Abstract: Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immuno-stimulating agents.

Abstract: The present invention relates to fractions of sources and or preparations of human chorionic gonadotropin, such as fractions of human early pregnancy urine, which fractions have anti-HIV activity. The present invention further relates to pharmaceutical compositions comprising such fractions for treating the effects of HIV infection.

Abstract: The present invention highlights the role of acetyl-CoA carboxylase through its product malonyl-CoA in regulating fatty acid oxidation and synthesis, glucose metabolism and energy homeostasis. It discloses transgenic mice with inactivating mutations in the endogenous gene for the acetyl-CoA carboxylase 2 isoform of acetyl-CoA carboxylase. Inactivation of acetyl-CoA carboxylase 2 results in mice exhibiting a phenotype of reduced malonyl-CoA levels in skeletal muscle and heart, unrestricted fat oxidation, and reduced fat accumulation in the liver and fat storage cells. As a result, the mice consume more food but accumulate less fat and remain leaner than wild-type mice fed the same diet. These results demonstrate that inhibition of ACC2 acetyl-CoA carboxylase could be used to regulate fat oxidation and accumulation for purposes of weight control.

Abstract: A computer readable medium holding data of a molecular model of a ligand-gated ion channel receptor and/or a computer system for modeling said receptor are provided by the instant invention. The molecular model can be used to design novel compounds having activity as non-competitive inhibitors of the ion channel. A preferred embodiment of the invention relates to nicotinic acetylcholine receptors. Compounds having activity as non-competitive inhibitors of ligand-gated ion channel receptors and methods for inhibiting the receptor and treating diseases or disorders mediated by function of the receptor are also disclosed.

Abstract: Silicone liquid crystals, silicone vesicles, and silicone gels are formed by combining (i) an amine functional silicone or an organic amine compound, (ii) an organic epoxide containing at least two epoxy groups or an epoxy functional silicone containing at least two epoxy groups, and (iii) a fluid such as water, a silicone fluid other than a silicone used in (i) and (ii), and a polar organic compound or nonpolar organic compound other than organic compounds used in (i) and (ii) in which the polar and nonpolar organic compound are present at a concentration to provide a level of solids less than 40 percent by weight based on the weight of (i)-(iii). These silicone liquid crystals, silicone vesicles, and silicone gels are useful in personal care for preparing various skin, hair, and underarm products.

Abstract: The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an este

Abstract: Nucleosides and oligonucleosides functionalized to include carbamate functionality, and derivatives thereof. In certain embodiments, the compounds of the invention further include steroids, reporter molecules, reporter enzymes, lipophilic molecules, peptides or proteins attached to the nucleosides through the carbamate group.

Abstract: The invention concerns the use of antifungal agents, in particular those active on fungi of genus Candida, for preparing medicines for preventing or treating pathologies related to the presence in the human organism the following fungi: Entomocorticum sp., Stereum annosum, Phellinus igniarus, Peniophora pithya, Peniophora pieceae, Xilaria longipes, Rosellinia arcuata, Rosellinia necatrix, Multiclavula vernalis, Hericium coralloides, Hericium abietis, Hericium erinaceum, Hericium rivularis, Tricholoma terreum.

Abstract: An aqueous pharmaceutical composition suitable for oral delivery has an insoluble active substance and one or more wetting agents in liquid suspension. The composition contains floccules of the active ingredient and is substantially free of polyethelyne glycol, propylene glycol, glycerol and sorbitol. The formulation has an excellent shelf-life in which caking and sedimentation are inhibited. The composition may be resuspended upon light to moderate shaking.

Abstract: This invention provides methods of inducing an antiviral response in an individual comprising administering to the individual an effective amount of a LT-B blocking agent and a pharmaceutically acceptable carrier. In particular this invention provides methods for treating viral-induced systemic shock and respiratory distress.

Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having a disease which is mediated or characterized by mutations in the RET gene, or thyroid cancer, especially thyroid cancer harboring RET mutations, comprising administering to said animal a therapeutically effective amount of a compound which decreases the activity of the epidermal growth factor (EGF), especially a compound as defined herein.

Abstract: A process for producing new anticancer drugs such that the drugs can be administered in a nontoxic, proto-drug form and, subsequent to a time delay which allows for differential concentration in the targer cancer or invasive tissues or cells, the non-toxic drug is then modified by an activation drug to selectively provide toxic levels of a pharmacologically active agent to the target issue.

Abstract: Novel xylo nucleoside or xylo nucleotide analogs, polynucleotides comprising xylo nucleotide substitution, processes for their synthesis and incorporation into polynucleotides.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R′=H or O(═) as well as pharmaceuticals c

Abstract: Novel oligomers, and synthesis thereof, comprising one or more bi-, tri, or polycyclic nucleoside analogues are disclosed herein. The nucleoside analogues have a “locked” structure, termed Locked Nucleoside Analogues (LNA). LNA's exhibit highly desirable and useful properties. LNA's are capable of forming nucleobase specific duplexes and triplexes will single and double stranded nucleic acids. These complexes exhibit higher thermostability than the corresponding complexes formed with normal nucleic acids. The properties of LNA's allow for a wide range of uses such as diagnostic agents and therapeutic agents in a mammal suffering from or susceptible to, various diseases.

Abstract: The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which comprise a bioactive agent and an organocobalt complex. The bioactive agent is covalently bonded directly or indirectly to the cobalt atom of the organocobalt complex. The bioactive agent is released from the bioconjugate by the cleavage of the covalent bond between the bioactive agent and the cobalt atom in the organocobalt complex. The cleavage may occur as a result of normal displacement by cellular nucleophiles or enzymatic action, but is preferably caused to occur selectively as a predetermined release site by application of an external signal. The external signal may be light or photoexcitation, i.e. photolysis, or it may be ultrasound, i.e. sonolysis.

Abstract: The invention relates to a method of stimulating antibody-dependent cellular cytotoxicity to enhance the elimination of IgE-bearing B-cells comprising administering to a mammal an anti-IgE antibody, which binds to membrane bound IgE, but does not induce histamine release and administering an ISO to the mammal. The ISO may be a CpG containing oligonucleotide, or a modified CpG-containing oligonucleotide with an electron-withdrawing group at least at position C-5 of the cytosine in the CpG sequence. In addition, the method may include the administration of an allergen to improve desensitization therapy.

Abstract: Agents for treating pain, methods for producing the agents and methods for treating pain by administration to a patient of a therapeutically effective amount of the agent are disclosed. The agent may include a clostridial neurotoxin, a fragment or a derivative thereof, attached to a targeting component, wherein the targeting component is selected from a group consisting of compounds which selectively binds at the alpha-2B or alpha-2B/alpha-2C adrenergic receptor subtype(s) as compared to other binding sites, for example, the alpha-2A adrenergic receptor subtype.

Abstract: The disclosed nucleic acid primer sets, used in combination with quantitative amplification (PCR) of tissue cDNA, can indicate the presence of specific proteases in a tissue sample. Specifically, the present invention relates to expression of hepsin protease. The detected proteases are themselves specifically overexpressed in certain cancers, and the presence of their genetic precursors may serve for early detection of associated ovarian and other malignancies, and for the design of interactive therapies for cancer treatment.

Abstract: Methods of identifying a compound that selectively modulates at least one TLR-mediated cellular activity are disclosed. Generally, the methods include identifying a compound as a compound that selectively modulates at least one TLR-mediated cellular activity if the compound modulates one TLR-mediated cellular activity to a different extent than it modulates a second TLR-mediated cellular activity. Compounds so identified and pharmaceutical compositions including such compounds are also disclosed. Methods of selectively modulating immune cells and methods of treating certain conditions are also provided. Such methods include administering to cells or a subject a compound that selectively modulates a TLR-mediated cellular activity.

Abstract: In-situ gelation of a pectic substance. Composition, method of preparation, and method of use of a pectin in-situ gelling formulation for the delivery and sustained release of a physiologically active agent to the body of an animal. The pectin can be isolated from Aloe vera.

Abstract: The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which comprise a bioactive agent and an organocobalt complex. The bioactive agent is covalently bonded directly or indirectly to the cobalt atom of the organocobalt complex. The bioactive agent is released from the bioconjugate by the cleavage of the covalent bond between the bioactive agent and the cobalt atom in the organocobalt complex. The cleavage may occur as a result of normal displacement by cellular nucleophiles or enzymatic action, but is preferably caused to occur selectively as a predetermined release site by application of an external signal. The external signal may be light or photoexcitation, i.e. photolysis, or it may be ultrasound, i.e. sonolysis.

Abstract: The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which comprise a bioactive agent and an organocobalt complex. The bioactive agent is covalently bonded directly or indirectly to the cobalt atom of the organocobalt complex. The bioactive agent is released from the bioconjugate by the cleavage of the covalent bond between the bioactive agent and the cobalt atom in the organocobalt complex. The cleavage may occur as a result of normal displacement by cellular nucleophiles or enzymatic action, but is preferably caused to occur selectively as a predetermined release site by application of an external signal. The external signal may be light or photoexcitation, i.e. photolysis, or it may be ultrasound, i.e. sonolysis.

Abstract: A pharmaceutical and/or cosmetic product comprising first and second active ingredient-containing formulations for topical administration to a patient, wherein said product includes storage means whereby said formulations are maintained separately prior to dispense, together with dispense means which permit said formulations to be dispensed from said storage means, characterised in that (i) an active ingredient in at least one of said formulations is contained within a polymeric delivery system and (ii) both of said formulations comprise water-based carrier bases having substantially the same lipophilicity.

Abstract: Disclosed are bilayer matrices of a polysaccharide such as collagen (COL) and another polysaccharide such as hyaluronic acid (HA) with various COL/HA ratios. Each layer has a porous structure. These materials are useful for tissue regeneration, particularly when used with orthopedic implants and drug delivery.

Abstract: Anti-freeze protein which can be derived from Lichen, said protein having an apparent molecular weight of from 20 to 28 kDa and having an N-terminal amino acid sequence which shows at least 80% overlap with: A-P-A-V-V-M-G-D-A-E-S-F-G-A-I-A-H-G-G-L and modified versions and isoforms of this protein.

Abstract: Phosphorus acid derivatives and the like are used as an amplifier (potentiator) of plant defense responses induced by other materials (elicitors).

Abstract: The invention provides methods for treating a variety of cell proliferative diseases using an EGFR inhibitor.

Abstract: The present invention can provide novel compounds useful as orally administrable growth hormone releaser, more specifically a benzimidazolidinone derivative of formula (1) or a pharmaceutically acceptable salt thereof:

Abstract: This invention provides a method for identifying a treatment regime for a compound or composition effective in treating a PPAR mediated disease or condition. The method includes determingin a treatment regime for the compound or composition that causes expression of a surrogate market for PPAR delta activity whereby the determined dose and route of administration identifies an effective treatment protocol.

Abstract: The invention relates to a method of treating central nervous system disorders and other disorders by administering an alpha2delta ligand such as, for example, a compound of the formula 1

Abstract: The present invention relates to a composition for prevention and treatment of kidney diseases comprising one or more effective component(s) of a PAR-2 activating agent which is able to activate PAR-2 and a pharmaceutically acceptable carrier. The present invention further relates to a method for prevention and treatment of kidney diseases comprising administration of a composition for prevention and treatment of kidney diseases containing a PAR-2 activating agent which is able to activate PAR-2 to patients suffering from kidney diseases, and also relates to the use of a PAR-2 activating agent which is able to activate PAR-2 for the manufacture of a composition for prevention and treatment of kidney diseases. The present invention furthermore relates to a method for screening an effective ingredient for prevention and treatment of kidney diseases comprising screening of the activating action of the test substance to PAR-2.

Abstract: Titration of a combination of drugs or treatment modalities within individual subjects is carried out using an evolutionary operation (EVOP) direct-search procedure such as the Nelder-Mead simplex. Desirability functions are incorporated to define the main response of interest and additional responses or constraints. Statistical methodology for determining whether the titrated treatment combination has resulted in an improvement in patient response and for evaluating whether a therapeutic synergism exists is also incorporated. Inferences can be made about the efficacy of the combination or about the individual drugs or treatment modalities that comprise the combination. This approach allows every patient the potential to benefit from the combination under study and permits the consideration of multiple endpoints simultaneously.

Abstract: The present invention relates to binding pockets of receptor tyrosine kinases (RTKs). The binding pockets may regulate the kinase domain of the receptor tyrosine kinases. In particular, the invention relates to a crystal comprising a binding pocket of a receptor tyrosine kinase that regulates the kinase domain of the receptor tyrosine kinase EphB2. The crystal may be useful for modeling and/or synthesizing mimetics of a binding pocket or ligands that associate with the binding pocket. Such mimetics or ligands may be capable of acting as modulators of receptor tyrosine kinase receptor activity, and they may be useful for treating, inhibiting, or preventing diseases modulated by such receptors. Methods are also provided for regulating the kinase domain of an RTK by changing a binding pocket of the RTK that regulates the kinase domain from an autoinhibited state to an active state or from an active state to an autoinhibited state.

Abstract: The invention concerns a novel &bgr;-secretase, a method of partially purifying this novel &bgr;-secretase, and its use in assays to screen for potential drug candidates against Alzheimer's disease and other neurological diseases. The novel &bgr;-secretase has an estmated molecular weight of about 32-39 kDa or 22-26 kDa in HEK293 cell membrane extracts and human brain samples, respectively, as calculated from radiation inactivation analysis, and has a pH optimum at about pH 6.5-7.0.

Abstract: High throughput screening assays for the identification of potential therapeutic agents able to modulate the activity of enzymes of fatty acid biosynthesis, especially desaturases and/or elongases, are disclosed along with therapeutic uses of the agents identified by such assays for the prevention and/or treatment of diseases related to fatty acid metabolism. Substrates useful in such assays are also described.

Abstract: Methods are disclosed for identifying histamine receptor modulators that affect mast cell or basophil chemotaxis, and the use of such histamine H4 receptor modulators for the prevention, treatment, induction, or other desired modulation of asthma and/or allergic responses, or diseases and/or conditions that are modulated, affected or caused by asthma or allergic responses. Also disclosed is the use of histamine H4 receptor modulators for the prevention, treatment, induction, or other desired modulation of mast cell or basophil chemotactic responses, such as migration to a particular site, or diseases and/or conditions that are modulated, affected or caused by mast cell or basophil chemotaxis.

Abstract: The infection of a mammalian host by a microorganism can be prevented or treated through the disruption of the C. albicans homologue of adenylate cyclase-associated protein gene. These methods may be used in the identification, prevention or treatment of microbial infection of mammalian hosts such as immunocompromised or immunosuppressed humans, for example, those having AIDS or undergoing transplantation or anti-cancer therapy.

Abstract: Methods of diagnosing and/or of treating tumors by administering a nucleoside analogue which is activated by thymidylate synthase and/or thymidine kinase enzyme into a diagnostic or toxic metabolite, and uridine analogue compounds, and compositions of same having a pharmaceutically acceptable carrier. For diagnostic applications, compounds containing a label and methods of use of such compounds are described.

Abstract: The invention encompasses a method for treating or preventing an inflammatory disease or condition in a mammalian patient in need of such treatment or prevention comprising administering to said patient a compound that is capable of simultaneously binding PPAR&agr; and PPAR&ggr; or concomitantly administering a compound that selectively binds PPAR&agr; with a compound that selectively binds PPAR&ggr; in an amount that is effective to treat or prevent the inflammatory disease or condition.

Abstract: The invention encompasses a method for preventing the rupture of atherosclerotic plaques in a mammalian patient in need of such prevention comprising administering to said patient a compound that is capable of simultaneously binding or binding and activating PPAR&agr; and PPAR&ggr; or concomitantly administering a selective PPAR&agr; agent with a selective PPAR&ggr; agent in an amount that is effective to prevent the rupture of atherosclerotic plaques. The invention also encompasses a method for increasing atherosclerotic plaque stability in a mammalian patient in need thereof comprising administering to said patient a compound that is capable of simultaneously binding or binding and activating PPAR&agr; and PPAR&ggr; or concomitantly administering a selective PPAR&agr; agent with a selective PPAR&ggr; agent in an amount that is effective to increase plaque stability.

Abstract: A compound of the formula (I) having a binding activity to the cannabinoid type 2 receptor: 1

Abstract: A compound which acts as an antagonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with bladder hypersensitivity, such as urinary incontinence, which is often associated with irritable bowel syndrome (IBS) and a compound which acts as an agonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with a poorly functioning bladder, such as urinary bladder hypoactivity following prostectomy.

Abstract: Screening methods for identifying compounds that regulate skeletal muscle atrophy or hypertrophy, regulate the activity or expression of the vasoactive intestinal peptide receptors (VPAC) or regulate expression of vasoactive intestinal peptide (VIP) or VIP analogs are provided. Methods for the prophylactic or therapeutic treatment of skeletal muscle atrophy utilizing VPAC as the target for intervention are described.

Abstract: A rapidly disintegrating tablet for oral administration of acid-labile active ingredients is described. The rapidly disintegrating tablet for oral administration of an acid-labile active ingredient comprises a plurality of individual active ingredient units together with pharmaceutical excipients, where the acid-labile active ingredient is present in the individual active ingredient units in a matrix composed of a mixture comprising at least one solid paraffin and one or more substances from the group of fatty alcohol, triglyceride and fatty acid ester, and where excipients which, on oral intake of the tablet, bring about rapid disintegration of the tablet are present.

Abstract: The present invention provides a method of inducing growth or enhancing survival of nervous tissue comprising contacting the nervous tissue with an amount of ebaf effective to induce the growth or enhance the survival of the nervous tissue. The present invention also provides a method for treating a subject having damaged or degenerated nervous tissue comprising administering to the subject an amount of ebaf effective to treat the damaged or degenerated nervous tissue in the subject. The present invention further provides a method for treating a neurodegenerative disease in a subject comprising administering an amount of ebaf effective to treat the neurodegenerative disease. The present invention still further provides a method for preventing the onset or reducing the severity of damaged or degenerated nervous tissue in a subject comprising administering an amount of ebaf effective to prevent the onset or reduce the severity of the damaged or degenerated nervous tissue.

Abstract: The present invention provides store operated calcium influx inhibitor compounds, pharmaceutical compositions, and methods of use. The compounds are useful for treating an inflammatory disease or treating an inflammatory reaction. Preferably, compounds, compositions and methods of this invention are used for treatment of inflammatory skin, pulmonary, musculoskeletal, and gastrointestinal diseases, as well as autoimmune disorders, transplantation treatment, and osteoporosis.

Abstract: Obesity is a common clinical problem in most developed nations and is also rapidly becoming a major health concern in developing nations. Overweight individuals frequently suffer from several metabolic disorders such as insulin resistance, type 2 diabetes and dyslipidemia.

Abstract: It has been found that syntaxin binds and regulates the nucleotide binding folds (NBFs) of sulfonylurea receptors (SURs) in a ATP- and ADP-dependent manner. The present invention therefore provides methods for identifying compounds that effect the binding between a syntaxin protein and a NBF1 and/or NBF2 of a sulfonylurea receptor (SUR). Compounds identified using the method of the invention are useful for treating and/or preventing diseases and/or conditions that have, as their underlying basis, a dysregulation of KAT 191 channels.

Abstract: The present invention relates to methods of treating cancer using a combination of at least two Akt inhibitors or a compound which is an inhibitor of Akt and an inhibitor of a protein kinase, which methods comprise administering to a mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound(s) which are inhibitors of Akt and compound(s) which are inhibitors of protein kinases. The invention also relates to methods of preparing such compositions.