A61K31/4353

Antifibrotic compounds and uses thereof

The present invention provides compounds having the general structural formula (I) ##STR00001##
and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

Antifibrotic compounds and uses thereof

The present invention provides compounds having the general structural formula (I) ##STR00001##
and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

COMBINATION TREATMENT OF LIVER DISEASES USING INTEGRIN INHIBITORS

The invention provides a pharmaceutical combination including an αvβ1 integrin inhibitor and at least one additional therapeutic agent for preventing, delaying or treating liver diseases or disorders. The at least one additional therapeutic agent may be a farnesoid X receptor (FXR) agonist. For example, the pharmaceutical combination includes (S)-2-(4-methyltetrahydro-2H-pyran-4-carboxamido)-9-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)nonanoic acid (Compound 1) and 2-[3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1, 3-ben-zothiazole-6-carboxylic acid (tropifexor).

COMBINATION TREATMENT OF LIVER DISEASES USING INTEGRIN INHIBITORS

The invention provides a pharmaceutical combination including an αvβ1 integrin inhibitor and at least one additional therapeutic agent for preventing, delaying or treating liver diseases or disorders. The at least one additional therapeutic agent may be a farnesoid X receptor (FXR) agonist. For example, the pharmaceutical combination includes (S)-2-(4-methyltetrahydro-2H-pyran-4-carboxamido)-9-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)nonanoic acid (Compound 1) and 2-[3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1, 3-ben-zothiazole-6-carboxylic acid (tropifexor).

COMBINATIONS

Disclosed herein are combinations of compounds for treating a disease or condition, such as cancer. A combination of compounds for treating a disease or condition can include a SERD inhibitor and another inhibitor (such as a CDK4/6 inhibitor, a selective aromatase inhibitor, a non-selective aromatase inhibitor, a mTOR inhibitor, a PI3K inhibitor, an ERK or a MEK inhibitor, AKT inhibitor, a BET inhibitor and an Aurora inhibitor), along with pharmaceutically acceptable salts of any of the foregoing.

COMBINATIONS

Disclosed herein are combinations of compounds for treating a disease or condition, such as cancer. A combination of compounds for treating a disease or condition can include a SERD inhibitor and another inhibitor (such as a CDK4/6 inhibitor, a selective aromatase inhibitor, a non-selective aromatase inhibitor, a mTOR inhibitor, a PI3K inhibitor, an ERK or a MEK inhibitor, AKT inhibitor, a BET inhibitor and an Aurora inhibitor), along with pharmaceutically acceptable salts of any of the foregoing.

METHODS OF TREATING OR PREVENTING VIRAL INFECTION WITH FLUORINATED AlphaV INTEGRIN ANTAGONISTS
20230129394 · 2023-04-27 ·

The present application relates to use of fluorinated compounds of Formula (I) in treating or preventing a viral infection or a condition or symptom associated with the viral infection.

METHODS OF TREATING OR PREVENTING VIRAL INFECTION WITH FLUORINATED AlphaV INTEGRIN ANTAGONISTS
20230129394 · 2023-04-27 ·

The present application relates to use of fluorinated compounds of Formula (I) in treating or preventing a viral infection or a condition or symptom associated with the viral infection.

PHARMACEUTICAL COMBINATION OF AN EP4 ANTAGONIST AND IMMUNE CHECKPOINT INHIBITORS FOR THE TREATMENT OF TUMOURS

The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2θ ±0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.

METHODS AND COMPOSITIONS FOR INDUCING APOPTOSIS IN CANCER STEM CELLS

Provided herein are pharmaceutical compositions and methods useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.