A61K31/4409

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.

AGENT FOR PROMOTING CORNEAL ENDOTHELIAL CELL ADHESION

The invention provides an agent for promoting adhesion of a corneal endothelial cell, containing a Rho kinase inhibitor, as well as a culture medium for a corneal endothelial cell, a solution for preservation of cornea, and a method of producing a corneal endothelial preparation, which includes culturing the corneal endothelial cell using the aforementioned culture medium.

4-AMINOPYRIDINE (4-AP) AND BONE MORPHOGENETIC PROTEIN 2 (BMP-2)

This document relates to methods and materials for using 4-aminopyridine (4-AP) and/or one or more derivatives of 4-AP. For example, a composition containing 4-AP and/or one or more derivatives of 4-AP can be administered (e.g., orally administered) to a mammal to increase a level of bone morphogenetic protein 2 (BMP-2) polypeptides within the mammal. For example, a composition containing 4-AP and/or one or more derivatives of 4-AP can be administered (e.g., orally administered) to a mammal having bone loss to increase the level of BMP-2 within the mammal, thereby treating the mammal's bone loss.

4-AMINOPYRIDINE (4-AP) AND BONE MORPHOGENETIC PROTEIN 2 (BMP-2)

This document relates to methods and materials for using 4-aminopyridine (4-AP) and/or one or more derivatives of 4-AP. For example, a composition containing 4-AP and/or one or more derivatives of 4-AP can be administered (e.g., orally administered) to a mammal to increase a level of bone morphogenetic protein 2 (BMP-2) polypeptides within the mammal. For example, a composition containing 4-AP and/or one or more derivatives of 4-AP can be administered (e.g., orally administered) to a mammal having bone loss to increase the level of BMP-2 within the mammal, thereby treating the mammal's bone loss.

Antifungal agents with enhanced activity in acidic pH
11534433 · 2022-12-27 · ·

Enfumafungin derivative triterpenoid antifungal compounds are used to treat or prevent fungal infections occurring in or under acidic conditions where the pH is lower than about 7, due to their unexpected, enhanced efficacy under such conditions. The enfumafungin derivative triterpenoids (or pharmaceutically acceptable salts or hydrates thereof) are inhibitors of (1,3)-β-D-glucan synthesis and are useful in the treatment or prevention of yeast or mold infections that occur in anatomic areas having a low pH, such as the vaginal cavity, or under acidic local environment conditions such of those seen in fungal abscesses, empyema, or upper gastrointestinal tract infections.

Antifungal agents with enhanced activity in acidic pH
11534433 · 2022-12-27 · ·

Enfumafungin derivative triterpenoid antifungal compounds are used to treat or prevent fungal infections occurring in or under acidic conditions where the pH is lower than about 7, due to their unexpected, enhanced efficacy under such conditions. The enfumafungin derivative triterpenoids (or pharmaceutically acceptable salts or hydrates thereof) are inhibitors of (1,3)-β-D-glucan synthesis and are useful in the treatment or prevention of yeast or mold infections that occur in anatomic areas having a low pH, such as the vaginal cavity, or under acidic local environment conditions such of those seen in fungal abscesses, empyema, or upper gastrointestinal tract infections.

SHORTENING TUBERCULOSIS THERAPY AND REDUCING RELAPSE BY CO-ADMINISTERING CHLOROQUINE IN TB AND HIV-TB COINFECTED CONDITIONS
20220395495 · 2022-12-15 ·

The present invention provides shortening TB Therapy and reducing relapse by co-administering Chloroquine with anti-TB drugs to drug-sensitive TB patients, multiple drug resistant (MDR) TB patients and TB patients co-infected with HIV-1. The present invention also provides shortening TB Therapy and reducing relapse by co-administering hydroxychloroquine with anti-TB drugs to drug-sensitive TB patients, multiple drug resistant (MDR) TB patients and TB patients co-infected with HIV-1.

SHORTENING TUBERCULOSIS THERAPY AND REDUCING RELAPSE BY CO-ADMINISTERING CHLOROQUINE IN TB AND HIV-TB COINFECTED CONDITIONS
20220395495 · 2022-12-15 ·

The present invention provides shortening TB Therapy and reducing relapse by co-administering Chloroquine with anti-TB drugs to drug-sensitive TB patients, multiple drug resistant (MDR) TB patients and TB patients co-infected with HIV-1. The present invention also provides shortening TB Therapy and reducing relapse by co-administering hydroxychloroquine with anti-TB drugs to drug-sensitive TB patients, multiple drug resistant (MDR) TB patients and TB patients co-infected with HIV-1.

Formulations, methods, and systems for treating genitourinary conditions

Provided are formulations and methods for treating one or more genitourinary conditions. The formulations may include a therapeutic agent that includes a calcium channel blocker, a rho kinase inhibitor, or a combination thereof. The methods may include locally administering a therapeutic agent into a ureter. Systems for delivering a therapeutic agent also are provided.