- Substituted (10H-phenothiazin-10-L)-propyl-1-piperazines
-
Substituted (10H-phenothiazin-10-yl)propyl-1-piperazines of the formula STR1 wherein R1, R2, R3, A, X, m, n and s are as hereinafter set forth, are described. The compounds of formula I, which contain a piperazine moiety combined by an ether linkage to different phenolic moieties, are useful as orally active long lasting antipsychotic agents.
- -
-
-
- β1-Selective Adrenoceptor Antagonists. 1. Synthesis and β-Adrenergic Blocking Activity of a Series of Binary (Aryloxy)propanolamines
-
A series of binary (aryloxy)propanolamines has been prepared and examined in vitro and in vivo for β-adrenoreceptor blocking activity.These symmetrical compounds consist of two (S)-(phenyloxy)propanolamine pharmacophores coupled through alkylenedioxy or poly(oxyethylenedioxy) linking units of varying lengths.Examples of such binary compounds linked through the 2,2', 3,3', and 4,4' positions in the aromatic rings of the pharmacophores have been prepared.In vitro and in vivo test data indicate that the 2,2' compounds tend to be selective β2-adrenergic blocking agents, the 4,4' binaries tend to be selective β1-blocking agents, and those compounds with 3,3' linkages exhibit intermediate selectivities.One of the 4,4'-linked binary compounds, 4s, exhibited potent, cardioselective β-blockade in vivo, which was of short duration and was accompanied by a prolonged tachycardia.
- Kierstead, R. W.,Faraone, A.,Mennona, F.,Mullin, J.,Guthrie, R. W.,et al.
-
p. 1561 - 1569
(2007/10/02)
-
- Process for inverting the configuration in optically active compounds
-
The invention relates to a process for inverting the configuration in optically active compounds of the formula STR1 in which Ar1 represents a monocyclic or polycyclic, carbocyclic or heterocyclic radical that has at least one ring of aromatic character and is bonded to the oxygen atom by way of a ring carbon atom, preferably of the ring of aromatic character, and R1 represents an optionally substituted aliphatic, cycloaliphatic or araliphatic hydrocarbon radical, or the salts thereof, characterised in that an optically active compound of the formula STR2 having a R(+) or S(-) configuration, in which R2 represents a monocyclic or polycyclic, carbocyclic or heterocyclic radical, or an optionally substituted aliphatic, cycloaliphatic or araliphatic hydrocarbon radical, is converted, by treating with a strong oxygen-containing inorganic or organic acid or halides thererof, into an optically active compound of the formula STR3 in which X? represents the anion of a strong, oxygen-containing inorganic or organic acid or of a halogen atom and the resulting compound of the formula III is hydrolysed, optionally by way of the corresponding free base as intermediate, to form a compound of the formula I of a configuration opposite to that of the starting material used and, if desired, a free compound of the formula I is converted into a salt or a resulting salt is converted into the free compound.
- -
-
-
- (S)-1-[2-(4-HYDROXY-S-(1-ALKYLAMINO-PROPOXY)PHENYLALKYL]-4-PHENYLPIPERAZINES
-
There are disclosed compounds of the formula STR1 wherein R 1 is selected from the group consisting of lower alkyl; R 8 is selected from the group consisting of--O--(CH 2) n--wherein n is 2 to 20, STR2 and R 6 is selected from the group consisting of hydrogen or lower alkoxy, and STR3 wherein R 1 is selected from the group consisting of lower alkyl; R 8 is selected from the group consisting of--O--(CH 2) n--wherein n is 2 to 20, STR4 and R 6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediates utilized to produce the end products. The end products have utility as agents exhibiting both α and selective β adrenergic blocking action.
- -
-
-
- Phenoxy substituted glycosides
-
1-Phenoxy-2-hydroxy-3-amino-propanes of the formula I EQU1 wherein R1 is a sugar residue and R2 is isopropyl, tert.-butyl or α-methyl-phenethyl optionally substituted in the phenyl part, and the salts thereof are useful as positively inotropic agents, especially in the treatment of insufficiency of the cardiac muscle.
- -
-
-