- Synthesis of 1,2,3-triazole ‘click’ analogues of thalidomide
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Click analogues of thalidomide were prepared from 3-azidoglutarimide and a diverse array of arylacetylenes and N-ethynyl/N-propargyl phthalimide derivatives. The sequence necessitated a new and scalable synthesis of the key click intermediate 3-azidoglutarimide. The dipolar cycloaddition reactions between the azidoglutarimide and the alkynyl coupling partners utilized a copper sulfate/sodium ascorbate reagent system in aqueous tetrahydrofuran and were first explored using substituted arylalkynes. Along with the click analogues of thalidomide, the click counterparts of the teratogenic and antiangiogenic thalidomide analogue EM-12 were prepared.
- Ronnebaum, Jarrid M.,Luzzio, Frederick A.
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- CRBN LIGANDS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
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Paragraph 00429; 00430; 00431
(2019/08/20)
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- IRAK DEGRADERS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 3208; 3209
(2019/07/10)
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- PROTEIN DEGRADERS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.
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Paragraph 00357; 00358
(2019/04/16)
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- CRBN LIGANDS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
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Paragraph 00289-00290
(2019/04/16)
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- SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION
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Disclosed are small molecules against cereblon to enhance effector T cell function. Methodos of making thes molecules and methods of using them to treat various disease states are also disclosed.
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Page/Page column 111-112
(2017/10/11)
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- HETEROCYCLIC-SUBSTITUTED BENZOFURAN DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Paragraph 0199
(2014/07/23)
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- HETEROCYCLIC-SUBSTITUTED BENZOFURAN DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 56
(2013/03/26)
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- HETEROCYCLIC-SUBSTITUED BENZOFURAN DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to compounds of formula (1) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 66-67
(2013/03/26)
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- COMPOUNDS COMPRISING A CYCLOBUTOXY GROUP
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The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals.
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Page/Page column 74-75
(2009/09/05)
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- FUSED OXAZOLES and THIAZOLES AS HISTAMINE H3- RECEPTOR LIGANDS
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The present invention relates to compounds comprising fused oxazole or thiazole derivatives of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, wherein A is a cyclic amine which is linked to the propylene group via an amino nitrogen; B is selected from the group consisting of heteroaryl, 5-8-membered heterocycloalkyl, 5-8-membered cycloalkyl; X is either N or CH; Y is either O or S.
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Page/Page column 89
(2008/06/13)
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- Substituted glutarimides and their use as inhibitors of IL-12 production
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Substituted glutarimides of formula I 1and their method of making. Also disclosed are pharmaceutical compositions comprising the glutarimidie, particularly as immunomodulators and as inhibitors of angiopathies, or haematological or oncological diseases, as well as a method for treating various diseases using the glutarimides.
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