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.

Disclosed are an E-configuration benzamide compound and pharmaceutical formulation and application thereof. The E-configuration benzamide compound has a structure represented by formula (I), with the chemical name of N-(2-amino-4-fluorophenyl)-4-[N-[(E)-3-(3-pyridine) acryl] aminomethyl] benzamide, and 3-pyridine acryl in the structural formula having E-configuration. The E-configuration benzamide compound represented by formula (I) has subtype selective histone deacetylated enzyme inhibitory activity, mainly inhibiting HDAC1, HDAC2, HDAC3 in type I HADC and HDAC10 in type IIb HDAC. The E-configuration benzamide compound represented by formula (I) can be used to treat diseases related to abnormal activity of the histone deacetylated enzyme, such as cancer, including lymphoma, solid tumor and blood system tumor and the like.

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.

Opioid receptor compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a condition mediated by an opioid receptor by administering an effective amount of the opioid receptor compound to a patient in need thereof.

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 provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.

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 disorders associated with selective subtype modulation of alpha 2 adrenergic receptors. In particular, the invention provides methods employing well-defined N-[1-(2 and / or 3-substituted-phenyl)-alkyl]-(4,5-dihydro-1H-imidazol-2-yl)-amines and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation, such as ocular disorders, pain and central nervous system (CNS) motor disorders.

The invention relates to a three-dimensional crystal structure model of alpha1-AR subtype protein and an establishment method thereof. The establishment method comprises the following steps of searching a protein crystal database with an amino acid sequence of the alpha1-AR subtype protein as a probe and obtaining a homologous template beta2-AR with the highest similarity through comparison with the amino acid sequence; utilizing a Prime module of (formula) to carry out homology modeling on the alpha1-AR subtype protein; and adopting an Macromodel module to optimize protein obtained by homology modeling and obtaining the three-dimensional crystal structure model of the alpha1-AR subtype protein through model evaluation. The invention provides model conformations of three alpha1-AR subtype proteins, namely alpha1A-AR, alpha1B-AR and alpha1D-AR and provides the basis for accurately researching structure-function relationship between a target spot and an antagonist; a possible binding packet is modelled, a key residue is found, and the theoretical basis is provided for explaining the selectivity of an alpha1-AR subtype selective antagonist.

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.