Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.

Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.

Abstract: This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or —(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, —(1-4C)alkyl or —OR16; —R4 is —H, —(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; —(1-6C)alkyl, —(2-6C)alkenyl or —(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; —(1-6C)alkyl, —(2-6C)alkenyl, —(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, —(1-4C)alkyl, —(1-4C)alkoxy, —(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or —(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or —(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or —(1-4C)alkyl; —R13 is —H, —(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, —(

Abstract: An intrauterine system is disclosed for use in the treatment of dysfunctional uterine bleeding; menorraghia; dysmenorrhoea; endometriosis; uterine fibroids; climacteric complaints; osteoporosis; and urogenital atrophy. The system is formed by a frame defining an interior space for receipt of a deposit of a therapeutically effective dose of a biologically active compound. The frame has an open structure allowing access to a substantial part of an outer surface of the deposit, and the deposit has a rate controlling structure that controls a rate of release of the compound within the uterus. One or more retention elements are provided on the frame for retaining the frame within the uterus of a female mammal.

Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.

Abstract: Disclosed herein is a drug delivery system consisting of one or more compartments and comprising a progestogenic compound dissolved in a thermoplastic polyethylene vinylacetate copolymer. Also disclosed are a contraceptive kit or hormone-replacement therapy kit comprising the drug delivery system, and a combination preparation that simultaneously provides contraception and treatment of a sexually transmitted disease comprising the drug delivery system.

Abstract: The present invention relates compounds of the formula (I) oligosaccharide-spacer-A??(I), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO2—R1][CO—NR2—CH(4-benzamidine)-CO—NR3R4].

Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.

Abstract: There is disclosed a method for increasing retinal and optic nerve head oxygen tension by application of a composition comprising carbonic anhydrase inhibitors to the eye.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.