4994-14-3Relevant academic research and scientific papers
Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity
Meyers, Kenneth,Cogan, Derek A.,Burke, Jennifer,Arenas, Raquel,Balestra, Michael,Brown, Nicholas F.,Chen, Zhidong,Cerny, Matthew A.,Clifford, Holly E.,Colombo, Federico,Fader, Lee,Frederick, Kosea S.,Guo, Xin,Goldberg, Daniel,Hornberger, Keith R.,Kugler, Stanley,Lord, John,Marshall, Daniel R.,Moss, Neil,Parmentier, Jean-Huges,Richman, Jeremy R.,Schmenk, Jennifer,Weldon, Steven M.,Yu, Maolin,Zhang, Michael
supporting information, p. 979 - 984 (2018/01/02)
6,7-Dihydro-5H-2,1-benzisoxazol-4-one analogs are potent inhibitors of aldosterone synthase (CYP11B2) with selectivity over the highly homologous enzyme cortisol synthase (CYP11B1). These compounds are unique among inhibitors of CYP11B2 in their lack of a
CYCLOALKYL-SUBSTITUTED IMIDAZOLE DERIVATIVE
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Paragraph 0270-0272, (2013/03/26)
A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents -CH2-CHR5-CH2-NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
NOVEL HETEROCYCLE COMPOUNDS
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Page/Page column 46, (2009/04/24)
The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.
Carbon-13 magnetic resonance: hydrogen involvement in γ-anti substituent effects
Forrest, T. P.,Thiel, J.
, p. 2870 - 2875 (2007/10/02)
Chemical shifts have been determined for the carbons in a series of 3,3-dimethylcyclohexyl derivatives, (substituent = H, CH3, NH2, OH, Cl, Br, I).Comparison of the γ-anti substituent effects at carbons 3 and 5 indicates that presence of axial protons on these carbons causes increased shielding by all of the above substituents.The shielding by γ-anti substituents is decreased by the replacement of either the α or γ protons by methyl groups; the extent of the decrease is dependent upon the substituent and upon the position of the hydrogen which is replaced.
