C07D213/58

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##

Imaging contrast agents and uses thereof

Provided are macrocyclic compounds having a macrocyclic core which has at least one macrocyclic donor and at least one pendant group which has at least one donor group. The macrocyclic compounds can be complexed to Fe(II) and Ni(II). The macrocyclic compounds can be used in imaging methods. For example, the compounds can be used MRI paraCEST contrast agents.

Imaging contrast agents and uses thereof

Provided are macrocyclic compounds having a macrocyclic core which has at least one macrocyclic donor and at least one pendant group which has at least one donor group. The macrocyclic compounds can be complexed to Fe(II) and Ni(II). The macrocyclic compounds can be used in imaging methods. For example, the compounds can be used MRI paraCEST contrast agents.

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:

##STR00001##

wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:

##STR00001##

wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Amido compounds as RORγt modulators and uses thereof

Amido compounds are disclosed that have a formula represented by the following: ##STR00001##
and wherein Cy.sup.1, Cy.sup.2, n1, n2, R.sup.1a, R.sup.1b, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.

Amido compounds as RORγt modulators and uses thereof

Amido compounds are disclosed that have a formula represented by the following: ##STR00001##
and wherein Cy.sup.1, Cy.sup.2, n1, n2, R.sup.1a, R.sup.1b, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.