C07D295/092

SELECTIVE CONNEXIN HEMICHANNELS BLOCKERS FOR THE TREATMENT OF EPILEPSY
20180050029 · 2018-02-22 ·

The present invention provides connexin hemichannel blockers for the treatment of epilepsy.

In particular, the present invention relates to organic compounds which act as selective blockers connexin hemichannels which are useful in the treatment of epilepsy.

In another embodiment of the present invention there is provided a composition comprising a selective connexin hemichannels blocker compounds useful in the treatment of epilepsy in combination with other antiepileptic compounds.

Amido-substituted azole compounds

The present invention relates to amido-substituted azole compounds of general formula (I), in which X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, 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 neoplasms, as a sole agent or in combination with other active ingredients. ##STR00001##

Amido-substituted azole compounds

The present invention relates to amido-substituted azole compounds of general formula (I), in which X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, 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 neoplasms, as a sole agent or in combination with other active ingredients. ##STR00001##

Antibacterial agents

Antibacterial compounds of formula (I) are provided: ##STR00001##
as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

Antibacterial agents

Antibacterial compounds of formula (I) are provided: ##STR00001##
as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

ANTIBACTERIAL AGENTS

Antibacterial compounds of formula (I) are provided:

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as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

NOVEL AROMATIC MOLECULES

The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

##STR00001##

AMIDO-SUBSTITUTED AZOLE COMPOUNDS

The present invention relates to amido-substituted azole compounds of general formula (I), in which X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, 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 neoplasms, as a sole agent or in combination with other active ingredients.

##STR00001##

USE OF ARYLALKANOLAMINES AS SIGMA-1 RECEPTOR ANTAGONISTS

The present invention relates to the use of arylalkanolamine compounds with sigma-1 receptor antagonist activity. In particular, the said arylalkanolamine compounds are useful in the treatment of conditions selected from the abuse of psychotropic substances such as cocaine or amphetamines, pain and cancer.

USE OF ARYLALKANOLAMINES AS SIGMA-1 RECEPTOR ANTAGONISTS

The present invention relates to the use of arylalkanolamine compounds with sigma-1 receptor antagonist activity. In particular, the said arylalkanolamine compounds are useful in the treatment of conditions selected from the abuse of psychotropic substances such as cocaine or amphetamines, pain and cancer.