- BICYCLIC INHIBITORS OF HISTONE DEACETYLASE
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Provided herein are compounds of Formula I and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone deacetylases (HDAC).
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Paragraph 00250
(2020/02/06)
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- 2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
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Paragraph 00802
(2016/07/05)
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- SULPHONAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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Disclosed are compounds having the general formula (I) as defined herein, the preparation thereof, and the use thereof for the prophylaxis or treatment of any disease involving a dysfunction associated with the orexin 2 receptor such as obesity, appetite or taste disorders including cachexia, anorexia and bulimia, diabetes, metabolic syndromes, vomiting and nausea, depression and anxiety, addictions, mood and behaviour disorders, schizophrenia, sleep disorders, restless legs syndrome, memory learning disorders, sexual and psychosexual dysfunctions, pain, visceral or neuropathic pain, hyperalgesia, allodynia, digestive disorders, irritable bowel syndrome, neuronal degenerescence, ischaemic or haemorrhagic attacks, Cushing's disease, Guillain-Barré syndrome, myotonic dystrophy, urinary incontinence, hyperthyroidism, pituitary function disorders, hypertension or hypotension.
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Page/Page column 67
(2010/11/28)
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- IMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABA-A RECEPTOR COMPLEX
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This invention relates to novel imidazole derivatives of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
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Page/Page column 18
(2008/06/13)
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- Substituted thiazoles as immunoregulants
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Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.
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- 5R,6S,8R-2-(1-Methyl-2-imidazolylmethylthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid
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There is disclosed the antibacterial 5R,6S,8R-2-(1-methyl-2-imidazolylmethylthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid, its pharmaceutically acceptable salts and esters as well as compositions containing them and methods for their use.
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