C07C229/46

Modulators of liver receptor homologue 1 (LRH-1) and uses

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.

Pharmaceutically active compounds

The invention is directed to compounds of general formula (I) ##STR00001##
and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Pharmaceutically active compounds

The invention is directed to compounds of general formula (I) ##STR00001##
and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Tetrahydronaphthalene derivative

A compound of general formula (I-1): ##STR00001## wherein the symbols are defined in the specification, has a selective S1P.sub.5 receptor binding activity and modulates the function of an S1P.sub.5 receptor, and can therefore be a therapeutic agent for a S1P.sub.5-mediated disease, for example, neurodegenerative diseases such as schizophrenia, Binswanger's disease and the like.

Tetrahydronaphthalene derivative

A compound of general formula (I-1): ##STR00001## wherein the symbols are defined in the specification, has a selective S1P.sub.5 receptor binding activity and modulates the function of an S1P.sub.5 receptor, and can therefore be a therapeutic agent for a S1P.sub.5-mediated disease, for example, neurodegenerative diseases such as schizophrenia, Binswanger's disease and the like.

Production method for 1-amino cyclopropane carboxylic acid nonhydrate

1-Aminocyclopropanecarboxylic acid non-hydrate can be obtained by treating 1-aminocyclopropanecarboxylic acid hydrochloride with a tertiary amine in the presence of a C.sub.3-C.sub.4 alcohol and water, keeping the reaction mixture at 50 C. or below, collecting the precipitated crystal of 1-aminocyclopropanecarboxylic acid 0.5 hydrate by filtration, and heating the obtained crystal to 80 to 245 C.

Production method for 1-amino cyclopropane carboxylic acid nonhydrate

1-Aminocyclopropanecarboxylic acid non-hydrate can be obtained by treating 1-aminocyclopropanecarboxylic acid hydrochloride with a tertiary amine in the presence of a C.sub.3-C.sub.4 alcohol and water, keeping the reaction mixture at 50 C. or below, collecting the precipitated crystal of 1-aminocyclopropanecarboxylic acid 0.5 hydrate by filtration, and heating the obtained crystal to 80 to 245 C.

PRODUCTION METHOD FOR 1-AMINO CYCLOPROPANE CARBOXYLIC ACID NONHYDRATE

1-Aminocyclopropanecarboxylic acid non-hydrate can be obtained by

treating 1-aminocyclopropanecarboxylic acid hydrochloride with a tertiary amine in the presence of a C.sub.3-C.sub.4 alcohol and water, keeping the reaction mixture at 50 C. or below,
collecting the precipitated crystal of 1-aminocyclopropanecarboxylic acid 0.5 hydrate by filtration, and heating the obtained crystal to 80 to 245 C.

INHIBITOR OF INDOLEAMINE-2,3-DIOXYGENASE (IDO)
20200046697 · 2020-02-13 ·

The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating a disease associated with IDO, for example, cancer or an infectious disease (e.g., viral or bacterial infectious diseases). Also, provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

##STR00001##

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.