摘要:
Disclosed are compounds of the formula: wherein: A, B, C, E, F, and G are substituents as defined herein, which compounds bind to the benzodiazepine site of GABAA receptors and are therefore useful in treatment of central nervous system (CNS) diseases.
摘要:
Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, A, B, C, D and W are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.
摘要:
Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein n, R1, R2, R3, W, Q, and X are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.
摘要:
In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
摘要:
A surgical clip applier is provided including a housing; at least one handle pivotably connected to the housing; a channel assembly extending distally from the housing; a plurality of clips loaded in the clip carrier; a drive channel translatably supported in the housing and the channel assembly, the drive channel being translated upon actuation of the at least one handle; and a counter mechanism supported in the housing, the counter mechanism including indicia visible through the housing, wherein the indicia corresponds to a quantity of clips loaded in the clip applier, wherein the indicia decrements upon each firing of the clip applier resulting in a reduction in the quantity of clips remaining of the plurality of clips.
摘要:
Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.
摘要:
Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要:
In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
摘要:
This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
摘要:
Methods are provided that are useful in assaying compounds for cognitive enhancing properties, anxiolytic properties, hypnotic properties, or antidepressant properties. These methods involve determining the in vitro efficacy and EC50 of the compounds at defined series of cloned GABAA subtype receptors composed of specific variants of α, β, and γ subunits in order to develop and an activity profile for each compound. Optionally, the binding affinities of the compounds at GABAA receptors are also determined. As an additional step the in vivo effects of the compounds may be tested in animal models.
摘要翻译:提供了可用于测定化合物的认知增强性质,抗焦虑性质,催眠性质或抗抑郁药性质的方法。 这些方法包括确定在由α,β和γ亚基的特异性变体组成的限定的克隆的GABA亚型亚型受体系列中的化合物的体外功效和EC 50 为每个化合物开发和活动资料。 任选地,还测定了化合物在GABA A A受体上的结合亲和力。 作为附加步骤,可以在动物模型中测试化合物的体内作用。