76196-68-4Relevant academic research and scientific papers
SUBSTITUTED BENZAMIDES AS MODULATORS OF TREX1
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Paragraph 0094-0095, (2021/12/08)
Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.
1,3,4-OXADIAZOLE SULFONAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 2265; 2266; 2267, (2017/02/24)
The present invention relates to novel compounds represented by the formula I having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. (I) The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases.
LSD1 INHIBITORS AND USES THEREOF
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, (2016/11/17)
Provided are novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSDl. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSDl.
Medicinal Chemical Studies on Antiplasmin Drugs. VI. Aza Analogs of 4-Aminomethylbenzoic Acid
Isoda, Sumiro,Yamaguchi, Hitoshi,Satoh, Yoshinari,Miki, Tosaku,Hirata, Miyoshi
, p. 1408 - 1414 (2007/10/02)
Four aza analogs of 4-aminomethylbenzoic acid (1) were prepared as part of a search for new antiplasmin drugs. 5-Aminomethylpyridine-2-carboxylic acid (5) was prepared by the hydrogenation of methyl 5-cyanopyridine-2-carboxylate (4), followed by alkaline hydrolysis.Similarly, 6-aminomethylpyridine-3-carboxylic acid (7) was prepared from ethyl 6-cyanopyridine-3-carboxylate (6). 5-Aminomethylpyrimidine-2-carboxylic acid (12) was obtained from methyl 5-methylpyrimidine-2-carboxylate (8) via the phthalimido derivative (10). 2-Aminomethylpyrimidine-5-carboxylic acid (25) was obtained by the reaction of benzyloxycarbonylaminoacetamidine (22) with ethoxycarbonylmalonaldehyde (18) in acetic acid, followed by deblocking of the protected groups.Treatment of benzoylaminoacetamidine (14) with acetylacetone (15) in acetic acid provided 2-benzoylaminomethyl-4,6-dimethylpyrimidine (16), whereas in the presence of K2CO3, 2-amino-3-benzoylamino-4,6-dimethylpyridine (17) was obtained together with a trace of 16.No compound showed more potent antiplasmin activity than tranexamic acid (2), but 5 was more active than 1.Keywords - antiplasmin drug; 4-aminomethylbenzoic acid; tranexamic acid; bioisostere; aminomethylpyridinecarboxylic acid; aminomethylpyrimidinecarboxylic acid; pyridine ring closure; pyrimidine ring closure; benzoylaminoacetamidine; benzyloxycarbonylaminoacetamidine
