Abstract: Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.

Abstract: Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.

Abstract: This disclosure relates to methods of treating or preventing cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases such as cystic fibrosis, chronic obstructive pulmonary disease, chronic pancreatitis, chronic bronchitis, asthma, mucus formation, comprising administering an effective amount of a 2-amino-N?-benzylidene-acetohydrazide compound or derivative thereof to a subject in need thereof. In certain embodiments, the 2-amino-N?-benzylidene-acetohydrazide compound is ((E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(m-tolylamino)acetohydrazide; or (E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(p-tolylamino)acetohydrazide.

Abstract: Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.

Abstract: This disclosure relates to methods of treating or preventing cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases such as cystic fibrosis, chronic obstructive pulmonary disease, chronic pancreatitis, chronic bronchitis, asthma, mucus formation, comprising administering an effective amount of a 2-amino-N?-benzylidene-acetohydrazide compound or derivative thereof to a subject in need thereof. In certain embodiments, the 2-amino-N?-benzylidene-acetohydrazide compound is ((E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(m-tolylamino)acetohydrazide; or (E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(p-tolylamino)acetohydrazide.

Abstract: Methods of treating leukodystrophy are provided. Accordingly there is provided a method of treating leukodystrophy in a subject, the method comprising administering to the subject a therapeutically effective amount of an agent capable of up-regulating activity and/or expression of a component participating in a Sigma-1 Receptor (Sig-1R) signaling pathway. Also provided are agents and methods of up-regulating activity of Sig-1R in a cell and treating a disease that can benefit from up-regulating activity of Sig-1R. Also provided are agents and methods of modulating activity of sonic hedgehog (SHH) in a cell and treating a disease that can benefit from modulating activity of SHH.

Abstract: This disclosure relates to methods of treating or preventing cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases such as cystic fibrosis, chronic obstructive pulmonary disease, chronic pancreatitis, chronic bronchitis, asthma, mucus formation, comprising administering an effective amount of a 2-amino-N?-benzylidene-acetohydrazide compound or derivative thereof to a subject in need thereof. In certain embodiments, the 2-amino-N?-benzylidene-acetohydrazide compound is ((E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(m-tolylamino)acetohydrazide; or (E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(p-tolylamino)acetohydrazide.

Abstract: This disclosure relates to methods of treating or preventing cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases such as cystic fibrosis, chronic obstructive pulmonary disease, chronic pancreatitis, chronic bronchitis, asthma, mucus formation, comprising administering an effective amount of a 2-amino-N?-benzylidene-acetohydrazide compound or derivative thereof to a subject in need thereof. In certain embodiments, the 2-amino-N-benzylidene-acetohydrazide compound is ((E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(m-tolylamino)acetohydrazide; or (E)-N?-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(p-tolylamino)acetohydrazide.

Abstract: Methods and materials are provided for the production of glycosylated GLP-1 peptides that exhibit improved properties. The methods and materials of the present invention may be used for treatment of metabolic conditions, such as Syndrome X and diabetes.

Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

Abstract: A stretching and exercise device has a first strap member having a pair of end portions, a second strap member having a pair of end portions, and a pair of resistance members connected between respective end portions of the first and second strap members. A third strap member has a pair of end portions attached to respective first and second surface portions of the second strap member. A fourth strap member is attached to a third surface portion of the second strap member different from the first and second surface portions thereof.

Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

Abstract: The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds, particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.

Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

Abstract: The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds, particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.

Abstract: The invention is directed to a method for generating possible conformations of a molecule comprising the steps of:a) selecting a first conformation of the molecule characterized by a first set of coordinates associated with each atom in the molecule by the presence of a pattern of forces among such atoms and by a series of intrinsic forces associated with each atom;b) varying the pattern of forces among such atoms in a non-random manner and randomly varying the series of intrinsic forces associated with each atom so as to generate a second conformation of the molecule characterized by a second set of coordinates associated with each atom in the molecule, by a second pattern of forces among each atom and by a second series of intrinsic forces associated with each atom; andc) randomly varying the second set of coordinates so as to obtain a third set of coordinates and thereby generating such possible conformations of the molecule.