- PARG INHIBITORY COMPOUNDS
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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 00356; 00357; 00358; 00359
(2016/07/05)
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- 2-ARYLTHIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
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The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
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Page/Page column 96
(2010/11/28)
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- CHEMOKINE RECEPTOR BINDING COMPOUNDS
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The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. Thesd compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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Page/Page column 87-88
(2008/06/13)
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- CYCLIZATION REACTIONS OF N-(2-CHLOROETHYLCARBAMOYL) AMINO ACIDS
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Intramolecular cyclization of the N-(2-chloroethylcarbamoyl) derivatives of glycine, valine and phenylalanine give imidazolidone, oxazoline and hydantoin derivatives.The imidazolidone and oxazoline derivatives possess alkylating activity toward NBP, but the hydantoins do not.N-(2-Chloroethylcarbamoyl)glycine reacts with the mercapto group of cysteine; thus, this alkylating group may be useful for receptor labelling.
- Vargha, H. S.,Medzihradszky-Schweiger, H.,Ruff, F.,Medzihradszky, K.
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p. 2255 - 2258
(2007/10/02)
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