C07D403/10

3,3-difluoroallylamines or salts thereof and pharmaceutical compositions comprising the same

The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

CD38 INHIBITORS
20230025807 · 2023-01-26 ·

The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD.sup.+ or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).

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CD38 INHIBITORS
20230025807 · 2023-01-26 ·

The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD.sup.+ or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).

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FXIA INHIBITORS AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF

Provided in the present invention is a series of selective Factor XIa (FXIa) inhibitors, relating to the technical field of chemical drugs. The present invention also relates to pharmaceutical compositions containing said compounds and a use of said compounds in drugs for the treatment of diseases such as thromboembolism.

Carboxylic Acid Containing Azetidinyl Compounds for the Treatment of Neurodegenerative Diseases

Provided herein are compounds and compositions thereof for modulating S1P5. In some embodiments, the compounds and compositions are provided for treatment of neurological diseases.

Carboxylic Acid Containing Azetidinyl Compounds for the Treatment of Neurodegenerative Diseases

Provided herein are compounds and compositions thereof for modulating S1P5. In some embodiments, the compounds and compositions are provided for treatment of neurological diseases.

Light-Emitting Device and Light-Emitting Apparatus

A light-emitting device with high resistance to heat in a fabrication process is provided. The light-emitting device includes an EL layer between an anode and a cathode. The EL layer includes at least a light-emitting layer and an electron-transport layer that includes a first electron-transport layer in contact with the light-emitting layer and a second electron-transport layer in contact with the first electron-transport layer. The first electron-transport layer includes a first heteroaromatic compound including at least one heteroaromatic ring. The second electron-transport layer includes a second heteroaromatic compound that includes at least one heteroaromatic ring and is different from the first heteroaromatic compound. The first heteroaromatic compound has a difference of 20° C. or less between the crystallization temperature (Tpc) of a powder state and the crystallization temperature (Ttc) of a thin film state. The second heteroaromatic compound has a difference of 100° C. or less between Tpc and Ttc.

Light-Emitting Device and Light-Emitting Apparatus

A light-emitting device with high resistance to heat in a fabrication process is provided. The light-emitting device includes an EL layer between an anode and a cathode. The EL layer includes at least a light-emitting layer and an electron-transport layer that includes a first electron-transport layer in contact with the light-emitting layer and a second electron-transport layer in contact with the first electron-transport layer. The first electron-transport layer includes a first heteroaromatic compound including at least one heteroaromatic ring. The second electron-transport layer includes a second heteroaromatic compound that includes at least one heteroaromatic ring and is different from the first heteroaromatic compound. The first heteroaromatic compound has a difference of 20° C. or less between the crystallization temperature (Tpc) of a powder state and the crystallization temperature (Ttc) of a thin film state. The second heteroaromatic compound has a difference of 100° C. or less between Tpc and Ttc.

5-membered heteroaryl carboxamide compounds for treatment of HBV

The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

5-membered heteroaryl carboxamide compounds for treatment of HBV

The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.