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

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Showing 61 - 70 of 462 results

Status:
Investigational
Source:
INN:algestone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Algestone is a progesterone like female hormone. Algestone is a C21-steroid that is pregn-4-ene substituted by oxo groups at position 3 and 20 and hydroxy groups at positions 16 and 17. It has a role as a progestin. It is a 20-oxo steroid, a 16alpha-hydroxy steroid, a 17-hydroxy steroid, a C21-steroid, a 3-oxo-Delta(4) steroid and a tertiary alpha-hydroxy ketone. It derives from a hydride of a pregnane. Algestone is used as anti-inflammatory drug (topical) and combination with enanthate as injectable contraceptive.
Status:
Investigational
Source:
INN:alalevonadifloxacin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levonadifloxacin is the S-(-) isomer of the benzoquinolizine fluoroquinolone nadifloxacin and is two- to four-fold more active than the racemic mixture. Levonadifloxacin is a potent antibacterial agent against Gram-positive bacteria especially against methicillin resistance Staphylococcus aureus. It also possesses potent bactericidal activity against other resistant variants like quinolone-resistant Staphylococcus aureus, vancomycin and glycopeptide intermediate Staphylococcus aureus and vancomycin resistant Staphylococcus aureus. Intravenous dosage form developed to treat complicated skin and skin structure infections and has recently completed Phase III studies in India and Phase I studies in USA.
Status:
Investigational
Source:
JAN:ROTRAXATE HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Rotraxate (also known as TEI 5103 or TG 51) is an anti-ulcerative agent. Experiments on rodents have shown that only the oral and gastric route of administration lead to the anti-ulcer effect. This drug increased gastric mucosal blood flow and possibly promoted the healing process of peptic ulcers. However, the further development of this drug was discontinued.
Status:
Investigational
Source:
INN:clinafloxacin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Clinafloxacin is a broad-spectrum fluoroquinolone antibiotic that was originally developed and subsequently abandoned in the late 1990s as a human health antibiotic for respiratory diseases. Clinafloxacin displays broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic pathogens by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 ug/ml) as well as topoisomerase IV (IC50 = 1.62 ug/ml).
Status:
Investigational
Source:
INN:salacetamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Salacetamide is a derivative of salicylic acid. It is analgesic, anti-inflammatory and antipyretic agent.
Status:
Investigational
Source:
INN:desomorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Desomorphine is the common name for 4,5--epoxy-17- methylmorphinan-3-ol or dihydrodesoxymorphine-D. It is an opioid analogue and morphine derivative in which the 6-hydroxyl group and the double bond at carbons 7 and 8 of morphine are reduced. Desomorphine can cross the blood–brain barrier, binding to opioid receptors, similar to the pharmacokinetic distribution of all phenanthrene-structured alkaloids. Taking Desomorphine causes euphoria as well as sedative and analgesic relief. In addition to its faster onset than other powerful painkillers drugs such as morphine, desomorphine also initiates less sedative effects and seems to have favorable postoperative results, such as reduced need for catheterization, less dizziness, and decreased vomiting incidence. In comparison with Morphine, Desomorphine is faster reduced. It follows that it has to be taken it more frequently to get the same effects. Furthermore, it causes side effects such as respiratory and gastrointestinal problems and increased blood pressure. In addition, Desomorphine’s withdrawal symptoms are up to three times longer than Morphine’s. This leads to the conclusion that Desomorphine is more addictive. At present, desomorphine is classified as a narcotic drug (DEA code number 9055) in Schedule I of the U.S. Controlled Substances Act and is listed as a controlled substance under the international Single Convention on Narcotic Drugs of 1961.
Status:
Investigational
Source:
INN:nifurprazine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

The nitrofuran derivative, nifurprazine, is a topical antibacterial agent used mainly for the treatment of animal diseases. It is a trypanocidal drug. Nifurprazine proved to be the most promising derivative since it was redox-cycled by both T. cruzi LipDH and TR and had pronounced antiparasitic effects in cultures of T. cruzi and Trypanosoma brucei.
Status:
Investigational
Source:
INN:droloxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Droloxifene, a derivative of the triphenylethylene drug tamoxifen, is a novel selective estrogen receptor modulator (SERM). Droloxifene also exhibits more rapid pharmacokinetics, reaching peak concentrations and being eliminated much more rapidly than tamoxifen. Its higher affinity to the estrogen receptor, higher anti-estrogenic to estrogenic ratio, more effective inhibition of cell growth and division in estrogen receptor-positive cell lines, and lower toxicity give it theoretical advantages over tamoxifen in the treatment of human breast cancer. Short-term toxicity was generally mild, and similar to that seen with other antiestrogens. Droloxifene appears active and tolerable. It may have a particular role in situations in which rapid pharmacokinetics, or an increased antiestrogenic to estrogenic ratio, are required. Droloxifene may also be a potentially useful agent for the treatment of postmenopausal osteoporosis because it can prevent estrogen deficiency-induced bone loss without causing uterine hypertrophy. Droloxifene may have an effect on bone and breast tissue because it induces apoptosis. Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.
Status:
Investigational
Source:
INN:tomoxiprole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tomoxiprole belongs to the class of 3-alkyl-2-aryl-3H-naphth (1,2-d)imidazoles. It is a nonsteroidal anti-inflammatory compound that was reported to have low ulcerogenic potential. Tomoxiprole inhibition of cyclooxygenase-2 but not cyclooxygenase-1 is time-dependent. It has anti-inflammatory activity in various anti-inflammatory models such as carrageenin and nystatin oedemas, cotton pellet granuloma and adjuvant arthritis. The anti-inflammatory potency of tomoxiprole is greater than that of acetylsalicylic acid and phenylbutazone, but lower than that of indomethacin. Tomoxiprole reduced PGE2 and 6-keto-PGF1 alpha levels more effectively in inflamed tissue than in gastric mucosa when assayed in in vivo experiments, whereas indomethacin and other non-steroidal anti-inflammatory drugs are equally effective in both systems.
Status:
Investigational
Source:
INN:lamifiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LAMIFIBAN is a potent and selective nonpeptide glycoprotein IIb/IIIa antagonist. It inhibits platelet aggregation and thrombus formation by preventing the binding of fibrinogen to platelets. It was in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes but showed no significant effects on clinical outcomes.