- Novel hamamelitannin analogues for the treatment of biofilm related MRSA infections–A scaffold hopping approach
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Antimicrobial research is increasingly being focused on the problem of resistance and biofilm formation. Hamamelitannin (HAM) was recently identified as an antimicrobial potentiator for conventional antibiotics towards Staphylococcus aureus. This paper de
- Vermote, Arno,Brackman, Gilles,Risseeuw, Martijn D.P.,Coenye, Tom,Van Calenbergh, Serge
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p. 757 - 770
(2017/02/10)
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- 1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES
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The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 289
(2016/07/05)
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- Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket
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Structure-based design led to the discovery of a novel class of renin inhibitors in which an unprecedented phenyl ring filling the S1 site is attached to the phenyl ring filling the S3 pocket. Optimization for several parameters including potency in the p
- Yuan, Jing,Simpson, Robert D.,Zhao, Wei,Tice, Colin M.,Xu, Zhenrong,Cacatian, Salvacion,Jia, Lanqi,Flaherty, Patrick T.,Guo, Joan,Ishchenko, Alexey,Wu, Zhongren,McKeever, Brian M.,Scott, Boyd B.,Bukhtiyarov, Yuri,Berbaum, Jennifer,Panemangalore, Reshma,Bentley, Ross,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Singh, Suresh B.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
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p. 4836 - 4843
(2011/09/16)
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- BENZAMIDE DERIVATIVES, THEIR PREPARATION AND USES IN MEDICINE THEREOF
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The present invention discloses novel benzamide derivatives represented by general formula (I), their preparation, pharmaceutical compositions containing the derivatives and their use as medicament, especially as a 5-HT4 stimulator, wherein the
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Page/Page column 9
(2010/06/15)
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- BENZAMIDE DERIVATIVES, THEIR PREPARATION AND USES IN MEDICINE THEREOF
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The present invention discloses novel benzamide derivatives represented by general formula (I), their preparation, pharmaceutical compositions containing the derivatives and their use as medicament, especially as a 5-HT4 stimulator, wherein the
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Page/Page column 8-9
(2010/08/22)
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- RENIN INHIBITORS
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Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the t
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Page/Page column 30
(2010/08/07)
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- Renin Inhibitors
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Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 51
(2010/12/29)
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- RENIN INHIBITORS
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Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 96
(2008/12/04)
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- RENIN INHIBITORS
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Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 112; 113
(2008/12/04)
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- N-BENZYL-MORPHOLINE DERIVATIVES AS MODULATORS OF THE CHEMOKINE RECEPTOR
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The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
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Page/Page column 28-29
(2008/06/13)
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- DIAMINOPROPANOL RENIN INHIBITORS
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Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease me
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Page/Page column 78
(2008/06/13)
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- PIPERIDINE AND MORPHOLINE RENIN INHIBITORS
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Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
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- ASPARTIC PROTEASE INHIBITORS
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The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
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Page/Page column 175-176
(2010/11/27)
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- CYSTEINE PROTEASE INHIBITORS
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Stereoisomers of the formula (III) wherein R is H or C1-C3 optionally halo-substituted alkyl; or pharmaceutically acceptable salts, hydrates or N-oxides thereof have utility in the treatment of disorders mediated by inappropriate exp
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Page/Page column 28
(2008/06/13)
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- MORPHOLINE DERIVATIVES AS DOPAMINE RECEPTOR SUBTYPE LIGANDS
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A class of substituted morpholine derivatives of formula STR1 wherein Y represents an optionally substituted bicyclic heteroaromatic ring system containing one or two nitrogen atoms, the ring system comprising a six-membered aromatic or heteroaromatic ring fused to a five-or six-membered heteroaromatic ring; and Z represents an optionally substituted arylalkyl, aryloxymethyl or arylalkoxymethyl group, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia.
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- Synthesis and biological activities of the optical isomers of (±)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]me thyl]benzamide (Mosapride)
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The enantiomers, (S)-(-)-1 and (R)-(+)-1, of (+)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]met hyl]benzamide (mosapride) [(+)-1], a new and selective gastroprokinetic agent, were prepared from optically active [4-(4-fluorobenzyl)-2-morpholinyl]methylamines (S)-(-)-4 and (R)-(+)-4, respectively. The requisite (S)-(-)-4 and (R)-(+)-4 were prepared by optical resolution of [4-(4-fluorobenzyl)-2-morpholinyl]methyl p-toluenesulfonate [(+)-5] using (-)- and (+)-N-(p-toluenesulfonyl)glutamic acids, followed by amination of the tosyloxy groupe of (R)-(-)-5 and (S)-(+)-5, respectively. The absolute configurations of (R)-(-)-5 and (S)-(+)-5 were determined on the basis of an asymmetric synthesis of (R)-(-)-5 from (S)-(+)-benzyl glycidyl ether [(S)-(+)-11]. Mosapride and its enantiomers, (S)-(-)-1 and (R)-(+)-1, were essentially equipotent in serotonin 5-HT4 receptor agonistic activity on the electrically evoked contractions in isolated guinea pig ileum.
- Morie,Kato,Harada,Yoshida,Matsumoto
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p. 877 - 882
(2007/10/02)
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- FACILE SYNTHESIS OF OPTICALLY ACTIVE SULFONATES OF 4-tert-BUTOXYCARBONYL-2-HYDROXYMETHYLMORPHOLINE
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Optically active sulfonates of 4-tert-butoxycarbonyl-2-hydroxymethylmorpholine were prepared from 1,2:5,6-di-O-D-mannitol by practical procedures.These compounds are versatile intermediates for optically active isomers of a number of neuropharmacologicall
- Yanagisawa, Hiroaki,Kanazaki, Takuro
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p. 105 - 109
(2007/10/02)
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- Coumarin derivatives, their preparation and their use in the treatment of cerebrovascular disorders
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Compounds of formula (I): [in which: A is a group of formula (II) or (III): R1, R2 and R3 are hydrogen, lower alkyl or halogen; R4 is hydrogen, lower alkyl or aralkyl; R5 and R6 are hydrogen or lower alkyl; R7 a
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