321890-25-9Relevant academic research and scientific papers
Small conformationally restricted piperidine N-arylsulfonamides as orally active γ-secretase inhibitors
Josien, Hubert,Bara, Thomas,Rajagopalan, Murali,Asberom, Theodros,Clader, John W.,Favreau, Leonard,Greenlee, William J.,Hyde, Lynn A.,Nomeir, Amin A.,Parker, Eric M.,Pissarnitski, Dmitri A.,Song, Lixin,Wong, Gwendolyn T.,Zhang, Lili,Zhang, Qi,Zhao, Zhiqiang
, p. 5330 - 5335 (2007)
The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide γ-secretase inhibitors is reported. Lowering molecular weight including the use of conformational constraint led to compounds with less CYP 3A4 liability com
DERIVATIVES OF 6-(2,3-DICHLOROPHENYL)-1,2,4-TRIAZIN-5- AMINE
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Paragraph 0440, (2015/07/07)
The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.
8-Phenyl-6, 9-dihydro-[1,2,4] triazolo[3,4-i]purin-5-one derivatives
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, (2008/06/13)
8-phenyl-6,9-dihydro-[1,2,4]triazolo[3,4-i]purin-5-one derivatives of formula (I): wherein: R1, R2 and R3 each independently represent: hydrogen; an alkyl group which is unsubstituted or substituted by a hydroxy, alkoxy, alkylthio, amino, mono- or di-alkylamino, hydroxycarbonyl, alkoxycarbonyl, acylamino, carbamoyl or alkylcarbamoyl group; or a group of formula —(CH2)n—R6 wherein n is an integer from 0 to 4 and R6 represents: a cycloalkyl group; a phenyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, hydroxy, alkylenedioxy, alkoxy, amino, mono- or di-alkylamino, nitro, cyano or trifluoromethyl groups; or a 3 to 7-membered ring comprising from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulphur, which ring may be unsubstituted or substituted by one or more halogen atoms or hydroxy, phenyl, alkoxycarbonyl, amino, mono- alkylamino, di-alkylamino or hydroxycarbonyl groups or one or more alkyl groups which may in turn be unsubstituted or substituted by one or more halogen atoms or hydroxy, alkoxy, hydroxyalkoxy, phenyl, alkoxycarbonyl, amino, mono- or di-alkylamino or hydroxycarbonyl groups; either R4 and R5 together with the nitrogen atom to which they are attached form a 3 to 7-membered ring comprising a total of from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulphur, which ring may be unsubstituted or substituted by one or more halogen atoms or hydroxy, oxoalkyl, carbamoyl, hydroxycarbonyl, alkoxycarbonyl, trifluoroacetyl, amino, mono- or di-alkylamino groups or an alkylene group, or one or more alkyl, alkenyl or alkynyl groups which may in turn be unsubstituted or substituted by one or more halogen atoms or hydroxy, alkoxy, hydroxyalkoxy, amino or mono- or di-alkylamino groups, or R4 and R5 independently represent hydrogen, an amidino group or an alkyl, alkenyl or alkynyl group which may be unsubstituted or substituted by one or more halogen atoms or hydroxy, alkoxy, alkylthio, amino, mono- or di-alkylamino groups, or R4 represents hydrogen or an alkyl group and R5 represents a group of formula —(CH2)n—R7 wherein n is an integer from 0 to 4 and R7 represents: a cycloalkyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, hydroxy, alkylenedioxy, alkoxy, amino, mono- or di-alkylamino, alkylamido, nitro, cyano or trifluoromethyl groups; a phenyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, hydroxy, alkylenedioxy, alkoxy, amino, mono- or di-alkylamino, nitro, cyano or trifluoromethyl groups; or a 3 to 7-membered ring comprising from 1 to 4 heteroatoms selected from nitrogen, oxygen and sulphur, which ring may be unsubstituted or substituted by one or more halogen atoms or hydroxy, alkoxy, phenyl, alkoxycarbonyl, amino, mono-alkylamino, di-alkylamino or hydroxycarbonyl groups or one or more alkyl groups which may be unsubstituted or substituted by one or more halogen atoms or hydroxy, alkoxy, hydroxyalkoxy, phenyl, alkoxycarbonyl, amino, mono- or di-alkylamino or hydroxycarbonyl groups; or a pharmaceutically acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as PDE 5 inhibitors.
