- I. Discovery of a novel series of CXCR3 antagonists. Multiparametric optimization of N,N-disubstituted benzylamines
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N,N-Disubstituted benzylamine derivatives have been identified as CXCR3 antagonists. Compounds were optimized to improve affinity and selectivity, to increase metabolic stability in human and mouse liver microsomes, to increase Caco-2 permeability. Optimization was supported by monitoring physico-chemical properties using both experimental and computational means. Several compounds with double-digit nanomolar CXCR3 affinity, favorable selectivity, microsomal stability, Caco-2 permeability and human hepatocyte clearance have been identified.
- Bata, Imre,T?m?sk?zi, Zsuzsanna,Buzder-Lantos, Péter,Vasas, Attila,Szeleczky, Gábor,Bátori, Sándor,Barta-Bodor, Veronika,Balázs, László,Ferenczy, Gy?rgy G.
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supporting information
p. 5418 - 5428
(2016/11/11)
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- Cycloalkane carboxylic acid derivatives as CXCR3 receptor antagonists
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Paragraph 0070-0072
(2013/06/27)
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- CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Page/Page column 43
(2013/06/27)
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- Substituted B-amino acid derivatives as CXCR3 receptor antagonist
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Paragraph 0071; 0072; 0073
(2014/01/07)
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- SUBSTITUTED ?-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Page/Page column 42; 43
(2014/01/07)
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