- Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline
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Parkinson's disease (PD) is associated with elevated levels of hMAO-B in the brain, and MAO-B has been recognized a successful target for developing anti-PD drugs. Herein we report rasagiline derivatives as novel potent and selective hMAO-B inhibitors. Th
- Xiao, Xuan,Zhang, Xing-Xing,Zhan, Mei-Miao,Cheng, Kai,Li, Shiyu,Xie, Zhouling,Liao, Chenzhong
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- TETRAHYDRONAPHTHALENE DERIVATIVE
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A compound shown by general formula (I-1) (in the formula, all symbols are as stated in the specification.) has selective S1P5 receptor-binding activity. Adjusting this activity make s it possible to obtain a therapeutic agent for S1P5-mediated diseases,
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Paragraph 0240
(2018/12/13)
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- Indane derivative and synthetic method and medicinal application thereof
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The invention discloses an indane derivative and a synthetic method and medicinal application thereof. The structural general formula is as shown in the specification. The indane derivative disclosed by the invention has excellent inhibitory activity and high selectivity on MAO-B.
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Paragraph 0067; 0068; 0069; 0070
(2017/09/02)
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- NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OSTEOPOROSIS
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Novel tricyclic compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
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- NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS
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Novel tricyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
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- NOVEL 3-HYDROXY-5-ARYLISOTHIAZOLE DERIVATIVE
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[Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
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Page/Page column 73
(2012/06/30)
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- MAO-B inhibitors useful for treating obesity
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The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin
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Page/Page column 15
(2008/06/13)
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- AMINOPHENYLPROPANOIC ACID DERIVATIVE
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A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.
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Page/Page column 88
(2010/11/24)
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- Method of use of enantiomers of trans-indeno[1,2-b]-1,4-oxazines
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The (R,R)-enantiomers of trans-indeno[1,2-b]-1,4-oxazines demonstrate dopaminergic activity, whereas the (S,S)-enantiomers demonstrate α-adrenergic antagonist activity. They are prepared by cyclization of the appropriate chiral 2-amino-1-hydroxyindane.
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- Directionality of Proton Transfer in Solutions. Three Systems of Known Angularity
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Three compounds were synthesized each possessing rigid carbon frameworks that hold an oxygen base near a mobile C-H proton in well-defined angular and distance relationships: 2-iodo-4-hydroxyindan, endo-5-hydroxybicycloheptan-2-one, and endo-2-hydroxy-exo-6-bromomethylheptane.Effective proton transfer was detected with the second and third compounds but not the first.The data suggest that C-to-O proton transfer with severely bent O/H/C angles (106 deg) is permissible if the O-H distance is less than the sum of the van der Waals radii. "Long distance" catalysis at active sites of enzymes appears unlikely.
- Menger, F. M.,Chow, J. F.,Kaiserman, H.,Vasquez, P. C.
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p. 4996 - 5002
(2007/10/02)
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