1053228-29-7Relevant academic research and scientific papers
Synthesis and evaluation of FAK inhibitors with a 5-fluoro-7H-pyrrolo[2,3-d]pyrimidine scaffold as anti-hepatocellular carcinoma agents
Gong, Chaochao,Huang, Jian,Liu, Yue,Tan, Hanyi,Zhang, Jiawei,Zhang, Qian
, (2021/07/02)
Focal adhesion kinase (FAK) is a ubiquitous intracellular non-receptor tyrosine kinase, which is involved in multiple cellular functions, including cell adhesion, migration, invasion, survival, and angiogenesis. In this study, a series of 7H-pyrrolo[2,3-d
PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS FOR TREATING FAMILIAL DYSAUTONOMIA
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Page/Page column 47, (2020/08/28)
The present description relates to compounds of formula (I) useful for improving pre-mRNA splicing in a cell. In particular, another aspect described herein relates to substituted pyrrolo[2,3-d]pyrimidine compounds, forms, and pharmaceutical compositions
PYRAZOLOPYRIMIDINE DERIVATIVES AS KINASE INHIBITOR
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Page/Page column 91, (2018/02/03)
The present invention relates to a pyrazolopyrirmidine derivative, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with ki
COMPOUND, COMPOSITIONS, AND METHODS
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Page/Page column 177, (2017/08/01)
Compounds having activity as LRRK2 inhibitors are disclosed. The compounds are of formula (I) including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
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Page/Page column 40-41, (2017/04/11)
The present invention is directed to 4'-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment,
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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Page/Page column 59-60, (2013/12/03)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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Page/Page column 58, (2012/11/14)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula (I), wherein the variables are as defined herein.
Pyrrolopyrimidinyl axl kinase inhibitors
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Page/Page column 18, (2010/08/18)
Compounds represented by Formula (I): are useful in treating diseases, such as cancer, that are mediated and/or associated (at least in part) with Axl kinase. The compounds can be formulated as pharmaceutically acceptable compositions for administration t
INHIBITORS OF PROTEIN KINASES
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Page/Page column 129, (2009/12/05)
The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
7-Halogenated 7-deazapurine 2′-deoxyribonucleosides related to 2′-deoxyadenosine, 2′-deoxyxanthosine, and 2′- deoxyisoguanosine: Syntheses and properties
Seela, Frank,Xu, Kuiying
experimental part, p. 1083 - 1105 (2009/02/07)
A series of 7-fluorinated 7-deazapurine 2′-deoxyribonucleosides related to 2′-deoxyadenosine, 2′-deoxyxanthosine, and 2′-deoxyisoguanosine as well as intermediates 4b - 7b, 8, 9b, 10b, and 17b were synthesized. The 7-fluoro substituent was introduced in 2,6-dichloro-7-deaza-9H-purine (11a) with Selectfluor (Scheme 1). Apart from 2,6-dichloro-7-fluoro-7-deaza-9H-purine (11b), the 7-chloro compound 11c was formed as by-product. The mixture 11b/11c was used for the glycosylation reaction; the separation of the 7-fluoro from the 7-chloro compound was performed on the level of the unprotected nucleosides. Other halogen substituents were introduced with N-halogenosuccinimides (11a→11c - 11e). Nucleobase-anion glycosylation afforded the nucleoside intermediates 13a - 13e (Scheme 2). The 7-fluoro- and the 7-chloro-7-deaza-2′-deoxyxanthosines, 5b and 5c, respectively, were obtained from the corresponding MeO compounds 17b and 17c, or 18 (Scheme 6). The 2′-deoxyisoguanosine derivative 4b was prepared from 2-chloro-7-fluoro-7-deaza-2′-deoxyadenosine 6b via a photochemically induced nucleophilic displacement reaction (Scheme 5). The pKa values of the halogenated nucleosides were determined (Table 3). 13C-NMR Chemical-shift dependencies of C(7), C(5), and C(8) were related to the electronegativity of the 7-halogen substituents (Fig. 3). In aqueous solution, 7-halogenated 2′-deoxyribonucleosides show an approximately 70% S population (Fig. 2 and Table 1).
