C07D403/12

Substituted pyrazole-pyrimidines, variants thereof, and uses therefore

Disclosed herein are substituted pyrazole-pyrimidine compounds of Formula I and variants thereof for the treatment, for example, of diseases associated with P2X purinergic receptors: ##STR00001##
In one embodiment, the P2X3 and/or P2X2/3 antagonists disclosed herein are potentially useful, for example, for the treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.

N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
20180000832 · 2018-01-04 ·

The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1),

##STR00001## wherein A.sup.1, Y and Z all represent rings.

N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
20180000832 · 2018-01-04 ·

The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1),

##STR00001## wherein A.sup.1, Y and Z all represent rings.

2-(PYRAZIN-2-YLCARBONYLAMINOMETHYL) BENZIMIDAZOLIUM COMPOUNDS AS EPITHELIAL SODIUM CHANNEL INHIBITORS
20180002314 · 2018-01-04 ·

The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z.sup.− have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.

##STR00001##

2-(PYRAZIN-2-YLCARBONYLAMINOMETHYL) BENZIMIDAZOLIUM COMPOUNDS AS EPITHELIAL SODIUM CHANNEL INHIBITORS
20180002314 · 2018-01-04 ·

The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z.sup.− have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.

##STR00001##

TETRA- AND PENTASUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS USEFUL IN THE TREATMENT OF RESPIRATORY DISEASES
20180002312 · 2018-01-04 ·

The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).

##STR00001##

TETRA- AND PENTASUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS USEFUL IN THE TREATMENT OF RESPIRATORY DISEASES
20180002312 · 2018-01-04 ·

The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).

##STR00001##

ZINC COMPLEXES OF HYDRAZONES AND (THIO)SEMICARBAZONES AND THEIR USE FOR THE TREATMENT OF CANCER

The invention provides complexes of Zn2+ of formulae (la) and (IIa) that are useful for treating cancer, as well as compositions and kits comprising such complexes.

##STR00001##

ZINC COMPLEXES OF HYDRAZONES AND (THIO)SEMICARBAZONES AND THEIR USE FOR THE TREATMENT OF CANCER

The invention provides complexes of Zn2+ of formulae (la) and (IIa) that are useful for treating cancer, as well as compositions and kits comprising such complexes.

##STR00001##

(THIO, OXO, AND SELENO) SEMICARBAZONE DERIVATIVES AND THEIR USE FOR TREATING CANCER

The invention provides compounds of formula I and II and salts thereof, wherein R.sup.1, R.sup.2, Y, R.sup.3, and R.sup.4 have any of the meanings described in the specification, as well as compositions comprising such compounds and salts, and methods for treating cancer using such compounds and salts.

##STR00001##