192810-12-1Relevant articles and documents
Enantioselectivity Induced by Stereoselective Interlocking: A Novel Core Motif for Tropos Ligands
Scholtes, Jan Felix,Trapp, Oliver
, p. 11707 - 11714 (2019)
Well-defined supramolecular interactions are a powerful tool to control the stereochemistry of a catalytic reaction. In this paper, we report a novel core motif for fluxional 2,2′-biphenyl ligands carrying (S)-amino acid-derived interaction sites in 5,5′-
Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm
Park, Kaapjoo,Lee, Byoung Moon,Hyun, Kwan Hoon,Han, Taedong,Lee, Dong Hoon,Choi, Hyun Ho
, p. 296 - 301 (2015)
Novel acetylenyl-containing benzamide derivatives were synthesized and screened using an in vitro assay measuring increases in glucokinase activity stimulated by 10 mM glucose concentration and glucose uptake in rat hepatocytes. Lead optimization of an acetylenyl benzamide series led to the discovery of several active compounds via in vitro enzyme assays (EC50 40% at 50 mg/kg). Of the active compounds tested, 3-(3-amino-phenylethynyl)-5-(2-methoxy-1-methyl-ethoxy)-N-(1-methyl-1H-pyrazol-3-yl)-benzamide (19) was identified as a potent glucokinase activator exhibiting an EC50 of 27 nM and eliciting a 2.16-fold increase in glucose uptake. Compound 19 caused a glucose AUC reduction of 47.4% (30 mg/kg) in an OGTT study in C57BL/6J mice compared to 22.6% for sitagliptin (30 mg/kg). Single treatment of the compound 19 in C57BL/6J mice elicited basal glucose lowering activity without any significant evidence for hypoglycemia risk. Compound 19 was therefore selected as a candidate for further preclinical development for the treatment of type 2 diabetes.
NOVEL HETEROARYL-TRIAZOLE COMPOUNDS AS PESTICIDES
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Page/Page column 120-121; 132-133, (2021/01/29)
The present invention relates to novel heteroaryl-triazole and heteroaryl-tetrazole compounds of the general formula (I), in which the structural elements R1, R2, R3, 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.
NOVEL HETEROARYL-TRIAZOLE COMPOUNDS AS PESTICIDES
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Page/Page column 105, (2021/06/04)
The present invention relates to novel heteroaryl-triazole compounds of the general formula (I), in which the structural elements X, R1, R2, R3, R4 and R5 have the meaning given in the description, to
NOVEL HETEROARYL-TRIAZOLE COMPOUNDS AS PESTICIDES
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Page/Page column 90-91, (2021/11/13)
The present invention relates to novel heteroaryl-triazole compounds of the general formula (I), in which the structural elements X, R1, R2, R3 and R4 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.
Design, Synthesis, and Evaluation of Novel Auxin Mimic Herbicides
Do-Thanh, Chi-Linh,Vargas, Jose J.,Thomas, Joseph W.,Armel, Gregory R.,Best, Michael D.
, p. 3533 - 3537 (2016/06/01)
Due to the key roles of auxins as master regulators of plant growth, there is considerable interest in the development of compounds with auxin-like properties for growth management and weed control applications. Herein, we describe the design and multiste
AMIDOMETHYL-BIARYL DERIVATIVES COMPLEMENT FACTOR D INHIBITORS AND USES THEREOF
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Page/Page column 57, (2016/06/28)
The present invention provides a compound of formula (I): (I) 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.
1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES
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Page/Page column 140, (2016/07/05)
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.
SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND COMBINATION THERAPY THEREWITH
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Page/Page column 105, (2015/05/19)
Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided, including compounds which modulate subtype 1 of the S1P receptor, and methods of their therapeutic and/or prophylactic use in combination with at least one other medicament adapted for treatement of a malcondition for which activation of S1P1 is medically indicated, such as multiple sclerosis.
DERIVATIVES OF 1 H-PYRAZOLO[3,4-B]PYRIDINE AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
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Paragraph 00282, (2015/03/13)
The present invention discloses compounds according to Formula (I): wherein R1, R2, R3, R4, L, and X are as defined herein. The present invention relates to compounds,methods for their production, pharmaceutical