Abstract: The present invention relates to a safe and efficient system to improve haemostatic control by immobilization of Tissue Factor protein to a dressing material suitable for use as or in a wound dressing, bringing Tissue Factor in direct contact to the wound. The present invention aims at using immobilized Tissue Factor to generate a “thrombin burst”, a process by which thrombin, the most important constituent of the coagulation cascade is released very rapidly. There is no systemic release of the protein Tissue Factor into the vascular bed. The linked protein Tissue Factor can be used alone or in combination with other human proteins or components to optimise haemostasis.

Abstract: There is provided an ex-vivo insect screening model to accurately determine blood-brain barrier penetration of different nanoparticles in order to improve the compound screening procedures/processes in the early drug discovery process. This object offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.

Abstract: There is provided insect models that are aimed to reflect vertebrate blood-brain barrier (BBB) penetration. Investigation of BBB penetration is extremely important in drug discovery; successful CNS drugs have to cross the BBB, while BBB penetration may cause unwanted side effects for peripheral acting drugs. Specifically, the present invention relates to the use of insects in screening for substances with a biological effect on the brain or central nervous system and/or effect on a disease or disorder of the brain or central nervous system. It further relates to use of such insects in screening for substances that have a desired biological activity and which do not cross the blood brain barrier.

Abstract: There is provided insect screening models to determine gastrointestinal absorption of different chemical compounds in vertebrates, and in particular humans, in order to improve the compound screening procedures/processes in the early drug discovery process. This offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.

Abstract: There is provided an ex-vivo insect screening model to accurately determine blood-brain barrier penetration of different chemical compounds in order to improve the compound screening procedures/processes in the early drug discovery process. This object offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.

Abstract: There is provided a method and model insects for screening the effects of nanoparticles on brain barrier function and integrity. The method involves exposing the insect brain-barrier to the nanoparticle(s) of interest and exposing the nanoparticle treated insect brain barrier to one or more suitable marker(s) of the function and integrity of the brain barrier.

Abstract: There is provided an ex-vivo insect screening model to determine blood-brain barrier penetration of different chemical compounds. The method comprises the steps: • Optionally anesthetizing the insect • Fixing the head of the insect • Dissecting out the brain of the insect head thereby removing the brain from its cuticle • Optinally removing the neural lamella of the brain • Treating the brain with a solution of the chemical compound • Washing anf homogenising or ultra sound disintegrating the brain • Determining the concentration of the chemical compound in the homogenised brain material and • Calculating the penetration of the chemical compound through the blood-brain barrier The concentration of the chemical compound is determined by LC/MS and the chemical compound can be a CNS drug.

Abstract: There is provided an ex-vivo insect screening model to accurately determine blood-brain barrier penetration of different nanoparticles in order to improve the compound screening procedures/processes in the early drug discovery process. This object offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.

Abstract: There is provided insect screening models to determine gastrointestinal absorption of different chemical compounds in vertebrates, and in particular humans, in order to improve the compound screening procedures/processes in the early drug discovery process. This offers many advantages relative to prior technologies since insect models are more reliable tools for the decision-making process than the existing in vitro models, and will speed up the drug screening process and reduce the late phase attrition rate. Moreover, it will reduce the number of mammals sacrificed during the drug discovery phase.

Abstract: There is provided a new methodology for initial assessment of compound PK. The invention is generally particular useful for efficient screening of and assessment of PK profiles of newly synthesized compounds in the early phase of drug discovery.

Abstract: Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I).

Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided tha

Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is

Abstract: There is provided insect models that are aimed to reflect vertebrate blood-brain barrier (BBB) penetration. Investigation of BBB penetration is extremely important in drug discovery; successful CNS drugs have to cross the BBB, while BBB penetration may cause unwanted side effects for peripheral acting drugs. Specifically, the present invention relates to the use of insects in screening for substances with a biological effect on the brain or central nervous system and/or effect on a disease or disorder of the brain or central nervous system. It further relates to use of such insects in screening for substances that have a desired biological activity and which do not cross the blood brain barrier.

Abstract: Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*.

Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH,or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided that

Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is