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Restrict the search for
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Aglepristone (RU 46534) is a competitive progesterone antagonist; it binds to progesterone receptors (PRs) without inducing the molecular cascade associated with progesterone. Its affinity to PRs is higher than progesterone (3.12, 3.8, and 9.26 times greater in the bitch, doe rabbit,and queen, respectively). Aglepristone can therefore beused in various progesterone-dependent physiological orpathologic conditions, with the aim of blocking the action of progesterone. Aglepristone has proven to be an effective and safe means of inducing pregnancy termination or parturition in a large number of domestic species. In domestic species, aglepristone is routinely used for the treatment of pyometra and feline mammary fibroadenomatous hyperplasia, both of which are progesterone dependent. Aglepristone is marketed under the brand name Alizin used as the treatment option for unwanted mating and pregnancy in dogs
Class (Stereo):
CHEMICAL (ABSOLUTE)
ISOPROPICILLIN is semisynthetic penicillin.
Status:
Investigational
Source:
NCT01532518: Phase 2 Interventional Completed Colic
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Menarini was developing oral nepadutant (MEN 11420), a potent and selective tachykinin neurokinin-2 receptor antagonist, for the treatment of infant colic. Nepadutant has been used in trials studying the treatment of colic, infantile colic, and infantile functional gastrointestinal disorders. MEN 11420 is a glycosylated derivative of the potent, selective, conformationally-constrained tachykinin NK2 receptor antagonist MEN 10627. MEN 11420 competitively bound with high affinity to the human NK2 receptor stably transfected in CHO cells, displacing radiolabelled [125I]-neurokinin A and [3H]-SR 48968 with Ki values of 2.5+/-0.7 nM (n = 6) and 2.6+/-0.4 nM (n = 3), respectively.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Benorterone (or SKF 7690), a steroidal antiandrogen that was studied in the treatment of acne, seborrhea, and hirsutism in women but was never marketed.
Status:
Investigational
Source:
JAN:THIOINOSINE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
THIOINOSINE (Methylmercaptopurine riboside, NSC- 40774) is a purine derivative with antineoplastic and anti-angiogenic properties. THIOINOSINE is readily converted in cells to its active form, 6-methylmercaptopurine ribonucleoside 5'- monophosphate (MMPR-P), by the enzyme adenosine kinase. THIOINOSINE inhibits amidophosphoribosyltransferase, the first committed step in de novo purine synthesis, and inhibits fibroblast growth factor-2 (FGF2)-induced cell proliferation. It has been used similarly to Mercaptopurine in the treatment of Leukemia. It has being tested in clinical trials for advanced pancreatic cancer.
Class (Stereo):
CHEMICAL (MIXED)
Viprostol (also known as CL115,347), a prostaglandin E2 congener that was studied as an antihypertensive agent. Viprostol has a potent and prolonged blood pressure lowering effect in many models of hypertension. In clinical studies, viprostol has been demonstrated to lower arterial blood pressure significantly in man following transdermal and/or intravenous administration. The antihypertensive action of viprostol has been suggested to be the result of peripheral vasodilatation. In addition, the drug participated in a clinical trial in normal subjects and in patients with Raynaud's phenomenon. It was found the optimal dosage was 1000 ug; the effect could last for 84 hours; higher dosage may be associated with a "steal" phenomenon.
Status:
Investigational
Source:
NCT01313572: Phase 3 Interventional Terminated Coronary Artery Disease
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Apadenoson (BMS-068645) is a selective adenosine 2A agonist that contains a methyl ester group which undergoes esterase hydrolysis to its acid metabolite. Apadenoson had been in phase III clinical trials by Forest (now a part of Allergan) for the treatment of coronary artery disease. However, this study has been terminated.
Status:
Investigational
Source:
INN:piridicillin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Piridicillin is the semi-synthetic penicillin. It has exhibited broad-spectrum activity in vitro against gram-positive cocci, except penicillin G-resistant Staphylococcus aureus, and against gram-negative bacilli. Piridicillin is reported to be more active in-vitro than piperacillin, azlocillin or ticarcillin against Ps. aeruginosa. It is unstable at alkaline pH and displays marked inoculum independence.
Class (Stereo):
CHEMICAL (ABSOLUTE)
ROTAMICILLIN was developed as an antibiotic that has never been marketed.
Status:
Investigational
Source:
NCT03019185: Phase 2/Phase 3 Interventional Completed Alport Syndrome
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Bardoxolone methyl, the C-28 methyl ester of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid (CDDO) known as CDDO-Me or RTA 402, is one of the derivatives of synthetic triterpenoids. Bardoxolone methyl directly blocks IKKbeta activity and thereby the NF-kappaB pathway by interacting with Cys-179 in the IKKbeta activation loop. Binding of bardoxolone methyl to Kelch-like erythroid cell-derived protein with CNC homology-associated protein 1 (Keap1) disrupts its critical cysteine residues, leading to the release of the nuclear factor erythroid 2-related factor 2 (Nrf2), which hinders its ubiquitination and finally leads to its stabilization and nuclear translocation. In the nucleus, Nrf2 activates the transcription of phase 2 response genes, leading to a coordinated antioxidant and anti-inflammatory response. In addition, it acts as an antagonist of the peroxisome proliferator-activated receptor gamma. Through Keap1/Nrf2 and nuclear factor-κB pathways, this agent can modulate the activities of a number of important proteins that regulate inflammation, redox balance, cell proliferation and programmed cell death. This agent is generally well tolerated, but it may increase adverse cardiovascular events. Presently, it is being further tested for the treatment of patients with chronic kidney disease, cancer, and pulmonary arterial hypertension.