A61P5/14

TRICYCLIC ATROPISOMER COMPOUNDS
20170355673 · 2017-12-14 ·

Disclosed are compounds of Formula (I): or a salt thereof, wherein Q is: or; and X, R.sub.1a, R.sub.1b, R.sub.3, R.sub.4, and R.sub.5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

##STR00001##

Phosphoinositide 3-Kinase Inhibitors with a Zinc Binding Moiety
20250230169 · 2025-07-17 ·

The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Anti-TNF alpha antibodies which selectively inhibit TNF alpha signalling through the p55R

The present invention provides anti-TNFα antibodies which selectively inhibit TNFα signalling through the p55R. In particular the present invention provides anti-TNFα antibodies which selectively inhibit TNFα signalling through the p55R relative to the p75R.

Nanoparticle and polymer formulations for thyroid hormone analogs, antagonists, and formulations and uses thereof
09839614 · 2017-12-12 · ·

Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric nanoparticle form of thyroid hormone agonist, partial agonist or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Nanoparticle forms of thyroid hormone or thyroid hormone analogs as well as uses thereof are also disclosed.

Methods of inducing indolamine 2,3—dioxygenase (IDO)
09839674 · 2017-12-12 · ·

A composition and method for using a composition, the composition having at least two compounds, each of which induces indolamine 2,3-dioxygenase, for the treatment of an autoimmune disorder or disease or immune rejection of transplants or gene therapeutically modified cells, wherein the inducers have different mechanism of action and wherein the composition gives rise to a synergistic effect on the IDO levels.

Compositions and methods for altering second messenger signaling

The present disclosure provides, among other things, novel cyclic-GMP-AMP (cGAMP) analogs, mimics, mimetics and variants, and compositions and kits thereof; methods of using the compounds as described herein for treating cancer, and immune disease, disorders, or conditions; methods of using the compounds as described herein for modulating cGAS and STING; and methods of designing or characterizing a cGAS modulator.

IMIDAZOLOTHIAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASE

Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.

COMPOUNDS ACTIVE TOWARDS BROMODOMAINS

Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

##STR00001##

PHARMACEUTICAL COMBINATION COMPRISING A SELECTIVE S1P1 RECEPTOR AGONIST
20170348287 · 2017-12-07 · ·

The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.

Inhibitors of T-cell activation

The present invention provides a bispecific biologic comprising a ligand specific for CTLA-4 and a ligand specific for a pMHC complex.