C07D265/22

Benzoxazinone derivatives for treatment of skin diseases
09695194 · 2017-07-04 · ·

The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein 5 (KLK5), and human kallikrein 14 (KLK14). More specifically, the invention relates to the use of substituted 3,1-benzoxazin-4-ones being selective inhibitors of human skin kallikreins for the treatment of skin diseases, more specifically for the treatment of inflammatory skins diseases, especially Netherton syndrome.

Benzoxazinone derivatives for treatment of skin diseases
09695194 · 2017-07-04 · ·

The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein 5 (KLK5), and human kallikrein 14 (KLK14). More specifically, the invention relates to the use of substituted 3,1-benzoxazin-4-ones being selective inhibitors of human skin kallikreins for the treatment of skin diseases, more specifically for the treatment of inflammatory skins diseases, especially Netherton syndrome.

Methods and compositions for inhibition of bromodomain-containing proteins

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

Methods and compositions for inhibition of bromodomain-containing proteins

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Fused heterocyclic compounds as ion channel modulators

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: ##STR00001##
wherein Q, R.sup.1, X.sup.1, X.sup.2, Y and R.sup.2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Fused heterocyclic compounds as ion channel modulators

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: ##STR00001##
wherein Q, R.sup.1, X.sup.1, X.sup.2, Y and R.sup.2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

PROCESS METHODS FOR PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

PROCESS METHODS FOR PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.