A TLR-independent adjuvant compound that corresponds in structure to Formula I, below, or its pharmaceutically acceptable salt is disclosed in

##STR00001##

which X, Y, Z, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and W are defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.

A TLR-independent adjuvant compound that corresponds in structure to Formula I, below, or its pharmaceutically acceptable salt is disclosed in

##STR00001##

which X, Y, Z, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and W are defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.

Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.

Described herein are salts of 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofuran-2-carboxamide, in particular that of formula (I):

##STR00001##

wherein HA is naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, oxalic acid, benzenesulfonic acid, or sulfuric acid, or hydrates thereof, and crystalline forms thereof characterized by the powder X-ray diffraction diagram and the 13C CP/MAS NMR solid state spectrum. Also described are compositions, methods of use and preparation thereof.

Described herein are salts of 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofuran-2-carboxamide, in particular that of formula (I):

##STR00001##

wherein HA is naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, oxalic acid, benzenesulfonic acid, or sulfuric acid, or hydrates thereof, and crystalline forms thereof characterized by the powder X-ray diffraction diagram and the 13C CP/MAS NMR solid state spectrum. Also described are compositions, methods of use and preparation thereof.

The present invention provides acyl sulfonamide compounds of general formula (I):

##STR00001## in which X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6′ R.sup.a and R.sup.b are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treating and/or prophylaxing diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

The present invention provides acyl sulfonamide compounds of general formula (I):

##STR00001## in which X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6′ R.sup.a and R.sup.b are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treating and/or prophylaxing diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, W, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, X.sub.7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

##STR00001##

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, W, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, X.sub.7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

##STR00001##

Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.