- Compound serving as IRAK inhibitor
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The present invention relates to a compound suitable for the treatment of cancer and inflammatory diseases associated with interleukin-1 receptor associated kinase (IRAK), particularly relates to a compound serving as an IRAK4 inhibitor and a preparation
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Paragraph 0093-0096
(2020/09/01)
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- TRANS-3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
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Page/Page column 83
(2009/03/07)
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- 2-ALKYLBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS
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Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.
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Page/Page column 14-15
(2008/12/08)
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- 2-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
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Page/Page column 76
(2008/12/07)
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- Benzamide derivatives having a vasopressin antagonistic activity
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This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1is aryl optionally substituted with lower alkoxy, etc., R2is lower alkyl, etc., R3is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
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- Benzimidazole compounds
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Benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.
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