- Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors
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The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead compounds.
- Ioannidis, Stephanos,Lamb, Michelle L.,Davies, Audrey M.,Almeida, Lynsie,Su, Mei,Bebernitz, Geraldine,Ye, Minwei,Bell, Kirsten,Alimzhanov, Marat,Zinda, Michael
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scheme or table
p. 6524 - 6528
(2010/05/18)
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- PYRAZOLYL-AMINO-SUBSTITUTED PYRAZINES AND THEIR USE FOR THE TREATMENT OF CANCER
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The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 71
(2008/12/04)
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- HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
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Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.
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Page/Page column 65
(2008/06/13)
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- Process for preparing 3-alkoxy-5-alkylpyrazin-2-amines
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A process for preparing 3-alkoxy-5-alkylpyrazin-2-amines of the general formula: STR1 wherein R1 is a C1-4 -alkyl group or an aryl group and R2 is a C1-4 -alkoxy group or an aryloxy group, starting either from a
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- Pteridines. 47. Preparation and Chemistry of 2-Amino-6-carbalkoxy-3-cyano-5-substituted Pyrazine 1-Oxides: Synthesis of Pterin-6-carboxaldehyde
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A new procedure for the synthesis of 2-amino-3-cyano-5-substituted pyrazines 9, useful intermediates for the synthesis of pteridines, is described.Oximation of β-keto esters 2 followed by reaction with aminomalononitrile provides 2-amino-6-carbalkoxy-3-cyano-5-substituted pyrazine 1-oxides 5.Protection of the amino group as its ((dimethylamino)methylene)amino derivative 9 followed by SN2 decarbalkoxylation provides pyrazines 10 which on removal of the protecting group and deoxygenation give pyrazines 8.This method is designed to be of use in cases where the β-keto ester cannot be converted directly to the corresponding α-keto aldoxime 3.The procedure is applied to the synthesis of 2-amino-3-cyano-5-(dimethoxymethyl)pyrazine (8a), an intermediate in the synthesis of pterin-6-carboxaldehyde (1).
- Taylor, Edward C.,Dumas, Donald J.
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p. 2485 - 2489
(2007/10/02)
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