A61K31/496

PHARMACEUTICAL PREPARATION COMPRISING BREXPIPRAZOLE AND SUBSTITUTED BETA-CYCLODEXTRIN

Provided is an aqueous pharmaceutical preparation comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (compound (I)) or a salt thereof, which shows improved water solubility of compound (I) or a salt thereof achieved by addition of substituted β-cyclodextrin. The present invention provides a pharmaceutical preparation comprising compound (I) or a salt thereof, and substituted β-cyclodextrin.

PHARMACEUTICAL PREPARATION COMPRISING BREXPIPRAZOLE AND SUBSTITUTED BETA-CYCLODEXTRIN

Provided is an aqueous pharmaceutical preparation comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (compound (I)) or a salt thereof, which shows improved water solubility of compound (I) or a salt thereof achieved by addition of substituted β-cyclodextrin. The present invention provides a pharmaceutical preparation comprising compound (I) or a salt thereof, and substituted β-cyclodextrin.

Tablet Comprising 7-[4-(4-benzo[b]thiopen-4-yl-piperazin-1 -yl)butoxy]-1H-Quinolin-2-One or a Salt Thereof
20180008600 · 2018-01-11 · ·

This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability.

The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer, containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.

Tablet Comprising 7-[4-(4-benzo[b]thiopen-4-yl-piperazin-1 -yl)butoxy]-1H-Quinolin-2-One or a Salt Thereof
20180008600 · 2018-01-11 · ·

This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability.

The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer, containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.

ANTIFIBROTIC COMPOUNDS AND USES THEREOF

The present invention provides compounds having the general structural formula (I)

##STR00001##

and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

ANTIFIBROTIC COMPOUNDS AND USES THEREOF

The present invention provides compounds having the general structural formula (I)

##STR00001##

and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

ANTHELMINTIC COMPOUNDS, COMPOSITIONS AND METHOD OF USING THEREOF
20180009754 · 2018-01-11 · ·

The present invention relates to novel anthelmintic compounds of formula (IA) below:

##STR00001## wherein, Y is selected from the group consisting of —H, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl; and Z is selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl. Variables Ring A, Ring B, Ring C, X.sub.1, X.sub.6, and X.sub.8 are as defined herein. The invention also relates to parasiticidal compositions comprising the compounds, and methods and uses of the compounds for treating and preventing parasitic infections and infestations in animals.

ANTHELMINTIC COMPOUNDS, COMPOSITIONS AND METHOD OF USING THEREOF
20180009754 · 2018-01-11 · ·

The present invention relates to novel anthelmintic compounds of formula (IA) below:

##STR00001## wherein, Y is selected from the group consisting of —H, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl; and Z is selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl. Variables Ring A, Ring B, Ring C, X.sub.1, X.sub.6, and X.sub.8 are as defined herein. The invention also relates to parasiticidal compositions comprising the compounds, and methods and uses of the compounds for treating and preventing parasitic infections and infestations in animals.

FUROQUINOLINEDIONES AS INHIBITORS OF TDP2
20180009822 · 2018-01-11 ·

Compounds of Formula I and the pharmaceutically acceptable salts thereof are disclosed Formula I. The variables X.sup.1, X.sup.2, and R.sup.1-4 are disclosed herein. The compounds are useful for treating cancer and related proliferative diseases. Pharmaceutical compositions containing compounds of Formula I and methods of treatment comprising administering compounds of Formula I are also disclosed.

##STR00001##

FUROQUINOLINEDIONES AS INHIBITORS OF TDP2
20180009822 · 2018-01-11 ·

Compounds of Formula I and the pharmaceutically acceptable salts thereof are disclosed Formula I. The variables X.sup.1, X.sup.2, and R.sup.1-4 are disclosed herein. The compounds are useful for treating cancer and related proliferative diseases. Pharmaceutical compositions containing compounds of Formula I and methods of treatment comprising administering compounds of Formula I are also disclosed.

##STR00001##