- EP300/CREBBP INHIBITOR
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The present invention provides a compound having excellent histone acetyltransferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.
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Paragraph 0233; 0234; 0262; 0263
(2020/05/30)
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- SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES
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The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
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Page/Page column 19
(2011/04/14)
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- SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES
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The present invention relates to compounds of formula (I) wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
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Page/Page column 45
(2009/11/29)
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- PHOSPHONIC ACID DERIVATES AND THEIR USE AS P2Y12 RECEPTOR ANTAGONISTS
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The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).
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Page/Page column 94
(2009/07/03)
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- β-Lactones as a new class of cysteine proteinase inhibitors: inhibition of hepatitis A virus 3C proteinase by N-Cbz-serine β-Lactone
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Formula presented N-Benzyloxycarbonyl-L-serine β-lactone (1) is shown to irreversibly inactivate the 3C cysteine proteinase of hepatitis A virus (HAV) with kinact = 0.70 min-1, KI = 1.84 x 10-4 M and kinact/KI = 3800 M-1 min-1 at an enzyme concentration of 0.1 μM. Mass spectrometric and HMQC NMR studies using 13C-labeled 1 show that the active site cysteine (Cys-172) thiol of the HAV 3C proteinase attacks the β-position (i.e. C-4) of the oxetanone ring, thereby leading to ring opening and alkylation of the sulfur. In contrast, the enantiomer of this β-lactone, 2, is a reversible competitive inhibitor (Ki = 1.50 x 10-6 M) at similar enzyme concentrations. The β-lactone motif represents a new class of inhibitors of cysteine proteinases.
- Lall, Manjinder S.,Karvellas, Constantine,Vederas, John C.
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p. 803 - 806
(2008/02/12)
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- AMINOBUTANOIC ACID COMPOUNDS HAVING METALLOPROTEASE INHIBITING PROPERTIES
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Aminobutanoic acids of the following formula (I): STR1 where R 1-R 5 are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatm
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- SOLID-PHASE SYNTHESIS OF A NATURALLY OCCURING β-(1-5)-LINKED D-GALACTOFURANOSYL HEPTAMER CONTAINING THE ARTIFICAL LINKAGE ARM L-HOMOSERINE
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The glycosyl donor 2,3-di-O-benzoyl-5-O-levulinoyl-6-O-pivaloyl-β-D-Galactofuranosyl chloride and properly-protected L-homoserine covalently bound to polystyrene were employed for the stereoregular formation of a D-galactofuranosyl heptamer containing β-(1-5)-interglycosidic bond and a β-linked L-homoserine via a solid phase approach
- Veeneman, G. H.,Notermans, S.,Liskamp, R. M. J.,Marel, G. A. van der,Boom, J. H. van
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p. 6695 - 6698
(2007/10/02)
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