Patent classifications
A61K31/24
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Anat Inhibitors and Methods of Use Thereof
Inhibitors of a critical brain enzyme, N-acetyltransferase (ANAT), and methods of discovering, making and using the same for the treatment of disease are disclosed.
ANTI-INFECTIVE AND ANTI-VIRAL COMPOUNDS AND COMPOSITIONS
Lysosomally accumulated substances that release a nitroxy group, or a short chain fatty acid or a product of anaerobic metabolism or a thiol or a sulfide often from an ester or similar labile linkage have anti-inflammatory, anti-cancer and anti-bacterial activity. They are useful in treating infectious, inflammatory and malignant disease and are immune stimulatory, promote zinc uptake, disable endosomal reactions and synergise anti-viral action of protease inhibitors. The compounds are useful for the treatment of bacterial, viral and mixed pneumonias.
ANTI-INFECTIVE AND ANTI-VIRAL COMPOUNDS AND COMPOSITIONS
Lysosomally accumulated substances that release a nitroxy group, or a short chain fatty acid or a product of anaerobic metabolism or a thiol or a sulfide often from an ester or similar labile linkage have anti-inflammatory, anti-cancer and anti-bacterial activity. They are useful in treating infectious, inflammatory and malignant disease and are immune stimulatory, promote zinc uptake, disable endosomal reactions and synergise anti-viral action of protease inhibitors. The compounds are useful for the treatment of bacterial, viral and mixed pneumonias.
Biologically active cannabidiol analogs
Biologically active cannabidiol analogs comprising a compound of the formula ##STR00001##
wherein one of R.sub.1 or R.sub.2 or both is/are the residue of a moiety formed by the reaction of an amino group of the amino acid ester of R.sub.1 or R.sub.2 or both with a dicarboxylic acid or a dicarboxylic acid derivative and the other R.sub.1 or R.sub.2 (in the case of the mono) is the residue of a dicarboxylic acid or dicarboxylic acid derivative or Hydrogen (H), (i.e. underivatized), and salts thereof. These CBD analogs are be useful in pain management in oncology and other clinical settings in which neuropathy is presented. Furthermore, these CBD-analogs are useful in blocking the addictive properties of opiates.
Biologically active cannabidiol analogs
Biologically active cannabidiol analogs comprising a compound of the formula ##STR00001##
wherein one of R.sub.1 or R.sub.2 or both is/are the residue of a moiety formed by the reaction of an amino group of the amino acid ester of R.sub.1 or R.sub.2 or both with a dicarboxylic acid or a dicarboxylic acid derivative and the other R.sub.1 or R.sub.2 (in the case of the mono) is the residue of a dicarboxylic acid or dicarboxylic acid derivative or Hydrogen (H), (i.e. underivatized), and salts thereof. These CBD analogs are be useful in pain management in oncology and other clinical settings in which neuropathy is presented. Furthermore, these CBD-analogs are useful in blocking the addictive properties of opiates.
COMPOSITION AND METHODS FOR THE TREATMENT OF MYOPIA
Compositions and methods useful in slowing, inhibiting, or regressing the progression of myopia, while minimizing pupil dilation and light sensitivity are provided herein. Provided compositions can include a muscarinic receptor antagonist and a miotic agent.
COMPOSITION AND METHODS FOR THE TREATMENT OF MYOPIA
Compositions and methods useful in slowing, inhibiting, or regressing the progression of myopia, while minimizing pupil dilation and light sensitivity are provided herein. Provided compositions can include a muscarinic receptor antagonist and a miotic agent.
METHOD FOR IMPROVING THE STABILITY OF A PHARMACEUTICAL COMPOSITION COMPRISING A HIGH PENETRATION DRUG, AND THE PHARMACEUTICAL COMPOSITION OBTAINED THEREFROM
Provided are pharmaceutical compositions comprising at least one high penetration drug (HPD) that has at least one protonated amino group in its molecular and is capable of penetrating across one or more biological barriers in high rates, methods for improving the stability of the pharmaceutical compositions, and methods of using the pharmaceutical compositions for preventing, diagnosing and/or treating condition or disease in human, animals and plants.