Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —S—R14; and other substituents are as defined in the specification.

Abstract: The invention concerns RAC-PK and fragments thereof, as well as activators and inhibitors of RAC-PK for use as medicaments, particularly in the treatment of diseases concerned with abnormalities in processes modulated by insulin, such as cellular proliferation, insulin deficiency and/or excess blood sugar levels. Moreover, the invention provides RAC-PK for use in screening potential mimics or modulators thereof. A method for screening for agents capable of affecting the activity of GSK3 is also disclosed. The invention further provides a screening kit comprising the RAC-PK as an active principle, and a method for screening compounds which are candidate mimics or modulators of RAC-PK activity comprising detecting specific interactions between the candidate compounds and RAC-PK. There is also provided a process for activating RAC-PK comprising treatment thereof with a phosphatase inhibitor.

Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N?; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.

Abstract: The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.

Abstract: The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.

Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —C?C—R10, —O—R12, —S—R14, or —NR24R25; and other substituents are as defined in the specification.

Abstract: In one embodiment, a female electrical connector comprises a socket having slots and electrical contacts. At least one of the electrical contacts can be movable between an open electrical circuit position where the electrical contacts are not in electrical communication and the socket is electrically inactive and a closed electrical circuit position where the electrical contacts are in electrical communication and the socket is electrically active. In one embodiment, an electrical box can comprise a container formed from a base having sides extending therefrom to define a cavity and the female electrical connector.

Abstract: The invention concerns RAC-PK and fragments thereof, as well as activators and inhibitors of RAC-PK for use as medicaments, particularly in the treatment of diseases concerned with abnormalities in processes modulated by insulin, such as cellular proliferation, insulin deficiency and/or excess blood sugar levels. Moreover, the invention provides RAC-PK for use in screening potential mimics or modulators thereof. A method for screening for agents capable of affecting the activity of GSK3 is also disclosed. The invention further provides a screening kit comprising the RAC-PK as an active principle, and a method for screening compounds which are candidate mimics or modulators of RAC-PK activity comprising detecting specific interactions between the candidate compounds and RAC-PK. There is also provided a process for activating RAC-PK comprising treatment thereof with a phosphatase inhibitor.

Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)? or N?; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively.

Abstract: The invention relates to kinase inhibitors of the formula (I) in which —R1 to R4=H; ether or polyether, amino; NO2; NH— carbamate; NH—CO—R, with R such as defined above; N3 and derivatives thereof of the 1,2,3-triazole type; —R5=—OH; halogen; —OR with R such as defined above; OH-carbamate; OH-carbonate; NH2, NH-carbamate; NH—CO—R, with R such as defined above; N3 and derivatives thereof of the 1,2,3-triazole type; N(R9, R10); —R5?=H or a C1-C12 alkyl, —R6=H; R; (R or R?)3—Si, with R such as defined above; optionally substituted aryl, heteroaryl; halogen (iodine); alkynyl; —R7 and R8=H, C1-C12 alkyl; —R9 and R10=H, R (or R?) such as defined above. These compounds can be used as kinase inhibitors in particular for treating cancer.

Abstract: In one embodiment, a light comprises: a body portion, a base, and an electrical power cord connected to the body and capable of establishing electrical communication between the light source and an electricity source. The body portion can comprise a lens, a light source, a reflector, a body connection, and a focusing element. The focusing element can be configured to create relative movement between the light source and the reflector, such that, when in use, a spread of a light beam from the light source can be adjusted. The base comprise can comprise a mounting element and a base connector capable of connecting to the body connection.

Abstract: A kit of parts comprising two or more protein kinase substrate polypeptides, each said substrate polypeptide comprising a specificity conferring portion (which is different for each said kinase substrate polypeptide) and a phosphorylatable portion, wherein the phosphorylatable portions of each polypeptide are capable of being bound in a phosphorylation state-sensitive manner by the same specific binding partner, for example and antibody preparation, and wherein the said specific binding partner is not an antibody specific for phosphotyrosine, phosphoserine or phosphothreonine. The phosphorylatable portion preferably comprises the amino acid sequence LSFAEPG.

Abstract: In one embodiment, an electrical box can comprise: a container formed from a base having sides extending therefrom to define a cavity; a cover configured to cover the cavity when in a closed position; and a female electrical connector disposed in the cavity when the cover is in the closed position. A socket of the female electrical connector can be capable of receiving a male electrical connector. Even when the electrical box is connected to live wiring, when the cover is in an open position, current cannot flow to the socket, and when the cover is in a closed position, current can flow to the socket. In another embodiment, an electrical box can comprise: a container; a cover configured to cover the cavity when in a closed position; and a female electrical connector physically connected to the cover such that the female electrical connector moves as the cover is opened.

Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)? or N?, provided that at least one of A and B is —N?, n is 1-3, m is 0-3, and R14 are as defined herein.

Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N?; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.

Abstract: The present invention provides compounds for use in the preparation of pharmaceutical formulations and medicaments, which alleviate learning and/or mental impairment in people suffering from Down's syndrome.

Abstract: The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.

Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzoazepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is -C?C-R10, -O-R12, -S-R14, or -NR24R25; and other substituents are as defined in the specification.