EP1968568A4 - INHIBITORS OF Akt ACTIVITY - Google Patents
INHIBITORS OF Akt ACTIVITYInfo
- 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- Withdrawn
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
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
MY162590A (en) | 2005-12-13 | 2017-06-30 | Incyte Holdings Corp | Heteroaryl substituted pyrrolo[2,3-b] pyridines and pyrrolo[2,3-b] pyrimidines as janus kinase inhibitors |
KR20080083680A (en) | 2005-12-23 | 2008-09-18 | 스미스클라인 비참 코포레이션 | Azaindole inhibitors of aurora kinases |
GB0617161D0 (en) * | 2006-08-31 | 2006-10-11 | Vernalis R&D Ltd | Enzyme inhibitors |
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 |
JP5363997B2 (en) * | 2007-02-07 | 2013-12-11 | 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 |
EP3495369B1 (en) | 2007-06-13 | 2021-10-27 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
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. |
CA2704266A1 (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 |
CN101910134B (en) * | 2007-12-07 | 2014-03-19 | 沃泰克斯药物股份有限公司 | Processes for producing cycloalkylcarboxiamido-pyridine benzoic acids |
US8329709B2 (en) * | 2008-01-09 | 2012-12-11 | Genentech, Inc. | 5H-cyclopenta[D]pyrimidines as AKT protein kinase inhibitors |
SI2288610T1 (en) | 2008-03-11 | 2016-11-30 | Incyte Holdings Corporation | Azetidine and cyclobutane derivatives as jak inhibitors |
WO2009158372A1 (en) * | 2008-06-26 | 2009-12-30 | Smithkline Beecham Corporation | Inhibitors of akt activity |
JP2012516344A (en) | 2009-01-30 | 2012-07-19 | 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 | Crystalline N-{(1S) -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 |
KR20120023018A (en) * | 2009-04-30 | 2012-03-12 | 스미또모 가가꾸 가부시키가이샤 | Thiophene derivative |
MX2011012262A (en) | 2009-05-22 | 2012-01-25 | 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 |
TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
PT2486041E (en) | 2009-10-09 | 2013-11-14 | Incyte Corp | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
SI3354652T1 (en) | 2010-03-10 | 2020-08-31 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
SG10201910912TA (en) | 2010-05-21 | 2020-01-30 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
BR112013012502A2 (en) | 2010-11-19 | 2019-03-06 | Incyte Corporation | substituted cyclobutyl pyrrolopyridine and derivative pyrrolopyrimidine derivatives as jak inhibitors |
US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
EP2741747A1 (en) | 2011-08-10 | 2014-06-18 | 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 |
MD20140130A2 (en) | 2012-06-29 | 2015-04-30 | Pfizer Inc. | Novel 4-(substituted-amino)-7H-pyrrolo[2,3-d]pyrimidines as LRRK2 inhibitors |
JP6276762B2 (en) * | 2012-08-02 | 2018-02-07 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | Substituted pyrroles active as kinase inhibitors |
DE102012019369A1 (en) | 2012-10-02 | 2014-04-03 | Merck Patent Gmbh | 7-Azaindolderivat |
SG11201503695XA (en) | 2012-11-15 | 2015-06-29 | Incyte Corp | Sustained-release dosage forms of ruxolitinib |
EA030705B1 (en) | 2013-03-06 | 2018-09-28 | Инсайт Холдингс Корпорейшн | Processes and intermediates for making a jak inhibitor |
TW201533043A (en) * | 2013-04-18 | 2015-09-01 | Lundbeck & Co As H | Arylpyrrolopyridine derived compounds as LRRK2 inhibitors |
ES2792549T3 (en) | 2013-08-07 | 2020-11-11 | Incyte Corp | Sustained-release dosage forms for a JAK1 inhibitor |
CA2933767C (en) | 2013-12-17 | 2018-11-06 | 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 |
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 |
TW201613919A (en) | 2014-07-02 | 2016-04-16 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
AU2016322813B2 (en) | 2015-09-14 | 2021-04-01 | Pfizer Inc. | 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 |
AU2017292646A1 (en) | 2016-07-05 | 2019-02-07 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
EP3523294A4 (en) | 2016-09-28 | 2021-01-13 | 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 |
US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
CN111433213B (en) * | 2017-12-13 | 2023-03-10 | 哈尔滨珍宝制药有限公司 | Salt forms and crystalline forms thereof as Akt inhibitors |
PL3746429T3 (en) | 2018-01-30 | 2022-06-20 | Incyte Corporation | Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
WO2019191684A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Treatment of hidradenitis suppurativa using jak inhibitors |
JP7402857B2 (en) * | 2018-04-04 | 2023-12-21 | エピオダイン,インク. | Opioid receptor modulators and related products and methods |
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 |
TW202043198A (en) * | 2019-01-17 | 2020-12-01 | 美商Ifm Due有限公司 | 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)
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101223914B1 (en) * | 2003-11-21 | 2013-01-18 | 어레이 바이오파마 인크. | Akt protein kinase inhibitors |
-
2006
- 2006-12-21 JP JP2008547763A patent/JP2009521504A/en not_active Withdrawn
- 2006-12-21 EP EP06846739A patent/EP1968568A4/en not_active Withdrawn
- 2006-12-21 WO PCT/US2006/062453 patent/WO2007076423A2/en active Application Filing
Patent Citations (4)
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)
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 |
WO2007076423A3 (en) | 2007-11-29 |
JP2009521504A (en) | 2009-06-04 |
WO2007076423A2 (en) | 2007-07-05 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
17P | Request for examination filed |
Effective date: 20080704 |
|
AK | Designated contracting states |
Kind code of ref document: A2 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 |
|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
|
18D | Application deemed to be withdrawn |
Effective date: 20110609 |