185-72-8Relevant academic research and scientific papers
Design of iodinated radioligands for SPECT imaging of central human 5-HT4R using a ligand lipophilicity efficiency approach
Babin, Victor,Bouillon, Jean-Philippe,Cailly, Thomas,Davis, Audrey,Dubost, Emmanuelle,Fabis, Frédéric,Lohier, Jean-Fran?ois,Millet, Philippe,Pigrée, Gilbert,Reboul, Vincent,Tournier, Benjamin B.
, (2020/01/25)
A series of iodinated ligands for the SPECT imaging of 5-HT4 receptors was designed starting from the previously reported hit MR-26132. We focused on the modulation of the piperidine-containing lateral chain by introducing hydrophilic groups in order to decrease the liphophilicity of the new ligands. All the synthesized compounds were tested for their binding affinities on 5-HT4Rs and based on the Ligand Lipophilicity Efficiency approach, compound 13 was further selected for radioiodination with iodine-125 and imaging experiments. Compound 13 showed its ability to displace the specific signal of the reference compound [125I]SB-207710 but no significant detection of [125I]13 was observed in vivo in SPECT experiments.
NON-FUSED TRICYCLIC COMPOUNDS
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Paragraph 00515, (2018/11/26)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
AMINO-QUINOLINES AS KINASE INHIBITORS
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Page/Page column 59, (2018/06/22)
Disclosed are compounds having the formula:wherein R 1 , R 2 , R 3 and Z are as defined herein, and methods of making and using the same.
OXYSTEROLS AND METHODS OF USE THEREOF
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Paragraph 00136, (2017/10/31)
Compounds are provided according to Formula (I), and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein A, R1, and R5 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
ANTI-BACTERIAL COMPOUNDS
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Page/Page column 114, (2017/06/28)
A compound of Formula (II): for use in the prevention or treatment of a bacterial infection.
AMINO-QUINOLINES AS KINASE INHIBITORS
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Page/Page column 68; 69, (2018/05/15)
Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
AMINO-QUINOLINES AS KINASE INHIBITORS
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Paragraph 0128, (2016/10/31)
Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
TRIAZOLYL DERIVATIVES AS SYK INHIBITORS
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Page/Page column 90, (2014/04/17)
Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
FURO[3,4-C]QUINOLINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
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Page/Page column 46; 47, (2013/03/26)
The present invention relates to compounds defined by formula (I), wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol
Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation
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Paragraph 0269-0272, (2013/08/28)
The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol es
