The present invention provides compounds of Formula I (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

##STR00001##

The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.

The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.

Disclosed are compounds, compositions and methods for treating and/or ameliorating diseases, syndromes, disorders, or conditions associated with AR mutant receptors linked to castration-resistant prostate cancer, in a subject, including a mammal and/or human, in need thereof, who has demonstrated resistance to a first or second generation AR antagonist, comprising, consisting of, and/or consisting essentially of, administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula (I)

##STR00001##

wherein R.sub.1, G, R.sub.10, and R.sub.11 are defined herein.

The present invention features a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

The present invention features a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

The invention provides compounds of the formula (I): (I) wherein A.sup.1, A.sup.2, R.sup.2, R.sup.4, B.sup.1, B.sup.2, X, X.sup.1, n, a and b are as defined are defined in the specification, to pharmaceutical compositions comprising the compounds and the compounds for use as medicaments. The compounds potentiate AMPA receptor function and are expected to be useful in the treatment of central nervous system disorders, for example in the treatment of depressive disorders, mood disorders and cognitive dysfunction associated with neuropsychiatric disorders such as schizophrenia.

##STR00001##

The invention provides compounds of the formula (I): (I) wherein A.sup.1, A.sup.2, R.sup.2, R.sup.4, B.sup.1, B.sup.2, X, X.sup.1, n, a and b are as defined are defined in the specification, to pharmaceutical compositions comprising the compounds and the compounds for use as medicaments. The compounds potentiate AMPA receptor function and are expected to be useful in the treatment of central nervous system disorders, for example in the treatment of depressive disorders, mood disorders and cognitive dysfunction associated with neuropsychiatric disorders such as schizophrenia.

##STR00001##

The present disclosure relates to thiazolo-pyridine, oxazolo-pyridine, pyrrolo-pyridine, pyrrolo-pyrazine and pyrrolo-pyrimidine compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling.

The present disclosure relates to thiazolo-pyridine, oxazolo-pyridine, pyrrolo-pyridine, pyrrolo-pyrazine and pyrrolo-pyrimidine compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling.