55144-54-2

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• 14548-38-0 6-chloro-1-indanone 

Relevant academic research and scientific papers

Synthesis and bioactivity of substituted indan-1-ylideneaminoguanidine derivatives

In our efforts to discover more potent and lasting NHE1 inhibitors, we designed and synthesized a series of substituted indan-1-ylidene aminoguanidine derivatives (5). NHE1 inhibitory activity of twenty-one compounds 5 was evaluated in a rat platelet swelling assay. It is found that most of the tested compounds possess NHE1 inhibitory effects. 2-(5-methoxybenzimidazol-2-ylthio)-5-chloro-2,3-dihydroinden-1-ylidene aminoguanidine hydrobromide (5m) proved to be sixty-nine times more potent than cariporide. Furthermore, when tested in vivo, compound 5m also displayed superior cardioprotective effects against SD rat myocardial ischemic-reperfusion injury over those of cariporide.

Imidazo?1,2-A! pyrazine-4-one, preparation thereof and drugs containing same

Compounds of formula (1) STR1 wherein either R is C=R3, C(R4)R5 or CH--R6, R1 and R2 are hydrogen, halogen, alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar, --N=CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO3 H, R3 is oxygen, NOH, NO-alk-COOK or CH--R7, R4 is alkyl, -alk-Het or alk-Ar, R5 is alkyl, -alk-Het or -alk-Ar, or C(R4)R5 is cycloalkyl, R6 is hydroxy, alkyl, NR8 R9, -alk-OH, -alk-NR8 R9, -alk-Ar or -alk-Het, R7 is hydroxy, alkyl, phenyl, -alk-Ar, -alk-Het, NR10 R11 or a heterocyclic ring, R8 and R9 are alkyl, or R8 is hydrogen and R9 is hydrogen or alkyl, --COR12, --CSR30 or --SO2 R13, R10 and R11 are alkyl or cycloalkyl, R12 is alkyl, cycloalkyl, phenyl, --COO-alk, --CH2 --COOX, --CH2 NH2, --NH-alk, --NH--Ar, --NH2 or --NH-Het, R13 is alkyl or phenyl, R30 is --NH-alk, --NH--Ar, --NH2 or --NH-Het, R13 is alkyl or phenyl, R30 is --NH-alk, --NH--Ar, --NH2 or --NH-Het; or R is a 2-imidazolylmethyl radical and each of R1 and R2 is a hydrogen atom. The compounds of formula (I) are α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor gylcine modulation site ligands.

IMIDAZO(1,2-A)-INDENO (1,2-E) PYRAZIN-4-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Pharmaceutical compositions containing, as the active principle, compounds of formula (I): STR1 wherein R, R 1 and R. sub.2 are as defined in the description, or salts thereof, the novel compounds of formula (I), and the preparation thereof. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, this receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NDMA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

Thiazolidine derivatives

Thiazolidine derivatives of the formula I STR1 in which the substituents R1 to R7 have the meanings as indicated in the following and which have in the free form or in the form of their non toxic acid addition salts valuable pharmaceutical properties, processes for preparing them, pharmaceutical preparations on the basis of these compounds and their use as medicines.