1290117-21-3Relevant articles and documents
N-CYCLOHEXYL-5-(THIAZOL-5-YL)-1H-INDOLE-7-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS CD38 INHIBITORS FOR INCREASING NAD+ AND FOR THE TREATMENT OF E.G. MUSCULAR DISORDERS
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Page/Page column 103-104, (2021/05/07)
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+ 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).
Macro-cyclic immuno-modulator
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Paragraph 0234-0237; 0243-0247, (2020/08/12)
The invention provides a macro-cyclic immuno-modulator, and discloses a compound shown as a formula I, and a tautomer, an enantiomer, a pharmaceutically acceptable salt, a crystal form, hydrate or solvate thereof. Experiment results show that the compound can be effectively combined with STING and has a good STING protein excitation function. Therefore, the compound can be used as an STING agonist, can be used to treat various related diseases, and has a very good application prospect in preparing medicines for treating diseases related to STING activity, especially medicines for treating inflammatory and autoimmune diseases, infectious diseases, cancers or precancerous syndromes.
STK4 INHIBITORS FOR TREATMENT OF HEMATOLOGIC MALIGNANCIES
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Paragraph 00719, (2017/01/09)
The application relates to compounds of Formula (I'): which modulate the activity of a kinase (e.g., STK4), a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of a kinase, such as STK4.