A61K31/438

TREATMENT OF GASTROPARESIS WITH TRIAZASPIRO[4.5]DECANONE
20230114615 · 2023-04-13 ·

Provided herein is a method of treating or alleviating one or more symptoms of a disorder, disease, or condition mediated by a dopamine D.sub.2 or D.sub.3 receptor with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof. Also provided herein is a method of increasing the serum prolactin level with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof.

TREATMENT OF GASTROPARESIS WITH TRIAZASPIRO[4.5]DECANONE
20230114615 · 2023-04-13 ·

Provided herein is a method of treating or alleviating one or more symptoms of a disorder, disease, or condition mediated by a dopamine D.sub.2 or D.sub.3 receptor with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof. Also provided herein is a method of increasing the serum prolactin level with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof.

SSTR5 ANTAGONISTS

This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

SSTR5 ANTAGONISTS

This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

SSTR5 ANTAGONISTS

This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

USE OF JAK INHIBITORS IN PREPARATION OF DRUGS FOR TREATING JAK KINASE-RELATED DISEASES

Disclosed is the use of a JAK inhibitor [1,2,4]-triazolo-[1,5-a]0pyridine compound in the preparation of drugs for treating autoimmune, inflammatory or allergic diseases, or diseases such as transplant rejection. The JAK inhibitor [1,2,4]-triazolo-[1,5-a]-pyridine compound comprises a compound as shown in formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof. The JAK inhibitor has a good efficacy in animal model tests of diseases such as autoimmune, inflammatory or allergic diseases.

USE OF JAK INHIBITORS IN PREPARATION OF DRUGS FOR TREATING JAK KINASE-RELATED DISEASES

Disclosed is the use of a JAK inhibitor [1,2,4]-triazolo-[1,5-a]0pyridine compound in the preparation of drugs for treating autoimmune, inflammatory or allergic diseases, or diseases such as transplant rejection. The JAK inhibitor [1,2,4]-triazolo-[1,5-a]-pyridine compound comprises a compound as shown in formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof. The JAK inhibitor has a good efficacy in animal model tests of diseases such as autoimmune, inflammatory or allergic diseases.

3-substituted piperidine compounds for Cbl-b inhibition, and use thereof

Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.

3-substituted piperidine compounds for Cbl-b inhibition, and use thereof

Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.

Indolizine derivatives and their application in medicine

This invention relates to indolizine derivatives and their use in medicine. In particular, the present invention discloses novel substituted indolizine derivatives of formula I, or an isotopically labeled compound thereof, or an optical isomer thereof, a geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. The invention also relates to the use of these compounds in medicine. ##STR00001##