Abstract: The present invention relates to compositions and methods of use, wherein the composition comprises a conjugate of a bacterial superantigen and an antibody moiety. More particularly, the bacterial superantigen has been modified to decrease seroreactivity with retained superantigen activity.

Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including 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.

Abstract: Compounds of formula (I) for clinical treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection and malignant neoplasia. A pharmaceutical composition comprising a compound of formula (I) in an amount giving a daily dosage of from 0.005 mg/kg to 10 mg/kg body weight, in particular from 0.025 mg/kg to 2 mg/kg body weight.

Abstract: A compound of formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R? is hydrogen, C1-C4 alkyl, C1-C3 alkoxy; halogen, trifluoromethyl or OCHxFy, R? is hydrogen, fluoro or chloro, that R? being fluoro or chloro only when R? is fluoro or chloro; R3 is hydrogen or C1-C5 alkyl R4 is hydrogen, CH2OCOC(CH3)3, pharmaceutically acceptable inorganic or organic cations, or COR4? wherein R4? is C1-C5 alkyl, phenyl, benzyl or phenethyl; R7 is methyl or ethyl; one of A and B is sulphur and the other is C—R2; when A is S, R2 is selected from hydrogen and methyl, with the proviso that R2 is methyl only when R3 is not hydrogen; and when B is S, R2 is hydrogen; and any tautomer thereof. A pharmaceutical composition comprising a compound of formula (I), a method of treating malignant tumours or diseases resulting from autoimmunity or pathologic inflammation.

Abstract: A method for inactivating target cells in the presence of T cells by bringing the two types of cells in contact with a superantigen (SAG) in the presence of an immune modulator, characterized in that at least one of the superantigen and the immune modulator is in the form of a conjugate between a “free” superantigen (Sag) and a moiety targeting the conjugate to the target cells. A superantigen conjugate complying with the formula (1): (T)x(Sag)y(IM)z; a) T is a targeting moiety, Sag corresponds to a free superantigen, IM is an immune modulator that is not a superantigen and T, Sag and IM are linked together via organic linkers B; b) x, y and z are integers that typically are selected among 0-10 and represent the number of moieties T, Sag and IM, respetively, in a given conjugate molecule, with the provision that y>0 and also one or both of x and z>0. The superantigen conjugate is preferably a triple fusion protein.

Abstract: A process for the preparation of the compounds of general formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.

Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including 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.

Abstract: E-cinnamic amides of piperazine derivatives according to formula (I) wherein X is chloro or fluoro and R1 is an aromatic or heteroaromatic group, their pharmaceutically acceptable salts or solvates. The invention also relates to pharmaceutical compositions containing a compound of formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of compounds of formula (I), as well as methods for treating mammals suffering from inflammatory, autoimmune, proliferative or hyperproliferative diseases by administering a compound having the formula (I) to said mammal.

Abstract: Compounds of formula (I) wherein X is a fluorine or a chlorine atom; the methyl groups located at the 2- and 5-position of the piperazine ring are in trans-configuration to each other; Y is NH or O; R1 is selected front hydrogen, chloro, bromo, nitro, methyl or trifluoromethyl; R2 is selected from hydrogen, halo, methyl, trifluoromethyl, methoxy or trifluoromethoxy; or a pharmaceutically acceptable salt or solvate thereof, The invention also relates to pharmaceutical compositions containing a compound of formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of compounds of formula (I), as well as methods for treating mammals suffering from inflammatory, autoimmune, proliferative or hyperproliferative diseases by administering a compound having the formula (I) to said mammal.

Abstract: A stable solid pharmaceutical composition consisting essentially of an effective amount of a salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.

Abstract: Compounds of formula (I) for clinical treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection and malignant neoplasia. A pharmaceutical composition comprising a compound of formula (I) in an amount giving a daily dosage of from 0.005 mg/kg to 10 mg/kg body weight, in particular from 0.025 mg/kg to 2 mg/kg body weight.

Abstract: A process for the preparation of the compounds of general formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.

Abstract: The present invention relates to a carrier for introduction of substances into cells comprising a modified major capsid protein L1 of human papillomavirus (HPV-L1 protein) devoid of type-specific epitopes causing production of neutralising antibodies. The invention also includes an oligo- or polynucleotide coding for said carrier, vaccines comprising said carrier or said oligo- or polynucleotide, as well as methods of using the carrier or the oligo- or polynucleotide in vaccination against viral, bacterial or parasite infections as well as against development of certain cancers. Especially, infections of human papillomavirus and the development of cancer as a consequence of such infections are recognised.

Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including 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.

Abstract: The invention relates to a selection method and the products identified using the selection method which includes the steps of identifying one or more binding structures to a target structure using one or more libraries. The method includes the steps of reacting a first library with the displayed target structure to bind some of the binding structures to the displayed target structure, separating the displayed target structure and bound binding structures from unbound binding structures, and recovering bound or unbound binding structures. The bound or unbound binding structures can be amplified to create enriched libraries of binding structures. Binding structures thus identified are directed to target structures which are displayed in vivo and/or in situ.

Abstract: A process for the preparation of the compounds of general formula (I) 1

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.