- HETEROARYL-TRIAZOLE COMPOUNDS AS PESTICIDES
-
The present invention relates to novel heteroaryl-triazole compounds of the general formula (I), in which the structural elements X, Y, R1, R2, R3a, R3b, R4 and R5 have the meaning given in the description, to formulations and compositions comprising such compounds and for their use in the control of animal pests including arthropods and insects in plant protection and to their use for control of ectoparasites on animals.
- -
-
Page/Page column 129
(2021/08/27)
-
- Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
-
Following up the open initiative of anti-malarial drug discovery, a GlaxoSmithKline (GSK) phenotypic screening hit was developed to generate hydroxyethylamine based plasmepsin (Plm) inhibitors exhibiting growth inhibition of the malaria parasite Plasmodium falciparum at nanomolar concentrations. Lead optimization studies were performed with the aim of improving Plm inhibition selectivity versus the related human aspartic protease cathepsin D (Cat D). Optimization studies were performed using Plm IV as a readily accessible model protein, the inhibition of which correlates with anti-malarial activity. Guided by sequence alignment of Plms and Cat D, selectivity-inducing structural motifs were modified in the S3 and S4 sub-pocket occupying substituents of the hydroxyethylamine inhibitors. This resulted in potent anti-malarials with an up to 50-fold Plm IV/Cat D selectivity factor. More detailed investigation of the mechanism of action of the selected compounds revealed that they inhibit maturation of the P. falciparum subtilisin-like protease SUB1, and also inhibit parasite egress from erythrocytes. Our results indicate that the anti-malarial activity of the compounds is linked to inhibition of the SUB1 maturase plasmepsin subtype Plm X.
- Zogota, Rimants,Kinena, Linda,Withers-Martinez, Chrislaine,Blackman, Michael J.,Bobrovs, Raitis,Pantelejevs, Teodors,Kanepe-Lapsa, Iveta,Ozola, Vita,Jaudzems, Kristaps,Suna, Edgars,Jirgensons, Aigars
-
supporting information
p. 344 - 352
(2018/12/11)
-
- Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-g
-
A novel structural class of iminopyridine derivative 1 was identified as a potent and selective human α1D adrenoceptor (α1D adrenergic receptor; α1D-AR) antagonist against α1A- and α1B-AR through scre
- Sakauchi, Nobuki,Kohara, Yasuhisa,Sato, Ayumu,Suzaki, Tomohiko,Imai, Yumi,Okabe, Yuichi,Imai, Shigemitsu,Saikawa, Reiko,Nagabukuro, Hiroshi,Kuno, Haruhiko,Fujita, Hisashi,Kamo, Izumi,Yoshida, Masato
-
p. 2989 - 3002
(2016/05/19)
-
- PROPHYLACTIC AGENT OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY
-
A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.
- -
-
Paragraph 0126
(2013/03/26)
-
- SUBSTITUTED AMINOBUTYRIC DERIVATIVES AS NEPRILYSIN INHIBITORS
-
The present invention provides a compound of formula (I') or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
Page/Page column 172
(2010/12/26)
-
- Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof
-
The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1-X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
- -
-
Page/Page column 201
(2010/11/24)
-
- Aminoacetamide acyl guanidines as beta-secretase inhibitors
-
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
- -
-
Page/Page column 20
(2008/06/13)
-
- NOVEL INDOLOPYRIDINES , BENZOFURANOPYRIDINES AND BENZOTHIENOPYRIDINES
-
Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and X have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.
- -
-
Page/Page column 34
(2008/06/13)
-
- BACE INHIBITORS
-
The present invention provides BACE inhibitors of Formula (I): methods for their use and preparation, and intermediates for their preparation.
- -
-
Page/Page column 108-109
(2008/06/13)
-
- N-acetonylbenzamides and their use as fungicides
-
Certain N-acetonylbenzamides exhibit low phytotoxicity and are useful for control of a wide range of fungi, including phytopathogenic fungi of the classes Oomycetes, Ascomycetes, Deuteromycetes and Basidiomycetes.
- -
-
-