摘要:
Compounds of formula I are useful for suppressing appetite, for altering macronutrient preferences, for suppressing obsessive-compulsive behavior, and for inhibiting cravings and substance abuse: ##STR1## wherein R.sub.1 and R.sub.3 are each independently H, hydroxy-alkyl, alpha-cyanoalkyl, SO.sub.3 H, SO.sub.2 NH.sub.2, or C(O)R, where R is OH, NH.sub.2, lower alkoxy, benzyloxy, or aliphatic amino acyl;R.sub.2 and R.sub.9 are each independently H, lower alkyl, benzyl, succinyl, or C(O)R.sub.4, where R.sub.4 is H, lower alkyl, hydrocarboxy-lower alkylene, or lower alkoxycarboxy-lower alkylene; andR.sub.5, R.sub.6, R.sub.7, and R.sub.8 are each independently H, halo, lower alkyl, hydroxy, lower alkoxy, or two adjacent radicals form methylenedioxy or ethylenedioxy;with the proviso that R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are not simultaneously H.
摘要:
Disclosed is a method of selecting analgesic agents based on their selective ability to block tetrodotoxin-insensitive sodium channels, particularly in comparison to blocking tetrodotoxin-sensitive sodium channels. Also disclosed is a novel class of compounds that is selective for blocking tetrodotoxin-insensitive sodium channels.
摘要:
The present invention provides a compound of Formula I: (I) and methods for improving memory in a subject by administering a therapeutically effective amount of the compound.
摘要:
A novel class of peptides selectively block class E voltage-gated calcium channels. The class is exemplified by HG peptides such as HG-1, which is isolated from the venom-producing cells of the tarantula Hysterocrates gigas. Also disclosed are methods of producing blocking class E channels using the peptides. HG peptides have utility, for example, in inhibiting oxytocin release and for use as anticonvulsants.
摘要:
The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
摘要:
The present invention relates to the compounds of formula I as well as to their use as PIM kinase inhibitors and, thereby, their use for treating oncological diseases, particularly of the hematopoietic system, the liver and the prostate gland.
摘要:
A novel class of peptides selectively block class E voltage-gated calcium channels. The class is exemplified by HG peptides such as HG-1, which is isolated from the venom-producing cells of the tarantula Hysterocrates gigas. Also disclosed are methods of producing blocking class E channels using the peptides. HG peptides have utility, for example, in inhibiting oxytocin release and for use as anticonvulsants.
摘要:
The present invention provides a compound of Formula (I) and methods for improving memory, inhibiting rho kinase 1 or 2, inhibiting PIM kinase, or inhibiting IRAK1 kinase in a subject by administering a therapeutically effective amount of the compound.
摘要:
The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.