Abstract: The present invention relates to novel neuraminidase activity inhibitors and use thereof for prophylaxis and treatment of influenza infection, that is to fluorosubstituted4-acetamido-5-guanidino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylic acids and their esters of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, wherein R is hydrogen, an optionally substituted C1-C5alkyl, C2-C5alkenyl or C2-C5alkynyl; Rf is CH2F or CHF2. A pharmaceutical composition is provided, a method for its preparation, as well as a method for prophylaxis and treatment of viral diseases.

Abstract: The present invention relates to (S)-proline sulfonamide compounds of formula (I) wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.

Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or

Abstract: The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based on the EGFR inhibitory effect of the compound. A compound represented by the following Formula (I) or a salt thereof.

Abstract: Compositions containing calcium citrate malate wherein the calcium citrate malate exhibits one or more of: a pore area of at least about 30 m2/g; a dissolution rate of at least about 95% by weight of the calcium citrate malate in less than about 120 seconds.

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

Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.

Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-I) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers.

Abstract: The present invention relates to compounds for treatment that protects the endothelium, prevent pathologic thrombus formation in the microcirculation and preserve platelet number and function and thus may be related to minimizing or preventing development of organ failure, including multiple organ failure (MOF), and, hence, death in critically ill patients by administration of agent(s) limiting the platelets ability to aggregate and form clots and/or by agents modulating/preserving endothelial integrity and/or by agent(s) increasing the rate of thrombus lysis, and Another aspect of the invention related to by a cell-based whole blood viscoelastical haemostatic assay identifying critically ill patients at increased risk of development of organ failure, including multiple organ failure (MOF) and death.

Abstract: The present invention relates to the benzimidazole-4-carboxamide derivatives, their preparation methods, pharmaceutical compositions and their uses; wherein X represents monosubstituted or bissubstituted or polysubstitued C1-C14 alkoxy, monosubstituted or bisubstituted or polysubstitued C1-C14 alkyl, monosubstituted or bisubstituted or polysubstitued C2-C14 alkenyl, monosubstituted or bisubstituted or polysubstitued C6-C14 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom; Y represents hydrogen, monosubstituted or bisubstituted or polysubstitued C1-C16 alkyl, monosubstituted or bisubstituted or polysubstitued C6-C12 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom.

Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt. sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.

Abstract: In one embodiment, provided is a composition including a prostaglandin compound for modulating stem cell proliferation and/or differentiation in a mammalian subject. In another embodiment, the instant application is directed to a composition which includes a prostaglandin compound for modulating proliferation and/or differentiation of stem cells of a mammalian subject, in which the stem cells are contacted directly or indirectly with the composition of the invention.

Abstract: Methods of treating at least one condition chosen from pain, inflammation, and fever in a critically ill patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen using a first dosage regimen, wherein the first dosage regimen produces a first pharmacokinetic profile in critically ill patients that is about equivalent to a second pharmacokinetic profile produced by administration of the intravenous pharmaceutical composition using a second dosage regimen of ibuprofen to non-critically ill patients, wherein the at least one condition of the critically ill patient is thereby treated.

Abstract: Embodiments of the invention include glycerol esters and use of the same for active agent delivery systems and methods. In an embodiment, the invention includes an active agent eluting device including a glycerol ester, an active agent dispersed within the glycerol ester, the active agent eluting device configured to elute the active agent from the glycerol ester in response to degradation of the glycerol ester. In an embodiment, the invention includes a composition including a glycerol ester; an active agent dispersed within the glycerol ester; the active agent eluting device configured to elute the active agent from the glycerol ester in response to degradation of the glycerol ester. Other embodiments are also included herein.

Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.

Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that suppress or down-regulate microRNA expression in dermal fibroblast, resulting in enhanced production of collagen, elastin and/or fibrillin in the skin. Also provided are methods for screening for activity against specific microRNAs and the methods of using active agents identified by the screening protocol in the treatment of skin.

Abstract: The invention provides a topical formulation adapted for treatment of a skin condition comprising (i) at least one retinoid; and (ii) salicylic acid or an ester, amide, salt, or solvate thereof. The invention also includes a kit for treatment of skin conditions comprising a retinoid and salicylic acid, as well as a method of treating skin conditions utilizing the inventive formulation and kit.

Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.

Abstract: The invention herein generally relates to pharmaceutical formulations and methods of treating an overweight or obese subject, and overweight- or obesity-related conditions.

Abstract: The present disclosure relates to combinations comprising (a) methotrexate, and (b) a DHODH inhibitor and their uses.