The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), ##STR00001##
to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.

The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), ##STR00001##
to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.

Compounds of formulae (I) and (II), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.

##STR00001##

Compounds of formulae (I) and (II), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.

##STR00001##

An antitumor formulation comprising a biphenyl compound having LSD1 inhibitory activity or a salt thereof and one or more other antitumor agents that are administered in combination, the compound being represented by Formula (I): ##STR00001##
wherein ring A, ring B, R1 to R6, l, m, and n are as defined in the specification.

An antitumor formulation comprising a biphenyl compound having LSD1 inhibitory activity or a salt thereof and one or more other antitumor agents that are administered in combination, the compound being represented by Formula (I): ##STR00001##
wherein ring A, ring B, R1 to R6, l, m, and n are as defined in the specification.

The invention relates to coated particles with a taste-masked drug substance. The particles comprise a core with a melt-agglomerated active pharmaceutical ingredient (API), optionally a thermolabile API, and a coating comprising a triglyceride and a surfactant. The particles exhibit immediate drug release and a storage-stable release profile. Moreover, the invention provides a hot-melt granulation and hot-melt coating method for manufacturing such coated particles, and pharmaceutical compositions comprising the coated particles. The method allows the granulation of APIs with small particle sizes (e.g., mean particle size below 150 μm, or even below 100 μm or 50 μm) into core particles, as well as coating said core particles, at moderate temperatures, thereby preventing the degradation of thermolabile active pharmaceutical ingredients.

The invention relates to coated particles with a taste-masked drug substance. The particles comprise a core with a melt-agglomerated active pharmaceutical ingredient (API), optionally a thermolabile API, and a coating comprising a triglyceride and a surfactant. The particles exhibit immediate drug release and a storage-stable release profile. Moreover, the invention provides a hot-melt granulation and hot-melt coating method for manufacturing such coated particles, and pharmaceutical compositions comprising the coated particles. The method allows the granulation of APIs with small particle sizes (e.g., mean particle size below 150 μm, or even below 100 μm or 50 μm) into core particles, as well as coating said core particles, at moderate temperatures, thereby preventing the degradation of thermolabile active pharmaceutical ingredients.

Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof: wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, A, L, R.sup.1, R.sup.2, R.sup.5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

##STR00001##

Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof: wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, A, L, R.sup.1, R.sup.2, R.sup.5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

##STR00001##