C07D235/24

MIF MODULATORS
20180162813 · 2018-06-14 ·

The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.

Fused ring analogues of anti-fibrotic agents

The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Fused ring analogues of anti-fibrotic agents

The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Benzimidazole and imadazopyridine carboximidamide compounds

The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: ##STR00001##
or pharmaceutically acceptable salts thereof, in which X, L, n, m, R.sup.1, R.sup.2a, R.sup.2b, R.sup.n, R.sup.m, and R.sup.t are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

Benzimidazole and imadazopyridine carboximidamide compounds

The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: ##STR00001##
or pharmaceutically acceptable salts thereof, in which X, L, n, m, R.sup.1, R.sup.2a, R.sup.2b, R.sup.n, R.sup.m, and R.sup.t are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

Compounds for affinity chromatography and for extending the half-life of a therapeutic agent

Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.

Compounds for affinity chromatography and for extending the half-life of a therapeutic agent

Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.

Selective D3 dopamine receptor agonists and methods of their use

The disclosure of a compound of Formula I or a pharmaceutically acceptable salt thereof ##STR00001## The variables W, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the disclosure. The disclosure provides a compound or salt of Formula I together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula I is administered to the patient together with one or more additional active agents.

Selective D3 dopamine receptor agonists and methods of their use

The disclosure of a compound of Formula I or a pharmaceutically acceptable salt thereof ##STR00001## The variables W, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the disclosure. The disclosure provides a compound or salt of Formula I together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula I is administered to the patient together with one or more additional active agents.

BICYCLIC COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS
20240368137 · 2024-11-07 ·

Provided herein are compounds that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease