PE20090365A1 - IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS - Google Patents

IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS

Info

Publication number
PE20090365A1
PE20090365A1 PE2008001001A PE2008001001A PE20090365A1 PE 20090365 A1 PE20090365 A1 PE 20090365A1 PE 2008001001 A PE2008001001 A PE 2008001001A PE 2008001001 A PE2008001001 A PE 2008001001A PE 20090365 A1 PE20090365 A1 PE 20090365A1
Authority
PE
Peru
Prior art keywords
cr7r8
imidazopyrazines
nr5r6
ethyl
protein kinase
Prior art date
Application number
PE2008001001A
Other languages
Spanish (es)
Inventor
David B Belanger
Angela D Kerekes
Zhaoyang Meng
Jayram R Tagat
Sara J Esposite
Yushi Xiao
Bheemashankar K Kulkarni
Yonglian Zhang
Patrick J Curran
Ronald J Doll
Tao Yu
Amit K Mandal
M Arshad Siddiqui
Original Assignee
Schering Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40002934&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20090365(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of PE20090365A1 publication Critical patent/PE20090365A1/en

Links

Classifications

    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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

Abstract

REFERIDA A COMPUESTOS DERIVADOS DE IMIDAZOPIRAZINAS DE FORMULA I, EN EL QUE R ES H, CN, -NR5R6, -N(R5)C(O)R6, ENTRE OTROS; R1 ES H, FLUOR, FENILO, TETRAHIDROISOQUINOLILO, ENTRE OTROS; R2 ES H, 2-FENETILO, 1,2,4-TIADIAZOLILO, BENZOFURAZANILO, ENTRE OTROS; R3 ES HETEROCICLIL-(CR7R8)n-X, HETEROCICLENIL-(CR7R8)n-X, HETEROARIL-(CR7R8)n-X O ARIL-(CR7R8)n-X; n ES DE 1 A 6; X ES -NR5R6, -OR5, SO2R5, ENTRE OTROS; R7 Y R8 SON H, ETILO, n-PROPILO, NAFTILO, CICLOHEXILMETILO, ENTRE OTROS; R5 ES ISOPROPILO, ETIL-SH, PIPERIDINILMETILO, ENTRE OTROS; R6 ES PIRROLIDINONA, 2-PIRIDINILMETILO, 2-NAFTALENMETOXI, FENOXICARBONILO, ENTRE OTROS. SON SELECCIONADOS II, III, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y COMPOSICION FARMACEUTICA CON UN SEGUNDO COMPONENTE ADICIONAL, TAL COMO CITARABINA, DOCETAXEL, TESTOLACTONA, RITUXIMAB, ENTRE OTROS. DICHOS COMPUESTOS SON MODULADORES DE PROTEINQUINASA MEDIANTE LA INHIBICION DE UNA AURORA QUINASA, POR LO QUE SON DE UTILIDAD EN PROCESOS DE HIPERPROLIFERACION CELULAR Y/O CANCERREFERRING TO COMPOUNDS DERIVED FROM IMIDAZOPYRAZINES OF FORMULA I, IN WHICH R IS H, CN, -NR5R6, -N (R5) C (O) R6, AMONG OTHERS; R1 IS H, FLUORINE, PHENYL, TETRAHYDROISOQUINOLYL, AMONG OTHERS; R2 IS H, 2-PENETHYL, 1,2,4-THADIAZOLYL, BENZOFURAZANIL, AMONG OTHERS; R3 IS HETEROCYCLIL- (CR7R8) n-X, HETEROCICLENIL- (CR7R8) n-X, HETEROARYL- (CR7R8) n-X OR ARIL- (CR7R8) n-X; n IS FROM 1 TO 6; X IS -NR5R6, -OR5, SO2R5, AMONG OTHERS; R7 AND R8 ARE H, ETHYL, n-PROPYL, NAPHTHYL, CYCLOHEXYLMETHYL, AMONG OTHERS; R5 IS ISOPROPYL, ETHYL-SH, PIPERIDINYL METHYL, AMONG OTHERS; R6 IS PYRROLIDINONE, 2-PYRIDINYL METHYL, 2-NAPHTHALENMETOXY, PHENOXYCARBONYL, AMONG OTHERS. THEY ARE SELECTED II, III, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL PREPARATION AND COMPOSITION PROCEDURE WITH A SECOND ADDITIONAL COMPONENT, SUCH AS CITARABIN, DOCETAXEL, TESTOLACTONE, RITUXIMAB, AMONG OTHERS. SUCH COMPOUNDS ARE PROTEINKINASE MODULATORS THROUGH THE INHIBITION OF AN AURORA KINASE, SO THEY ARE USEFUL IN CELLULAR HYPERPROLIFERATION AND / OR CANCER PROCESSES

PE2008001001A 2007-06-14 2008-06-11 IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS PE20090365A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US94399907P 2007-06-14 2007-06-14
US98793207P 2007-11-14 2007-11-14

Publications (1)

Publication Number Publication Date
PE20090365A1 true PE20090365A1 (en) 2009-04-04

Family

ID=40002934

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001001A PE20090365A1 (en) 2007-06-14 2008-06-11 IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS

Country Status (10)

Country Link
EP (1) EP2170892A2 (en)
JP (1) JP2010529195A (en)
CN (1) CN101772500A (en)
AR (1) AR066958A1 (en)
CA (1) CA2690557A1 (en)
CL (1) CL2008001745A1 (en)
MX (1) MX2009013729A (en)
PE (1) PE20090365A1 (en)
TW (1) TW200911811A (en)
WO (1) WO2008156614A2 (en)

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AU2010238361B2 (en) 2009-04-16 2015-08-06 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Imidazopyrazines for use as kinase inhibitors
TW201107329A (en) * 2009-07-30 2011-03-01 Oncotherapy Science Inc Fused imidazole derivative having ttk inhibitory action
US8993535B2 (en) 2009-09-04 2015-03-31 Merck Sharp & Dohme Corp. Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
US20120220581A1 (en) 2009-10-30 2012-08-30 Janssen-Cilag, S.A. IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
AR080754A1 (en) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv IMIDAZO DERIVATIVES (1,2-A) PIRAZINA AND ITS USE AS PDE10 INHIBITORS
US9199999B2 (en) * 2010-06-01 2015-12-01 Bayer Intellectual Property Gmbh Substituted imidazopyrazines
JP2014501496A (en) * 2010-10-20 2014-01-23 ユニヴェルシテ ボルドー セガラン Signature of clinical outcome in gastrointestinal stromal tumor and method of treatment of gastrointestinal stromal tumor
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012080230A1 (en) * 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft 6 substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
US8673905B2 (en) * 2011-03-17 2014-03-18 Hoffmann-La Roche Inc. Imidazo pyrazines
EP2714681B1 (en) 2011-05-25 2015-06-24 Bristol-Myers Squibb Company Substituted sulfonamides useful as antiapoptotic bcl inhibitors
WO2013000924A1 (en) 2011-06-27 2013-01-03 Janssen Pharmaceutica Nv 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES
RU2657540C2 (en) 2012-06-26 2018-06-14 Янссен Фармацевтика Нв Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl- [1,2,4]triazolo[4,3-a]quinoxaline compounds and pde 10 inhibitors for use in treatment of neurological or metabolic disorders
CA2875057C (en) 2012-07-09 2021-07-13 Janssen Pharmaceutica Nv Imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyrazine compounds and their use as inhibitors of the phosphodiesterase 10 enzyme
CN106488915B (en) 2014-02-13 2020-10-02 因赛特公司 Cyclopropylamines as LSD1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3626713B1 (en) 2014-02-13 2021-09-29 Incyte Corporation Cyclopropylamines for use as lsd1 inhibitors
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
EA035534B1 (en) 2015-08-12 2020-06-30 Инсайт Корпорейшн Salts of an lsd1 inhibitor
SG11201809299QA (en) 2016-04-22 2018-11-29 Incyte Corp Formulations of an lsd1 inhibitor
US11690847B2 (en) 2016-11-30 2023-07-04 Case Western Reserve University Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof
AU2018215678A1 (en) 2017-02-06 2019-08-22 Board Of Regents Of The University Of Texas System Compositions and methods of modulating short-chain dehydrogenase activity
KR102633530B1 (en) * 2017-03-31 2024-02-02 오리진 온콜로지 리미티드 Compounds and compositions for treating blood disorders
CN107954977A (en) * 2017-12-15 2018-04-24 上海鼎雅药物化学科技有限公司 The synthetic method of Raltitrexed intermediate
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* Cited by examiner, † Cited by third party
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PE20050081A1 (en) * 2002-09-23 2005-03-01 Schering Corp NEW IMIDAZOPYRAZINES AS INHIBITORS OF CYCLINE-DEPENDENT KINASES
US7576085B2 (en) * 2002-09-23 2009-08-18 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
CA2587192A1 (en) * 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
AR056785A1 (en) * 2005-11-10 2007-10-24 Schering Corp IMIDAZO COMPOUNDS [1,2-A] PIRAZINAS, USEFUL AS INHIBITORS, REGULATORS OR MODULATORS OF PROTEINQUINASAS

Also Published As

Publication number Publication date
CA2690557A1 (en) 2008-12-24
AR066958A1 (en) 2009-09-23
JP2010529195A (en) 2010-08-26
EP2170892A2 (en) 2010-04-07
CN101772500A (en) 2010-07-07
MX2009013729A (en) 2010-01-25
TW200911811A (en) 2009-03-16
WO2008156614A2 (en) 2008-12-24
CL2008001745A1 (en) 2008-12-05
WO2008156614A3 (en) 2009-02-12

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