Abstract: This invention relates to pharmaceutical compositions consisting of a semisynthetic derivative of vinca alkaloid, stable at room temperature, in which said derivative is present in the form of a freeze dried product obtained in the presence of at least one carbohydrate.

Abstract: Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds.

Abstract: The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.

Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.

Abstract: Curcumin, a polyphenol extracted from the rhizome turmeric, has been polymerized to produce a polymer material having a backbone of one or more repeating structural units, at least one of which comprises a curcumin monomer residue. These curcumin-containing polymers have a wide range of pharmacological activities, including, among others antitumor, antioxidant, antiinflammatory, antithrombotic and antibacterial activities. Certain species of these polymers have exhibited remarkable antitumor activity. Water-soluble curcumin derivatives and their use as prodrugs and prodrug carriers are also disclosed.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.

Abstract: The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract: A radioactive compound having the formula: and pharmaceutically-acceptable salts thereof, wherein R1 and Ar are as defined in the specification, enantiomers, in vivo-hydrolysable precursors, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them and uses of them for diagnostic and analytic purposes.

Abstract: An oil body carrier, its uses in target therapy and/or detection, and a fusion protein comprised therein are provided. The oil body carrier comprises: a) the fusion protein, comprising an oil body protein and a ligand peptide, an antibody peptide, a cell penetrating peptide, or combinations thereof, and b) a lipid, wherein the weight/volume (?g/?l) ratio of the fusion protein and the lipid is at least about 1/25, and the average particle size of the oil body carrier is about 10 nm to about 2,000 nm.

Abstract: Compositions and methods for mucosal delivery of agents are provided. The compositions are intended for administration to mucosal surface, such as oral, gastrointestinal and nasal mucosa. The compositions provided contain one or more mucoadhesive proteins and an agent to be delivered. Methods for delivery of agents using the compositions provided herein are also provided.

Abstract: Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis, cancer and/or another condition responsive to stimulation of thiol-containing compound transport.

Abstract: A polyethylene glycol (PEG) aerogel particles having an average particle diameter not substantially above about 2?, a volumetric porosity of greater than about 50%, and pore sizes capable of retaining drug molecules. A method for preparing such polyethylene glycol (PEG) aerogel particles includes initiating a catalyzed reaction using a catalyst of PEG forming ingredients to form PEG particles; partially drying the formed PEG particles under conditions to control pore size; and subjecting the partially dried formed PEG particles to CO2 supercritical extraction for form the PEG aerogel particles. Drug molecules include chemotherapeutic agents. The surface of the PEG aerogel particles are reactable with a variety of agents, for example, to selectively target tumors, protects irreversible damage to labile proteins, and protects degradation of sensitive drugs with subsequent loss of biological efficacy.

Abstract: The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.

Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.

Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.

Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: The invention provides for compositions and methods for predicting an individual's responsitivity to cancer treatments and methods of treating cancer. In certain embodiments, the invention provides compositions and methods for predicting an individual's responsitivity to chemotherapeutics, including platinum-based chemotherapeutics, to treat cancers such as ovarian cancer. Furthermore, the invention provides for compositions and methods for predicting an individual's responsivity to salvage therapeutic agents. By predicting if an individual will or will not respond to platinum-based chemotherapeutics, a physician can reduce side effects and toxicity by administering a particular additional salvage therapeutic agent. This type of personalized medical treatment for ovarian cancer allows for more efficient treatment of individuals suffering from ovarian cancer.

Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract: The invention provides an array comprising a substrate and a set of addressable elements, wherein each addressable element comprises (i) a polynucleotide that specifically binds to a target molecule, (ii) a polypeptide that specifically binds to target molecule, or (iii) a combination of (i) and (ii), wherein the target molecule is selected from the group of cancer-related target molecules as defined herein. Related kits, methods, and uses as described herein are further provided by the invention.

Abstract: A process for advantageously producing tablets having an improved release property and an excellent stability to change with time is provided. The process is for producing tablets containing a morphinan compound represented by the Formula (I) below or pharmaceutically acceptable acid addition salt thereof and an acidic substance such as fumaric acid, maleic acid or adipic acid, and characterized in that the morphinan compound or a pharmaceutically acceptable acid addition salt thereof is granulated by wet granulation together with (an) excipient(s) prior to adding the acidic substance thereto.

Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract: The present invention relates to anhydrous crystalline vinflunine salts obtained with 1 or 2 equivalents of a pharmaceutically acceptable mineral or organic acid [Acid] 1 or 2 in which [Acid] represents hydrobromic, sulfuric, lactic and fumaric acids for the group of water-soluble crystalline salts, and para-toluene sulfonic, benzoic, mandelic and para-hydroxy benzoic acids for the group of relatively insoluble crystalline salts.

Abstract: A therapeutic agent for sepsis and various symptoms accompanying sepsis (such as septic shock, disseminated intravascular coagulation syndrome, adult respiratory distress syndrome and multiple organ dysfunction) is disclosed. The therapeutic agent for sepsis according to the present invention comprises as an effective ingredient an opioid ? receptor agonist compound such as (?)-17-(cyclopropylmethyl)-3,14?-dihydroxy-4,5?-epoxy-6?[N-methyl-trans-3-(3-furyl)acrylamide] oxide derivative. The opioid ? receptor agonist compound may be administered as it is or in the form of a pharmaceutical composition prepared by mixing the compound with a known pharmaceutically acceptable acid, carrier or vehicle orally or parenterally.

Abstract: A method of treating a FLT3-mediated condition in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I), The conditions that can be treated by the compounds of the present invention and the definitions for the variables in formula (I) are provided herein.

Abstract: Chronic pain is alleviated in a mammal suffering there from by administering to the mammal a chronic pain alleviating amount of a nontoxic N-methyl-D-aspartate receptor antagonist such as dextromethorphan, dextrorphan, ketamine or pharmaceutically acceptable salt thereof, in combination with a ?-opiate analgesic such as tramadol or an analogously acting molecular entity, and a capsaicin or an ester of capsaicin, and optionally in sustained release dosage form.

Abstract: A method of enhancing the activity of lysosomal ?-Galactosidase A (?-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.

Abstract: The present invention relates to a method of treating obesity in a subject by administering to the subject a compound having the formula: wherein n is from 0 to 8; R1 is CH2OH, CH(OH)R5, CH2OR5, CO2R5, C(O)NH2, C(O)NHR5, C(O)NR5R6, C(O)NHNH2, C(O)NHNHR5, C(O)NHNR5R6, C(O)NR5NH2, C(O)NR5NHR6, C(O)NR5NR6R7, C(O)NHNH(C(O)R5), C(O)NHNR5(C(O)R6), C(O)NR5NH(C(O)R6), C(O)NR5NR6(C(O)R7), CN, or C(O)R5; R2 is H, unsubstituted or substituted alkyl, YH, YR8, YR8R9, YR8YR9YR10, YC(O)R8, C(O)YR8, C(O)NH2, C(O)NHR8, C(O)NR8R9, NH2, NHR8, NR8R9, NHC(O)R8, or NR8C(O)R9; R3 and R4 are the same or different and are selected from the group consisting of H, halogens, unsubstituted or substituted alkyl, OH, OR NH2, NHR10, NR10R11, NHC(O)R10, or NR10C(O)R11; R5, R6, R7, R8, R9, R10, and R11 are the same or different and are selected from the group consisting of H, unsubstituted alkyl, substituted alkyl, unsubstituted aryl and substituted aryl; R12 is selected from the group consisting of H, unsubstituted alkyl, and substituted

Abstract: Azole compounds containing carbamoyl group and pharmaceutically useful salts thereof are described. The compounds are effective anticonvulsants which are used in the treatment of disorders of the central nervous system, especially as anxiety, depression, convulsion, epilepsy, migraine, bipolar disorder, drug abuse, smoking, ADHD, obesity, sleep disorder, neuropathic pain, stroke, cognitive impairment, neurodegeneration, stroke and muscle spasm.

Abstract: The present invention provides methods of treating of disorders characterized by defective mitochondrial activity. In particular compounds of the present invention can be used in the treatment metabolic diseases and neurodegenerative diseases. The methods are also useful to increase oxidative phosphorylation or to decrease reactive oxygen species (ROS) production in a subject in need thereof.

Abstract: The present invention provides improved treatment methods by the administration of the non-physiologic D-isomer of an IDO inhibitor.

Abstract: The present invention comprises compositions and methods for delivery systems of agents, including therapeutic compounds, pharmaceutical agents, drugs, detection agents, nucleic acid sequences and biological factors. In general, the nanotherapeutic compositions of the present invention comprise a platform comprising a colloidal metal, a targeting ligand such a tumor necrosis factor, a stealth agent such as polyethylene glycol, and one or more diagnostic or therapeutic agents for delivery. The invention also comprises methods and compositions for making such nanotherapeutic compositions and for the treatment of cancer.

Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations thereof, and use thereof for prevention and treatment of disorders such as septic shock and organ damage.

Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.

Abstract: The invention pertains to a method of using oxymorphone in the treatment of pain by providing a patient with an oxymorphone dosage form and informing the patient or prescribing physician that the bioavailability of oxymorphone is increased in patients with renal impairment.

Abstract: The invention pertains to a method of using oxymorphone in the treatment of pain by providing a patient with an oxymorphone dosage form and informing the patient or prescribing physician that the bioavailability of oxymorphone may be increased in patients with hepatic impairment.

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 present invention relates to methods of alleviating pain with the administration of norketamine with a narcotic. More particularly, the invention provides a method of alleviating pain through the administration of a dose of norketamine, which, if administered alone would provide sub-optimal analgesic relief, yet provides analgesic relief when combined with a narcotic. In some embodiments, the combination of norketamine with a narcotic, further allows for the administration of a dose narcotic, which would be sub-optimal if used alone, but provides adequate pain relief in combination with norketamine. The invention relates to self-management of pain on an outpatient basis comprising administering via conventional routes, including transdermal, nasal, rectal, oral, transmucosal, intravenous, intramuscular, and other routes, one or more doses of norketamine/opioid compositions effective to alleviate pain to a subject suffering from pain.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain.

Abstract: This invention features opioid compounds having activity at kappa and mu receptors, methods for preparing the mu/kappa opioids, and methods for the treatment of pain or a dopamine dysregulation disease, such as schizophrenia, attention deficit hyperactivity disorder (ADHD), attention deficit hyperactivity disorder (ADD), Parkinson's disease, hyperprolactinemia, depression, and addiction.

Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8–12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compounds are effective to enhance glucocerebrosidase activity.

Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).

Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8-12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compoiunds are effective to enhance glucocerebrosidase activity.

Abstract: A method of enhancing the activity of lysosomal &agr;-Galactosidase A (&agr;-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.

Abstract: A therapeutic agent for sepsis and various symptoms accompanying sepsis (such as septic shock, disseminated intravascular coagulation syndrome, adult respiratory distress syndrome and multiple organ dysfunction) is disclosed. The therapeutic agent for sepsis according to the present invention comprises as an effective ingredient an opioid &kgr; receptor agonist compound such as (−)-17-(cyclopropylmethyl)-3,14&bgr;-dihydroxy-4,5&agr;-epoxy-6&bgr;[N-methyl-trans-3-(3-furyl)acrylamide] oxide derivative. The opioid &kgr; receptor agonist compound may be administered as it is or in the form of a pharmaceutical composition prepared by mixing the compound with a known pharmaceutically acceptable acid, carrier or vehicle orally or parenterally.

Abstract: Glucoside and glucuronide derivatives of hydromorphone, dihydromorphine, and dihydroisomorphine and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising a glucoside or glucuronide derivative of hydromorphone, dihydromorphine, or dihydroisomorphine or a pharmaceutically acceptable salt thereof; and methods for treating or preventing pain in a patient comprising administering to a patient in need thereof a glucoside or glucuronide derivative of hydromorphone, dihydromorphine, or dihydroisomorphine or a pharmaceutically acceptable salt thereof are disclosed.