C07D295/205

METHODS FOR SYNTHESIZING N-(PHENYLSULFONYL)BENZAMIDE COMPOUNDS AND INTERMEDIATES THEREOF

Disclosed is a method for synthesizing N-(phenylsulfonyl)benzamide compound and intermediate thereof. The method comprises a method for synthesizing a compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain the compound 1; wherein R is C.sub.1-C.sub.8 alkyl. The present disclosure synthesizes three intermediate compounds required by the target compound and their preparation methods for the first time. Using the method disclosed in the present disclosure to synthesize the target compound 3 has the advantages of high yield, good purity, easy-to-obtain reaction raw materials, suitable for industrial production.

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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.

CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
20170342230 · 2017-11-30 ·

A chemical blowing agent is described that includes at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can, for example, be incorporated into thermally expandable baffle and/or reinforcement elements, which can be used in automotive manufacturing and building insulation.

CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
20170342230 · 2017-11-30 ·

A chemical blowing agent is described that includes at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can, for example, be incorporated into thermally expandable baffle and/or reinforcement elements, which can be used in automotive manufacturing and building insulation.

Substituted inhibitors of menin-MLL and methods of use

The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins with compositions of Formula (II-A). The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions of Formula (II-A) for use in these methods are also provided. ##STR00001##

COMPOUND AS A UBR BOX DOMAIN LIGAND

The present specification relates to a compound as a UBR box domain ligand. The present specification provides a small molecule compound that binds to the UBR box domain. Further, the present specification provides a composition for inhibiting UBR box domain substrate binding, including a ligand compound that binds to a UBR box domain, a pharmaceutical composition for treating UBR-related disease, and a use thereof.

RHEIN AMIDE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF, AND INHIBITOR OF HEPATOCELLULAR CARCINOMA (HCC) WITH SPECIFIC RECQL4 EXPRESSION

A rhein amide derivative and a preparation method and use thereof, and a drug for treating hepatocellular carcinoma (HCC) caused by a specific expression of RECQL4. The rhein amide derivative has a structure shown in any one of formulas I to IV. The rhein amide derivative has a relatively strong inhibitory effect on proliferation of HCC cells SNU-398 with RECQL4 high expression. Development of a novel anti-cancer drug for RECQL4 high expression-caused HCC and clinical personalized treatment of the RECQL4 high expression-caused HCC.

NOVEL MITOCHONDRIAL UNCOUPLERS FOR TREATMENT OF METABOLIC DISEASES AND CANCER
20170334869 · 2017-11-23 ·

The present disclosure relates to benzamide compounds, prodrugs of the compounds, pharmaceutical compositions containing the compounds and/or the prodrugs and methods of using the compounds, prodrugs and pharmaceutical compositions in the treatment of diseases related to lipid metabolism including diabetes, Non-Alcholic Fatty Liver Disease (NAFLD), Non-Alcholic Steathohepatitis (NASH), diseases caused by abnormal cell proliferation including cancer, psoriasis, and infectious diseases.

NOVEL MITOCHONDRIAL UNCOUPLERS FOR TREATMENT OF METABOLIC DISEASES AND CANCER
20170334869 · 2017-11-23 ·

The present disclosure relates to benzamide compounds, prodrugs of the compounds, pharmaceutical compositions containing the compounds and/or the prodrugs and methods of using the compounds, prodrugs and pharmaceutical compositions in the treatment of diseases related to lipid metabolism including diabetes, Non-Alcholic Fatty Liver Disease (NAFLD), Non-Alcholic Steathohepatitis (NASH), diseases caused by abnormal cell proliferation including cancer, psoriasis, and infectious diseases.

STAT3 inhibitors and their anticancer use

In one aspect, the invention relates to substituted 6-amino-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide analogs and derivatives thereof, substituted 4-amino-5H-naphtho[1,8-cd]isothiazol-5-one 1,1-dioxide analogs and derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.