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

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Showing 831 - 840 of 14117 results

Status:
Investigational
Source:
INN:meglucycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Meglucycline is an antibiotic.
Status:
Investigational
Source:
INN:tiprenolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tiprenolol (DU21445) has been shown by both in vitro and in vivo animal experiments, to possess strong beta-adrenergic blocking but a relatively less strong negative inotropic activity. The same report also demonstrated by its inhibiting influence on spontaneous mobility of rat uterus, an intrinsic beta-sympathomimetic activity. Tiprenolol reveals effects similar to propranolol. Tiprenolol was shown to have significantly less heart rate slowing effect at rest than propranolol. However, all other measurements failed to show any difference of statistical significance between the two drugs with respect to any negative inotropic or beta‐blocking activity. The administration of tiprenolol or propranolol depressed the arterial pressure and caused the deaths of some dogs in which a coronary artery had been ligated.
Status:
Investigational
Source:
INN:tigemonam
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.
Status:
Investigational
Source:
Skin Pharmacol Appl Skin Physiol. 2003;16(4):263-70.: Not Applicable Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:cefetecol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefetecol is a broad-spectrum cephemcarboxylate derivative with antibacterial activity patented by British pharmaceutical company Glaxo Group Ltd.
Status:
Investigational
Source:
NCT01929044: Phase 3 Interventional Completed Intestinal Diseases
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Anisodamine is a naturally occurring atropine derivative that has been isolated, synthesized and characterized by scientists in the People's Republic of China. Anisodamine is a non-specific cholinergic antagonist. Anisodamine has been shown to interact with and disrupt liposome structure which may reflect its effects on cellular membranes. Experimental evidence implicates anisodamine as an anti-oxidant that may protect against free radical-induced cellular damage. Its cardiovascular properties include depression of cardiac conduction and the ability to protect against arrhythmia induced by various agents. Anisodamine is a relatively weak alpha(1) adrenergic antagonist which may explain its vasodilating activity. Its anti-thrombotic activity may be a result of inhibition of thromboxane synthesis. Numerous therapeutic uses of anisodamine have been proposed including treatment of septic shock, various circulatory disorders, organophosphorus (OP) poisoning, migraine, gastric ulcers, gastrointestinal colic, acute glomerular nephritis, eclampsia, respiratory diseases, rheumatoid arthritis, obstructive jaundice, opiate addiction, snake bite and radiation damage protection. The primary therapeutic use of anisodamine has been for the treatment of septic shock. Several mechanisms have been proposed to explain its beneficial effect though most mechanisms are based upon the assumption that anisodamine ultimately acts by an improvement of blood flow in the microcirculation. Preliminary studies suggest another important therapeutic use of anisodamine is for the treatment of OP poisoning. Anisodamine has been employed therapeutically since 1965 in the People’s Republic of China primarily to improve blood flow in circulatory disorders such as septic shock, disseminated intravascular coagulation (DIC) and as an antidote to organophosphate poisoning.
Status:
Investigational
Source:
NCT00262990: Phase 3 Interventional Completed Ovarian Cancer
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Patupilone is a compound isolated from the myxobacterium Sorangium cellulosum. Similar to paclitaxel, Patupilone induces microtubule polymerization and stabilizes microtubules against depolymerization conditions. In addition to promoting tubulin polymerization and stabilization of microtubules, this agent is cytotoxic for cells overexpressing P-glycoprotein, a characteristic that distinguishes it from the taxanes. Epothilone B may cause complete cell-cycle arrest. Patupilone failed a phase III trial for ovarian cancer in 2010.
Status:
Investigational
Source:
INN:mideplanin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mideplanin (MDL 62873), a teicoplanin amide derivative, was studied as an antibacterial agent against Gram-positive bacteria. However, further, development appears to have been discontinued.
Status:
Investigational
Source:
NCT01235520: Phase 3 Interventional Completed Schizophrenia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Bitopertin is a Glycine transporter type 1 inhibitor which was developed by Hoffmann-La Roche for the treatment of patients with schizophrenia. The drug was shown to be potent in vitro, however it failed to meet primary endpoints in phase III. Bitopertin was also tested for the treatment of obsessive-compulsive disorder, but the development stopped in phase II.
Status:
Investigational
Source:
NCT01874756: Phase 2 Interventional Terminated Schizophrenia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Synthetic compound Erteberel (LY500307) is a highly potent and selective ERβ agonist; it has a 12-fold higher affinity for ERβ than ERα and exhibits 32-fold more functional potency. LY500307 was well tolerated in benign prostatic hypertrophy (BPH) patients with no side effects and it is currently being tested in phase 2 clinical trials for improving negative symptoms and cognitive impairment associated with Schizophrenia. In BPH clinical trial incidence of adverse events was comparable between treatment groups, and no clinically meaningful changes in laboratory tests were observed.