Patent classifications
C07D235/20
2-amino-benzimidazole derivatives and their use as 5-lipoxygenase and/or prostaglandin E synthase inhibitors
The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X.sup.1 and X.sup.2 are independently, at each occurrence, CR.sup.5 or N; Y is C.sub.1-C.sub.6 alkylene, wherein alkylene is optionally substituted with one to two C.sub.1-C.sub.3 alkyl groups; R.sup.1 is selected from the group consisting of hydrogen, halogen, C.sub.1-C.sub.6 alkoxy, —NH.sub.2, —NHR.sup.6, —NR.sup.7R.sup.8 and —NH—(R.sup.9).sub.n—R.sup.10, n being 0 or 1; R.sup.2 is selected from the group consisting of hydrogen, halogen, C.sub.1-C.sub.6 alkyl, —NH.sub.2, —NHR.sup.6, —NR.sup.7R.sup.8 and —NH—(R.sup.9).sub.n—R.sup.10; R.sup.3 is selected from the group consisting of hydrogen, hydroxyl, OR.sup.11, —NR.sup.7R.sup.8, C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.10 cycloalkyl, C.sub.1-C.sub.3 haloalkyl, —C(O)NHR.sup.11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four R.sup.a groups; and R.sup.4 is selected from the group consisting of —NH.sub.2, —N(R.sup.12)(V).sub.pR.sup.13, —NH(V).sub.p—OR.sup.14, —NHC(O)R.sup.15, and groups of formula 1a shown below, and their use in the treatment of diseases, in particular inflammatory diseases, cancer, stroke and/or Alzheimer's disease. ##STR00001##
2-amino-benzimidazole derivatives and their use as 5-lipoxygenase and/or prostaglandin E synthase inhibitors
The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X.sup.1 and X.sup.2 are independently, at each occurrence, CR.sup.5 or N; Y is C.sub.1-C.sub.6 alkylene, wherein alkylene is optionally substituted with one to two C.sub.1-C.sub.3 alkyl groups; R.sup.1 is selected from the group consisting of hydrogen, halogen, C.sub.1-C.sub.6 alkoxy, —NH.sub.2, —NHR.sup.6, —NR.sup.7R.sup.8 and —NH—(R.sup.9).sub.n—R.sup.10, n being 0 or 1; R.sup.2 is selected from the group consisting of hydrogen, halogen, C.sub.1-C.sub.6 alkyl, —NH.sub.2, —NHR.sup.6, —NR.sup.7R.sup.8 and —NH—(R.sup.9).sub.n—R.sup.10; R.sup.3 is selected from the group consisting of hydrogen, hydroxyl, OR.sup.11, —NR.sup.7R.sup.8, C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.10 cycloalkyl, C.sub.1-C.sub.3 haloalkyl, —C(O)NHR.sup.11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four R.sup.a groups; and R.sup.4 is selected from the group consisting of —NH.sub.2, —N(R.sup.12)(V).sub.pR.sup.13, —NH(V).sub.p—OR.sup.14, —NHC(O)R.sup.15, and groups of formula 1a shown below, and their use in the treatment of diseases, in particular inflammatory diseases, cancer, stroke and/or Alzheimer's disease. ##STR00001##
HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ARENAVIRUS INFECTION
The invention relates to compounds of structural formula I
##STR00001##
wherein A, D, and E are independently N or C—R.sup.3, G, H, and J are independently N or C, K is N or C—H, L is N, N—R.sup.3 or C—R.sup.3, and A, D, E, G, H, J, K, and L together cannot have more than 4 N, R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl, (C.sub.2 to C.sub.9) heteroaryl, and 5-indolyl, wherein each of the said (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl is substituted with at least one R.sup.4a group, and wherein said (C.sub.2 to C.sub.9) heteroaryl is C-attached, and R.sup.2 is selected from the group consisting of
##STR00002##
HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ARENAVIRUS INFECTION
The invention relates to compounds of structural formula I
##STR00001##
wherein A, D, and E are independently N or C—R.sup.3, G, H, and J are independently N or C, K is N or C—H, L is N, N—R.sup.3 or C—R.sup.3, and A, D, E, G, H, J, K, and L together cannot have more than 4 N, R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl, (C.sub.2 to C.sub.9) heteroaryl, and 5-indolyl, wherein each of the said (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl is substituted with at least one R.sup.4a group, and wherein said (C.sub.2 to C.sub.9) heteroaryl is C-attached, and R.sup.2 is selected from the group consisting of
##STR00002##
Broad spectrum antibacterial activity of novel bisbenzimidazoles targeting topoisomerase IA and the synergistic composition of bisbenzimidazole with efflux pump inhibitors against pathogenic bacteria
The present invention relates to potent antibacterial activity of novel bisbenzimidazoles (SP12a and SP12b) against both Gram positive and Gram negative bacteria and a synergistic composition comprising Bisbenzimidazole (HN12b) in combination with Efflux pump inhibitors against most of the pathogenic bacterial strains.
Broad spectrum antibacterial activity of novel bisbenzimidazoles targeting topoisomerase IA and the synergistic composition of bisbenzimidazole with efflux pump inhibitors against pathogenic bacteria
The present invention relates to potent antibacterial activity of novel bisbenzimidazoles (SP12a and SP12b) against both Gram positive and Gram negative bacteria and a synergistic composition comprising Bisbenzimidazole (HN12b) in combination with Efflux pump inhibitors against most of the pathogenic bacterial strains.
ORGANIC LIGHT EMITTING DIODE AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME
The present disclosure relates to an OLED that includes a first electrode; a second electrode facing the first electrode; a first emitting material layer including a first host being an anthracene derivative and a first dopant being a pyrene derivative and positioned between the first and second electrodes; and a first electron blocking layer including an electron blocking material of an amine derivative including a polycyclic aryl group and positioned between the first electrode and the first emitting material layer, wherein at least one of hydrogen atoms in the anthracene derivative and the pyrene derivative is deuterated.
ORGANIC LIGHT EMITTING DIODE AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME
The present disclosure relates to an OLED that includes a first electrode; a second electrode facing the first electrode; a first emitting material layer including a first host being an anthracene derivative and a first dopant being a pyrene derivative and positioned between the first and second electrodes; and a first electron blocking layer including an electron blocking material of an amine derivative including a polycyclic aryl group and positioned between the first electrode and the first emitting material layer, wherein at least one of hydrogen atoms in the anthracene derivative and the pyrene derivative is deuterated.
Organic light-emitting device
The present specification relates to an organic light emitting diode.
Organic light-emitting device
The present specification relates to an organic light emitting diode.