This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

Piperazine derivatives and their use as anti-inflammatory agents

Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates) wherein R, R?1, R2, R3, R4, R21, R27, R28?, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhan cing acetylcholine release with acetylcholinesterase inhibitors.

Benzylpiperidines and piperazines as muscarinic antagonists

Identification and chemical synthesis of mdl 105,212, a non-peptide tachykinin antagonist with high affinity for nk1 and nk2 receptors

The invention relates to new compositions with pyscho- tropic activity which comprise a compound of formula 1 as the active substance. The compounds of formula 1 are for the greater part new compounds. The invention therefore also relates to these new compounds and to the preparation thereof in a manner known for the synthesis of analogous compounds.

New pharmaceutical compositions having a psychotropic activity

Synthesis and antitumor testing of certain new fused triazolopyrimidine and triazoloquinazoline derivatives

1-Aryl- and 1-(arylmethyl)-4-guanylpiperazines and other heterocyclic and alicyclic guanidine derivatives

Heating of 1- and 2-naphthylamine hydrochlorides and of 5- and 6-tetralylamine hydrochlorides with diethanolamine hydrochloride produced naphthylpiperazines la and Ila and tetralylpiperazines Ilia and IVa. These secondary amines were treated with ethyl chloroformate or with acetic anhydride and then reduced; or underwent an addition of methyl acrylate or acrylonitrile and then were reduced; or finally underwent alkylation by 4-methoxyphen acyl bromide and 4-chloro^-fluorobutyrophenone to the corresponding N-alkyl derivatives which were evaluated pharmacologically. l-(6-Tetralyl)-4-methylpiperazine ( IVd) displayed a marked antireserpine effect in the test of eyelid ptosis in mice, 4-[3-(4-fluorobenzoyl)propyl]-l-(6-tetralyl)piperazine (IVk) was active neuroleptically. 1-Arylpiperazine derivatives have been often reported as neurotropic and cardiovascular agents; for the case that the aryl substituent is phenyl or a substituted phenyl, several examples of this type were reported recently1. The aryl in these compounds can also be bicyclic or tricyclic and can contain heteroatoms; thus, e.g., l-(2-pyridyl)piperazine derivative "azaperone" is a sedative used in veterinary practice2, the l-(2-pyrimidyl)piperazine derivative "piribedil" has the properties of a peripheral vasodilatant and a potential antiparkinsonic3 , l-(2-quinolyl) piperazine is the "quipazine"4 with serotoninergic and antitremorine activity, the l-(2-purinyl)piperazines are central depressants5, l-(thieno [2,3-d] pyrimidine-4-yl)piperazines show antihistamine activity6, l-(5-methyl-5if-pyrimido [3,4-6]-l,4-benzoxazin-3-yl)-4-methylpiperazine is the antidepressant agent "azaphene"7; on the other hand, l-(2- and 3-phenothiazinyl)piperazines displayed no interesting pharmacodynamic activity8. Little attention has been devoted to the napThthylpiperazines; patents9,10 report a central depressant activity for l-(l-aryl-2-propyl)-4-(naphthyl)piperazines and a sedative, myorelaxant and analgesic activity for l-(dihydronaphthyl)piperazines. The present communication contributes to the present knowledge of the pharmacodynamics of naphthylpiperazines and tetralylpiperazines. Prelog and Blazek11 described the preparation of l-(l-naphthyl )piperazine (la) and l-(2-naphthyl)piperazine (II a) by reactions of naphthylamine s with bis(2-bromo

http://www.electronicsandbooks.com/eab1/manual/Magazine/C/Collection%20of%20Czechoslovak%20Chemical%20Communications/V40(1975)/1975_1612.pdf

Naphthylpiperazines and tetralylpiperazines: synthesis and pharmacological properties*

1-(2,4,6-Trimethylbenzyl)piperazine and some of its 4-substituted derivatives: Synthesis and pharmacological screening

Potential neuroleptics; N-aralkyl, N-(aroylalkyl) and N-pyridyl derivatives of 10-piperazino-10,11-dihydrodibenzo[ b,f ]thiepins

Cyclic amidines derived from benz[ c,d ]indole and 4,5-dihydro-3 H -1-benzazepine including some related compounds: Synthesis and pharmacological screening

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