Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substitutents are defined as in Claim 1.

Abstract: We disclose a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such as SCS in the presence of an adrenal incidentaloma.

Abstract: The present invention is directed to new oral formulations of chemotherapeutic agents, their process of preparation as well as their therapeutic uses. More specifically, said invention is related to nanoparticles comprising at least one chemotherapeutic agents as an active ingredient, at least one polymer and at least one cyclic oligosaccharide capable of complexing said camptothecin derivative, said nanoparticles being for therapeutic oral administration.

Abstract: The present invention relates to new quinoline inhibitors of tyrosine kinases, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Provided herein are methods for identifying a subject afflicted with chronic lymphocytic leukemia who is responsive to treatment with a chemotherapeutic agent by detecting the presence or absence of at least one APOE4 allele in the subject, the presence of an APOE4 allele identifying the subject as responsive to the treatment. Also provided are methods of treating a subject afflicted with chronic lymphocytic leukemia, including administering an estrogenic agent, an androgen withdrawal agent, an apoE4 peptide or mimetic thereof, and/or a chemotherapeutic agent in an amount effective to treat said chronic lymphocytic leukemia. Methods of determining a prognosis for a patient diagnosed with chronic lymphocytic leukemia are also provided. In addition, methods for stratifying a subject into a subgroup of a clinical trial and methods for identifying a patient in a clinical trial of a treatment for chronic lymphocytic leukemia are herein provided.

Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.

Abstract: Compositions and methods for treating, preventing and/or delaying the onset and/or the development of diseases and disorders of the central nervous system are disclosed. The present disclosure relates to indoloquinoline compounds that are capable of inhibiting at least one protein kinase, and to methods for preparing and uses of such compounds. The compounds described herein are administered to patients to achieve a therapeutic effect.

Abstract: Disclosed is the oral use of dopamine partial agonists and the physiologically acceptable salts thereof in order to create a pharmaceutical preparation for treating the restless legs syndrome, which effectively controls the symptoms while having a significantly smaller undesired effect of a medicament than medicaments known in prior art.

Abstract: Disclosed are new classes of phenanthridinium derivatives, most notably dihydro-imidazo-phenanthridinium (DIP) compounds. The compounds are prepared by the reaction of the middle b ring of a phenanthridinium core with primary amines to form the DIP compounds. This reaction can also be applied to other classes of starting compounds which comprise a 6-membered ring aromatic heterocycle having a ring nitrogen and at least one alpha hydrogen atom which can be reacted with a primary amine. Also disclosed is a method of using the DIP compounds for treatment of ovarian cancer.

Abstract: The present invention provides new methods of treating bowel disease (BD) by increasing a durability of response; treating BD in males; treating BD in adolescent subjects; treating bloating due to BD in males; and methods of maintaining remission of BD.

Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an anti-tumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, said rings being linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.

Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.

Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.

Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

Abstract: The subject invention concerns materials and methods for treating oncological disorders in a person or animal using any agent or compound that inhibits uptake of glucose into a cell. The subject invention also concerns methods for inducing apoptosis and inhibiting the proliferation or survival of a cell. In one embodiment, the methods comprise administering an effective amount of an agent or compound that inhibits the activity of one or more glucose transporter proteins, such as Glut-1. An antibody that binds to and inhibits a glucose transporter protein can be used in the present methods.

Abstract: This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.

Abstract: Treatment of traveler's diarrhea in subjects having hepatic encephalopathy using rifaximin is disclosed.

Abstract: Biomass (e.g., plant biomass, animal biomass, microbial, and municipal waste biomass) is processed to produce useful products, such as food products and amino acids.

Abstract: The present disclosure provides lipid-containing compositions, including targeted liposomes encapsulating drug, and pharmaceutical formulations thereof, as well as methods for the making and using the lipid-containing compositions, including the use of the targeted liposomes in the treatment of cancer and other diseases.

Abstract: Biomass (e.g., plant biomass, animal biomass, microbial, and municipal waste biomass) is processed to produce useful products, such as food products and amino acids.

Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an anti-tumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, wherein the rings are linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.

Abstract: This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection.

Abstract: The present invention provides methods and compositions for predicting patient responses to cancer treatment using a proliferation gene signature. These methods can comprise measuring in a biological sample from a patient the levels of gene expression of a group of the genes designated herein. The present invention also provides for microarrays that can detect expression from a group of genes.

Abstract: The invention relates to a compound of general formula I, II, III, IV, V, VI, VII, VIII, IX, X or a tautomer and the stereochemically isomeric forms thereof or pharmaceutically acceptable salts thereof, a N-oxide form thereof or a pro-drug thereof. The compound is usable as a medicament for the treatment of mycobacterial disease.

Abstract: A method of producing water-insoluble anti-cancer drug in the form of particulates, the method including preparing a water-insoluble anti-cancer drug having at least one multiple bond in the structure, and irradiating said water-insoluble anti-cancer drug with a laser beam having a wavelength of a low absorption portion in the vicinity of the foot of an absorption curve on the long wavelength side within the absorption band until said water-insoluble anti-cancer drug is formed into particulates having an average particle diameter of 50 to 200 nm.

Abstract: The present invention provides methods of treating or preventing a substance-related disorder using selective delta opioid receptor-1 (DOP-R1) agonists, delta opioid receptor-2 (DOP-R2) antagonists, and/or mu opioid receptor (MOP-R) antagonists, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof. The methods provided herein further comprise administering a therapeutically effective amount of a combination of a DOP-R1 agonist and a DOP-R2 antagonist. The methods also comprise administering a therapeutically effective amount of a combination of a DOP-R1 agonist and an MOP-R antagonist. The methods provided herein further comprise administering a therapeutically effective amount of a combination of a DOP-R1 agonist and a DOP-R2 antagonist and a MOP-R antagonist. The invention also relates to compositions containing the same. The invention also relates to methods of determining delta opioid receptor specificity of candidate agents.

Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

Abstract: The present invention provides RecA inhibitors, compositions containing them, systems for identifying or characterizing them, and methods of using them.

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 relates to a liposomal pharmaceutical preparation containing a multivalent ionic drug, a process for the preparation of the liposomal pharmaceutical preparation, and a use thereof in the treatment of diseases, in which the liposome has a size of about 30-80 nm, and the phospholipid bilayer has a phospholipid with a Tm higher than body temperature, so that the phase transition temperature of the liposome is higher than the body temperature.

Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

Abstract: Compounds of formula G1-L-G2, where G1, is a radical structurally close to cryptolepine, -L- is a single covalent bond or a covalent linking biradical selected from —(CH2)rNR??(CH2)s— and —(CH2)rNR??(CH2)sNR??(CH2)t—, —R?? and —R?? are radicals, same or different, selected from the group consisting of H and (C1-C3)-alkyl; r, s and t are an integer from 1 to 3 and -G2 is H or a radical structurally close to -G1, are intercalators. They are compounds which intercalate between DNA base pairs, and are useful as therapeutic agents against cancer, as assess by an in vitro test of citotoxicity with human leukemia cells Jurkat E6-1 and human carcinoma cells GLC-4. Preferred compounds are those where -G1 is bonded to -L- through a carbonyl amino and -L- is —(CH2)3NCH3(CH2)3— or —(CH2)2NCH3(CH2)sNCH3(CH2)2— where s=2 or 3.

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: Disclosed herein are drug compounds that have MDR-inverse activity and thus are effective against multidrug-resistant cells. Exemplary compounds disclosed herein have the structure: Examples of the disclosed compounds have been found to have, inter alia, efficacy in directly treating multidrug resistant cells, rendering multidrug resistant cells susceptible to other chemotherapeutics and in some instances reversing multidrug resistance.

Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of inflammation and cancer.

Abstract: Method for predicting the survival of a patient suffering from NSCLC to an antimicrotubule agent based chemotherapy treatment which comprises the step of determining the methylation state of a nucleic acid encoding CHFR in a biological sample from the patient, wherein the presence of methylation is indicative of longer survival of said patient as a response to said chemotherapy treatment. The methylation status of the CHFR gene can be easily determined in a serum sample.

Abstract: Disclosed herein are indolo[3,2-c]quinoline compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R and m are given the definitions as set forth in the Specification and Claims. These compounds can be used to inhibit both growth of cancer cells and activity of telomerase.

Abstract: This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.

Abstract: A pesticide composition solution is provided. The pesticide composition includes an effective amount of active ingredient according to the formula I and a pesticide adjuvant, Wherein: R1 is Na or K, and R2 is H or OH. The pesticide composition solution in this invention can be processed using simple methods, does not require the use of organic solvents, can reduce environmental pollution, and will greatly lower pesticide production costs. In addition to the good pest control effect of the pesticide composition solution, the potassium salt contained in the solution can provide nutrients to crops, and promote plant growth. This pesticide composition solution is safe and reliable in use.

Abstract: Various calcium channel blockers and pharmaceutical compositions containing these compounds are disclosed. Calcium channel blockers are compounds capable of inhibiting calcium ion channels. Methods for preparing calcium channel blockers and their use as calcium channel antagonists are also disclosed.

Abstract: Provided herein are tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analogs and derivatives, compositions comprising an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog and/or derivative and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, a reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, an ocular or opthalmologic disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, contrast induced nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog or derivative.

Abstract: The present invention relates to novel derivatives of flavopereirine and methods for manufacture thereof. The novel derivatives of flavopereirine are useful for inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention more specifically relates to the use of derivatives of flavopereirine for the inhibition and/or prevention of cancer of the ovary, breast, prostate, pancreas, oral cavity, lung, colon, and larynx.

Abstract: The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I: In Formula I, R1 is H, C1-6 alkyl, or C1-6 alkyl-aryl. Each of R2 and R4 of Formula I are independently H, halogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkoxy, —OR2a, —SR2a, —C(O)R2a, —C(O)OR2a, —C(O)NR2aR2b, —NR2aR2b, C1-6 alkyl-NR2aR2b, —N(R2a)C(O)R2b, —N(R2a)C(O)OR2b, —N(R2a)C(O)NR2aR2b, —OP(O)(OR2a)2, —S(O)2OR2a, —S(O)2NR2aR2b, —CN, —NO2, cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Each of R2a and R2b of Formula I are independently H, C1-6 alkyl, C1-10 heteroalkyl or C1-6 alkyl-aryl. R3 of Formula I is absent, C1-6 alkyl or N-oxide. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.

Abstract: Compounds, compositions and methods for the treatment of malignancy are disclosed.

Abstract: Sustained release pharmaceutical composition comprising at least one poorly soluble active agent(s), at least one solubilizer, a release rate controlling polymer system consisting of an acid-soluble polymer and a pH-dependent polymer, and optionally other pharmaceutically acceptable excipients. The present invention also describes a process for preparation of such compositions and method of using such compositions. The sustained release compositions are useful in providing therapeutically effective levels of active agent(s) for extended periods of time.

Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.

Abstract: Provided are non-steroidal tricyclic compounds that are modulators of androgen receptors and methods for making and using such compounds.

Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: Kratom (Mitragynia speciosa korth) is recognized increasingly as a remedy for opioid withdrawal by individuals who self-treat chronic pain and/or generalized substance abuse. For example, opioid withdrawal from an abrupt cessation of opiate abuse may be self-managed by using Kratom. Further, high-throughput molecular screening identified that a major component of Kratom (i.e., for example, mitragyinine) displayed high binding affinity at mu, delta and kappa opiate receptors. The present invention contemplates that Kratom extract may also be useful for the treatment of other addictive drugs besides opiate derivatives.

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.