445003-37-2Relevant academic research and scientific papers
Synthesis and SAR studies of novel benzodiazepinedione-based inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB)
Letourneau, Jeffrey J.,Stroke, Ilana L.,Hilbert, David W.,Cole, Andrew G.,Sturzenbecker, Laurie J.,Marinelli, Brett A.,Quintero, Jorge G.,Sabalski, Joan,Li, Yanfang,Ma, Linh,Pechik, Igor,Stein, Philip D.,Webb, Maria L.
supporting information, p. 3601 - 3605 (2018/11/10)
Synthesis and structure-activity relationships (SAR) of a novel series of benzodiazepinedione-based inhibitors of Clostridium difficile toxin B (TcdB) are described. Compounds demonstrating low nanomolar affinity for TcdB, and which possess improved stability in mouse plasma vs. earlier compounds from this series, have been identified. Optimized compound 11d demonstrates a good pharmacokinetic (PK) profile in mouse and hamster and is efficacious in a hamster survival model of Clostridium difficile infection.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
-
Paragraph 0255; 0256, (2015/11/25)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Modulators of methyl modifying enzymes, compositions and uses thereof
-
Page/Page column 235; 236; 257; 258; 259, (2015/12/26)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
DIHYDROFURAN DERIVATIVES AS INSECTICIDAL COMPOUNDS
-
Page/Page column 282, (2013/03/26)
The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4
ISOTHIAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS
-
Page/Page column 244, (2013/03/28)
The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C-H, C-R5/
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
-
Paragraph 00521; 00522; 00579; 00580, (2013/06/05)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
-
Paragraph 00152; 00153, (2013/06/05)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
INSECTICIDAL COMPOUNDS
-
Page/Page column 114-115, (2013/02/27)
The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C-H, C-R5, or nitrogen; B1--B2--B3--B4 is -CH2-C=N-CH2-, -CH2-N-CH2-CH2-, -CH2-C=CH-0- or -CH=C-CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy- C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C=O or C=S; Y2, Y3 and Y4 are independently CR7R8, C=0, C=S, N-R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
DIHYDROFURAN DERIVATIVES AS INSECTICIDAL COMPOUNDS
-
Page/Page column 36, (2013/02/28)
The present invention relates to compounds of formula (I) wherein Q is Q1 or Q2 P is P1, heterocyclylor heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Y1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
DIHYDROFURAN DERIVATIVES AS INSECTICIDAL COMPOUNDS
-
Page/Page column 73, (2011/09/19)
The present invention relates to compounds of formula (I) wherein Q is Q1 or Q2 P is P1, heterocyclylor heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Y1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
