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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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (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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CN102428087B (en) 2009-04-16 2015-06-17 卡洛斯三世国家癌症研究中心基金会 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
ES2651296T3 (en) 2009-10-30 2018-01-25 Janssen Pharmaceutica, N.V. Imidazo [1,2-b] pyridacin 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
WO2012052954A1 (en) * 2010-10-20 2012-04-26 Universite Bordeaux Segalen Signatures of clinical outcome in gastro intestinal stromal tumors and method of treatment of gastroinstestinal 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
CA2821834A1 (en) * 2010-12-17 2012-06-21 Bayer Intellectual Property Gmbh 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
BR112013033375B1 (en) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivatives of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline, their use, pharmaceutical composition that comprises them, process of preparation thereof, sterile solution and intermediate compound
CA2872216C (en) 2012-06-26 2021-07-20 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
JP6174695B2 (en) 2012-07-09 2017-08-02 ヤンセン ファーマシューティカ エヌ．ベー． Inhibitor of phosphodiesterase 10 enzyme
PL3466955T3 (en) 2014-01-13 2021-06-28 Aurigene Discovery Technologies Limited The method of obtaining oxazolo [4,5-B] pyridine and thiazolo [4,5-B] pyridine derivatives as inhibitors of IRAK4 in the treatment of cancer
EP3626713B1 (en) 2014-02-13 2021-09-29 Incyte Corporation Cyclopropylamines for use as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
JP6602779B2 (en) 2014-02-13 2019-11-06 インサイト・コーポレイション Cyclopropylamines as LSD1 inhibitors
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines 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
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
MA51438A (en) 2015-04-03 2021-04-14 Incyte Corp HETEROCYCLIC COMPOUNDS USED AS LSD1 INHIBITORS
SI3334709T1 (en) 2015-08-12 2025-03-31 Incyte Holdings Corporation LSD1 INHIBITOR SALTS
MA44725A (en) 2016-04-22 2019-02-27 Incyte Corp LSD1 INHIBITOR FORMULATIONS
JP7595413B2 (en) 2016-11-30 2024-12-06 ケース ウエスタン リザーブ ユニバーシティ Combination of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof - Patents.com
CA3052466A1 (en) 2017-02-06 2018-08-09 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
IL269536B (en) * 2017-03-31 2022-07-01 Aurigene Discovery Tech Ltd Compounds and preparations for the treatment of 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
US12336982B2 (en) 2018-11-21 2025-06-24 Rodeo Therapeutics Corporation Compositions and methods of modulating short-chain dehydrogenase activity
EP4143190A1 (en) * 2020-04-29 2023-03-08 F. Hoffmann-La Roche AG 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
EP4319750A4 (en) 2021-04-08 2025-02-26 Curis, Inc. COMBINATION THERAPIES FOR THE TREATMENT OF CANCER
TW202304911A (en) * 2021-04-23 2023-02-01 大陸商南京明德新藥研發有限公司 Pyridinamide 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
WO2024088192A1 (en) * 2022-10-26 2024-05-02 Js Innopharm (Suzhou) Ltd. An aurora a inhibitor for use in treatments of cancers

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ATE377600T1 (en) * 2002-09-23 2007-11-15 Schering Corp IMIDAZOPYRAZINE AS CDK INHIBITORS
US7576085B2 (en) * 2002-09-23 2009-08-18 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
WO2006053121A2 (en) * 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
TW200804386A (en) * 2005-11-10 2008-01-16 Schering Corp Imidazopyrazines as protein kinase inhibitors

Also Published As

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

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