- NOVEL IMIDAZOLE COMPOUND AND USE THEREOF AS MELANOCORTIN RECEPTOR AGONIST
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The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I] [wherein: Ring A represents an optionally substituted aryl group or the like; R1 represents a hydrogen atom, an optionally substituted alkyl group, or the like; R2 represents a hydrogen atom, a halogen atom, or the like; and R3 represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.
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- Pharmaceutical compositions (by machine translation)
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[Problem] imidazole compound or its pharmacologically acceptable salt in the melanocortin receptor activity that operates as an active ingredient of a pharmaceutical composition comprising. "I" general formula [a]" Formula, the aryl group may be substituted A ring represents a; R1 Represents a hydrogen atom, or an alkyl group which may be substituted represented; R2 Represents a hydrogen atom, a halogen atom or represents a; R3 The alkyl group may be substituted " represented by the imidazole compound, its pharmacologically acceptable salt as an active ingredient in a pharmaceutical composition. [Drawing] no (by machine translation)
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- RECEPTOR FUNCTION REGULATING AGENT
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An agent for regulating 14273 receptor function, which is useful as a preventing or treating drug for diabetes mellitus, hyperlipidemia or the like, is provided. An agent for regulating 14273 receptor function comprising a compound containing an aromatic ring and a group capable of releasing a cation.
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Page/Page column 89
(2010/11/23)
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- Neighbourgroup Participation with the Dehydrogenation of Cyclic Amines of the o-Substituted Aniline Type
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The 2-Aminobenzylalcohols 1a - c produced with mercury-edta dehydrogenation the lactams 6a - c; the pipecoline 2b yielded the benzoxazine 3b indicating the participation of the nucleophilic hydroxymethyl group. The 2-aminobenzaldehydes showed a different behaviour in dependence on the ring size of the amine part: 7a, b led - via intermediate reaction of the hemiaminal 9 with the electrophilic formyl function - to the lactams 11a, b, while 7c gave rise to the aminoaldehyde 12 as major product and similarly the pipecoline 15 to the aminoketone 16. From 2′-(4-morpholinyl)-acetophenone (22) were received the lactam 31 and the aminoethanol 32, both by a twofold dehydrogenation.
- Moehrle,Mehrens
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p. 1369 - 1378
(2007/10/03)
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- 2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6- tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors
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Substituted 2-sulfinylimidazoles were synthesized and investigated as potential inhibitors of gastric H+/K+-ATPase. The 4,5-unsubstituted imidazole series 6-11 and the 1,4,5,6-tetrahydrocyclopent[d]imidazole series 12 were found to be potent inhibitors of the acid secretory enzyme H+/K+- ATPase. Structure-activity relationships indicate that the substitution of 2- pyridyl groups at the 1-position of the imidazole moiety combined with (2- aminobenzyl)sulfinyl groups at the 2-position leads to highly active compounds with a favorable chemical stability. Other substitution patterns in the imidazole moiety result in reducing biological activities. 2-[(2- Aminobenzyl)sulfinyl]-1-[2-(3-methylpyridyl)]-1,4,5,6- tetrahydrocyclopent[d]imidazole (12h, T-776) was selected for further development as a potential clinical candidate. Extensive study on the acid degradation of 12h indicates a mechanism of action different from that of omeprazole, the first H+/K+-ATPase inhibitor introduced to the market.
- Yamada,Yura,Morimoto,Harada,Yamada,Honma,Kinoshita,Sugiura
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p. 596 - 604
(2007/10/03)
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