Patent classifications
C07F9/65068
2-ARYLBENZIMIDAZOLES AS PPARGC1A ACTIVATORS FOR TREATING NEURODEGENERATIVE DISEASES
The compound 2-(4-tert-Butylphenyl)-1H-benzo[d]imidazol-5-ol:
##STR00001##
and its use are disclosed. The compound activates Ppargc1a and, as a consequence, is useful for treating neuroinflammation and for treating a variety of neurodegenerative diseases.
MEBENDAZOLE PRODRUGS WITH ENHANCED SOLUBILITY AND ORAL BIOAVAILABILITY
Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.
2-arylbenzimidazoles as PPARGC1A activators for treating neurodegenerative diseases
The compound 2-(3-tert-Butylphenyl)-4,6-difluoro-1H-benzo[d]imidazole and its use are disclosed: ##STR00001##
The compound activates Ppargc1a and, as a consequence, is useful for treating neuroinflammation and for treating a variety of neurodegenerative diseases.
2-ARYLBENZIMIDAZOLES AS PPARGC1A ACTIVATORS FOR TREATING NEURODEGENERATIVE DISEASES
The compound 2-(3-tert-Butylphenyl)-4,6-difluoro-1H-benzo[d]imidazole and its use are disclosed:
##STR00001##
The compound activates Ppargc1a and, as a consequence, is useful for treating neuroinflammation and for treating a variety of neurodegenerative diseases.
METHOD OF SYNTHESIZING INDOLE COMPOUNDS
A method of synthesizing indole compounds. The method may include allyllating an indole compound, oxidizing the resulting -indolepropene, and reductively aminating the resulting indoleacetaldehyde, providing a tryptamine. The indole compound may be substituted with a functional group on the indole ring or may be unsubstituted indole. The method may include substitution, oxidation or other derivatization of the indole ring of the indole compound, of tryptophan, of the tryptamine, or of intermediates. The method may include oxidizing tryptophan or a ring-substituted tryptophan analogue and reductively aminating the resulting indoleacetaldehyde, providing a tryptamine. The method may be applied in a telescoped approach without isolation of intermediates. The method may be applied to production of indoles, -indolepropenes, indole propyl diols, indoleacetaldehydes and tryptamines. Compounds from each of these classes of compounds are also provided herein.
Organic semiconductive layer comprising phosphine oxide compounds
The present invention relates to an. organic semiconductive layer which is an electron transport layer and/or an electron injection layer and/or an n-type charge generation layer, the organic semiconductive layer comprising at least one compound of formula (1) wherein R.sup.1 and R.sup.2 are each independently selected from C.sub.1 to C.sub.16 alkyl; Ar.sup.1 is selected from C.sub.6 to C.sub.14 arylene or C.sub.3 to C.sub.12 heteroarylene; Ar.sup.2 is independently selected from C.sub.14 to C.sub.40 arylene or C.sub.8 to C.sub.40 heteroarylene; R.sup.3 is independently selected from H, C.sub.1 to C.sub.12 alkyl or C.sub.10 to C.sub.20 aryl; wherein each of Ar.sup.1, Ar.sup.2 and R.sup.3 may each independently be unsubstituted or substituted with at least one C.sub.1 to C.sub.12 alky group; n is 0 or 1; and m is 1 in case of n=0; and m is 1 or 2 in case of n=1, phosphine oxide compounds comprised therein and to organic electroluminescent devices comprising such layers and compounds. ##STR00001##
MEVALONATE PATHWAY INHIBITOR AS HIGHLY-EFFICIENT VACCINE ADJUVANT
Disclosed are inhibitors of mevalonate pathway as an efficient vaccine adjuvant and use thereof. In particular, the inhibitor is an acetoacetyl-CoA transferase inhibitor, a HMG-CoA synthase inhibitor, a HMG-CoA reductase inhibitor, a mevalonate kinase inhibitor, a phosphomevalonate kinase inhibitor, a mevalonate-5-pyrophosphate decarboxylase inhibitor, an isopentenyl pyrophosphate isomerase inhibitor, a farnesyl pyrophosphate synthase inhibitor, a geranylgeranyl pyrophosphate synthase inhibitor or a geranylgeranyl transferase (I, II) inhibitor. Also disclosed is an immunogenic composition comprising inhibitors of mevalonate to pathway as an adjuvant.
Organic Semiconductive Layer Comprising Phosphine Oxide Compounds
The present invention relates to an organic semiconductive layer which is an electron transport layer and/or an electron injection layer and/or an n-type charge generation layer, the organic semiconductive layer comprising at least one compound of formula (1)
##STR00001## wherein R.sup.1 and R.sup.2 are each independently selected from C.sub.1 to C.sub.16 alkyl; Ar.sup.1 is selected from C.sub.6 to C.sub.14 arylene or C.sub.3 to C.sub.12 heteroarylene; Ar.sup.2 is independently selected from C.sub.14 to C.sub.40 arylene or C.sub.8 to C.sub.40 heteroarylene; R.sup.3 is independently selected from H, C.sub.1 to C.sub.12 alkyl or C.sub.10 to C.sub.20 aryl; wherein each of Ar.sup.1, Ar.sup.2 and R.sup.3 may each independently be unsubstituted or substituted with at least one C.sub.1 to C.sub.12 alky group; n is 0 or 1; and m is 1 in case of n=0; and m is 1 or 2 in case of n=1, phosphine oxide compounds comprised therein and to organic electroluminescent devices comprising such layers and compounds.
PHOSPHINE-UREA LIGANDS FOR TRANSITION METAL CATALYZED CROSS-COUPLING REACTIONS
Carbon-carbon bond forming reactions are the cornerstone of organic chemistry. A new class of ligands was developed for transition metal catalyzed cross-coupling reactions. These phosphine-urea ligands incorporate a urea subunit into the backbone of the ligand, which is designed to bind to the organometallic coupling partner and simultaneously facilitate and direct transmetalation of the nucleophile. Synthetic routes were designed and executed to synthesize phosphine-urea ligands. These ligands catalyze a wide variety of cross-coupling reactions including Suzuki, Negishi, and Buchwald-Hartwig cross-couplings. Aryl-aryl, alkyl-aryl, and alkyl-alkyl CC cross-couplings are performed successfully with these ligands. In addition, specific chiral phosphine-urea ligands catalyze Negishi cross-couplings enantioselectively from a racemic alkylzinc nucleophile.
Bicyclic heteroaryl derivatives as ectonucleotide pyrophosphatase phosphodiesterase 1 inhibitors
The present disclosure provides certain bicyclic heteroaryl compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. In some embodiments, the bicyclic heteroaryl compounds includes those of Formula (I). Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds. ##STR00001##