39 results about "Subtype selective" patented technology

A compound having selective modulating activity at the alpha 2B and or alpha 2C adrenergic receptor subtypes is represented by the general Formula (1): wherein R1-R6 is independently selected from the group consisting of H, C1-6 alkyl, halogen, CH2OH, CH2N(R7)2) CH2CN, C(O)R8, CF3, and aryl; wherein R7 is H or C1-6 alkyl; and R8 is H, C1-6 alkyl or aryl. The compounds of Formula (1) can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.

The present invention provides a compound of the formula:or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Y, Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

The invention discloses an E-configuration benzamide compound and a medicinal preparation thereof and an application thereof. The E-configuration benzamide compound has a structure shown as a formula (I), a chemical name is N-(2-amino-4-fluorophenyl)-4-[N-[(E)-3-(3-pyridine)acryloyl]aminomethyl]benzamide, in the structural formula, the configuration of 3-pyridinyl acryl is E configuration. The E-configuration benzamide compound has subtype selective histone deacetylase inhibition activity, which mainly inhibits HDAC1, HDAC2, and HDAC 3 in an I type of HDAC as well as HDAC10 in a IIb type of HDAC. The E-configuration benzamide compound shown in the formula (I) can be used for treating the disease related to histone deacetylase activity abnormity, such as cancer comprising lymphoma, solid tumor and blood hematological malignancy.

The invention specifically discloses a 1 ‑High-throughput screening cell model of AR subtype-selective antagonists and its construction method and application. The construction method is to use α 1 ‑AR three subtypes (α 1A ,α 1B ,α 1D ) eukaryotic expression plasmid, reporter gene and internal reference plasmid were co-transfected into host cells, and a transient cell model was established. Antagonists and agonists to be screened were added to the cell model successively. After a period of co-culture, the cells were lysed and the lysates were processed. Assay of luciferase activity, determine the relative expression of reporter gene and internal control, so as to evaluate the effect of the drug on α 1 ‑AR three subtypes: α 1A 、α 1B and alpha 1D inhibitory activity. This method passes model stability, volatility inspection and model verification. available for alpha 1 ‑High-throughput screening of AR subtype-selective antagonists can be further used to screen potential drugs for the treatment of benign prostatic hyperplasia.

This invention relates to a method for modulating α2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to novel heteocyclic compounds and pharmaceutical compositions containing said compounds. In addition the invention relates to the treatment of depression, an anxiety disorder, a psychiatric disorder, a learning or cognitive disorder, a sleep disorder, a convulsive or seizure disorder or pain

The invention provides methods for treating pain in mammals. In particular, the invention provides well-defined aminoimidazolines, aminothiazolines, and aminooxazo lines and pharmaceutical compositions thereof to treat pain.