U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1261 - 1270 of 21518 results

Status:
Investigational
Source:
Nucleic Acid Ther. Feb 2019;29(1):16-32.: Phase 1 Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



β-N-Acetyl-D-galactosamine (GalNAc) is an amino sugar derived from galactose found in O-linked and N-linked glycans. As an essential sugar, the role is basically the same for N-acetylgalactosamine as it is for the others, which is to enhance cellular communication. Although there has not been much research to date, what has been done reveals that this saccharide may inhibit the growth of some tumors. For example, colon cancer patients have only half the normal amounts of N-acetylgalactosamine. Studies have shown that colon cancer cells that metastasize make more mucin, making them more likely to form metastases. Therefore, it appears that N-acetylgalactosamine plays an important role in preventing this formation from occurring. N-acetylgalactosamine and N-acetylglucosamine glycans is a predictor of metastasis and poor prognosis in a number of human adenocarcinomas, including breast cancer. Lower than normal levels of this sugar has been found in patients with heart disease implying that these conditions may be reversed if a supplementation of N-acetylgalactosamine were to be added to the diet. It appears that β-N-Acetyl-D-galactosamine plays a role in joint function, sweeping away destructive free radicals that can cause inflammation. N-acetylgalactosamine also seems to play an important role in the immune system. Contained in macrophages and neutrophils, it may play a significant role in the etiology of joint inflammation and could be important in such conditions as rheumatoid arthritis. In humans, it is the terminal carbohydrate forming the antigen of blood group A. N-acetylgalactosamine (GalNAc) is a well-defined liver-targeted moiety benefiting from its high affinity with asialoglycoprotein receptor (ASGPR). By conjugating it directly to the oligonucleotides or decorating it to a certain delivery system as a targeting moiety, GalNAc has achieved compelling successes in the development of nucleic acid therapeutics in recent years. Several oligonucleotide modalities are undergoing pivotal clinical studies, followed by a blooming pipeline in the preclinical stage. N-Acetyl-D-galactosamine is used in affinity chromatography, protein chromatography and in carbohydrate matrices. N-Acetyl-D-galactosamine has been used to study periodontal disease and to facilitate the design of potent small-molecule ice recrystallization inhibitors. N-Acetyl-D-galactosamine has also been used to demonstrate a molecular shuttle between extracellular and cytoplasmic space allows for monitoring of GAG biosynthesis.
Status:
Investigational
Source:
JAN:JOSAMYCIN PROPIONATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Josamycin propionate, a tasteless josamycin derivative suitable for the preparation of pediatric oral suspension. After oral administration Josamycin propionate underwent metabolic transformation to Josamycin, semi-synthetic 16-membered ring macrolide, that acts via protein synthesis inhibition.
Sipatrigine (BW 619C89), a blocker of neuronal Na+ and Ca2+ channels, has neuroprotective efficacy. This drug was in phase II studies in stroke patients who received iv infusions of sipatrigine. The main adverse events observed were hallucinations and vomiting. The Phase II trial was terminated when Glaxo merged with Wellcome and a decision was made to develop the NMDA (glycine site) receptor antagonist gavestinel (from Glaxo), which showed no efficacy in a randomized, double blind, placebo- controlled trial. It was also assumed, that sipatrigine could have therapeutic potential for major depression and bipolar depression through antagonism of the two-pore-domain K+ channel TREK-1. but further evaluation of its antidepressant therapeutic and toxic effects in animal models is needed before clinical application.
Status:
Investigational
Source:
INN:enisoprost
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Enisoprost is a prostaglandin E1 analog. Enisoprost exerts immunosuppressive activity and gastric antisecretory effect. Enisoprost was being studied for the treatment of peptic ulcer and transplant rejection. Enisoprost development has been discontinued.
Status:
Investigational
Source:
INN:noracymethadol
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Status:
Investigational
Source:
NCT01041677: Phase 2 Interventional Completed Obesity
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Johnson and Johnson was developing usistapide, a microsomal triglyceride transfer protein (MTTP) inhibitor, for the treatment of obesity and type 2 diabetes. Usistapide, also known as JNJ-16269110 and R256918, has been used in trials studying the treatment of obesity, overweight, metabolic diseases, nutrition disorders, and nutritional and metabolic diseases. Usistapide was removed from the company pipeline and appears to have been discontinued.
Status:
Investigational
Source:
NCT00113438: Phase 2 Interventional Completed Cancer
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Combretastatin is a phenol derivative isolated from the bark of Combretum caffrum, commonly known as South African Bush Willow. Combretastatin is an effective antimitotic agent, and like colchicine, inhibited tubulin polymerization and stimulated tubulin-dependent GTP hydrolysis.
Status:
Investigational
Source:
NCT02533336: Phase 3 Interventional Terminated Malaria
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FENPYROXIMATE is a pyrazole acaricide widely used in the prevention of acarids (mites) in fruit plant gardens. It is a potent inhibitor of the mitochondrial proton-translocating NADH-quinone oxidoreductase (complex I).
Status:
Investigational
Source:
NCT01261988: Phase 1 Interventional Completed Ostomy
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Penoxsulam, a fluorinated benzenesulfonamid rice herbicide is sold under the brand name Granite. Penoxsulam is an acetolactate synthase inhibitor that kills plants through a mechanism not present in animals and has few to no adverse effects on most species. Besides, was found that Chlorella Vulgaris dietary supplementation could protect the commercially valuable freshwater fish Oreochromis niloticus against penoxsulam toxicity and may be a potential feed supplement for Nile tilapia in aquaculture.
Status:
Investigational
Source:
INN:maridomycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Maridomycin is a macrolide antibiotic. Sreptomyces sp. No. B-5050 was found to produce maridomycin. Maridomycin was found to be composed of six components, maridomycins I, II, III, IV, V and VI. Their structures are different from each other in acyl moieties at C3 and C4" positions. Maridomycins I, II, III, IV, V and VI showed similar antibacterial spectra against Gram-positive bacteria including acid-fast bacteria. Maridomycin has bacteriostatic activity rather than bactericidal activity. Prominent therapeutic effect was observed against certain Gram-positive bacterial infection in mice.

Showing 1261 - 1270 of 21518 results