39650-67-4Relevant academic research and scientific papers
Design, synthesis and neuroprotective evaluation of novel tacrine-benzothiazole hybrids as multi-targeted compounds against Alzheimer's disease
Keri, Rangappa S.,Quintanova, Catarina,Marques, Sérgio M.,Esteves, A. Raquel,Cardoso, Sandra M.,Santos, M. Amélia
, p. 4559 - 4569 (2013/07/26)
Alzheimer's disease (AD) is a multifactorial disorder with several target proteins contributing to its etiology. In search for multifunctional anti-AD drug candidates, taking into account that the acetylcholinesterase (AChE) and beta-amyloid (Aβ) aggregat
SUBSTITUTED PROPIONYL DERIVATIVES
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, (2008/06/13)
The present invention relates to a compound represented by the following formula (1): [wherein, X1represents a carboxyl group which may be esterified or the like group; Y1represents a single bond, -O- or -N(R1)-; at least one of A1, A2and A3is a group represented by the following formula (2): -R2-a1-R3-a2→{wherein, R2represents a divalent C2-12hydrocarbon group, R3represents a single bond or a divalent C1-12hydrocarbon group, a1and a2individually represent a single bond, -S-, -SO-, -SO2-, -SO2NH-, -O-, -N(R4)-, -CON(R5)-, -C(=O)- or - Si(R6)(R7)- and → means bonding with Q1, Q2or Q3}, the remaining one or two of A1, A2and A3are the same or different and each independently represents a group represented by the following formula (3): -R8-a3-R9-a4→{wherein, R8and R9individually represent a single bond or a divalent C1-12hydrocarbon group, a3and a4individually represent a single bond, -S-, -SO-, -SO2-, -SO2NH-, -O-, - N(R10)-, -CON(R11)-, -C(=O)- or -SI(R12)(R13)- and → means bonding with Q1, Q2or Q3},; at least one of Q1, Q2and Q3represents a cyclic hydrocarbon group or heterocyclic group and the remaining one or two of Q1, Q2and Q3individually represent a hydrogen atom, a carboxyl group which may be esterified, a hydrocarbon group or a heterocyclic group] or salt thereof; and a pharmaceutical comprising the same as an effective ingredient. The compound exhibits strong squalene synthetase inhibitory action and is therefore useful as a pharmaceutical for the treatment·prevention of hypercholesterolemia, hyperlipemia or arteriosclerosis.
Process for preparing a 2(ω-aminoalkyl)-1,3-heterocyclic compounds
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, (2008/06/13)
2-(ω-AMINOALKYL)-1,3-HETEROCYCLIC COMPOUNDS ARE PREPARED BY REACTING A COMPOUND SELECTED FROM THE GROUP OF A DIAMINE, AN AMINOHYDROXY AND AN AMINOTHIOL COMPOUND, SAID COMPOUND HAVING THE FORMULA: EQU1 wherein EQU2 A is a bivalent chain of 2 or 3 carbon atoms, which can also be part of a bivalent, optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical, and X is oxygen, sulphur or the group EQU3 wherein R7 is as defined herein with a lactam having the formula EQU4 WHEREIN B is selected from the group of a single bond, oxygen, sulphur, the group EQU5 wherein R6 is as defined herein, and arylene, R1, r2, r3 and R4, which may be the same or different, are selected from the group of hydrogen, halogen, nitro and optionally substituted aliphatic, cycloaliphatic, araliphatic and aromatic, R5, r6 and R7, which may be the same or different, are selected from the group of hydrogen and optionally substituted aliphatic, cycloaliphatic, araliphatic and aromatic, and n and m, which may be the same or different, are intergers of from 1 to 14, with the proviso that the sum of n and m does not exceed 15, At a temperature of from 100° to 300°C in the presence of at least a catalytic quantity of an acid and/or an acid catalyst.
