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.

Abstract: The 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 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 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: (I) or a pharmaceutically acceptable acid addition salt thereof, where; 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 (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: A system and method for monitoring a monitored subject is disclosed. In a broad aspect, the method comprises activating a monitoring service to send notification messages to the monitored subject, sending at least one notification message to a monitored subject in accordance with a first notification schedule, determining if a response to the at least one notification message sent at the sending step is received from the monitored subject within a pre-specified time period, and invoking a non-response system state when a response to the at least one notification message is not received from the monitored subject within the pre-specified time period, wherein a non-response message is sent to a monitoring party at the invoking step. Various features of the system and method are disclosed herein.

Abstract: The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.

Abstract: Substantially pure two kinase domain protein kinases comprising the amino acid sequences provided in the description, variants, fusions, fragments, or derivatives thereof useful in screening assays for drugs. Applications thereof in the modulation of CREB, COX2 and IL2 activities.

Abstract: A method of activating serum and glucocorticoid-induced protein kinase (SGK) is provided wherein the SGK is phosphorylated. The SGK may be phosphorylated by PDK1 and/or a preparation containing PDK2 activity. A method of identifying a compound that modulates the activity of SGK is provided, wherein the activity of SGK is measured by measuring the phosphorylation by SGK of a polypeptide comprising an amino acid sequence corresponding to the consensus sequence (Arg/Lys; preferably Arg)-X-(X/Arg)-X-X-Ser/Thr)-Z wherein X indicates any amino acid, X/Arg indicates any amino acid, with a preference for arginine, and Z indicates that the amino acid residue is preferably a hydrophobic residue. The SGK may be activated by phosphorylation.

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 an 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: a method of inhibiting a protein kinase that has a threonine or less bulky residue at the position equivalent to Thr 106 in SAPK2a/p38, and not mammalian SAPK2a/p38 or SAPK2b/p38?2, is provided, wherein the protein kinase is exposed to a pyridinyl imidazole inhibitor. The protein kinase may be a TGF? type-I or type-II receptor.

Abstract: A method for a parent to monitor the status of a child when the child is away from home, in which a notification engine sends regular text messages to the child. If after a selected number of messages have been sent, the child has not responded to the notification engine within a selected time, then a non-response message is sent to the parent. The child can also send a trouble message to the notification engine which will then also notify the parent. The parent can access a log of responses to check the system status at any time.

Abstract: A method of identifying a compound which modulates the interaction between a PP1c and a regulatory subunit thereof, the method comprising determining whether a compound enhances or disrupts the interaction between (a) a PP1c or a fragment, variant, derivative or fusion thereof or a fusion of a fragment, variant or derivative and (b) a regulatory subunit which is able to bind to PP1c or a PP1c-binding fragment, variant, derivative or fusion of the subunit or a fusion of the fragment, variant or derivative. A method of affecting cellular metabolism or function, the method comprising administering to a cell (a) a compound which modulates the interaction between a PP1c and a regulatory subunit thereof or (b) a compound which mimics the effect of a regulatory subunit of PP1c or (c) a peptide capable of binding a PP1c and which affects the ability of PP1c to bind to a particular target and/or affects the regulation of PP1c activity, or a functional equivalent thereof.

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 compounds of formula (I), which are antagonists of the 5-HT6 receptor.

Abstract: The invention relates to the use of a substance, which detects sgk2 and/or sgk3, for diagnosing diseases connected with a disturbance of ion channel activity, in particular, sodium and/or potassium channels. The invention also relates to the use of an active ingredient for treating the aforementioned diseases, said active ingredient influencing the expression and/or the function of sgk2 and/or sgk3 and regulating the elimination of Na+ and/or K+ as a result.

Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines

Abstract: The present invention relates to a method of identifying a compound which blocks the activation of a stress-activated protein kinase selected from the group consisting of SAPK4 and SAPK3 by SKK3. The method includes contacting the stress-activated protein kinase with the compound and determining whether the compound enhances or disrupts the interaction between the stress-activated protein kinase and SKK3. The invention further relates to a screening assay, a method of identifying agents able to influence the activity of a stress-activated protein kinase and a method of activating a stress-activated protein kinase.

Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines