Astra Aktiebolag

University System of Maryland

Astrazeneca Ab

Cornell University

Aktiebolaget Astra

Mats Torbjorn Linderberg

Svante Bertil Ross

Seth-Olov Thorberg

Stefan Berg

Robert Schwarcz

Bengt Ulff

Birgitta Kristina Gotthammar

Susanna Karin Bjork

Kerstin Margareta Persson

Johan Per Luthman

Barry K Carpenter

Substituted 1,2,3,4-tetrahydronaphthalene derivatives

The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having formula (I) wherein X is N or CH; Y is NR CH , CH NR , NR CO, CONR or NR SO wherein R is H or C -C alkyl; R is H, C -C alkyl or C -C cycloalkyl; R is C -C alkyl, C -C cycloalkyl or (CH ) -aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; R is C -C alkyl, C -C cycloalkyl, OCF , OCHF , OCH F, halogen, CONR R , CN, CF , OH, C -C alkoxy, NR R , SO CH , SO CF , SO NR R , an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C -C alkyl; or COR ; wherein R , R and R are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

Substituted chroman derivatives

Intermediates in the preparation of substituted chroman derivatives

The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I

Hydroxylated anthranilic acid derivatives

The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.7 =H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.

Compounds

3-hydroxy anthanilic acid derivatives

The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H, alkyl, aryl and arylalkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, OCF.sub.3 and SCF.sub.3 with the proviso that the compound of formula I wherein R.sup.1 and R.sup.2 =H, X=Br and Y=Me is excluded;

New compounds

Growing community of inventors

Sodertalje, Sweden

Mats Torbjorn Linderberg