A61K31/4709

MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

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.

MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

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.

SELECTIVE ESTROGEN RECEPTOR DEGRADERS

Novel selective estrogen receptor degraders (SERDs) according to the formula:

##STR00001##

pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R.sup.1 or R.sup.2 is independently selected from Cl, F, —CF.sub.3, or —CH.sub.3, and the other is hydrogen, and methods for their use are provided.

SELECTIVE ESTROGEN RECEPTOR DEGRADERS

Novel selective estrogen receptor degraders (SERDs) according to the formula:

##STR00001##

pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R.sup.1 or R.sup.2 is independently selected from Cl, F, —CF.sub.3, or —CH.sub.3, and the other is hydrogen, and methods for their use are provided.

COMBINATION OF ZIDOVUDINE AND FLUOROQUINOLONE ANTIBIOTIC

The present invention relates to a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and a fluoroquinolone antibiotic or a pharmaceutically acceptable derivative or prodrug thereof, for use in treating a microbial infection, particularly a bacterial infection such as a urinary tract infection.

COMBINATION OF ZIDOVUDINE AND FLUOROQUINOLONE ANTIBIOTIC

The present invention relates to a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and a fluoroquinolone antibiotic or a pharmaceutically acceptable derivative or prodrug thereof, for use in treating a microbial infection, particularly a bacterial infection such as a urinary tract infection.

COMBINATION OF A CBP/P300 BROMODOMAIN INHIBITOR AND A KRAS INHIBITOR FOR THE TREATMENT OF CANCER

The present invention is inter alia concerned with (i) a combination of a CBP/p300 bromodomain inhibitor and a KRAS inhibitor for use in the treatment of a patient suffering from cancer, wherein the cancer exhibits an oncogenic alteration in the KRAS; (ii) a kit comprising (a) a pharmaceutical dosage form comprising a CBP/p300 bromodomain inhibitor and (b) a pharmaceutical dosage form comprising a KRAS inhibitor, and (iii) a pharmaceutical dosage form comprising a CBP/p300 bromodomain inhibitor and a a KRAS inhibitor.

COMBINATION OF A CBP/P300 BROMODOMAIN INHIBITOR AND A KRAS INHIBITOR FOR THE TREATMENT OF CANCER

The present invention is inter alia concerned with (i) a combination of a CBP/p300 bromodomain inhibitor and a KRAS inhibitor for use in the treatment of a patient suffering from cancer, wherein the cancer exhibits an oncogenic alteration in the KRAS; (ii) a kit comprising (a) a pharmaceutical dosage form comprising a CBP/p300 bromodomain inhibitor and (b) a pharmaceutical dosage form comprising a KRAS inhibitor, and (iii) a pharmaceutical dosage form comprising a CBP/p300 bromodomain inhibitor and a a KRAS inhibitor.

COMBINATION OF A CBP/P300 BROMODOMAIN INHIBITOR AND A KRAS INHIBITOR FOR THE TREATMENT OF CANCER

The present invention is inter alia concerned with (i) a combination of a CBP/p300 bromodomain inhibitor and a KRAS inhibitor for use in the treatment of a patient suffering from cancer, wherein the cancer exhibits an oncogenic alteration in the KRAS; (ii) a kit comprising (a) a pharmaceutical dosage form comprising a CBP/p300 bromodomain inhibitor and (b) a pharmaceutical dosage form comprising a KRAS inhibitor, and (iii) a pharmaceutical dosage form comprising a CBP/p300 bromodomain inhibitor and a a KRAS inhibitor.

Imidazotriazines and Imidazopyrimidines as Kinase Inhibitors

The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.