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Cupric Formate (Copper(II) formate) is an inorganic salt derived from formic acid. It is used as antibacterial agent in the treatment of cellulose. Effective fungicide.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Y-33075 is potent and selective ROCK (Rho-associated coiled-coil-forming protein kinase) inhibitor, developed by Yoshitomi Pharmaceutical Industries for encephalomyelitis treatment. In rabbits and in monkeys, Y-33075 lowers IOP in a dose-dependent fashion. An increase in regenerating axons of RGCs in 100 mM Y-33075-treated eyes is observed compared with saline-treated eyes. Y-33075 dose-dependently increases the number of RGCs with regenerating axons. Both Y-33075 induces a concentration-dependent relaxation in rabbit ciliary arteries precontracted with a high-potassium (high-K) solution. The amplitude of relaxation induced by Y-33075 is not affected by either 100 μM N (G)-nitro-L: -arginine methyl ester (L: -NAME) or 10 μM indomethacin. In Ca2 -free solution, Y-27632 and Y-39983 significantly inhibit the transient contraction of ciliary arteries induced by 10 μM histamine. However, neither Y-27632 nor Y-39983 affects the elevation of [Ca2 ](i) induced by high-K solution and histamine.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
FK-960 [N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate], a novel putative anti-dementia drug of piperazine derivative, ameliorates memory deficits in a variety of animal models of dementia in rats and monkeys, and also augments long-term potentiation (LTP) in the mossy fiber-CA3 pathway in guinea-pig hippocampal slices. FK-960 acts as Serotonin modulator. FK-960 had been in phase II clinical trials by Fujisawa Pharmaceutical (now Astellas) for the treatment of Alzheimer's disease (AD). However this study was suspended. In 2003 Phase-II for Alzheimer's disease in USA was discontinued and in Jul 2004 - Phase-II for Cognition disorders in Europe.
A thiomalic acid or mercaptosuccinic acid is a dicarboxylic acid containing a thiol functional group. Mercaptosuccinic acid is used in the preparation of mercaptosuccinic acid diethyl ester by reaction with ethanol. It is also used as a brightening agent in metal plating. Further, it serves as an intermediate for the synthesis of corrosion inhibitors, soil fumigants, active pharmaceutical ingredients and electroplating agents. Mercaptosuccinic acid is widely used in the synthesis of various biologically active sulfur containing compounds such as the antileukemic spiro[indoline-3,2'-thiazolidine]-2,4'-diones, and the antimicrobial and antitubercular 4-thiazolidinones. It is also used as a building block in the synthesis of novel polyanionic inhibitors of human immunodeficiency virus and other viruses, and as a starting material in the synthesis of isocysteine, an important non-proteinogenic amino acid in a potent peptide inhibitor of stromelysin. In addition, sodium salt of the anionic Au(I) complex of 2-mercaptosuccinic acid is an effective antiarthritic drug.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
The investigational psychopharmacologic drug candidate CP 615003 (NGD 91-3) is a potent subtype-selective partial agonist at the GABA-A receptor complex. It was designed to be fast acting without causing the sedation, memory impairment, addiction or potentiation of effects of alcohol associated with conventional anti-anxiety medication. Tissue distribution studies conducted during early clinical development of CP 615003 suggested limited brain penetration. In the Phase II clinical study, subjects tested at the high dose of NGD 91-3 showed a trend toward efficacy that did not achieve statistical significance.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
SB-743921 is a synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits the ATP-binding domain of the kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis. SB-743921 has greater than 40,000 fold selectivity for KSP over other kinesins. SB-743921 has demonstrated promising anti-cancer activity in a variety of in vivo and in vitro human cancer models in preclinical studies. Furthermore, anti-cancer effect has been demonstrated in taxane-refractory malignancies with SB-743921. Toxicity studies demonstrated predictable neutropenias and gastrointestinal toxicities without clear evidence of neurotoxicity. The recommended phase II dose for SB-743921 as a 1-h infusion every 21 days is 4 mg/m2.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
The selective serotonin reuptake inhibitor fluoxetine consists of equal amounts of R and S stereoisomers (antidepressant Prozac (racemic fluoxetine). Binding to the transporter confirmed selectivity of R- and S-fluoxetine for the 5-HT transporter versus the dopamine (DA) and norepinephrine (NE) human transporters. In addition, receptor binding studies demonstrated significant affinity of R-fluoxetine, but not S-fluoxetine, for human 5-HT(2A) and 5-HT(2C) receptor subtypes. R-fluoxetine acts as an antagonist at 5-HT(2A) and 5-HT(2C) receptors. The attempt to develop a single-enantiomer formulation of fluoxetine for the treatment of depression was unsuccessful. Eli Lilly has terminated its licensing and development agreement with Marlborough, Mass.-based Sepracor for (R)-fluoxetine, the single-isomer version of Lilly's antidepressant Prozac.R-enantiomer of fluoxetine, at its highest administered dose, led to statistically significant prolongation of cardiac repolarization in phase II studies; the studies were subsequently stopped.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
PNU-142633 is selective 5HT1D partial agonist, developed by Pharmacia & Upjohn, Inc. It failed in phase II clinical trials against acute migraine, and its development was discontinued.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
