- FUMARATE SALT OF (R)-3-(1-(2,3-DICHLORO-4-(PYRAZIN-2-YL)PHENYL)-2,2,2-TRIFLUOROETHYL)-1-METHYL-1-(1-METHYLPIPERIDIN-4-YL) UREA, METHODS OF PREPARATION, AND USES THEREOF
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Provided are various embodiments relating to fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, and methods of producing and using the same to treat conditions and disorders associated with an increase of ghrelin level, such as food abuse, alcohol addiction, and other disorders (e.g., Prader-Willi syndrome). Also provided are various embodiments relating to crystalline HM04 free base, different crystalline forms of HM04 fumarate salt, and methods of producing the same.
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Paragraph 00104; 00132; 00133
(2019/07/19)
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- 5-HT2C receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs
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Agonists of the 5-HT2C receptor have attracted much attention as therapeutic agents for the treatment of obesity. Subtype selectivity against other 5-HT2 receptors is one of the most important prerequisites for reducing side effects. We present the synthesis of N-methyl-N-(1- methylpiperidin-4-yl)benzenesulfonamide analogs and their structure-activity relationship studies on 5-HT2A and 5-HT2C receptors. Although the compounds showed nanomolar activity to the 5-HT2C receptor, their selectivity against the 5-HT2A receptor was modest to low. Molecular modeling studies using homology modeling and docking simulation revealed that selectivity originated from subtype specific residues. The observed binding modes and receptor-ligand interactions provided us a clue for optimizing the selectivity against the 5-HT2A receptor.
- Jang, Jae Wan,Baek, Je-Sook,Choi, Gil Don,Park, Woo-Kyu,Cho, Yong Seo,Baek, Du-Jong,Pae, Ae Nim
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experimental part
p. 347 - 352
(2012/02/04)
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- Tetracyclic benzimidazole derivatives and combinatorial libraries thereof
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The present invention relates to novel tetracyclic benzimidazole derivative compounds of the following formula: wherein R1to R10have the meanings described in here. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing tetracyclic benzimidazole derivative compounds.
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- Benzenesulfonamide derivatives and their use as MEK inhibitors
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Benzenesulfonamides of formula (I), in which W is OR1, NR2OR1, NRARB, NR2NRARB, or NR2(CH2)2-4NRARBand the other variables as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.
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- SUBSTITUTED THIENOBENZODIAZEPINONES AND SALTS THEREOF
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Compounds of the formula STR1 wherein R is 1-methyl-4-piperididinyl, 4-methyl-1-piperazinyl, or 3-or 3-tropanyl, each of which may optionally have another methyl substituent attached to the heterocyclic ring;R 1 is hydrogen or alkyl of 1 to 4 carbon atoms;R 2 is hydrogen, halogen or alkyl of 1 to 4 carbon atoms; andX is oxygen,--NH--or--N(CH. sub.3)--;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
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