C07D451/00

THERAPEUTIC COMPOUNDS AND SYNTHESIS

The invention provides compounds of Formula 1:

##STR00001##

or a stereoisomer, pharmaceutically acceptable salt, or mixture thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

THERAPEUTIC COMPOUNDS FOR PAIN AND SYNTHESIS THEREOF

The invention provides compounds of Formula 1:

##STR00001##

and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

THERAPEUTIC COMPOUNDS FOR PAIN AND SYNTHESIS THEREOF

The invention provides compounds of Formula 1:

##STR00001##

and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

THERAPEUTIC COMPOUNDS FOR PAIN AND SYNTHESIS THEREOF

The invention provides compounds of Formula 1:

##STR00001##

and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

THERAPEUTIC COMPOUND FOR PAIN AND SYNTHESIS THEREOF

The invention provides compounds of Formula XXIII:

##STR00001##

wherein R.sub.1 is hydrogen, alkyl, acyl, or silyl, R.sub.2 is hydrogen, alkyl, benzyl, acyl, or ester, and R.sub.3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Compounds and methods for treating diabetes

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor .sub.2A. The compounds may also bind to and are an antagonist of the adrenergic receptor .sub.2B; or the compounds are not antagonists of the adrenergic receptor .sub.2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

Compounds and methods for treating diabetes

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor .sub.2A. The compounds may also bind to and are an antagonist of the adrenergic receptor .sub.2B; or the compounds are not antagonists of the adrenergic receptor .sub.2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

HETEROCYCLIC GLP-1R AGONISTS

Disclosed herein are heterocyclic compounds that activate GLP-1R pathways. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the GLP-1R agonists are disclosed, alone or in combination with other therapeutic agents, for the treatment of diabetes, obesity, and other diseases or conditions dependent on GLP-1R pathways.