C07D407/04

Method for producing intermediate useful for synthesis of SGLT inhibitor

A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.

FLAVAN-3-OL ANALOGS AND ANTI-INFLAMMATORY ACTIVITY
20230159482 · 2023-05-25 ·

Provided herein are compounds useful in the treatment of inflammatory diseases, pharmaceutical compositions comprising the same, and methods of use and preparation thereof. The compounds exhibit inhibitory effects on the expression and secretion of pro-inflammatory cytokines, such as IL-1β, IL-6 and TNF-α.

FLAVAN-3-OL ANALOGS AND ANTI-INFLAMMATORY ACTIVITY
20230159482 · 2023-05-25 ·

Provided herein are compounds useful in the treatment of inflammatory diseases, pharmaceutical compositions comprising the same, and methods of use and preparation thereof. The compounds exhibit inhibitory effects on the expression and secretion of pro-inflammatory cytokines, such as IL-1β, IL-6 and TNF-α.

PRODRUGS, ANALOGS OR DERIVATIVES OF KAEMPFEROL AS ANTIVIRAL AGENTS
20230064951 · 2023-03-02 ·

The present invention relates to compounds which can inhibit host cell ACE2 receptor, viral spike S protein, Spike protein-ACE2 receptor interface, RNA-dependent RNA polymerase (RdRp), helicase and exoribonuclease activity. Particularly the invention relates to kaempferol analogs, derivatives and prodrugs as antiviral agents specific to Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) or SARS-CoV-2 and SARS (Severe, acute respiratory syndrome coronavirus).

PRODRUGS, ANALOGS OR DERIVATIVES OF KAEMPFEROL AS ANTIVIRAL AGENTS
20230064951 · 2023-03-02 ·

The present invention relates to compounds which can inhibit host cell ACE2 receptor, viral spike S protein, Spike protein-ACE2 receptor interface, RNA-dependent RNA polymerase (RdRp), helicase and exoribonuclease activity. Particularly the invention relates to kaempferol analogs, derivatives and prodrugs as antiviral agents specific to Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) or SARS-CoV-2 and SARS (Severe, acute respiratory syndrome coronavirus).

2-SUBSTITUTED AMINO-NAPHTH (1,2-D) IMIDAZOL-5-ONE COMPOUNDS OF PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
20230116786 · 2023-04-13 ·

Provided herein are therapeutic and/or prophylactic compounds for mitochondrial or oxidative stress diseases such as cancer, amyotropic lateral sclerosis, Creutzfeldt-Jakob disease, Machado-Joseph disease, spinocerebellar ataxia, Huntington disease, Parkinson disease, Alzheimer disease, myocardial infarction, cerebral infarction, diseases related to aging, diabetes, alcoholic liver injury, chronic obstructive pulmonary disease, mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and the like, wherein the compound is represented by formula (1), or reduced forms thereof, or pharmaceutically acceptable salts thereof.

##STR00001##

2-SUBSTITUTED AMINO-NAPHTH (1,2-D) IMIDAZOL-5-ONE COMPOUNDS OF PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
20230116786 · 2023-04-13 ·

Provided herein are therapeutic and/or prophylactic compounds for mitochondrial or oxidative stress diseases such as cancer, amyotropic lateral sclerosis, Creutzfeldt-Jakob disease, Machado-Joseph disease, spinocerebellar ataxia, Huntington disease, Parkinson disease, Alzheimer disease, myocardial infarction, cerebral infarction, diseases related to aging, diabetes, alcoholic liver injury, chronic obstructive pulmonary disease, mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and the like, wherein the compound is represented by formula (1), or reduced forms thereof, or pharmaceutically acceptable salts thereof.

##STR00001##

MGluR7 agonist compounds for treating mGluR7-regulated diseases, disorders, or conditions

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof ##STR00001##
wherein Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy. The present invention further provides methods of treating at least one disease, disorder, or condition associated with the glutamatergic and GABAergic signalling pathways regulated in full or in part by metabotropic glutamate receptor 7 (mGluR7) by administering a compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject. The compound may be a selective agonist of mGluR7, which modulates the release of at least one neurotransmitter in the subject.

MGluR7 agonist compounds for treating mGluR7-regulated diseases, disorders, or conditions

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof ##STR00001##
wherein Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy. The present invention further provides methods of treating at least one disease, disorder, or condition associated with the glutamatergic and GABAergic signalling pathways regulated in full or in part by metabotropic glutamate receptor 7 (mGluR7) by administering a compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject. The compound may be a selective agonist of mGluR7, which modulates the release of at least one neurotransmitter in the subject.

PROCESSES FOR THE PREPARATION OF ORTHO-ALLYLATED HYDROXY ARYL COMPOUNDS

The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).

##STR00001##