A61K31/517

EXPANDED DOSAGE REGIMENS FOR INTEGRIN INHIBITORS
20230028658 · 2023-01-26 ·

The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I):

##STR00001##

or a salt thereof, wherein R.sup.1, R.sup.2, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION

Disclosed are small molecules against cereblon to enhance effector T cell function. Methodos of making thes molecules and methods of using them to treat various disease states are also disclosed.

SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION

Disclosed are small molecules against cereblon to enhance effector T cell function. Methodos of making thes molecules and methods of using them to treat various disease states are also disclosed.

IMPROVEMENTS IN ULTRASOUND-MEDIATED THERAPY
20230226184 · 2023-07-20 · ·

The present invention relates to the field of ultrasound-mediated therapeutic treatments in combination with gas-filled microvesicles. It relates in particular to enhancing the efficacy of a combined therapeutic treatment of gas-filled microvesicles and ultrasound, by reducing the vasospasm effect caused by said therapeutic treatment.

IMPROVEMENTS IN ULTRASOUND-MEDIATED THERAPY
20230226184 · 2023-07-20 · ·

The present invention relates to the field of ultrasound-mediated therapeutic treatments in combination with gas-filled microvesicles. It relates in particular to enhancing the efficacy of a combined therapeutic treatment of gas-filled microvesicles and ultrasound, by reducing the vasospasm effect caused by said therapeutic treatment.

METHODS OF USE FOR PYRIMIDINES AS FERROPORTIN INHIBITORS

The subject matter described herein is directed to ferroportin inhibitor compounds of Formula (I) and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.

METHODS OF USE FOR PYRIMIDINES AS FERROPORTIN INHIBITORS

The subject matter described herein is directed to ferroportin inhibitor compounds of Formula (I) and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.

Targeting mitochondrial fission through mDIVI-1 derivatives

Derivatives of mDIVI-1 may be used to target and eliminate cancer stem cells. Disruption in the mitochondrial dynamics balance plays a role in cancer. Proteins involved in regulating mitochondrial dynamics represent potential targets for cancer treatment. Mitochondrial fission protein DRP1 is such a target. Derivatives of mDIVI-1 inhibit DRP1, and have demonstrated inhibition of tumorsphere forming capacity, migration and stemness-related signaling in breast cancer cells. These properties result from induction of mitochondrial oxidative stress and reduction of mitochondrial metabolism in the target cancer cells. The potency of an mDIVI-1 derivative may be dramatically increased through addition of at least one membrane-targeting signal and/or a mitochondria-targeting signal.

Targeting mitochondrial fission through mDIVI-1 derivatives

Derivatives of mDIVI-1 may be used to target and eliminate cancer stem cells. Disruption in the mitochondrial dynamics balance plays a role in cancer. Proteins involved in regulating mitochondrial dynamics represent potential targets for cancer treatment. Mitochondrial fission protein DRP1 is such a target. Derivatives of mDIVI-1 inhibit DRP1, and have demonstrated inhibition of tumorsphere forming capacity, migration and stemness-related signaling in breast cancer cells. These properties result from induction of mitochondrial oxidative stress and reduction of mitochondrial metabolism in the target cancer cells. The potency of an mDIVI-1 derivative may be dramatically increased through addition of at least one membrane-targeting signal and/or a mitochondria-targeting signal.

Bicyclic-fused heteroaryl or aryl compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.