The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

The present disclosure relates to compositions comprising a transient receptor potential vanilloid-1 (TRPV1) antagonist and an alpha-2 adrenoreceptor agonist useful in the treatment of various forms of pain, including chronic pain (CP) syndromes, inflammatory pain and pain associated with neuropathy and other diseases and disease states; and methods of use thereof.

The present disclosure relates to compositions comprising a transient receptor potential vanilloid-1 (TRPV1) antagonist and an alpha-2 adrenoreceptor agonist useful in the treatment of various forms of pain, including chronic pain (CP) syndromes, inflammatory pain and pain associated with neuropathy and other diseases and disease states; and methods of use thereof.

The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.

The invention relates to compounds of formula (I):

##STR00001##

or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

The invention relates to compounds of formula (I):

##STR00001##

or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

The present invention relates to a compound exhibiting STAT3 inhibitory activity, or a pharmaceutically acceptable salt, solvate or hydrate of the same, and pharmaceutical uses of these. The compounds of the present invention efficiently inhibit the abnormal activity of STAT3 associated with various diseases and thus can be usefully utilized for the prevention and treatment of various STAT3-related diseases associated with cancer, autoimmune diseases, inflammatory diseases and the like.

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Provided is a process for synthesizing a functionalized cyclic dithiocarbamate.