The present disclosure provides methods and pharmaceutical compositions for treating or slowing the progression of cancers that overexpress the histone methyltransferase WHSC1, e.g., t(4; 14) multiple myeloma, by administering to a subject in need thereof a therapeutically effective amount of an inhibitor of the histone methyltransferase, SETD2.

The present disclosure provides methods and pharmaceutical compositions for treating or slowing the progression of cancers that overexpress the histone methyltransferase WHSC1, e.g., t(4; 14) multiple myeloma, by administering to a subject in need thereof a therapeutically effective amount of an inhibitor of the histone methyltransferase, SETD2.

The present disclosure relates to a Prp8 intein splicing inhibitor. The present disclosure further relates to a method of treating and/or preventing a fungal infection, said method comprising administering a Prp8 intein splicing inhibitor under conditions effective to treat and/or prevent a fungal infection. Also disclosed is a method of inhibiting Prp8 intein expression or activity in a cell or tissue, said method comprising administering a compound under conditions effective to inhibit Prp8 intein expression or activity in a cell or tissue. Further disclosed are methods for screening for compounds that inhibit Prp8 intein splicing comprising an assay and a kit for predicting the likelihood of Prp8 inhibition.

The present disclosure relates to a Prp8 intein splicing inhibitor. The present disclosure further relates to a method of treating and/or preventing a fungal infection, said method comprising administering a Prp8 intein splicing inhibitor under conditions effective to treat and/or prevent a fungal infection. Also disclosed is a method of inhibiting Prp8 intein expression or activity in a cell or tissue, said method comprising administering a compound under conditions effective to inhibit Prp8 intein expression or activity in a cell or tissue. Further disclosed are methods for screening for compounds that inhibit Prp8 intein splicing comprising an assay and a kit for predicting the likelihood of Prp8 inhibition.

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically acceptable carrier for topical or oral administration.

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically acceptable carrier for topical or oral administration.

The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R.sup.1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or phenyl; R.sup.2 is hydrogen, cyano, halogen, alkylsulfonyl, alkyl, cycloalkyl or alkoxy; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, alkyl or alkoxy; most groups being optionally substituted; with the proviso that at least one of R.sup.2, R.sup.3, R.sup.4 is H; X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are independently N or C; with the proviso that in each ring maximal one X is N.

##STR00001##

The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R.sup.1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or phenyl; R.sup.2 is hydrogen, cyano, halogen, alkylsulfonyl, alkyl, cycloalkyl or alkoxy; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, alkyl or alkoxy; most groups being optionally substituted; with the proviso that at least one of R.sup.2, R.sup.3, R.sup.4 is H; X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are independently N or C; with the proviso that in each ring maximal one X is N.

##STR00001##

The invention relates to a compound of formula (I), a salt thereof or a composition containing same as an acaricide, a method for reducing or preventing an infestation of an animal by a mite, comprising exposing the mite to a compound of formula (I), to a composition comprising a compound of formula (I), to one or more attractants for bees and a polymer, to a strap adapted for use in apiculture comprising a compound of formula (I) and to a hive comprising a compound of formula (I).

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.