Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.

Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.

Abstract: An oil composition containing 25-hydroxy Vitamin D3 and an oil is provided. In addition an emulsion, a microencapsulated oil composition, and a feed premix composition each containing 25-hydroxy Vitamin D3 are provided. Methods of making an oil composition, a microencapsulated oil composition, and a feed premix containing 25-hydroxy Vitamin D3 are also provided.

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract: The present invention relates compounds for stabilizing cells and methods of their use.

Abstract: Provided herein are method of treating, ameliorating, or delaying at least one symptom of a genetic blood disorder, e.g. sickle cell disorder or thalassemia, in a patient in need thereof, comprising administering a therapeutically effective amount of a Jak2 inhibitor. Also provided in part is a method of reducing an enlarged spleen in a patient suffering from thalassemia, comprising administering a therapeutically effective amount of a Jak2 inhibitor.

Abstract: Described herein are compounds that are inhibitors of one or more protein kinases. Also described are pharmaceutical compositions and medicaments that include the compounds described herein. Also described herein are methods of using such protein kinase inhibitors, alone and in combination with other compounds, for conditions or diseases mediated or dependent upon protein kinases.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Abstract: The invention provides methods and compositions for the delivery of lipophilic drugs that are useful for the treatment of various ophthalmological diseases, disorders, and pathologies, including the treatment of age-related macular degeneration, diabetic retinopathy, diabetic macular edema, cancer, and glaucoma.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Abstract: Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.

Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.

Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.

Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.

Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4? each independently H alkyl; or R4 and R4? together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.

Abstract: The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.

Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.

Abstract: The invention relates to a pharmaceutical dosage form which comprises a solid dispersion product comprising N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide or a salt, hydrate or solvate thereof, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer. The invention is further directed to processes for preparing the pharmaceutical dosage form and to use of the dosage form for treating proliferative disorders.

Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

Abstract: The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.

Abstract: This invention provides a class of compounds which are useful for specifically inhibiting cyclin-dependent kinases. This class of compounds finds use in treating diseases resulting from inappropriate activity of cyclin-dependent kinases, including cancer, viral infections (e.g., HIV) neurodegenerative disorders (e.g. Alzheimer's disease), and cardiovascular disorders (e.g. atherosclerosis). Moreover, certain members of this class are particularly useful for inhibiting cyclin-dependent kinase 7 and are especially useful for the treatment of breast cancer.

Abstract: Devices, systems, and methods are described herein for controlling the level of one or more target cell types in the blood fluid and/or lymph fluid of a vertebrate subject.

Abstract: The invention provides a multi-compartmented container suitable for the delivery of pharmaceuticals, medicines, vitamins, and the like.

Abstract: Purine derivatives of Formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors.

Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.

Abstract: This invention relates to therapeutic compositions comprising a surface active copolymer, such as poloxamer-188, in an amount effective to enhance microvascular blood flow and/or inflammation in injured skin or other tissue, and methods of using the therapeutic compositions of the invention to inhibit decreased blood flow associated with an injury, disease, or disorder.

Abstract: The present invention discloses compositions having particles comprising, inorganic element; one or more active ingredient and optionally a release rate modulating agent, suitable for the delivery of active ingredients to human and animal tissues. The particles are nanoparticles or microparticles or mixtures thereof, made preferably by sol-gel method. The compositions are useful for application to the topical or mucosal surfaces preferably in the form of creams, gels, lotions, dry powders, spray, foam and other suitable forms.

Abstract: The present invention relates to a method of determining the microbial bioburden in a wound (in particular a diabetic ulcer) in a test subject, the method comprising the step of measuring the level of a cytokine in a wound sample, wherein a cytokine level lower than a reference level indicates a significant microbial bioburden in the wound (or a cytokine level higher than a reference level indicates an insignificant microbial bioburden in the wound). The invention provides methods of diagnosis, prognosis and treatment of wound infection, and devices and kits for use in such methods.

Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.

Abstract: Provided is a granular agrochemical composition by which the problems accompanying the prior art granular agrochemical compositions can be overcome, which can be prepared in a simple formulation and by which sustained releasability of the agrochemically active ingredient is obtained so that the load on the environments can be decreased and the chemical damages caused by the agrochemically active ingredient can be alleviated or prevented. The granular agrochemical composition contains an acidic agrochemically active ingredient, a cationic surfactant and a basic substance. Inter alia, a pH of 5 or higher is obtained in a 1% by mass aqueous suspension thereof. Preferably, the acidic agrochemically active ingredient should have a pKa of 2 to 7 and the cationic surfactant should be one which is gelled or exhibits swellability in water.

Abstract: An oil composition containing 25-hydroxy Vitamin D3 and an oil is provided. In addition an emulsion, a microencapsulated oil composition, and a feed premix composition each containing 25-hydroxy Vitamin D3 are provided. Methods of making an oil composition, a microencapsulated oil composition, and a feed premix containing 25-hydroxy Vitamin D3 are also provided.

Abstract: The present invention provides for methods and compounds for treating brain trauma and disorders such as: ischemia, stroke, neurodegenerative disorders, opioid addiction, idiopathic pain, epilepsy, and depression. More specifically, the invention provides methods for designing and identifying inhibitors of mammalian agmatinase and for compounds identified by these methods.

Abstract: The invention relates to a cosmetic composition containing at least one 15-hydroxy-prostaglandin dehydrogenase inhibitor and cosmetically acceptable excipients. It also relates to a method of cosmetic treatment for promoting the growth and/or preventing or delaying the loss of hair, and the use of a 15-hydroxyprostaglandin dehydrogenase inhibitor for the preparation of a composition intended for controlling hair loss and/or for promoting hair regrowth.

Abstract: The present invention features compounds useful for inhibiting RNase P activity. These compounds can be used as therapeutics for treating or preventing a variety of bacterial infections. The compounds belong to several classes including mono- and bis-guanylhydrazones, guanylhydrazone mimetics, and benzothiazolium compounds. Exemplary compounds are compounds of formula I: Y—(NR?)k—U1—(NR?)I—A—(NR1)m—U2—(NR2)n—Z??I with substituents as described herein.

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 application of niacinamide, niacin, and niacin esters (nicotinic acid esters) derivatives of skin beneficial organic acids (henceforth called “derivatives”) for the synergistic treatment or prevention of topical disorders of skin such as acne, rosacea, skin wrinkles, age-spots, canker sores, striae distensae (stretch marks), pimples, and skin redness. These “derivatives” are made by a very simple in-situ method. These “derivatives” provide enhanced bioavailability of both ingredients that are combined to form such derivatives. The “derivatives” of present invention can be formulated in a wide variety of delivery systems including traditional water and oil emulsions, suspensions, colloids, solutions, or anhydrous systems.

Abstract: Disclosed is a method to stimulate or enhance sperm development in males and gonadal development in females by administration of an agent which results in a transiently level of a thyroid hormone such as T3 and increased gonadotropin levels in the blood.

Abstract: Compositions comprising an antibiotic, sulphonamide, at least one an antiquagul agent, e.g., clotrimazol (bis-phenyl-(2-chlorophenyl)-1-imidazolyl-methane), natamycin, or nystatin,and 5-nitro-metronidazol (5-nitro-inidazoles) e.g., (metronidazol or tinidazol or nimorazol) and a pharmaceutically acceptable carrier. The compositions are useful mainly as vaginal suppositories.

Abstract: The invention relates to a method of detecting concentrations of cyclooxygenase-2 in a mammal, the method comprising: administering to the mammal a diagnostically effective amount of a cyclooxygenase-2 selective agent, which is capable of being detected in vivo; and b) detecting the agent so the concentration of cyclooxygenase-2 is detected.

Abstract: Drug and multidrug resistant modulators of the formula: where R1 and R2 are independently hydrogen or halo; A is —CH2—CH2—, —CH2—CHR4—CH2—, or —CH2—CHR5—CHR6—CH2—, where R4 is —H, —OH, or acyloxy; one of R5 or R6 is —H, —OH, or acyloxy, and the other is —H; R3 is a polyaryl; and pharmaceutically acceptable salts and solvates thereof, are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed.

Abstract: A protective cream composition contains 15 to 40 wt % of an alkali metal fatty acid salt having from 8 to 18 carbon atoms, an effective amount of a topical agent such as an antimicrobial compound, 5 to 20 wt. % of a polyol effective as an emollient, 0.5 to 8.0 wt. %, of an alkali metal silicate, and the balance water. Such a composition can be applied to the skin to protect health care workers and other from infection. The cream dries to form a topical barrier on the skin, and also contains an agent effective against, for instance, viruses such as human HIV. Once a medical operation is completed, the film formed from the dried cream can be washed off with soap and water. Other topical agents present in the composition include, for instance, suncreens, insect repellents and chemical repellents.

Abstract: A protective cream composition contains 15 to 40 wt. % of an alkali metal fatty acid salt having from 8 to 18 carbon atoms, an effective amount an antimicrobial compound, 5 to 20 wt. % of a polyol effective as an emollient, 0.5 to 8.0 wt. %, of an alkali metal silicate, and the balance water. Such a composition can be applied to the skin to protect health care workers and others from infection. The cream dries to form a topical barrier on the skin, and also contains an agent effective against, for instance, viruses such as human HIV. Once a medical operation is completed, the film formed from the dried cream can be washed off with soap and water.