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Status:
Investigational
Source:
JAN:SPIZOFURONE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Spizofurone (also known as AG-629) is a spirobenzofuranone derivative patented by Japan's largest pharmaceutical company Takeda Chemical Industries, Ltd. as the anti-ulcer agent. In preclinical models Spizofurone dose-dependently increase in gastric mucosal blood flow in anesthetized dogs. The reduction in the gastric mucosal blood flow as induced by indomethacin was markedly improved by spizofurone. The topical action of spizofurone was confirmed in an in situ experiment using a stomach flap fixed to a lucite chamber. Spizofurone given orally or i.p. in a dose range of 25-200 mg/kg inhibited indomethacin-induced gastric antral ulcers in rats. Furthermore, spizofurone potentiated the inhibitory effect of prostaglandin E2 on indomethacin-induced gastric antral ulcers. The increase in alkaline secretion in bullfrog duodenal mucosa seen in the presence of spizofurone is mediated, at least in part, by stimulation of endogenous prostaglandins synthesis.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Spiroplatin is a metal drug and analog of the second generation for cisplatin, developed for the treatment of cancer. Spiroplatin induces DNA cross-linking, thereby inhibiting DNA replication and the synthesis of RNA and protein. Initial clinical trials of spiroplatin have shown that it can cause less nausea and vomiting than cisplatin, and can be administered without hydration due to less renal toxicity. However, with increasing doses, the marginal toxicity was both renal and hematologic. In addition, spiroplatin was devoid of significant antitumor effects in advanced ovarian cancer, a disease in which some response can be expected. Based on these data, further development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Lodiperon exhibited neuroleptic activity with very low liability to the extrapyramidal side effects. Its activity was greater than that of butropipazone and fluanisone, while of the same order of that of chlorpromazine; however, lodiperon showed a longer lasting activity and minor ability to produce catalepsy as compared with the reference drugs.
Status:
Investigational
Source:
NCT00126893: Phase 1 Interventional Terminated Myeloid Leukemia
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
CC-401 is a potent inhibitor of all three forms of c-Jun N-terminal Kinase (JNK) (Ki of 25 to 50 nM) and has at least 40-fold selectivity for JNK compared with other related kinases. Celgene was developing CC 401 for the treatment of cancer and inflammatory disorders. CC 401 was being developed in an IV formulation and was in a phase I trial in patients with refractory acute myelogenous leukaemia. However, trials have ended and the company is not pursuing CC 401, but will advance other JNK inhibitors.
Class (Stereo):
CHEMICAL (ACHIRAL)
Sulfasomizole is a sulfanilamide derivative patented by Chemie Grunenthal G. m. b. H. as an antibiotic with broad-spectrum activity. Sulfasomizole is active against a wide range of gram-positive and gram-negative organisms. Sulfasomizole is well absorbed and distributed in the body, and is readily excreted in the urine.
Class (Stereo):
CHEMICAL (ACHIRAL)
Elfazepam is a benzodiazepine and a feed intake stimulant. Administration of elfazepam can induce animals to eat large meals. While rumen fermentation per se is not influenced by elfazepam, ruminal and abomasal motility and secretory functions are reduced.
Class (Stereo):
CHEMICAL (ACHIRAL)
Elmustine (1-(2-hydroxyethyl)3-(2-chloroethyl)-3-nitrosourea or HECNU) is an alkylating agent with antineoplastic properties. Elmustine is monofunctional and bifunctional alkylating agent that form, in a quantitatively minor reaction, DNA-DNA crosslinks. In vitro, by far the most abundant alkylation products of DNA are those resulting from 2-hydroxyethylation. Elmustine is especially highly active against intracerebrally implanted
tumors. It was in Phase II clinical trials for the treatment of glioma. Elmustine development has been discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Elisartan (HN 65021) is a selective, orally active, nonpeptide angiotensin II (AT1) antagonist. It antagonizes angiotensin receptor-mediated vasoconstriction. Elisartan was being assessed for the treatment of hypertension.
Status:
Investigational
Source:
NCT00275197: Phase 2 Interventional Completed Depressive Disorder, Major
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Elzasonan (CP 448187) is a serotonin 1B/1D receptor antagonist. Elzasonan was primarily metabolized via oxidative N‐demethylation, N‐oxidation, and aryl hydroxylation. Pfizer was developing elzasonan for the treatment of anxiety and affective disorders however development has been discontinued.
Status:
Investigational
Source:
NCT01266174: Phase 2 Interventional Completed Cognitive Impairment
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Eltoprazine, a 5-HT1A/B receptor partial agonist, was created by Duphar in the 1980s (as DU-28853) and was subsequently developed by Solvay to treat pathological aggression. This drug is in clinical development for the treatment of Parkinson's disease levodopa-induced dyskinesia (PD-LID), Alzheimer's aggression and adult attention deficit hyperactivity disorder (adult ADHD). In addition, was shown, that the drug could be useful for normalizing prefrontal cognitive abilities, reducing aggression and impulsivity, and improving cognitive function in schizophrenia.