Patent classifications
C07D263/48
Inhibitors of Glutathione S-Transferases (GSTS) and NAD(P)H:Quinone Oxidoreductase 1 (NQO1), Pharmaceutical Compositions, and Uses in Managing Cancer
This disclosure relates to compounds that inhibit glutathione S-transferases (GSTs) and/or NAD(P)H:quinone oxidore-ductase 1 (NQO1) for uses in treating cancer. In certain embodiments, this disclosure relates to compositions and uses of N-(thia-zol-2-yl)-carboxamide derivatives such as a N-(5-nitrothiazol-2-yl)-carboxamide derivatives for treating cancer such as glioblastoma. In certain embodiments, this disclosure relates to pharmaceutical compositions comprising a N-(thiazol-2-yl)-carboxamide derivative such as a N-(5-nitrothiazol-2-yl)-carboxamide derivative which is a compound of formula (I), or derivative, prodrug or salt thereof and a pharmaceutically acceptable excipient, wherein X, R.sup.1, R.sup.2, and R.sup.3 substituents are reported herein.
Oxazole containing compounds as activators of IDO1 and AhR
Provided herein are methods and compositions related to a method of stimulating the immune system in a subject in need thereof by administering an agent that increases the level or activity of indoleamine 2,3-dioxygenase (IDO1) and/or aryl hydrocarbon receptor (Ahr).
Oxazole containing compounds as activators of IDO1 and AhR
Provided herein are methods and compositions related to a method of stimulating the immune system in a subject in need thereof by administering an agent that increases the level or activity of indoleamine 2,3-dioxygenase (IDO1) and/or aryl hydrocarbon receptor (Ahr).
2-AMINOARYL-5-ARYLOXAZOLE ANALOGS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
The present disclosure is concerned with 2-aminoaryl-5-aryloxazole compounds that are capable of activating NF-κB signaling. The present disclosure is also concerned with methods of using these compounds for the treatment of neurological disorders such as, for example, amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD), and neuromuscular disorders such as, for example, Duchenne muscular dystrophy (DMD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
2-AMINOARYL-5-ARYLOXAZOLE ANALOGS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
The present disclosure is concerned with 2-aminoaryl-5-aryloxazole compounds that are capable of activating NF-κB signaling. The present disclosure is also concerned with methods of using these compounds for the treatment of neurological disorders such as, for example, amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD), and neuromuscular disorders such as, for example, Duchenne muscular dystrophy (DMD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Novel Compounds for Treating Fibrosis and Inflammatory Conditions
Several biological targets have been implicated in the pathogenesis of lung, liver, renal and prostrate fibrotic proliferative diseases. While cannabinoid receptor-mediated signaling has emerged as a novel signaling pathway regulating fibrogenesis and inflammation, the present invention relates generally to biologically active compounds capable of interacting with one or more biological targets including the CB1 and/or the CB2 cannabinoid receptors, and comprise of neutral antagonists, neutral-peripheral antagonists, peripheral antagonists/inverse-agonists, compounds with mixed properties including CB1 antagonist/CB2 agonist properties, and allosteric properties for treating fibrosis of the liver, lung, kidney and the prostrate, and inflammatory conditions, including benign prostatic hyperplasia. Also, aspects of the invention are concerned with imidazoles, triazoles, thiazoles, oxazoles, pyrazoles and dihydropyrazoles containing the 4-(λ2-azaneyl)thiomorpholine 1,1-dioxide group or the 4λ2-thiomorpholine 1,1-dioxide group.
BENZOTHIOPHENE DERIVATIVE REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.
##STR00001##
Organic electroluminescent element, compound for use in the element, and light emitting device, display device, and illumination device using the element
The disclosure relates to organic electroluminescent elements, compounds for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): ##STR00001##
where R.sup.1 to R.sup.3 and R.sup.6 to R.sup.8 each independently represents a hydrogen atom, which may be a deuterium atom, or a substituent with a Hammett substituent constant σ.sub.p value of −0.15 or more, R.sup.5, R.sup.9 and R.sup.10 each independently represents a hydrogen atom or a substituent, L.sup.1 represents a divalent linking group, DG.sup.1 represents a donor group, and n1 represents 1 or 2, and where R.sup.1 to R.sup.3, R.sup.5 to R.sup.10, L.sup.1, and DG.sup.1 are not bound to each other to form a ring.
Organic electroluminescent element, compound for use in the element, and light emitting device, display device, and illumination device using the element
The disclosure relates to organic electroluminescent elements, compounds for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): ##STR00001##
where R.sup.1 to R.sup.3 and R.sup.6 to R.sup.8 each independently represents a hydrogen atom, which may be a deuterium atom, or a substituent with a Hammett substituent constant σ.sub.p value of −0.15 or more, R.sup.5, R.sup.9 and R.sup.10 each independently represents a hydrogen atom or a substituent, L.sup.1 represents a divalent linking group, DG.sup.1 represents a donor group, and n1 represents 1 or 2, and where R.sup.1 to R.sup.3, R.sup.5 to R.sup.10, L.sup.1, and DG.sup.1 are not bound to each other to form a ring.
OXIME ETHER COMPOUND AND APPLICATION THEREOF
The present invention discloses an oxime ether compound with novel structure. The structure is shown in general formula I. The definition of each substituent in the formula is provided in the description.
##STR00001##
The compound of general formula I has excellent microbicidal 1 activity, and has good control effects on plant bacterial diseases and fungal diseases. The present invention comprises an application of the compound of the general formula I as a microbicide in agriculture and other fields.