- Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists
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A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K+ channel and serotonin transporter.
- Cho, Kaimei,Ando, Makoto,Kobayashi, Kensuke,Miyazoe, Hiroshi,Tsujino, Toshiaki,Ito, Sayaka,Suzuki, Tomoki,Tanaka, Takeshi,Tokita, Shigeru,Sato, Nagaaki
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scheme or table
p. 4781 - 4785
(2010/07/06)
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- ARYL-ALKYLAMINES AND HETEROARYL-ALKYLAMINES AS PROTEIN KINASE INHIBITORS
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The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 is an aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R25 is attached; and R4 and R5 each are hydrogen or a substituent as defined in the claims
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Page/Page column 207
(2010/11/25)
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- 1-‘2-(4-HYDROXYPHENYL)-2-HYDROXYETHYL!-PIPERIDIN-4-OL COMPOUNDS AS NMDA RECEPTOR ANTAGONISTS
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This invention provides a compound of the formula (I), wherein R1 and R2 independently represents a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring carbon or the like; said aryl groups havin
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Page/Page column 42-43
(2010/02/11)
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- FUSED LACTAM COMPOUNDS
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This invention provides a compound the formula (I), wherein R1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or
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Page/Page column 55
(2010/02/11)
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