301666-81-9

Upstream product

• 1184950-48-8 3-bromo-6-(tert-butoxycarbonyl)-5,6,7,8-tetrahydro-1,6-naphthyridine 
• 625100-00-7 3-bromo-5,6,7,8-tetrahydro-1,6-naphthyridine 
• 129477-21-0 ethyl 5-bromo-2-methyl-pyridine-3-carboxylate 

Relevant academic research and scientific papers

Protein arginine methyltransferase 5 (PRMT5) inhibitor, pharmaceutical products thereof, and methods thereof

The present invention provides a PRMT5 inhibitor of formula (I); R1 is a non-hydrogen monovalent group; W is a direct bond or-NH-; T, U and V are independently from each other selected from C and N; R2 is H or halogen; m is 1 or 2; X is carbon, nitrogen or oxygen; Y is C or N; Z is a direct bond or carbon; R3 is H, a non-hydrogen monovalent group, an oxo group, a divalent spiro-forming group or adivalent bridge-forming group; and n is 1 or 2, and represents a single or double bond. The present invention also provides pharmaceutical products comprising the PRMT5 inhibitor and use thereof in the treatment of proliferative disorders such as cancer, metabolic disorders, hematological disorders, autoimmune diseases and inflammatory diseases.

INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5), PHARMACEUTICAL PRODUCTS THEREOF, AND METHODS THEREOF

The present invention provides PRMT5 inhibitors of Formula (I), wherein R1 is a non-hydrogen monovalent group; W is a direct bond or -NH-; T, U, and V are independently of each other selected from C and N; R2 is H or a halo; m is 1 or 2; X is a carbon, a nitrogen, or an oxygen; Y is C or N; Z is a direct bond or a carbon; R3 is H, a non-hydrogen monovalent group, an oxo group, a bivalent spiro ring-forming group, or a bivalent bridge-forming group; n is 1 or 2; and Formula (II) stands for a single bond or a double bond. Pharmaceutical products comprising the PRMT5 inhibitors and use thereof in treating proliferative disorders such as cancer, metabolic disorders, blood disorders, autoimmune diseases, and inflammatory diseases are also provided.

ISOQUINOLIN AND NAPHTHYDRIN COMPOUNDS

The present invention provides a compound of Formula I I wherein X is selected from the group consisting of CH and N; Q is selected from the group consisting of CH3 and H; R is selected from the group consisting of and; or a pharmaceutically acceptable salt thereof, compositions, methods to treat liver disease and NASH.

NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND BENAMIDE COMPOUNDS AND DRUGS CONTAINING THE SAME

Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form -(CH2)m-, -N=CH-, -CH=N-, or -(C1-6 alkyl)C=N-; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group -C(=O)N(R5)R6 or group -C(=O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, -SO2-, -SO-, -CH2-CH2-, or - CH=CH-, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents - (CH2)n-, -O-(CH2)i-, or -C(=O)NH-(CH2)i-.