Abstract: The present disclosure relates to fused N-arylsulfonamidyl-thienoisoquinoline compounds, derivatives and pharmaceutical compositions thereof, and methods and uses in inhibiting cancer cell growth, along with a supplemental anti-cancer agent. Centrosome targeting and microtubule depolymerisation are attractive in designing the present chemotherapeutic compounds. The various diseases and conditions treated include various types of cell cancers, and in vitro inhibition.

Abstract: A method of treating or preventing a neuroinflammatory and/or neurodegenerative disease in a subject by administering a pharmaceutically effective amount of a CB2 receptor agonist is described. The CB2 receptor agonist can be a compound according to formula I (structurally represented) or a pharmaceutically acceptable salt thereof, with R1 and R2 functional groups as defined herein. Administration of the CB2 receptor agonist activates CB2 receptors in the microglia, and can restore synaptic plasticity, cognition, and memory in subjects having elevated levels of amyloid-13 peptide in the brain.

Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of areata, endogenous acne, exogenous acne or acne rosacea.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

Abstract: The invention discloses methods for preventing or treating addiction by administering to a subject in need thereof a PARP inhibitor.

Abstract: The subject invention provides for cancer therapy.

Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.

Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.

Abstract: The subject invention provides for cancer therapy.

Abstract: The invention provides methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention provides a method of determining whether a subject suffers from, or is at risk of developing, and autophagy mediated disease state and/or condition by evaluating LC3 levels.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.

Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.

Abstract: Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.

Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.

Abstract: The invention discloses methods for preventing or treating addiction by administering to a subject in need thereof a PARP inhibitor.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.

Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.

Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.

Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical composition for use, e.g., in treatment of airway disorders.

Abstract: The compounds of a certain formula (1), in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.

Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.

Abstract: A method of treating or preventing an immune disorder, such as graft versus host disease, in a subject. The method includes the administering a SHIP1 inhibitor, such as 3?-aminocholestane, to a subject in need of treatment. Thus, SHIP1 inhibitors taught herein represent a novel class of small molecules that have the potential to enhance allogeneic transplantation, boost innate immunity and improve the treatment of hematologic malignancies.

Abstract: The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents.

Abstract: The subject matter of this application is directed to combinations of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol with other active compounds for the treatment of diabetes mellitus type 2 and/or type 1.

Abstract: The invention concerns screening molecules with anti-prion activity. More particularly, it concerns kits for screening molecules with anti-prion activity characterized in that they comprise in combination a [PSI+], phenotype yeast, an antibiogram and an agent for purifying prions at sub-efficient doses, said yeast including the ade1-14 allele of the ADE1 gene and an inactivated ERG6 gene, the screening methods, and a family of molecules with anti-prion activity isolated by the inventive screen. The invention is applicable to anti-prion agents for producing medicines in particular for treating neurodegenerative diseases involving protein aggregates.

Abstract: This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.

Abstract: The invention concerns screening molecules with anti-prion activity. More particularly, it concerns kits for screening molecules with anti-prion activity characterized in that they comprise in combination a [PSI+], phenotype yeast, an antibiogram and an agent for purifying prions at sub-efficient doses, said yeast including the adel-14 allele of the ADE1 gene and an inactivated ERG6 gene, the screening methods, and a family of molecules with anti-prion activity isolated by the inventive screen. The invention is applicable to anti-prion agents for producing medicines in particular for treating neurodegenerative diseases involving protein aggregates.

Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.

Abstract: The present invention overcomes the problems associated with existing drug delivery systems by delivering cannabinoids transdermally. Preferably, the cannabinoids are delivered via an occlusive body (i.e., a patch) to alleviate harmful side effects and avoid gastrointestinal (first-pass) metabolism of the drug by the patient.

Abstract: The present invention relates to a method of treating or preventing hyperproliferative disease in a body tissue of a subject, comprising the steps of administering to a subject in need thereof a therapeutically effective amount of an agent that induces double strand breaks in the DNA of the hyperproliferative cells of said body tissue; and subjecting the hyperproliferative cells of said body tissue prior to, simultaneously with or subsequent to step a) to hyperthermia to thereby induce in said cells the degradation, inhibition and/or inactivation of BRCA2.

Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.

Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.

Abstract: Described herein are compositions and methods for preventing and/or treating skin diseases including, but not limited to, psoriasis and atopic dermatitis as well as providing anti-aging benefits which results in reduced appearance of wrinkles and aged skin, improved skin color, treatment of photodamaged skin, improvement in skin's radiance and clarity and finish, and an overall healthy and youthful appearance of the skin, involving aberrant angiogenesis and hyperplasia employing one or more benzo[c]chromen-6-one derivatives.

Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.

Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.

Abstract: The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.

Abstract: The present disclosure relates to a sodium iodide symporter (NIS)-repressor binding sites (NRBS) consensus sequence consisting of a DNA molecule having the sequence 5?-T/C(G/A)GCCT(T/C)A(G/A)TTTCCCCA(T/C)CTGT-3?(the “consensus NRBS”). The disclosure further relates to methods of restoring iodide transport in dedifferentiated thyroid cancer cells by interfering with formation or function of the NIS repressor.

Abstract: Provided herein are compounds, compositions and methods for treating disorders mediated by abnormal cellular proliferation and processes for identifying such compounds.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.