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Restrict the search for
m sacubitril
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Ioglucomide is triiodoanilide derivative patented by Mallinckrodt, Inc. as nonionic x-ray contrast media for myelography. In preclinical studies the efficacy of ioglucomide and metrizamide were comparable. However, acute toxicity after intravenous injection or installation into cerebrospinal fluid was significantly less for ioglucomide. Also, in contrast to metrizamide, ioglucomide produced no evidence of any type of convulsive activity after subarachnoid administration.
Class (Stereo):
CHEMICAL (RACEMIC)
FLUDOREX is an antiemetic and anorexic agent.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rifamides (NSC-143418) are drugs used in the treatment of tuberculosis. They also have immunosuppressive activity, the exact mechanism of which is still unknown, although the ability of rifamides to inhibit tumor necrosis factor (TNF)-induced NF-kB activation may be associated with it. A variety of rifamide analogues exist, such as rifamycin B, rifapentine, rifamycin SV, rifabutin and rifampicin.
Status:
Investigational
Source:
NCT00033722: Phase 2 Interventional Unknown status Lung Cancer
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Lometrexol, formerly known as DDATHF; LY 264618; T-64 was the first glycinamide ribonucleotide formyl transferase (GARFT) inhibitor to be investigated clinically. Lometrexol had been in phase II clinical trial for the treatment non-small cell lung cancer (NSCLC). However, the studies have been discontinued by Tularik Inc, because Company had suggested, that drug would face competition from other companies in the indication
Status:
Investigational
Source:
NCT02272478: Phase 2/Phase 3 Interventional Unknown status Acute Myeloid Leukaemia
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Ganetespib (formerly called STA-9090) is a novel, injectable resorcinolic triazolone small molecule inhibitor of Hsp90, developed by Synta Pharmaceuticals. Ganetespib inhibits the growth of many tumor types in vitro and in vivo including AML, ALL, CML, NHL, neuroblastoma, Ewing sarcoma, rhabdoid cancer, rhabdomyosarcoma, melanoma, and carcinomas of the breast, lung, prostate, bladder and colon7-10,14-27. Ganetespib has being studied in multiple adult oncology indications. The 50% inhibitory concentrations (IC50) for Ganetespib against malignant mast cell lines are 10-50 times lower than that for 17-AAG, indicating that triazolone class of HSP90 inhibitors likely exhibits greater potency than geldanamycin based inhibitors. Ganetespib inhibits MG63 cell lines with IC50 of 43 nM. Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and serves as a potent Hsp90 inhibitor by causing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 and c-Met as well as Wilms' tumor 1. Ganetespib, at low nanomolar concentrations, potently arrests cell proliferation and induces apoptosis in a wide variety of human cancer cell lines, including many receptor tyrosine kinase inhibitor- and tanespimycin-resistant cell lines. Ganetespib exhibits potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those that express mutated kinases that confer resistance to small-molecule tyrosine kinase inhibitors. Ganetespib has been studied in 5 completed Synta-sponsored clinical trials (Studies 9090-02, 9090-03, 9090-04, 9090-05, and 9090-07) and 3 completed Synta-sponsored studies in normal healthy volunteers (9090-12, 9090-13, and 9090-15). Ganetespib is currently being studied in 6 Synta-sponsored clinical trials. Studies include: one Phase 1 study, three Phase 2 studies, one Phase 2b study, and one Phase 3 study. Ganetespib is also being studied in 24 Investigator Sponsored Trials (ISTs)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Quinpirole (LY 171,555) is a psychoactive drug and research chemical which acts as a selective D2 and D3 receptor agonist. Quinpirole is the most widely used D2 agonist in in vivo and in vitro studies. Specific quinpirole binding in rat brain was saturable, and dependent on temperature, membrane concentration, sodium concentration and guanine nucleotides. Saturation analysis revealed high affinity binding characteristics (KD = 2.3 nM) which were confirmed by association-dissociation kinetics. The regional distribution of [3H]quinpirole binding sites roughly paralleled the distribution of [3H]spiperone binding sites, with greatest densities present in the striatum, nucleus accumbens and olfactory tubercles. A variety of drugs, most notably monoamine oxidase inhibitors (MAOls), inhibit the binding of [3H]quinpirole, but not [3H]spiperone or [3H](-)N-n-Propylnorapomorphine, in rat striatal membranes by a mechanism that does not appear to involve the enzymatic activity of MAO. Clinically antidepressant MAOIs exhibited selectivity between sites labeled by [3H]quinpirole and [3H]spiperone as did a number of structurally related propargylamines and N-acylethylenediamine derivatives and other drugs such as debrisoquin and phenylbiguanide. Quinpirole has been shown to increase locomotion and sniffing behavior in mice and induces compulsive behavior symptomatic of obsessive compulsive disorder in rats.
Class (Stereo):
CHEMICAL (MIXED)
Odalprofen was used as an analgesic. Information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT02764385: Not Applicable Interventional Completed Smoking
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01051635: Phase 1 Interventional Completed Neoplasms
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Indimitecan, also known as LMP776, is a novel topoisomerase I inhibitor. A substance being studied in the treatment of cancer. It blocks certain enzymes that break and rejoin DNA strands. These enzymes are needed for cells to divide and grow. Blocking them may cause cancer cells to die. Indimitecan (LMP776) also helps anticancer drugs kill cancers that are resistant to some other drugs. LMP776 is a type of indenoisoquinoline and a type of topoisomerase inhibitor. In vitro, LMP776 induces TOP 1 cleavage at unique
genomic positions and causes cell cycle arrest in both S and G (2)-M phases. Protein linked DNA breaks were observed in cells treated with nanomolar concentrations of LMP776.
Status:
Investigational
Source:
INN:clonitazene [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Clonitazene is a synthetic opioid analgesic, structurally related to etonitazene. In the USA clonitazene is a schedule I narcotic controlled substance.