This invention relates to compounds that are inhibitors of HSP70 protein, and applications thereof.

This invention relates to compounds that are inhibitors of HSP70 protein, and applications thereof.

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR.sub.12R.sub.13; or one of P and Q is NR.sub.14 and the other is CR.sub.12R.sub.13; the group X—Y is —NHSO.sub.2— or —SO2NH—; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, heteroaryl, SO.sub.2NR.sub.16R.sub.17, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H or halo; and R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.16 and R.sub.17 are each independently H or alkyl; R.sub.15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

##STR00001##

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR.sub.12R.sub.13; or one of P and Q is NR.sub.14 and the other is CR.sub.12R.sub.13; the group X—Y is —NHSO.sub.2— or —SO2NH—; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, heteroaryl, SO.sub.2NR.sub.16R.sub.17, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H or halo; and R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.16 and R.sub.17 are each independently H or alkyl; R.sub.15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

##STR00001##

The present invention relates to an oral pharmaceutical composition comprising a carbamate compound of chemical formula 1, an isomer thereof, or a pharmaceutically acceptable salt, solvate, or hydrate thereof as an active ingredient, and a preparation method therefor.

The present invention relates to an oral pharmaceutical composition comprising a carbamate compound of chemical formula 1, an isomer thereof, or a pharmaceutically acceptable salt, solvate, or hydrate thereof as an active ingredient, and a preparation method therefor.

The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.

The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.

The present disclosure relates to an aqueous formulation comprising as an active ingredient a carbamate compound of Formula 1, or a pharmaceutically acceptable salt, solvate or hydrate thereof, poloxamer, and an aqueous carrier, wherein the aqueous formulation is in the form of a suspension formulation.

The present disclosure relates to an aqueous formulation comprising as an active ingredient a carbamate compound of Formula 1, or a pharmaceutically acceptable salt, solvate or hydrate thereof, poloxamer, and an aqueous carrier, wherein the aqueous formulation is in the form of a suspension formulation.