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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=google_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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material 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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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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SG175195A1 (en) 2009-04-16 2011-11-28 Ct Nac Investigaciones Oncologicas Cnio 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
NZ599597A (en) 2009-10-30 2013-05-31 Janssen Pharmaceutica Nv 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
ES2555261T3 (en) * 2010-06-01 2015-12-30 Bayer Intellectual Property Gmbh Imidazopyrazines substituted
ES2541054T3 (en) * 2010-10-20 2015-07-15 Université De Bordeaux Signatures of the clinical outcome in gastrointestinal stromal tumors and method of treatment of gastrointestinal stromal tumors
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
JP2013545776A (en) * 2010-12-17 2013-12-26 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 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
JP2014521595A (en) 2011-05-25 2014-08-28 ブリストル−マイヤーズ スクイブ カンパニー Substituted sulfonamides useful as anti-apoptotic 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
WO2014001314A1 (en) 2012-06-26 2014-01-03 Janssen Pharmaceutica Nv 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 the treatment of neurological or metabolic disorders
AU2013289284B2 (en) 2012-07-09 2017-03-30 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme
PL3805233T3 (en) 2014-01-13 2024-06-10 Aurigene Oncology Limited ENANCIOMERS (R) AND (S) (S)-N-(5-(3-hydroxypyrrolidin-1-yl)-2-morpholinooxazolo[4,5-b]pyridin-6-yl)-2-(2-methylpyridine -4-yl)oxazole-4-carboxamide as IRAK4 inhibitors for the treatment of malignancy
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
ME03654B (en) 2014-02-13 2020-07-20 Incyte Corp CYCLOPROPYLAMINE AS LSD1 INHIBITORS
PT3105226T (en) 2014-02-13 2019-11-06 Incyte Corp CYCLOPROPYLAMINS AS LSD1 INHIBITORS
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
KR102710120B1 (en) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Salt of LSD1 inhibitor
AR109452A1 (en) 2016-04-22 2018-12-12 Incyte Corp PHARMACEUTICAL FORMULATION OF AN LSD1 INHIBITOR AND TREATMENT METHOD
EP3548035A4 (en) 2016-11-30 2020-07-22 Case Western Reserve University COMBINATIONS OF 15 PGDH INHIBITORS WITH CORTICOSTEROIDS AND / OR TNF INHIBITORS AND USES THEREOF
CN110573154A (en) 2017-02-06 2019-12-13 卡斯西部储备大学 Compositions and methods for modulating short-chain dehydrogenase activity
CN120267671A (en) * 2017-03-31 2025-07-08 奥锐金肿瘤有限公司 Compounds and compositions for treating hematological 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
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
EA202191422A1 (en) 2018-11-21 2021-10-21 Кейс Вестерн Ризерв Юниверсити COMPOSITIONS AND METHODS FOR MODULATING THE ACTIVITY OF SHORT RENAL DEHYDROGENASE
JP7771084B2 (en) * 2020-04-29 2025-11-17 エフ． ホフマン－ラ ロシュ アーゲー Antibacterial 8-phenylamino-3-(pyrazol-4-yl)imidazo[1,2-a]pyrazine derivatives
CN116113406B (en) * 2020-07-10 2025-08-29 密歇根大学董事会 GAS41 inhibitors and methods of use
CN117120054A (en) 2021-04-08 2023-11-24 柯里斯公司 Combination therapy for the treatment of cancer
WO2022222995A1 (en) * 2021-04-23 2022-10-27 南京明德新药研发有限公司 Picolinamide compound
WO2023169438A1 (en) * 2022-03-07 2023-09-14 上海凌达生物医药有限公司 Nitrogen-containing heterocyclic cell cycle inhibitor compounds as well as preparation method therefor and use thereof
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TW200413378A (en) * 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
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BRPI0618520A2 (en) * 2005-11-10 2011-09-06 Schering Corp imidazopyrazines as protein kinase inhibitors

Also Published As

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

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