54591-62-7Relevant articles and documents
Compound with dual inhibitory activity TDO, IDOO1 and application of compound for treating neurodegenerative disease (by machine translation)
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Paragraph 0083; 0116-0119, (2020/10/06)
The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof, or a solvate thereof, which can selectively inhibit TDO, IDOO1, which has a significant inhibitory effect on TDO and/or IDOO1. In addition, the prepared compound has a remarkable anti-tumor effect, has a certain treatment effect on's disease and's disease, and has a good application prospect in the field of medicine preparation. (by machine translation)
PROLYL HYDROXYLASE INHIBITORS
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Page/Page column 16-17, (2010/07/10)
The invention described herein relates to certain 2,4-dioxo-l,2,3,4-tetrahydro-7- quinazolinecarboxamide derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
2-IMIDAZOLINE, 2-OXAZOLINE, 2-THIAZOLINE, AND 4-IMIDAZOLE DERIVATIVES OF METHYLPHENYL, METHOXYPHENYL, AND AMINOPHENYL ALKYLSULFONAMIDES AND UREAS AND THEIR USE
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, (2008/06/13)
The present invention concerns novel compounds represented by the Formula: STR1 wherein: A is R 1 q (R 3 R 60 N). sub.m (Z)(NR 2) n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C=O or SO 2 ; n is 1 with the proviso that, when Z is C=O, m is 1; X is--NH--,--CH 2--, or--OCH 2--; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R 1 is H, lower alkyl, or phenyl, with the proviso that, when R 1 is H, m is 1; R 2, R 3, R 60 are each independently H, lower alkyl, or phenyl; R 4, R 5, R. sup.6, and R 7 are each independently hydrogen, lower alkyl,--CF. sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R. sup.2 and R 7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5-or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or--CN, with the proviso that, when R 7 is hydroxyl or lower alkylsulfonamido, then X is not--NH--when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R 1 SO 2 NR 2--), (R. sup.3 R 60 NSO 2 NR 2--), or (R 3 R 60 NCONR 2--). The invention also includes the use of the above compounds, and compositions containing them, as alpha 1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.