A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001##
wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.

The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

##STR00001##

The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

##STR00001##

The present invention relates to novel crystalline forms of a quinolone compound of Formula (I). The invention also relates to processes for the preparation crystalline forms of the compound of Formula (I). Further the disclosure provides a process for the preparation of compound of Formula (I), intermediates, impurities and pharmaceutical compositions thereof.

##STR00001##

The present invention relates to novel crystalline forms of a quinolone compound of Formula (I). The invention also relates to processes for the preparation crystalline forms of the compound of Formula (I). Further the disclosure provides a process for the preparation of compound of Formula (I), intermediates, impurities and pharmaceutical compositions thereof.

##STR00001##

The invention provides a chemical entity of Formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.