Abstract: The present invention relates to compounds of the formula wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is hydrogen, lower alkyl, amino, pyrrolidin-3-ol, pyrrolidin-2-yl-methanol or —NHCH2CHROH; R3 is hydrogen or halogen; R is hydrogen, lower alkyl or —CH2OH; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof which are are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

Abstract: The invention relates to compounds of the general formula wherein R1 signifies hydrogen or hydroxy; R2 signifies hydrogen or methyl; and X signifies —O— or —CH2— and their pharmaceutically acceptable acid addition salts. It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

Abstract: The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.

Abstract: The present invention provides a method of treatment of a disease associated with neurodegeneration by administering a therapeutically effective amount of a compound of the general formula wherein Ar1 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by hydroxy, lower alkoxy, nitro, amino or methanesulfonamide; Ar2 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by lower alkyl or halogen; X is C, CH, C(OH) or N; Y is —CH2−, CH or O; Z —CH2—, —CH(CH3)— or —C(CH3)2—; R1 is hydrogen, lower alkyl or acetyl; A is C═O or —(CHR2)n—, wherein R2 is hydrogen, lower alkyl or hydroxy-lower alkyl; B is —(CH2)n—, O, —CH(OH)(CH2)n—, —CH(CH2OH)(CH2)n—, —(CH2)n CH(OH)— or —CH(CH2OH)—; - - - may be a bond; and n is 0-4, or pharmaceutically acceptable acid addition salts thereof.

Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are --O--CH.sub.2 O;R.sup.3 and R.sup.4 are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, --CONH.sub.2 or --SCH3; or taken together are --O--CH.sub.2 --O--;R.sup.5 is hydrogen or lower alkyl;X and Y are, independently from each other --CH(OH)--, --(CH.sub.2).sub.n --, --C(O)-- or --CH(lower alkoxy)-; andin, n and p are 1 or 2;and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by over activation of NMDA receptor subtypes.

Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula: ##STR1## wherein: A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.

Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are --O--CH.sub.2 O;R.sup.3 and R.sup.4 are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, --CONH.sub.2 or --SCH.sub.3 ; or taken together are --O--CH.sub.2 --O--;Y is --CH(OH)--, --(CH.sub.2).sub.n --, --C(O)-- or --CH(lower alkoxy)--; andm, n and p are 1 or 2;and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by over activation of NMDA receptor subtypes.

Abstract: The present invention relates to the use of compounds of general formula ##STR1## wherein R.sup.1 is hydrogen, halogen, lower alkyl or lower alkoxy;R.sup.2 is hydrogen;R.sup.3 is hydrogen, amino, ureido, lower alkylcarbonyl, lower alkyl-sulfonylamino, lower alkylcarbamoyl, carbamoyl, lower alkyloxycarbamoyl, lower alkylamino orR.sup.2 and R.sup.3 taken together are --(CH.sub.2).sub.m --X is methylene, hydroxymethylene, lower alkoxymethylene or carbonyl,n is 0, 1 or 2 andm is 3 or 4as well as pharmaceutically acceptable salts for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.

Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula ##STR1## wherein A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein x is --O--, --NH--, --CH.sub.2 --, --CH.dbd., --CO.sub.2 --, --CONH--, --CON(lower alkyl)--, --S-- and --SO.sub.2 --;R.sup.1 -R.sup.4 are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido;R.sup.5, R.sup.6 are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo;R.sup.7 -R.sup.10 are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy;n is 0 or 1;and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

Abstract: Compounds of general formula (Ia), (Ib) and (II), wherein R.sup.1 and R.sup.2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R.sup.3 R.sup.4 NS(O).sub.2 -- and R.sup.3 and R.sup.4 signify lower alkyl, and R.sup.2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH.sub.2 NHCH.sub.3, a bicyclic heterocycle with 1-3N atoms or a group --NR.sup.5 R.sup.6 or --OR.sup.5 in which R.sup.5 and R.sup.6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH.dbd.CH--, --CH.dbd.N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II).