1290117-21-3Relevant academic research and scientific papers
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).
IMMUNOMODULATOR
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Paragraph 0059; 0064; 0091-0092, (2021/12/18)
The present application discloses an immunomodulator, and specifically discloses a compound depicted by formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The compound provided in the present application can bind effectively to STING and has a good agonistic action on STING protein, and exhibits a good inhibitory effect on multiple tumors. Thus, the compound provided in the present application serves as a STING agonist and can be used for treating various related conditions. The compound provided in the present invention shows a very promising prospect for application thereof in the preparation of a medicament for treating a disease associated with STING activity (in particular, a medicament for treating an inflammatory disease, an allergic disease, an autoimmune disease, an infectious disease, a cancer or a precancerous syndrome) and in the preparation of an immune adjuvant, providing a novel option for clinically screening and/or preparing drugs for diseases associated with STING activity.
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.
COMPOUNDS FOR TREATING CERTAIN LEUKEMIAS
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Paragraph 0616-0617, (2020/03/28)
Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their
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.
INDOLE COMPOUNDS OR ANALOGUES THEREOF USEFUL FOR THE TREATMENT OF AGE-RELATED MACULAR DEGENERATION (AMD)
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Page/Page column 240-241, (2012/07/27)
The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
