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

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Showing 6931 - 6940 of 7691 results

Status:
Investigational
Source:
INN:guamecycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Guamecycline, a tetracycline derivative was studied in patients with broncho-pulmonary diseases and for the treatment of acute pneumopathies. However, information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT00447187: Phase 3 Interventional Terminated Corneal Diseases
(2007)
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Status:
Investigational
Source:
NCT01589432: Phase 2 Interventional Completed Diabetic Neuropathic Pain
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


ABT-639 is a T-type calcium (Cav3.2) channel antagonist that was in development with AbbVie for the treatment for pain. ABT-639 is a potent and selective T-type calcium channel blocker. ABT-639 effectively reduces nociceptive and neuropathic pain in rats. ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 uM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 uM). ABT-639 was significantly less active at other Ca²⁺ channels (e.g. Ca(v)1.2 and Ca(v)2.2) (IC₅₀ > 30 uM). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents.
Status:
Investigational
Source:
NCT03025308: Phase 3 Interventional Active, not recruiting Rheumatoid Arthritis
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.
Status:
Investigational
Source:
NCT03025308: Phase 3 Interventional Active, not recruiting Rheumatoid Arthritis
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.
Status:
Investigational
Source:
NCT03863574: Phase 2 Interventional Completed Non Alcoholic Steatohepatitis
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Saroglitazar, a dual peroxisome proliferator-activated receptor PPAR-α/γ agonist, was an emerging therapeutic option on glycemic and lipid parameters. The Zydus Group has launched LipaglynTM ((Saroglitazar) in India for diabetic dyslipidemia and hypertriglyceridemia with type 2 diabetes mellitus not controlled by statin therapy. In addition, saroglitazar participated in phase II clinical trials that completed enrolment in patients with primary biliary cholangitis and in patients with non-alcoholic steatohepatitis.
Status:
Investigational
Source:
NCT03563599: Phase 2 Interventional Completed Treatment-naïve, Sputum Smear-positive Patients With Drug-sensitive Pulmonary TB
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Q203 (6-chloro-2-ethyl-N-(4-(4-(4-(trifluoromethoxy)phenyl)piperidin-1-yl)benzyl)imidazo [1,2-a]pyridine-3-carboxamide) is an an imidazopyridine antitubercular compound. Q203 targets the cytochrome b subunit (QcrB) of the cytochrome bc1 complex. This complex is an essential component of the respiratory electron transport chain of ATP synthesis. Q203 inhibited the growth of multidrug-resistant (MDR) and extensively drug-resistant (XDR) M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight, which highlights the potency of this compound. In addition, Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Q203 is a promising new clinical candidate for the treatment of tuberculosis.
Status:
Investigational
Source:
INN:pentopril
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pentopril (CGS 13945) is a member of a series of l-glutarylindoline-2(S)-carboxylic acid derivatives. Pentopril was evaluated as an inhibitor of a cell-free preparation of angiotensin-converting enzyme (ACE) isolated from rabbit lung. Intravenous administration of incremental doses of pentopril to anesthetized normotensive rats produced a dose-related inhibition of angiotensin I (AI) pressor responses. The onset of inhibition of the A1 pressor response was rapid, and substantial inhibition occurred at 5 min after administration of the ACE inhibitors. Pentopril hydrolyzed in vivo to the biologically active free-acid form of CGS 13934. It was well tolerated in normal volunteers and hypertensive patients. Pentopril was developed for the treatment of both hypertension and congestive heart failure. Pentopril produced little clinical improvement and no biochemical improvement in a patients with rheumatoid arthritis.
Status:
Investigational
Source:
NCT00195325: Phase 1 Interventional Terminated Tumors
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.
Status:
Investigational
Source:
INN:oxmetidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxmetidine is an H2-receptor antagonist that was studied as a gastrointestinal agent. Oxmetidine possesses efficacy in the treatment of peptic ulcers. However, information about the further development of this drug is not available.

Showing 6931 - 6940 of 7691 results