C07D211/14

ANTAGONISTS OF GPR39 PROTEIN

Novel compounds that act as antagonists to human GPR39 protein are disclosed. Pharmaceutical compositions and methods of use for antagonists to human GPR39 protein are disclosed. In particular, methods of using the antagonists in the treatment of diseases or conditions including cardiovascular conditions, endocrine system and hormone disorders, cancer disorders, metabolic diseases, gastrointestinal and liver diseases, hematological disorders, neurological disorders and respiratory diseases are disclosed herein.

ArylSulfonamide-based matrix metalloprotease inhibitors

The present invention provides a compound of formula (I): ##STR00001##
said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

PHENYL-(AZA)CYCLOALKYL CARBOXYLIC ACID GPR120 MODULATORS
20170327457 · 2017-11-16 ·

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

##STR00001##

PHENYL-(AZA)CYCLOALKYL CARBOXYLIC ACID GPR120 MODULATORS
20170327457 · 2017-11-16 ·

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

##STR00001##

COMPOSITE PREPARATION, CONTAINING NOVEL 3-(4--(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE AND ANOTHER ACTIVE INGREDIENT, FOR PREVENTING OR TREATING METABOLIC DISEASES

The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.

COMPOSITE PREPARATION, CONTAINING NOVEL 3-(4--(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE AND ANOTHER ACTIVE INGREDIENT, FOR PREVENTING OR TREATING METABOLIC DISEASES

The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.

(DI)AMINATION OF ACTIVATED ALLENE COMPOUNDS, DERIVATIVES THEREOF, AND METHODS FOR SYNTHESIS OF THE SAME
20230174506 · 2023-06-08 ·

One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.

(DI)AMINATION OF ACTIVATED ALLENE COMPOUNDS, DERIVATIVES THEREOF, AND METHODS FOR SYNTHESIS OF THE SAME
20230174506 · 2023-06-08 ·

One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.

Method for preparing methylated amines

The present invention relates to a method for preparing methylated amines using carbon dioxide and to the use of the method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres and synthetic leathers, pesticides and fertilisers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres, synthetic leathers, pesticides and fertilisers, including a step of preparing methylated amines by the method according to the invention. The present invention also relates to a method for preparing marked methylated amines and to the uses thereof.

Method for preparing methylated amines

The present invention relates to a method for preparing methylated amines using carbon dioxide and to the use of the method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres and synthetic leathers, pesticides and fertilisers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres, synthetic leathers, pesticides and fertilisers, including a step of preparing methylated amines by the method according to the invention. The present invention also relates to a method for preparing marked methylated amines and to the uses thereof.