C07D215/60

Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
20210002228 · 2021-01-07 ·

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

##STR00001##

NITROCATECHOL DERIVATIVES AS COMT INHIBITORS

New compounds of formula I are described:

##STR00001##

The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

NITROCATECHOL DERIVATIVES AS COMT INHIBITORS

New compounds of formula I are described:

##STR00001##

The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

Substituted N,2-diarylquinoline-4-carboxamides and the use thereof as anti-inflammatory agents

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.

Substituted N,2-diarylquinoline-4-carboxamides and the use thereof as anti-inflammatory agents

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.

Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
20190218182 · 2019-07-18 ·

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

##STR00001##

Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
20190218182 · 2019-07-18 ·

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

##STR00001##

Metabolites of N-{4-([6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

The invention relates to metabolites of cabozantinib (I) as well as uses thereof. ##STR00001##

Metabolites of N-{4-([6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

The invention relates to metabolites of cabozantinib (I) as well as uses thereof. ##STR00001##

Compounds for inhibiting drug-resistant strains of HIV-1 integrase

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.