444344-91-6Relevant academic research and scientific papers
CYANO-PYRIMIDINE INHIBITORS OF EGFR/HER2
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, (2021/07/17)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with EGFR and/or HER2 activity.
NOVEL AMIDE AND AMIDINE DERIVATIVES AND USES THEREOF
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Page/Page column 32, (2010/11/03)
The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
BICYCLIC AMIDE DERIVATIVES
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Page/Page column 12, (2008/06/13)
Novel bicycloamide derivatives (general formula (1)) and pharmaceutically acceptable salts thereof effectively inhibit DPP-IV. The bicycloamide derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(4-carbamoylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).
BICYCLO DERIVATIVE
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Page/Page column 7, (2008/06/13)
A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor: One example is (2S,4S)-1-[[N-(4-methylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidi
BICYCLOESTER DERIVATIVE
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Page/Page column 12, (2010/11/24)
SUMMARY Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. SOLVING MEANS The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts there
Synthesis and antifolate evaluation of the aminopterin analogue with a bicyclo[2.2.2]octane ring in place of the benzene ring
Reynolds, Robert C,Johnson, Cheryl A,Piper, James R,Sirotnak, Frances M
, p. 237 - 242 (2007/10/03)
N-[4-[[2,4-diamino-6-pteridinyl)methyl]amino]bicyclo[2.2.2]octane-1- carbonyl]-L-glutamic acid (1) was synthesized and tested for antifolate activity. N-(4-Aminobicyclo[2.2.2]octane-1-carbonyl-L-glutamic acid dimethyl ester (6), the side chain precursor to subject compound 1, was synthesized readily via reported bicyclo[2.2.2]octane-1,4-dicarboxylic acid monoethyl ester (2). The side chain precursor 6 was alkylated by 6-(bromomethyl)-2,4-pteridinediamine (7). Subsequent ester hydrolysis then afforded 1. Antifolate and antitumor evaluation of 1 verses L1210 dihydrofolate reductase (DHFR) and three tumor cell lines (L1210, S180, and HL60) showed it to be ineffective. Although compound 1 was very similar to aminopterin structurally, the bicyclo[2.2.2]octane ring system in place of the phenyl ring in the p-aminobenzoate moiety effectively negates the stoichiometric binding displayed by many classical DHFR inhibitors bearing appropriate aromatic ring systems in the side chain.
