Abstract: The present invention relates to a novel heterocyclic compound, a pharmaceutical composition comprisining said compound, a method and use of said compound for clinical treatment of medical conditions which may benefit from immunomodulation, e.g. rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28. A method of screening compounds for their ability of inhibiting ligand-induced co-stimulatory receptor internalization pathways in immune competent human cells is described. Said immune competent human cells are incubated at conditions capable of inducing co-stimulatory receptor internalization in the presence of at least one test compound and the suppression of the ligand-induced co-stimulatory receptor internalization determined.

Abstract: The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is methyl, methoxy, fluoro, chloro, bromo, azido, trifluorometlhyl, or OCHxFy, wherein x=0−2, y=1−3 with the. proviso that x+y=3; R″ is hydrogen, fluoro or chloro; with the proviso that R″ is fluoro or chloro only when R′ is fluoro or chloro; R4 is hydrogen or pharmaceutically acceptable inorganic or organic cations; R5 is dimethylamino or nitro; R6 is hydrogen; and when R′ is azido R5 is also ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, trifluoromethyl, OCHxFy, wherein x=0−2, y=1−3 with the proviso that x+y=3, or R5 and R6 taken together are methylenedioxy; and any tautomer thereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier.

Abstract: Compounds of formula (I) and tautomers thereof are effective for the treatment of mammals suffering from diseases resulting from autoimmunity and pathological inflammation.

Abstract: A method for stimulation of transcription factor AP (activator protein)-1 by administering a compound of the formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, c-propyl, n-butyl, sec.-butyl, iso-butyl, tert.-butyl, c-butyl, n-pentyl, sec.-pentyl, iso-pentyl, tert.-pentyl, neo-pentyl, c-pentyl, c-hexyl and c-heptyl; RNa and RNb are the same or different and selected from hydrogen, methyl and ethyl; R2, R3, R5 and R6 are independently selected from hydrogen, methyl, methoxy, thiomethyl, hydroxy, fluoro, chloro, bromo, trifluoromethyl, phenyl and benzyl; n is 1, 2 or 3; R′ and R″ are the same or different and selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec.-butyl, and iso-butyl or R′ and R″ together form a saturated heterocyclic ring of 5-7 atoms; and pharmaceutically acceptable salts, hydrates and solvates thereof, to a mammal in need thereof.

Abstract: The invention is related to compounds of general formula (I) 1

Abstract: Compounds of formula (I) 1

Abstract: The invention relates to a method for the treatment of tumors in mammals by the administration of compounds of the general formula (I) wherein A is O41 or NR42 R43 wherein R41 is hydrogen or a pharmaceutically acceptable inorganic or organic cation, or CORA wherein RA is alkyl and aryl; R42 and R43 are hydrogen, C1-C4-alkyl, cyclopropyl, cyclopentyl or cyclohexyl; or R42 is benzyl or phenethyl, optionally mono- or disubstituted by methyl, iso-propyl methoxy, fluoro, chloro, bromo, dimethylamino, trifluoromethyl or nitro and R43 is hydrogen; or R42 and R43 form a 5- or 6-membered ring; or R42 is CORB wherein RB is alkyl or aryl, —CH2N(CH3)2 or —CH2CH2COOH or CORB is a 2-acyloxymethylbenzoyl group wherein RC is methyl, ethyl, phenyl or benzyl; R42 is COORD wherein RD is C1-C4-alkyl, phenyl or benzyl; or R42 is —CH2OCO-tert.

Abstract: The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R' is methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, or OCH.sub.x F.sub.y, whereinx=0-2, y=1-3 with the proviso that x+y=3, R" is hydrogen, fluoro or chloro; with the proviso that R" is fluoro or chloro only when R' is fluoro or chloro; R.sub.4 is hydrogen or pharmaceutically acceptable inorganic or organic cations;R.sub.5 is ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, trifluoromethyl, OCH.sub.x F.sub.y, or OCH.sub.2 CH.sub.x F.sub.y wherein x=0-2, y=1-3 with the proviso that x+y=3;R.sub.6 is hydrogen; or R.sub.5 and R.sub.6 taken together are methylenedioxy; and any tautomer thereof.The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier.

Abstract: The invention is related to compounds of general formula (I) ##STR1## wherein R is Me, Et, n-Pr, iso-Pr, n-Bu, iso-Bu, sec.-Bu or allyl; R' is hydrogen, Me, MeO, fluoro, chloro, brorno, CF.sub.3, or OCH.sub.x F.sub.y ; R" is hydrogen or fluoro, with the proviso that R" is fluoro when R' is fluoro; and further when R' and R" are both hydrogen, R is not Me; R.sub.4 is selected from hydrogen and pharmaceutically acceptable inorganic and organic cations; R.sub.5 is selected from MeS, EtS, n-PrS, iso-PrS, MeSO, EtSO, MeSO.sub.2 and EtSO.sub.2 ; wherein x=0-2, y=1-3 with the proviso that x+y=3; and Me is methyl, Et is ethyl, Pr is propsy and Bu is butyl; and any tautomer, optical isomer and racemate thereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier.

Abstract: The invention relates to compounds of general formula (I) ##STR1## wherein R is selected from ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl; R.sub.4 is selected from hydrogen and pharmaceutically acceptable inorganic and organic cations; R.sub.5 is selected from methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, CF.sub.3, and OCH.sub.x F.sub.y ; wherein x=0-2, y=1-3 with the proviso that x+y=3; R.sub.6 is hydrogen; or R.sub.5 and R.sub.6 taken together are methylenedioxy; and any tautomer hereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of the compounds of formula (I), as well as methods of treating mammals suffering from diseases resulting from autoimmunity and pathological inflammation by administering a compound having the formula (I) to said mammal.