- Synthesis method of 2-amino-3, 5-dihalogenated pyrazine
-
The invention relates to a synthesis method of 2-amino-3, 5-dihalogenated pyrazine, and the synthesis route is shown in the specification. In the formula, X1 is Cl, Br or I; X2 is Cl, Br or I; and X1 and X2 are different, a first halogen source provides X1, and a second halogen source provides X2. The synthesis method disclosed by the invention can be suitable for all types of 2-amino-3, 5-dihalogenated pyrazine except for fluorinated pyrazine. According to the method, the reaction conditions are mild, all reactions can be completed at the temperature of 80 DEG C or below and under the normal pressure condition, and special equipment is not needed; and the method has the advantages of high reaction yield, stable amplification yield, simple post-treatment, economy and convenience.
- -
-
Paragraph 0039-0040
(2021/08/11)
-
- PHENYL-2-HYDROXY-ACETYLAMINO-2-METHYL-PHENYL COMPOUNDS
-
The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders such as cancer.
- -
-
Page/Page column 17
(2018/11/22)
-
- INHIBITING ATAXIA TELANGIECTASIA AND RAD3-RELATED PROTEIN (ATR)
-
Novel compounds inhibiting ATR protein kinase include compounds of formula (I) disclosed herein, as well as liposome formulations comprising ATR protein kinase inhibitor compounds. The compositions are useful for the treatment of cancer.
- -
-
Paragraph 0031; 0032; 0033
(2017/08/08)
-
- SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. (I)
- -
-
Page/Page column 67
(2015/01/16)
-
- SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
-
Disclosed are compounds of formula (I) that are useful as hepatitis C virus (HCV) NSSB polymerise inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NSSB polymerise activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
- -
-
Page/Page column 70; 71
(2015/01/16)
-
- Pyrazine-based Syk kinase inhibitors
-
A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay.
- Forns, Pilar,Esteve, Cristina,Taboada, Lorena,Alonso, Juan Antonio,Orellana, Adelina,Maldonado, Mónica,Carre?o, Cristina,Ramis, Isabel,López, Manel,Miralpeix, Montserrat,Vidal, Bernat
-
scheme or table
p. 2784 - 2788
(2012/05/20)
-
- PYRAZINES USEFUL AS INHIBITORS OF ATR KINASE
-
The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula II; (Formula (II) wherein the variables are as defined herein.
- -
-
Page/Page column 44-45
(2011/12/02)
-
- Discovery of Potent and Selective Inhibitors of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Protein Kinase as Potential Anticancer Agents
-
DNA-damaging agents are among the most frequently used anticancer drugs. However, they provide only modest benefit in most cancers. This may be attributed to a genome maintenance network, the DNA damage response (DDR), that recognizes and repairs damaged DNA. ATR is a major regulator of the DDR and an attractive anticancer target. Herein, we describe the discovery of a series of aminopyrazines with potent and selective ATR inhibition. Compound 45 inhibits ATR with a Ki of 6 nM, shows >600-fold selectivity over related kinases ATM or DNA-PK, and blocks ATR signaling in cells with an IC50 of 0.42 μM. Using this compound, we show that ATR inhibition markedly enhances death induced by DNA-damaging agents in certain cancers but not normal cells. This differential response between cancer and normal cells highlights the great potential for ATR inhibition as a novel mechanism to dramatically increase the efficacy of many established drugs and ionizing radiation.
- Charrier, Jean-Damien,Durrant, Steven J.,Golec, Julian M. C.,Kay, David P.,Knegtel, Ronald M. A.,MacCormick, Somhairle,Mortimore, Michael,O'Donnell, Michael E.,Pinder, Joanne L.,Reaper, Philip M.,Rutherford, Alistair P.,Wang, Paul S. H.,Young, Stephen C.,Pollard, John R.
-
scheme or table
p. 2320 - 2330
(2011/06/17)
-
- PYRAZINE DERIVATIVES
-
The invention concerns pyrazine derivatives of the Formula (I) or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions
- -
-
Page/Page column 67
(2011/08/08)
-
- COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
-
The present disclosure relates to pyrazine compounds of formula (I) wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.
- -
-
Page/Page column 90
(2010/06/11)
-
- HETEROCYCLIC INHIBITORS OF c-MET AND USES THEREOF
-
The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders
- -
-
Page/Page column 45
(2008/06/13)
-
