C07D455/02

Substituted quinolizine derivatives useful as HIV integrase inhibitors

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9 and R.sup.10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject. ##STR00001##

NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES
20170334908 · 2017-11-23 ·

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

ANTIMICROBIAL 4-OXOQUINOLIZINES

This invention provides novel 4-oxoquinolizine compounds and their uses for a series of broad-spectrum antibiotics having no cross-resistance to existing or emerging classes of antibiotics. In addition the novel 4-oxoquinolizine compounds are useful against CDC Category A and B pathogens The invention also provides pharmaceutical compositions comprising certain 4-oxoquinolizines in combination with subinhibitory concentrations of polymyxin B against clinical isolates which are resistant to quinolones, carbapenems and other antimicrobial agents.

2-PYRIDONE ANTIMICROBIAL COMPOSITIONS

Disclosed herein are compounds of Formula I

##STR00001## wherein R.sup.1, R.sup.2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.

IL-17 ligands and uses thereof

Provided herein are novel ligands and pharmaceutical compositions thereof which modulate IL-17A. Also provided are methods for preparing the IL-17A modulators. Such compounds may be useful in the treatment and/or prevention of, for example, inflammation, cancer or autoimmune disease.

IL-17 ligands and uses thereof

Provided herein are novel ligands and pharmaceutical compositions thereof which modulate IL-17A. Also provided are methods for preparing the IL-17A modulators. Such compounds may be useful in the treatment and/or prevention of, for example, inflammation, cancer or autoimmune disease.

ANTIMICROBIAL 4-OXOQUINOLIZINES

This invention provides novel 4-oxoquinolizine compounds and their uses for a series of broad-spectrum antibiotics having no cross-resistance to existing or emerging classes of antibiotics. In addition the novel 4-oxoquinolizine compounds are useful against CDC Category A and B pathogens The invention also provides pharmaceutical compositions comprising certain 4-oxoquinolizines in combination with subinhibitory concentrations of polymyxin B against clinical isolates which are resistant to quinolones, carbapenems and other antimicrobial agents.

COMPOUNDS USEFUL AS IMMUNOMODULATORS

The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases

The present invention relates to novel fused heterocyclic or carbocyclic compounds of formula I ##STR00001##
wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising these compounds, and to their use for the treatment of vasopressin-related disorders.

Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases

The present invention relates to novel fused heterocyclic or carbocyclic compounds of formula I ##STR00001##
wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising these compounds, and to their use for the treatment of vasopressin-related disorders.