Patent classifications
C07D295/182
Compounds as HIF-1α inhibitors and manufacturing process thereof
The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.
Compounds as HIF-1α inhibitors and manufacturing process thereof
The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.
FATTY ACID ACETYLATED SALICYLATES AND THEIR USES
The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.
CONJUGATES OF AUXIN ANALOGS
Described herein are methods of enhancing formation and/or growth of an adventitious root in a plant and/or plant tissue, and/or for promoting grafting unification, enhancing fruit size and/or reducing flowering in a plant. The method comprises contacting at least a portion of the plant and/or plant tissue with a compound having Formula I:
##STR00001##
wherein X, Y and R.sub.1-R.sub.7 are as defined herein. Further described are compositions for enhancing formation and/or growth of an adventitious root in a plant and/or plant tissue, and/or for promoting grafting unification, enhancing fruit size and/or reducing flowering in a plant, comprising the abovementioned compound and a horticulturally acceptable carrier. Novel compounds having Formula I are also described herein.
NOVEL PENTADIENOYL PIPERIDINE DERIVATIVE AND USE THEREOF
The present invention relates to a novel pentadienoyl piperidine derivative, a pharmaceutical composition containing the same for prevention or treatment of metabolic diseases, and a functional food composition using the same for improvement or relief of metabolic diseases. The pentadienoyl piperidine derivative of the present invention inhibits the differentiation of preadipocytes, reduces body weight, visceral fat, blood lipid levels, and blood glucose levels, improves a blood liver function index, and suppresses metabolic inflammation responses. Thus, ultimately, the derivative can be usefully used as a medicine or a functional food composition, which exhibits the preventive or therapeutic activity for metabolic diseases selected from the group consisting of obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome.
NOVEL KRAS G12C PROTEIN INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present invention belongs to the field of medicinal chemistry, and relates to a novel KRAS G12C protein inhibitor, a preparation method and use thereof. In particular, the present invention provides a compound of formula I, which can be used as a high-efficiency KRAS G12C protein inhibitor and has various pharmacological activities against tumors, proliferative diseases, inflammation, autoimmune diseases, etc.
##STR00001##
MALIC ENZYME INHIBITORS
The present invention relates to novel compounds useful as malic enzyme (ME) inhibitors, processes for their preparation and use of these compounds for the therapeutic treatment of disorders mediated by ME such as cancers (e.g. pancreatic ductal adenocarcinoma (PDAC)) in humans.
MALIC ENZYME INHIBITORS
The present invention relates to novel compounds useful as malic enzyme (ME) inhibitors, processes for their preparation and use of these compounds for the therapeutic treatment of disorders mediated by ME such as cancers (e.g. pancreatic ductal adenocarcinoma (PDAC)) in humans.
Malic enzyme inhibitors
The present invention relates to novel compounds useful as malic enzyme (ME) inhibitors, processes for their preparation and use of these compounds for the therapeutic treatment of disorders mediated by ME such as cancers (e.g. pancreatic ductal adenocarcinoma (PDAC)) in humans. The novel compounds have a structure according to Formula I ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or deuterated analog thereof, wherein X, R.sub.1, R.sub.2 and Y are as described herein.
Malic enzyme inhibitors
The present invention relates to novel compounds useful as malic enzyme (ME) inhibitors, processes for their preparation and use of these compounds for the therapeutic treatment of disorders mediated by ME such as cancers (e.g. pancreatic ductal adenocarcinoma (PDAC)) in humans. The novel compounds have a structure according to Formula I ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or deuterated analog thereof, wherein X, R.sub.1, R.sub.2 and Y are as described herein.