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Restrict the search for
phenyl aminosalicylate
to a specific field?
Class (Stereo):
CHEMICAL (RACEMIC)
Pamatolol is a beta-Adrenergic receptor antagonist was studied as an Antiarrhythmic agent. The phase I clinical trial has shown that the drug was relatively cardioselective in man. Information about the further development of this drug is not available.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Pargeverine (also known as a propinox) is an antispasmodic drug that was studied for the treatment of disorders of the gastrointestinal tract, the uterus, and the gallbladder. Pargeverine showed a dual mechanism of action, it binds to muscarinic and calcium receptors that can be related to its antispasmodic activity. The clinical trial has shown that pargeverine was an effective drug in the treatment of moderate to severe colic pain of biliary origin. In addition, its efficacy and tolerability were determined in patients with moderate-to-severe acute intestinal colic pain. As a result, no differences in blood pressure or heart rate were found among treatments. The incidence of mouth dryness was significantly more frequent with the 20 mg and 30 mg doses of propinox than with the placebo or the 10 mg dose. Information about the current development of this drug is not available.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Enpiroline (WR 180,409) is an antimalarial compound. It demonstrates activity against Plasmodium falciparum both in vitro and in non-immune infected subjects. Additionally, it exerts antischistosomal activity.
Class (Stereo):
CHEMICAL (ACHIRAL)
Denaverine is a benzilacid derivative. It is a phenobarbital-type microsomal enzyme inducer. Denaverine has a relaxing effect on the prepartum uterus and provides an increased flexibility of the soft birth canal. In addition, it has a surface anaestetic effect and an anticonvulsive effect as well as a slightly tranquilizing and antipyretic effect. In veterinary medicine denaverine hydrochloride is used to regulate myometrial contractions during parturition. It is a regularly used substance in obstetrics in veterinary medicine in many European countries.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Clocinizine is an antihistamine derivative of diphenylmethylpiperazine. Clocinizine is a competitive and reversible H1 receptor antagonist. The drug is marketed in Spain under tradename Senioral in combination with phenylpropanolamine for temporary relief of nasal congestion in colds, rhinitis, and sinusitis.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Quinuclium Bromide Anhydrous is quinuclidinium derivative with potential analgesic activity. In preclinical studies, Quinuclium possessed significant chronic antihypertensive activity in mecamylamine- and renal-hypertensive dogs. Quinuclium was approximately 4 times more potent than guanethidine in the former model and 3 times as potent in the latter. Quinuclium reduced orthostatic blood pressure responses in unanesthetized rabbits but was approximately 10 times less potent than guanethidine. Quinuclium did not affect cardiac output, heart rate or stroke volume in anesthetized open-chest dogs and moderately increased mean blood pressure and total peripheral resistance. It produced diuresis and saluresis in anesthetized dogs but did not influence water or electrolyte urinary excretion in conscious rats. Quinuclium was more effective than guanethidine in blocking adrenergic neurons and depleting heart norepinephrine levels in experimental animals.
Status:
Investigational
Source:
NCT02303262: Phase 2 Interventional Completed Metastatic Leiomyosarcoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Mocetinostat is an rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. It is undergoing clinical trials for treatment of various cancers including bladder cancer, diffuse large B cell lymphoma, follicular lymphoma, myelodysplastic syndromes, non-small cell lung cancer. Fatigue, weight loss or anorexia were most common treatment-related adverse events.
Status:
Investigational
Source:
NCT00232258: Phase 2 Interventional Completed Ulcerative Colitis
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Nolpitantium (SR-140333) is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extravasation in rats. Nolpitantium was found to be effective in the modulation of the inflammatory response and airway remodeling in mice. Nolpitantium is reported to cause antagonism of the SP-induced relaxations of human isolated intralobar pulmonary arterial rings. Nolpitantium also blocked the activation of rat thalamic neurons after nociceptive stimulation. Nolpitantium has been shown to reduce the severity of inflammation in trinitrobenzene sulfonic acid-induced colitis in the rat colon. Nolpitantium inhibited mustard oil-induced plasma protein extravasations in the dorsal skin of the rat hind paw. Nolpitantium had been in some phase II clinical trials but further studies were discontinued.
Status:
Investigational
Source:
NCT02132468: Phase 2 Interventional Completed Neuroendocrine Tumors
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Combretastatin A4 is a vascular disrupting agent (VDA) that targets tumor vasculature to inhibit angiogenesis. Combretastatin A4 is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin and inhibits tubulin assembly. This tubulin-binding agent was originally isolated from an African shrub, Combretum caffrum. Combretastatin A4 is cytotoxic to umbilical-vein endothelial cells (HUVECs) and to a range of cells derived from primary tumors and these cytotoxicity profiles have been used to assess several novel analogs of the drug for future development. Combretastatin A4 has antitumor activity by inhibiting AKT function. The inhibited AKT activation causes decreased cell proliferation, cell cycle arrest, and reduced in vitro migration/invasiveness and in vivo metastatic ability. Several studies in mice have shown that a single administration of combretastatin A4 (100
mg/kg) does not significantly affect primary tumor growth. However, repeated administration (12.5 – 25.0mg/kg twice daily) for periods of 10 – 20 days resulted in approximately 50% retardation of growth of ectopic Lewis lung carcinoma and substantial growth delay of T138 spontaneous murine breast tumors. In clinical studies, Combretastatin A4 has been well tolerated in patients at doses up to 56 mg/m2, following a protocol of five daily 10-minute intravenous infusions every 21 days. The disodium combretastatin A4 phosphate prodrug is currently undergoing clinical trials in the UK and USA.
Status:
Investigational
Source:
NCT00935844: Phase 1 Interventional Completed Advanced Solid Tumors
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Millennium (a wholly-owned subsidiary of Takeda) was developing TAK- 901 for the treatment of cancer. TAK-901 is an inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. TAK-901 is in phase I clinical trials by Millennium Pharmaceuticals for the treatment of advanced hematological malignancies. TAK-901 had been in phase I clinical trials for solid tumors. However, this study was discontinued.
