- In vitro study and structure-activity relationship analysis of stilbenoid derivatives as powerful vasorelaxants: Discovery of new lead compound
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The development of vasorelaxant as the antihypertensive drug is important as it produces a rapid and direct relaxation effect on the blood vessel muscles. Resveratrol (RV), as the most widely studied stilbenoid and the lead compound, inducing the excellent vasorelaxation effect through the multiple signalling pathways. In this study, the in vitro vascular response of the synthesized trans-stilbenoid derivatives, SB 1-8e were primarily evaluated by employing the phenylephrine (PE)-precontracted endothelium-intact isolated aortic rings. Herein we report trans-3,4,4′-trihydroxystilbene (SB 8b) exhibited surprisingly more than 2-fold improvement to the maximal relaxation (Rmax) of RV. This article also highlights the characterization of the aromatic protons in terms of their unique splitting patterns in 1H NMR.
- Chan, Sock Ying,Loh, Yean Chun,Oo, Chuan Wei,Yam, Mun Fei
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- RENIN INHIBITORS
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The invention provides compounds, pharmaceutical compositions, kits, method of preparing, and method of using the compounds which exhibit renin and other S9 proteases activities and consist of the formula:—wherein the variables are as defined herein.
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Page/Page column 54-55
(2010/06/16)
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- PYRIMIDINE AND QUINAZOLINE DERIVATIVES
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This invention is concerned with compounds of the formula ( l ) wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 79
(2008/06/13)
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- PYRIDINE, QUINOLINE AND PYRIMIDINE DERIVATIVES
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This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 29
(2008/06/13)
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- BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES
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This invention relates to compounds of the formula wherein A, R1 to R3 are as defined in the specification and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridine and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 25
(2008/12/08)
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- PHENYL, PYRIDINE, QUINOLINE, ISOQUINOLINE, NAPHTHYRIDINE AND PYRAZINE DERIVATIVES
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This invention is concerned with compounds of the formulaand pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 79
(2008/06/13)
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- New blood coagulation factor inhibitors
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The invention relates to novel compounds with formula (I) wherein R1-R7 are as herein defined useful as blood coagulation factor inhibitors. The compounds (I) may be used for treatment of thrombotic conditions or as stabilizers of liquid formulations of blood coagulation factors, in particular liquid formulations of FVIIA, Factor VII variants, or Factor VII derivatives.
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Page/Page column 22
(2008/12/08)
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- BENZOOXAZOLE, OXAZOLOPYRIDINE, BENZOTHIAZOLE AND THIAZOLOPYRIDINE DERIVATIVES
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This invention is concerned with compounds of the formula (I) wherein X, A, B, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical
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Page/Page column 67
(2008/06/13)
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- Pyrimidine, quinazoline, pteridine and triazine derivatives
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This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 46-47
(2008/06/13)
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- Design of potent PPARα agonists
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Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARα agonists. Optimum PPARα potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARα potency of 0.002 μM and a selectivity ratio to PPARγ and PPARδ of 410 and 2000, respectively.
- Sauerberg, Per,Mogensen, John P.,Jeppesen, Lone,Bury, Paul S.,Fleckner, Jan,Olsen, Grith S.,Jeppesen, Claus B.,Wulff, Erik M.,Pihera, Pavel,Havranek, Miroslav,Polivka, Zdenek,Pettersson, Ingrid
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p. 3198 - 3202
(2008/02/05)
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- Amide derivatives as somatostatin receptor 5 antagonists
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This invention is concerned with compounds of the formula wherein R1 to R5, R5′ and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 24
(2008/06/13)
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- META-GUANIDINE, UREA, THIOUREA OR AZACYCLIC AMINO BENZOIC ACID DERIVATIVES AS INTEGRIN ANTAGONISTS
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The present invention relates to a class of compounds represented by the Formula Ior a pharmaceutically acceptable salt thereof, whereinA ispharmaceutical compositions thereof and methods of using such compounds and compositions as alphavbeta3 antagonists.
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