C07D215/54

Substituted quinoline analogs as aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors

The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R.sup.4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumors breast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis. The disclosure also includes pharmaceutical compositions containing a compound or salt of Formula I. ##STR00001##

Substituted quinoline analogs as aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors

The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R.sup.4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumors breast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis. The disclosure also includes pharmaceutical compositions containing a compound or salt of Formula I. ##STR00001##

Inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) and methods of use thereof

Compounds and methods for their preparation and use as therapeutic or prophylactic agents, for example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1).

Inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) and methods of use thereof

Compounds and methods for their preparation and use as therapeutic or prophylactic agents, for example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1).

Tetrahydroquinoline derivatives and a process of preparation thereof

The present disclosure provides tetrahydroquinoline derivatives of Formula (I) ##STR00001##
wherein X.sub.1 and X.sub.2 each, independently, are oxygen or sulphur; R.sub.1 is a lower alkoxy, or an optionally substituted aryl group; R.sub.2 is selected from a group consisting of hydrogen, lower alkyl, haloalkyl, or an amino group; R.sub.3 and R.sub.4 each, independently, are hydrogen, or lower alkyl groups; and R5 and R6 are optionally substituted aryl groups. The present disclosure also provides a method for making the compound of Formula (I).

Tetrahydroquinoline derivatives and a process of preparation thereof

The present disclosure provides tetrahydroquinoline derivatives of Formula (I) ##STR00001##
wherein X.sub.1 and X.sub.2 each, independently, are oxygen or sulphur; R.sub.1 is a lower alkoxy, or an optionally substituted aryl group; R.sub.2 is selected from a group consisting of hydrogen, lower alkyl, haloalkyl, or an amino group; R.sub.3 and R.sub.4 each, independently, are hydrogen, or lower alkyl groups; and R5 and R6 are optionally substituted aryl groups. The present disclosure also provides a method for making the compound of Formula (I).

SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY

Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R.sup.1-R.sup.7, X, X′, Y, Y′, Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

##STR00001##

SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY

Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R.sup.1-R.sup.7, X, X′, Y, Y′, Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

##STR00001##

QUINOLINE DERIVATIVES

The present disclosure provides a compound of Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Quinoline derivatives

The present invention covers new quinoline compounds of general formula (I), in which A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients. ##STR00001##