Abstract: Provided herein are compounds of formula (I)-(VI): wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.

Abstract: This documents provided methods and materials involved in treating bladder cancer. This document also provides methods and materials involved in identifying bladder cancer patients likely or unlikely to respond to treatment (e.g., BCG therapy).

Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: The invention discloses 4-(arylamino)selenophenopyrimidine derivatives of formula (I), hydrates, solvates, isomers, or pharmaceutically acceptable salts thereof; process for their preparation and methods of treating or inhibiting or controlling a cell proliferative disorders, particularly cancer using said compounds. Pharmaceutical compositions comprising 4-(arylamino)selenophenopyrimidine derivatives of formula (I) are useful for the treatment, inhibition, or control of cancer.

Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.

Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including an anthracycline. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including anthracycline and administering the therapy in subjects when it is found that anthracycline is likely to be effective.

Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.

Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.

Abstract: The present invention provides, e.g., compounds having the structure of formula (I): The present invention also provides pharmaceutical compositions that include such compounds, and methods for modulating murine double minute 2 protein (Mdm2) E3 ligase activity, particularly the Mdm2-MdmX hetero-complex E3 ligase activity, using such compounds.

Abstract: The present invention relates to a compound of General Formula (I) below, among others. In the Formula, Ar1 is an optionally substituted aryl or heteroaryl group; R1 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, or an optionally substituted aryl, aralkyl, or heteroaryl group; R2 is an optionally substituted aryl, aralkyl, or heteroaryl group; and R3 is a hydrogen atom or a C1-C6 alkyl group. A compound of the present invention has an excellent Weel kinase inhibiting effect, and is therefore useful in the filed of medicine, particularly in various types of cancer therapy.

Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.

Abstract: Novel methods of treating proliferative disorders characterized by elevated Her-2, and the patient is then administered an effective amount of an HSP90 inhibitor.

Abstract: Methods for modulating the level of a chemokine in a cell by administering to a cell an effective amount of a depside or an anthocyanin are provided. More particularly, a method for modulating the level of a chemokine in a cell by administering to a cell an effective amount of a depside having the structure of formula (IV): Formula (IV) wherein R is selected from H or CH3 or an anthocyanin selected from cyanidin 3-glucoside, delphinidin 3-glucoside, or combinations thereof, or an enantiomer, optical isomer, diastereomer, N-oxide, crystalline form, hydrate, or pharmaceutically acceptable salt thereof is provided. Also provided are compounds according to Formulas I-IV, pharmaceutical compositions, unit dosage forms, and food or feed supplements containing such compounds.

Abstract: The invention relates to the use of one or more cannabinoids, particularly THC and/or CBD in combination with a non-cannabinoid chemotherapeutic agent in the manufacture of a medicament for use in the treatment of cancer. In particular the cancer to be treated is a brain tumour, more particularly a glioma, more particularly still a glioblastoma multiforme (GBM). The non-cannabinoid chemotherapeutic agent may be a selective estrogen receptor modulator or an alkylating agent.

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: The present invention relates to a cancer sensitizer comprising chlorogenic acid or a derivative thereof. In particular, the present invention relates to a cancer sensitizer comprising chlorogenic acid or a derivative thereof, which can make cancer cells sensitive to anticancer agents to increase the therapeutic effect of anticancer agents. In addition, the present invention relates to a composition for inhibiting the chemo-resistance of cancer cells, comprising chlorogenic acid or a derivative thereof in combination with a pharmaceutically acceptable carrier, an anticancer composition comprising an anticancer agent in addition to the composition, and a method for disrupting the chemo-resistance of cancer cells, comprising administration of the cancer sensitizer.

Abstract: The invention relates to a multimeric, non-coding nucleic acid molecule for modulating the activity of the human or animal immune system, and to a production method therefor, and to a vaccine containing said multimeric, non-coding nucleic acid molecule. Said multimeric, non-coding nucleic acid molecules can be non-coding nucleic acid molecules that consist of at least two of said molecules (dimer) or assemblies of several non-coding nucleic acid molecules.

Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.

Abstract: The invention relates to a compound of general formula (I-0): wherein R1 means a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C3-C6 cycloalkyl group; R2, R3, R4 and R5 mean a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo-C1-C6 alkoxy group; R6 means a hydrogen atom, or a C1-C6 alkyl group; R7a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy-C1-C6 alkyl group, -Q2-N(R1c)R1d or a nitrogen-containing heterocyclic group; R8a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy-C1-C6 alkyl group; or R7a and R8a form, as taken together, a C2-C6 alkylene group, or R7a and R8a and the ring atoms to which they bond may form a spiro ring or a bicyclo ring; and X and Y mean a methine group or a nitrogen atom.

Abstract: The present invention relates to methods of treating a cancerous tumor in a subject comprising administering to the subject an effective amount of 3-bromopyruvate. The 3-bromopyruvate may be administered intraarterially directly to a tumor as a continuous intraarterial infusion. The present invention also relates to methods for identifying agents that inhibit type II hexokinase activity.

Abstract: The present invention describes polymer nanoparticles with a cationic surface potential, in which both hydrophobic and hydrophilic pharmaceutically active substances can be encapsulated. The hydrophilic and thus water-soluble substances are encapsulated in the particle core by co-precipitation through ionic complexing with a charged polymer. Both therapeutic agents and diagnostic agents can be used as pharmaceutically active substances for encapsulation. The cationic particle surface permits stable, electrostatic surface modification with partially oppositely charged compounds, which can contain target-specific ligands for improving passive and active targeting.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: The present invention relates to new quinazoline inhibitors of EGFR tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A combination of an mTOR inhibitor compound with one or more pharmaceutically active agents, for simultaneous, concurrent, separate or sequential use for preventing or treating a proliferative disease.

Abstract: The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.

Abstract: Disclosed are compositions and methods used to treat and/or prevent cancer and metabolic diseases, such as psoriasis. In one aspect, the present invention pertains to the use of cross-linking analogs of vitamin D and its metabolites employed for the treatment of prostate cancer.

Abstract: A preventive/therapeutic composition for free radical diseases, characterized by containing as an active ingredient at least one kind of a fullerene, a fullerene derivative, and a composite comprising a fullerene or fullerene derivative and an organic compound with which the fullerene or derivative has been modified or clathrated. The composition is reduced in side effects, has the high ability to eliminate free radicals in the body, and further has excellent preparation stability.

Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.

Abstract: The purposes of this invention are preparation of the non-mucin type synthetic compounds-carrier conjugated compounds which are stable against enzymes, and which have the ability of specific reactivity to induce immune response for cancer and HIV.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit outstanding effects on the cardiovascular system.

Abstract: Compounds of the formula I ##STR1## in which R signifies a possibly substituted amino group of the general formula --NR.sup.1 R.sup.2, whereby, independently of one another, R.sup.1 and R.sup.2 each signify hydrogen, lower alkyl, lower alkenyl or lower alkynyl or R represents a saturated, unsaturated or aromatic heterocyclic ring which can possibly be substituted once or twice by lower alkyl or halogen, alk signifies a valency bond, a methylene, a saturated or unsaturated, straight-chained or branched alkylene chain with 2-6 carbon atoms and R.sup.3, R.sup.4 and R.sup.5, in each case independently of one another, signify hydrogen, lower alkyl or benzyl, as well as their pharmacologically acceptable salts and enantiomers, whereby, for the case that R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3 and alk signifies a valency bond, R cannot be the dimethylamino group, processes for their preparation and medicaments which contain these compounds for the treatment of calcium metabolism diseases.

Abstract: A stable lyophilized composition of the antitumor alkylating agent thiotepa and a method of preparing such a composition via co-lyophilization of the active ingredient with a pharmaceutical acceptable alkalizing agent.

Abstract: The present invention relates to compounds of the Formula I: ##STR1## wherein R is hydrogen, alkyl, cycloalkyl, phenyl, or alkylphenyl, and n is 2 through 4, the production thereof, pharmaceutical compositions thereof, and their use in antineoplastic therapy.

Abstract: 9-Amino-2-phenylbicyclo-[3.3.1]nonanes and 9-amino-2-phenylbicyclo[3.3.1]non-2-enes of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is hydrogen, halogen, alkyl, alkoxy, dialkylamino, trifluoromethyl, hydroxyl, alkylthio, alkylsulfonyl or nitro, R.sup.3 and R.sup.4 are identical or different and each is hydrogen, alkyl or 1 to 5 or alkenyl or alkynyl of 2 to 5 carbon atoms, or benzyl, it also being possible for R.sup.3 and R.sup.4 together to form a saturated chain which contains from three to seven carbon atoms and can be substituted by phenyl, and where is a single or double bond, are used for producing drugs which act, in particular, on the central nervous system.