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Restrict the search for
phenyl aminosalicylate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Dacinostat (also known as LAQ824), is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. Dacinostat inhibits histone deacetylase enzymatic activities in vitro and transcriptionally activated the p21 promoter in reporter gene assays. Tumor cells treated with Dacinostat caused acetylation of HSP90 and degradation of its cargo oncoproteins. Flow cytometry studies revealed that both tumor cell lines and normal diploid fibroblasts arrested in the G2/M phase of the cell cycle after Dacinostat treatment. However, an increased sub-G1 population at 48 h (reminiscent of apoptotic cells) was only observed in the cancer cell lines treated with Dacinostat. Dacinostat exhibited antitumor effects in a xenograft animal models. In phase I trials, Dacinostat was well tolerated at doses that induced accumulation of histone acetylation, with higher doses inducing changes consistent with HSP90 inhibition. In another phase 1 in patients with advanced solid tumors, grade 3 or 4 toxicities were observed. Dacinostat had been in phase II clinical trials by Novartis for the treatment of solid tumors but further studies were discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Cinperene is an investigational compound proposed for clinical use as a strong and long-acting peripheral central anticholinergic. In animal models, cinperene inhibited mydriasis, pilocarpine-induced salivation, and lacrimation, scratching, hunching and other symptoms.
Status:
Investigational
Source:
NCT03348527: Phase 2 Interventional Completed Prostate Cancer
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Hydroxyflutamide is the major active metabolite of flutamide. Flutamide undergoes extensive first-pass metabolism by CYP1A2 to its metabolite hydroxyflutamide and its hydrolysis product, 3-trifluoromethyl-4-nitroaniline. Hydroxyflutamide is a more powerful antiandrogen in vivo, with higher affinity for the receptor than that of flutamide. Hydroxyflutamide is in phase II clinical trials for the treatment of prostate cancer. However, a drug resistance problem appears after about one year's treatment. Per-residue free energy decomposition analyses indicate that N705, T877, and M895 androgen receptor mutations are vital residues in the agonist/antagonist mechanism of hydroxyflutamide.
Status:
Investigational
Source:
JAN:CIPROQUAZONE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ciproquazone (SL-573) is a non-steroidal anti-inflammatory drug, a derivative of quinazolinone, discovered by Sumimoto Chemical Co. in the late 1970s. Ciproquazone acts as a reversible inhibitor of prostaglandin synthetase. In animal models, ciproquazone demonstrated antipyretic, analgesic and anti-inflammatory activity. The drug was evaluated in a clinical in acute purulent diseases in the field of orodental surgery.
Status:
Investigational
Source:
INN:pipequaline [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Pipequaline (PK-8165, 2-phenyl-4[2-(4-piperidinyl) ethyl]quinoline) is a benzodiazepine receptor partial agonist.
Status:
Investigational
Source:
NCT03439124: Phase 3 Interventional Completed Community-acquired Pneumonia (CAP)
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Emricasan (IDN- 6556 or PF-03491390) (3-[2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid) is a pan-caspase inhibitor. Testing in vitro enzyme assays demonstrated that emricasan efficiently inhibits all human caspases at low nanomolar concentrations. Preclinically, emricasan was effective in inhibiting apoptosis of sinusoidal endothelial cells. Emricasan has marked efficacy in models of liver disease after oral administration and thus, is an excellent candidate for the treatment of liver diseases characterized by excessive apoptosis. This drug is a first-in-class anti-apoptotic caspase inhibitor with demonstrated preliminary efficacy in liver-impaired patients in humans.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Netobimin is a carbamate compound which is used as an anthelmintic drug in veterinarymedicine. Netobimin-containing products are available as liquid suspensions which are intendedfor oral administration. Products are available for sheep and cattle. An oral dose of 7.5 mg/kg bw is recommended for the treatment of gastrointestinal infestations of roundworms and tapeworms;and 20 mg/kg bw is recommended for type II ostertagiasis and adult flukes. In order to be pharmacologically active, netobimin needs to be converted to the broad spectrumanthelmintic drug albendazole, by the splitting off of a side-chain and the formation of abenzimidazole group. This occurs naturally in the ruminant gut.
Status:
Investigational
Source:
NCT00726648: Phase 1/Phase 2 Interventional Completed Relapsing Multiple Sclerosis
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Zaurategrast (CDP323) is an ethyl ester prodrug of CT7758, a potent carboxylic acid antagonist of integrin alpha4-beta1 (α4β1) or very late antigen 4 (VLA4). CDP323 was under development with UCB and Biogen Idec for the treatment of multiple sclerosis. Its development was discontinued in 2009 based on inadequate interim efficacy data in a phase II clinical trial.
Status:
Investigational
Source:
NCT00763022: Phase 3 Interventional Completed Diabetes Mellitus
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Imiglitazar (also known as TAK-559) is a dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist patented by Japanese pharmaceutical company Takeda Chemical Industries for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance, and impaired glucose tolerance. Imiglitazar shows potent hypoglycemic and hypolipidemic activity and has been studied in clinical trials in treating subjects receiving a stable dose of insulin to control type 2 diabetes mellitus. Unfortunately, Imiglitazar shows hepatotoxicity and has never been marketed.
Status:
Investigational
Source:
NCT00163085: Phase 2 Interventional Completed Parkinson's Disease
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Traxoprodil (CP-101,606) is a potent, selective N-Methyl-D-aspartate (NMDA) receptor (NR2B subunit) antagonist under development by Pfizer for its potential as a neuroprotectant in head injury and neurodegenerative disease. It is in phase II trials in the US and in phase I in Japan for the potential treatment of head injury, such as, Depressive Disorder, Major and Parkinson's Disease. CP-101,606 does not protect against glutamate-induced neurotoxicity in cultured cerebellar neurons, up to a dose of 10 uM. These results are consistent with CP-101,606 being a potent NMDA antagonist, selective for the type of NMDA receptor associated with the hippocampus. Some further investigation revealed that CP-101,606 was associated with a dose-related dissociation and amnesia. These results support the hypothesis that glutamate antagonists may be useful antidyskinetic agents. However, future studies will have to determine if the benefits of dyskinesia suppression can be achieved without adverse cognitive effects.
