- COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS
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The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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Paragraph 00271-00272
(2017/03/21)
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- PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention relates to new pyrrolidine derivatives of the formula (I), to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 81
(2014/08/07)
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- PYRIMIDINE-SUBSTITUTED PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention relates to new pyrrolidine derivatives of the formula (I), wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceu
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Page/Page column 81
(2014/11/11)
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- NEW AZIRIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS ACETYL-COA CARBOXYLASE INHIBITORS
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The invention relates to new azetidine derivatives of the formula (I) wherein Ar1, Ar2, X, R, T and L are as defined in the description, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 71; 72
(2013/07/05)
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- AZETIDINE DERIVATIVES
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Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
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Paragraph 0413; 0414; 0415; 0416; 0417
(2013/06/28)
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- SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD
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Compounds are provided which have the structure of Formula (I): wherein R is hydrogen or C1-C4 alkyl; and each of R1 and R2 is independently hydrogen, C1-C4 alkyl, halo or C1-Cs
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Page/Page column 16
(2010/11/29)
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