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Restrict the search for
chlorphenesin carbamate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Carprazidil is oxadiazolopyrimidine derivative patented by pharmaceutical company Hoffmann-La Roche as a direct vasodilator and potent antihypertensive agent. In clinical trials, Carprazidil was evaluated in patients with moderate to severe arterial hypertension. Following the addition of Carprazidil to pre-existing therapy with diuretics and beta-blockers or sympatholytics, blood pressure in most of the patients was normalized within one month. Heart rate was only slightly increased. Orthostatic hypotension was not observed. Weight gain or oedema formation occurred in 14 patients within the first four weeks, but could be controlled satisfactorily by intensified diuretic therapy. After a mean duration of treatment of 2.8 months, plasma volume and plasma and urine sodium were unaltered, and plasma potassium was slightly decreased. Plasma renin activity was doubled, whereas plasma aldosterone concentrations were unaltered. No adverse side effects on hematological parameters, liver or renal function were observed, nor was antinuclear antibody detected.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Diphenan is p-benzyl-phenyl-carbamate. Various workers have reported that diphenan will rid children of oxyurids and it has been claimed to be nontoxic and tasteless and to have the advantage of being a vermicide as opposed to a vermifuge. An attempt has been made to assess the efficacy of diphenan as a vermicide. Diphenan was given far in excess of the normal dosage. Subsequent examnation showed few cures and these mostly in lightly infested children. The condition of many was unchanged and that of some worse after treatment. No toxic reactions were encountered. Moreover, diphenan was found to have no detectable anthelmintic effect when given in high dosage in the treatment of enterobiasis.
Class (Stereo):
CHEMICAL (ACHIRAL)
Bamnidazole was developed as an antiprotozoal agent against Tryhomonas, however, has never been marketed.
Status:
Investigational
Source:
NCT00052117: Phase 2 Interventional Completed HIV Infections
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Capravirine (S-1153, AG1549) is a 1,2,4,5-tetrasubstituted imidazole derivative patented by pharmaceutical company Shionogi as specific inhibitors of HIV-1 reverse transcriptase. However, safety and efficacy studies showed that Capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb.
Status:
Investigational
Source:
NCT00257621: Phase 2 Interventional Completed Infection, Human Immunodeficiency Virus I
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Brecanavir (previously known as VX-385), a HIV aspartyl protease inhibitor was developed for the treatment of HIV. The inhibition of HIV viral proteinase enzyme prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. Brecanavir reached Phase II development. However, GlaxoSmithKline announced to discontinue development brecanavir. Because of the inability to develop a viable oral dosage formulation capable of delivering the desired brecanavir levels in patients with multi-drug resistant HIV.
Status:
Investigational
Source:
NCT01086267: Phase 1/Phase 2 Interventional Completed Colorectal Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
BMS-908662 (previously known as XL281) is a small molecule Raf kinase inhibitor that lies immediately downstream of RAS and are key components of the RAS/RAF/MEK/ERK kinase-signaling pathway. Bristol-Myers Squibb has received an exclusive worldwide license to develop and commercialize antineoplastic agent XL281. BMS-908662 participated in phase I development for the treatment of patients with melanoma and in combination with cetuximab for patients with colorectal cancer. However, further, development has been discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Lemildipine is a 1,4-dihydropyridine calcium channel blocker which is under phase III development by Banyu (Merck and Co), in Japan, for its potential to treat hypertension and cerebrovascular ischemia. In one study, involving five patients with essential hypertension accompanied by cerebrovascular disorder, lemildipine, administered orally at doses of 5 to 20 mg/day, significantly lowered blood pressure and increased cerebral blood flow. Another study in 31 patients with essential hypertension demonstrated that lemildipine has significant pressure lowering effects without affecting serum lipids. Worldwide rights to market the drug have been assigned to Kowa in Japan.
Status:
Investigational
Source:
NCT02115282: Phase 3 Interventional Active, not recruiting Anatomic Stage III Breast Cancer AJCC v8
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Entinostat (MS-275) is an orally active, highly selective, small-molecule histone deacetylase inhibitor (HDACi) derived from benzamide. Entinostat preferentially inhibited HDAC1 versus HDAC3 and had no inhibitory activity toward HDAC8. The time to maximum plasma concentration (tmax) of entinostat ranged from 0.5 to 60h (median of 2h). Elimination of the drug was bi-exponential, with a terminal half-life of 30-80h. Entinostat is a well-tolerated that demonstrates promising therapeutic potential in both solid and hematologic malignancies. Its efficacy does not appear directly dose-related, and as such, more relevant biomarkers are needed to adequately assess its activity.
Status:
Investigational
Source:
INN:disermolide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Disermolide (discodermolide) is the immunosuppressant and antineoplastic agent. The marine natural product discodermolide was first isolated in 1990 from the deep-water Caribbean sponge Discodermia dissoluta. It attacks cancer cells in a similar way to the successful cancer drug Taxol that has become the best-selling anticancer drug in history. Discodermolide is a microtubule-stabilizing agent with potential for the treatment of taxol-refractory malignancies. Discodermolide is a drug that functions as an immunosuppressant and induces G2/M phase cell-cycle arrest in lymphoid and non-lymphoid cells. The cytotoxicity of discodermolide cause cell-cycle arrest by mitosis and an important alteration at the level of microtubules. Discodermolide is a potent inducer of accelerated senescence. At present, Phase I trials with discodermolide has been discontinued as a consequence of unsafe efficacy and toxicity results.
Class (Stereo):
CHEMICAL (ACHIRAL)
FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
