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

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Showing 431 - 440 of 623 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Flupirtine is a triaminopyridine derivative having a chemical structure - 2-amino-3-ethoxy-carbonylamino-6-4-fluoro-benzylamino-pyridine. The basic molecule used for synthesis of flupirtine was 2, 6-dichoro 3-nitropyridine. It was first synthesized in 1980s in Germany and was marketed by Degussa Pharma. Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European countries for the treatment of a variety of pain states. The therapeutic benefits seen with flupirtine relate to its unique pharmacological properties. Flupirtine displays indirect NDMA receptor antagonism via activation of potassium channels and is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. Neuronal hyperexcitability is a physiological component of many pain states such as chronic pain, migraine and neurogenic pain.
Status:
Possibly Marketed Outside US
Source:
Japan:Cepharanthine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cepharanthine (CEP) is a naturally occurring alkaloid extracted from the plant Stephania cepharantha Hayata. It has been widely used in Japan for more than 40 years to treat a wide variety of acute and chronic diseases. CEP inhibits tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppresses cytokine production. It has also been shown to scavenge free radicals and to have a protective effect against some of the responses mediated by pro-inflammatory cytokines such as TNF-α, interleukin (IL)-1β and IL6. CEP has successfully been used to treat a diverse range of medical conditions, including radiation-induced leukopenia, idiopathic thrombocytopenic purpura, alopecia areata, alopecia pityrodes, venomous snakebites, xerostomia, sarcoidosis, refractory anemia and various cancer-related conditions. No safety issues have been observed with CEP, and side effects are very rarely reported. Recently was described a transcriptomic approach confirmed that cepharanthine might have a potential innovative antiplasmodial mechanism of action. Cepharanthine could interfere with several important functions for Plasmodium survival and virulence as the mitochondrion, apicoplast, cytoadherence antigenic variation and Maurer’s clefts. Thus, cepharanthine might play an ongoing role in the progress on anti-malarial drug discovery efforts. Also using intravenous and oral administration of CEP was shown its protective effect for acute or late toxicity to the bladder/urethra and rectum. It was discovered, that acute urinary toxicity was significantly milder for the intravenous group than for the oral and non-administration groups. The protective efficacy of CEP was not approved for acute rectal toxicity, but late rectal toxicity was significantly milder for the intravenous group than for the oral group. Intravenous Cepharanthin administration may prevent acute or late toxicity by radiotherapy for prostate cancer.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Araprofen is an anti-inflammatory and analgesic agent.
Status:
Possibly Marketed Outside US
Source:
Danilon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



In 2012, two newly developed active pharmaceutical ingredients for horses and food producing animals were released on the German market for veterinary drug products. Those are the parenterally applicable first generation cephalosporin Cefalonium (Cepravin) and the nonsteroidal anti-inflammatory drug Suxibuzone (Danilon). Suxibuzone is a d drug for treatment of pain and inflammation associated with musculoskeletal conditions in the horse eg. osteoarthritic conditions, bursitis, laminitis and soft tissue inflammation. It is a prodrug of the phenylbutazone, which inactivates prostaglandin H synthase and prostacyclin synthase
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Mofebutazone (or monophenylbutazone) is a 3,5-pyrazolinedione derivative study for treating asthma and muscular pain. It was found that there was no increase in the incidence or severity of the asthmatic attacks during the course of mofebutazone treatment. The drug tended to improve the tested pulmonary ventilatory functions or at least to leave them unchanged. All the mofebutazone-treated individuals showed a dramatic reduction in the concentrations of PGE2, PGF2alpha, and LTs in their BAL, but there was no consistent correlation between the extent of reduction and the degree of benefit or worsening sustained by an individual patient. Mofebutazone was found to be excreted almost exclusively via the kidney
Status:
Possibly Marketed Outside US
Source:
Japan:Clidanac
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Clidanac is an anti-inflammatory agent developed in Japan for the treatment of rheumatoid arthritis. The drug is mixture of two isomers, d- and l-, and the d-form is more active than the l-form. Therapeutic effect of clidanac is mediated by the inhibition of prostaglandin biosynthesis.
Status:
Possibly Marketed Outside US
Source:
Japan:Protizinic Acid
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Protizinic acid is an elaborated member of propionic acid series, and is a cyclooxygenase inhibitor with antiinflammatory and antipyretic activity
Status:
Possibly Marketed Outside US
Source:
Japan:Nifenazone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Nifenazone is a drug that has been used as an analgesic for a number of rheumatic conditions. Later it was shown that nifenazone is not of significant value in the therapy of the chronic rheumatic disorders and that side-effects may be expected to occur, particularly in those patients who give a history of abnormal reactions to phenylbutazone and oxyphenbutazone.
Status:
Possibly Marketed Outside US
Source:
Fenazol Ointment 5%
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ufenamate is a topical analgesic. It is indicated for pain and inflammation associated with musculoskeletal and joint disorders. It is a COX inhibitor. Ufenamate is freely soluble in oil and is poorly soluble in water. It is used in the form of ointments or creams. It is manufactured under the brand name Combec in Japan. It is also an ingredient of Fenazol Ointment 5%, used in Japan for the treatment of eczema, dermatitis and herpes zoster.
Status:
Possibly Marketed Outside US
Source:
Telzenac by Altana
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Eltenac is a compound with a structural similarity to diclofenac with one benzol ring substituted by a tiophene ring. This modification has been shown to improve the absorption after topical application. Eltenac is an inhibitor of both cyclo-oxygenase-1 and -2. Eltenac had been in phase II clinical trial for the treatment of osteoarthritis of the knee. Eltenac is used in the alleviation of inflammation associated with musculoskeletal disorders and control of post-operative swelling, oedema and endotoxaemia in horses. The local skin reactions reported in humans were erythema, eczema, itching, rash and dry skin.

Showing 431 - 440 of 623 results