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

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Showing 1951 - 1960 of 42705 results

Status:
Investigational
Source:
JAN:CAROTEGRAST METHYL [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Carotegrast is phenylalanine derivative patented by pharmaceutical company Ajinomoto Co. for the treatment or prevention of inflammatory disease states related to the α4 integrin-dependent adhesion process. In preclinical studies, Carotegrast shows pharmacological activity in rheumatoid arthritis and inflammatory bowel disease.
Status:
Investigational
Source:
NCT01800838: Phase 1 Interventional Completed Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00769288: Phase 1 Interventional Completed Adult Grade III Lymphomatoid Granulomatosis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

1-(2-DEOXY-2-FLUORO-β-D-ARABINOFURANOSYL)URACIL (FAU) is a thymidine analog. In several cancer cell lines, FAU was phosphorylated intracellularly to its monophosphate, 1-(2-deoxy-2-fluoro--Darabinofuranosyl) uracil monophosphate (FAUMP), by thymidine kinase and methylated in the 5-position by thymidylate synthase to form the product, 1-(2-deoxy-2-fluoro- -D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FAU strongly inhibits the growth of tumor cells with high thymidylate synthase activity. FAU had been in phase I clinical trial for the treatment of advanced solid tumors.
Status:
Investigational
Source:
NCT02267278: Phase 2 Interventional Completed Myeloproliferative Diseases
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pracinostat is a pan-histone deacetylase inhibitor being tested in phase II of clinical trials for the treatment of sarcoma, prostate cancer, acute myeloid leukemia, myelofibrosis, myelodysplastic syndrome. The drug was shown to be active in vitro on HCT116 and HL-60 cells.
Status:
Investigational
Source:
NCT00405119: Phase 2 Interventional Completed Gastroesophageal Reflux Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LAVOLTIDINE, also known as loxtidine, is a highly potent and selective histamine H2-receptor antagonist. It is a member of triazoles. It produces gastric carcinoid tumors in rodents that is why its clinical development was discontinued.
Status:
Investigational
Source:
INN:isoxepac
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Isoxepac (also known) as HP-549 is a non-steroidal anti-inflammatory drug with analgesic activity. Isoxepac was studied in the clinical trial for the treatment of postoperative pain after knee surgery for meniscectomy. It was shown, that 200 mg of isoxepac would appear to be the minimal effective dose. In case of rheumatoid arthritis, isoxepac showed significantly fewer adverse effects.
Status:
Investigational
Source:
INN:becampanel [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Becampanel (AMP397) is an aminomethylquinoxalinedione AMPA receptor antagonist. Also, AMP397 demonstrates binding to hydroxyapatite. AMP397 has no genotoxic potential in vivo. In particular, no genotoxic metabolite is formed in mammalian cells, and, if formed by intestinal bacteria, is unable to exert any genotoxic activity in the adjacent intestinal tissue. AMP397 has a significant oral bioavailability of 22% in mice and approximately 50% in humans. It was under development for the potential treatment of status epilepticus and other types of seizures. However, this research has been discontinued. It is also being evaluated for use in the treatment of neuropathic pain and cerebrovascular ischemia.
Status:
Investigational
Source:
NCT00170911: Phase 2 Interventional Completed Osteoporosis
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Balicatib is a potent cathepsine K inhibitor that was developed for the treatment of knee osteoarthritis. The development of Balicatib was terminated in phase II due to the occurrence of skin rashes and rarer incidences of morphea-like skin changes.
Status:
Investigational
Source:
INN:imidoline [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

There is no much available information related to the biological and pharmacological application of imidoline, but this compound has been found to be as potent as chlorpromazine in increasing striatal DOPA accumulation and prolactin secretion in vivo. Imidoline exhibited only weak inhibitory activity towards dopamine-sensitive adenylate cyclase and 3H-spiroperidol binding to striatal membranes in vitro. A proposed active conformation involves intramolecular hydrogen bonding between the protonated dimethylamino group and the oxygen of the imidazolidinone ring. The spatial relationship between the amine nitrogen and phenyl ring in this conformation allows proper fit of imidoline with key dimensions described for the dopamine receptor.
Status:
Investigational
Source:
INN:mazapertine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.

Showing 1951 - 1960 of 42705 results