (en) 2005-12-13 2015-01-13 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-B]pyridines and pyrrolo[2,3-B]pyrimidines as Janus kinase inhibitors
US8987443B2 (en) 2013-03-06 2015-03-24 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
US9156845B2 (en) 2012-06-29 2015-10-13 Pfizer Inc. 4-(substituted amino)-7H-pyrrolo[2,3-d] pyrimidines as LRRK2 inhibitors
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US9216984B2 (en) 2009-05-22 2015-12-22 Incyte Corporation 3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane—or heptane-nitrile as JAK inhibitors
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
US9334274B2 (en) 2009-05-22 2016-05-10 Incyte Holdings Corporation 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
US9359358B2 (en) 2011-08-18 2016-06-07 Incyte Holdings Corporation Cyclohexyl azetidine derivatives as JAK inhibitors
US9464088B2 (en) 2010-03-10 2016-10-11 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
US9487521B2 (en) 2011-09-07 2016-11-08 Incyte Holdings Corporation Processes and intermediates for making a JAK inhibitor
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
US9580416B2 (en) 2014-07-02 2017-02-28 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase

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EP1926735A1 (en) 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
EA200870117A1 (en) 2005-12-23 2008-12-30 Смитклайн Бичам Корпорейшн AZAINDOL INHIBITORS AURORA-KINAZ
GB0617161D0 (en) * 2006-08-31 2006-10-11 Vernalis R&D Ltd Enzyme inhibitors
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
ES2543325T3 (en) * 2007-02-07 2015-08-18 Glaxosmithkline Llc Akt activity inhibitors
UY30892A1 (en) 2007-02-07 2008-09-02 Smithkline Beckman Corp AKT ACTIVITY INHIBITORS
CL2008001709A1 (en) 2007-06-13 2008-11-03 Incyte Corp Compounds derived from pyrrolo [2,3-b] pyrimidine, jak kinase modulators; pharmaceutical composition; and use in the treatment of diseases such as cancer, psoriasis, rheumatoid arthritis, among others.
PL2173752T5 (en) 2007-06-13 2022-12-05 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
AU2008331733A1 (en) 2007-11-02 2009-06-11 Vertex Pharmaceuticals Incorporated [1H- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase C-theta
ES2604555T3 (en) * 2007-12-07 2017-03-07 Vertex Pharmaceuticals Incorporated Process for producing cycloalkylcarboxyamido-pyridinebenzoic acids
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
EA017218B1 (en) 2008-03-11 2012-10-30 Инсайт Корпорейшн Azetidine and cyclobutane derivatives as jak inhibitors
US20110092423A1 (en) * 2008-06-26 2011-04-21 GlaxoSmithKline, LLC INHIBITORS OF Akt ACTIVITY
EP2400964A4 (en) 2009-01-30 2012-08-01 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
CN102459221A (en) * 2009-04-30 2012-05-16 住友化学株式会社 Thiophene derivative
EP2486041B1 (en) 2009-10-09 2013-08-14 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
DK2574168T3 (en) 2010-05-21 2016-05-09 Incyte Holdings Corp Topical formulation to a jak inhibitor
CA2827673C (en) 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
US9358229B2 (en) 2011-08-10 2016-06-07 Novartis Pharma Ag JAK PI3K/mTOR combination therapy
CN104507923B (en) * 2012-08-02 2018-02-09 内尔维阿诺医学科学有限公司 Substituted pyroles activating agent as kinase inhibitor
DE102012019369A1 (en) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
MY191357A (en) 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
TW201533043A (en) * 2013-04-18 2015-09-01 Lundbeck & Co As H Arylpyrrolopyridine derived compounds as LRRK2 inhibitors
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
WO2015092592A1 (en) 2013-12-17 2015-06-25 Pfizer Inc. 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
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
WO2017156071A1 (en) 2016-03-09 2017-09-14 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
AU2017336523B2 (en) 2016-09-28 2022-07-21 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
KR20190043437A (en) * 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 Heterocylic compound as a protein kinase inhibitor
TW201924683A (en) 2017-12-08 2019-07-01 美商英塞特公司 Low dose combination therapy for treatment of myeloproliferative neoplasms
WO2019114741A1 (en) * 2017-12-13 2019-06-20 南京明德新药研发股份有限公司 Salt serving as akt inhibitor and crystal thereof
CN112105608B (en) 2018-01-30 2023-07-14 因赛特公司 Process for the preparation of (1- (3-fluoro-2- (trifluoromethyl) isonicotinyl) piperidin-4-one
MX2022012285A (en) 2018-03-30 2023-08-15 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors.
WO2019195634A1 (en) * 2018-04-04 2019-10-10 Epiodyne, Inc. Opioid receptor modulators and products and methods related thereto
CN112888440A (en) 2018-10-16 2021-06-01 豪夫迈·罗氏有限公司 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

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Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9206187B2 (en) 2005-12-13 2015-12-08 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-B] pyridines and pyrrolo[2,3-B] pyrimidines as Janus kinase
US8933086B2 (en) 2005-12-13 2015-01-13 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-B]pyridines and pyrrolo[2,3-B]pyrimidines as Janus kinase inhibitors
US8946245B2 (en) 2005-12-13 2015-02-03 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US9334274B2 (en) 2009-05-22 2016-05-10 Incyte Holdings Corporation 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
US9216984B2 (en) 2009-05-22 2015-12-22 Incyte Corporation 3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane—or heptane-nitrile as JAK inhibitors
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
US9464088B2 (en) 2010-03-10 2016-10-11 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
US8933085B2 (en) 2010-11-19 2015-01-13 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
US9023840B2 (en) 2011-06-20 2015-05-05 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
US9359358B2 (en) 2011-08-18 2016-06-07 Incyte Holdings Corporation Cyclohexyl azetidine derivatives as JAK inhibitors
US9487521B2 (en) 2011-09-07 2016-11-08 Incyte Holdings Corporation Processes and intermediates for making a JAK inhibitor
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US9156845B2 (en) 2012-06-29 2015-10-13 Pfizer Inc. 4-(substituted amino)-7H-pyrrolo[2,3-d] pyrimidines as LRRK2 inhibitors
US9221845B2 (en) 2013-03-06 2015-12-29 Incyte Holdings Corporation Processes and intermediates for making a JAK inhibitor
US8987443B2 (en) 2013-03-06 2015-03-24 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
US9580416B2 (en) 2014-07-02 2017-02-28 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase

Also Published As

Publication number Publication date
EP1968568A4 (en) 2011-04-13
WO2007076423A2 (en) 2007-07-05
JP2009521504A (en) 2009-06-04
EP1968568A2 (en) 2008-09-17

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