Abstract: Disclosed is a trolox derivative-modified fat-soluble anti-cancer pharmaceutical compound having a structure as represented by formula I or II. An active moiety of the anti-cancer pharmaceutical compound, camptothecin or a camptothecin derivative, is covalently bonded to a lipophilic moiety, a trolox ester or a trolox amide, by a linking group to form the fat-soluble anti-cancer pharmaceutical compound. Also disclosed are a preparation, preparing method and use of the pharmaceutical compound.

Abstract: The present invention relates to combination comprising (i) an ErbB inhibitor; and (ii) a CDK inhibitor, or a pharmaceutically acceptable salt thereof, selected from: (a) roscovitine; (b) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-2-methyl-pentan-2-ol; (c) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-pentan-2-ol; and (d) (2R,3S-3-(6-((4,6-dimethylpyridin-3-ylmethylamino)-9-isopropyl-9H-purin-2-ylamino)pentan-2-ol. Further aspects of the invention relate to pharmaceutical products and pharmaceutical compositions comprising combinations according to the invention, and methods of treatment using the same.

Abstract: Stable pharmaceutical composition consisting of a hydrosoluble vinflunine salt and at least one diluent and one lubricant, said composition being in the form of a solid intended for oral administration. The hydrosoluble vinflunine salt is preferably Vinflunine ditartrate. The pharmaceutical composition is advantageously in the form of a capsule or tablet. The invention also concerns a method of treating cancer pathology comprising the oral administration of the pharmaceutical composition of the invention.

Abstract: The present invention provides novel conjugates of camptothecin and camptothecin analogs with a linker and an HSA-binding moiety. The novel conjugates are prodrug forms of the camptothecin or camptothecin analogs and can be used to treat mammalian cell proliferative diseases, such as cancer.

Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ?5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: The present invention relates to compositions and methods comprising resveratrol and uses thereof. Some embodiments include compositions and methods with increased bioavailability of resveratrol. Certain embodiments include compositions comprising resveratrol and a solubilizer. Particular embodiments include transmucosal delivery of resveratrol from the composition.

Abstract: There is described herein compounds, compositions and methods for inducing synthetic lethality in a cancer cell(s).

Abstract: Methods of treating blood disorders are described.

Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.

Abstract: The current application relates to the use of a compound selected from the group consisting of camptothecin and its analog, 10-hydroxy camptothecin, topotecan, irinotecan, 18-beta-glycyrrhetinic acid and its analog, carbinoxolone, etoposide, topoisomerase inhibitors, and combinations thereof, for the treatment of a synucleinopathy disease or disorder such as Parkinson's disease.

Abstract: The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.

Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

Abstract: The differential expression of select miRNA in plasma and bile among patients with PDAC, chronic pancreatitis (CP), and controls were measured. Patients (n=215) with treatment-naïve PDAC (n=77), CP with bile or pancreatic duct pathology (n=67), and controls (n=71) that had been prospectively enrolled in a Pancreatobiliary Disease Biorepository at the time of endoscopic retrograde cholangiopancreatography (ERCP) or endoscopic ultrasound (EUS) were identified. Controls were patients with choledocholithiasis but normal pancreata. The sample was separated into training (n=95) and validation (n=120) cohorts to establish and then test the performance of PDAC Signature Panels in diagnosing PDAC. The training cohort (n=95) included age-matched patients with CP and controls. Panels were derived from the differential expression of 10-candidate miRNA in plasma or bile.

Abstract: Disclosed are polymers containing a backbone comprising alternating N-protected hydroxymethylaniline units (“spacer”) and linker units.

Abstract: The present invention relates to the BAD pathway's influence on development, progression, chemo-sensitivity, and overall survival for multiple human cancers and its potential as a therapeutic target to increase chemo-sensitivity. BAD pathway expression was associated with the development and/or progression of breast, colon, and endometrial cancers, relapse-free survival from breast cancer, and overall survival from ovarian, colon, and brain cancers. Expression was also associated with in vitro sensitivity to a range of cytotoxic agents. pBAD levels were higher in cancer versus immortalized normal cells and chemo-resistant versus—sensitive cancer cells and associated with increased cell proliferation.

Abstract: Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, aryl substituted C1-6 alkyl, phosphate substituted C1-6 alkyl, amino-substituted C1-6 alkyl, carboxyl substituted C1-6 alkyl, hydroxyl substituted C1-6 alkyl, and amide-substituted C1-6 alkyl; R1 is selected from hydrogen and t-butoxycarbonyl substituted amino. Also provided in the present invention are the preparation method of the derivate and the use thereof in anti-tumor drug preparation.

Abstract: The present invention relates to a method for identifying a drug candidate for enhancing expression of p21cip1/waf1 in a human patient suffering from a medical condition that can be treated by enhancing expression of p21C?1/waf1. The method includes (a) providing a cell line comprising a nucleic acid sequence that comprises a p21cip1/waf1 promoter operationally ligated to a reporter domain; (b) exposing the cell line to a compound; and (c) identifying a compound that induces expression of the reporter domain. The compound that induces expression of the reporter domain is a drug candidate for treating a medical condition that can be treated by enhancing expression of p21cip1/waf1.

Abstract: The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.

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: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.

Abstract: The disclosure provides a biomedical composition, including: a hyaluronic acid; a modified histidine; and a polymer or C4-C20 alkane, wherein the modified histidine and the polymer or C4-C20 alkane are grafted to at least one primary hydroxyl group of the hyaluronic acid to allow the hyaluronic acid to form a hyaluronic acid derivative, wherein a graft ratio of the modified histidine is about 1-100%, and a graft ratio of the polymer or C4-C20 alkane is about 0-40%.

Abstract: Methods for treating a patient using therapeutic immune system neuromodulation and associated devices, systems, and methods are disclosed herein. One aspect of the present technology is directed to methods including modulating nerves proximate a vessel or duct of an immune system organ using an intravascularly or intraluminally positioned therapeutic element. One or more measurable physiological parameters corresponding to an immune system disorder, a condition associated with sympathetic activity in an immune system organ, or a condition associated with central sympathetic activity in the patient can thereby be reduced.

Abstract: Disclosed are novel camptothecin derivatives having anti-tumor activity (the basic structure thereof is as shown in the figure) and compositions of such compounds and use thereof. The compounds according to the present invention exhibit very good water solubility and stability, show good selectivity among drugs of the same category, and have a very high therapeutic index. Such compounds are promising as therapeutic agents for treating tumors.

Abstract: This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).

Abstract: The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

Abstract: Among other things, a method of treating a human having brain cancer is, the method comprising administering via a non-continuous dosing regimen to the human having brain cancer, a therapeutically effective amount of a pharmaceutical composition comprising a prodrug or a pharmaceutically acceptable salt thereof, wherein the non-continuous dosing regimen comprises administering the pharmaceutical composition no more frequently than once every seven days for at least two dosings.

Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.

Abstract: The present invention relates to compositions and methods for treating rectal disorders.

Abstract: In one embodiment, the present application discloses synthetic LDL nanoparticles comprising mixtures of components selected from the group consisting of phospholipids, triglycerides, cholesterol ester and free cholesterol; optionally further comprising an agent selected from the group consisting of natural antioxidants, ubiquinol and vitamin E, and methods for preparing the synthetic nanoparticles. The disclosed synthetic LDL nanoparticles are capable of selectively delivering lipophilic drugs and prodrugs to cellular targets expressing LDL receptors after intra venous injection.

Abstract: The subject invention relates to compositions and methods useful for the in vivo delivery of substantially water-insoluble drugs, like taxol. The use of specific composition and preparation conditions enables the reproducible production of unusually water-soluble formulation, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a re-dispersible dry powder comprising nanoparticles of drug. The innovation is also based on the fact that complementary partner is also an active drug but may have a different mode action with respect to primary molecule of the hybrid drug. The complementary molecule has multiple properties like antioxidant, antimicrobial, anti-inflammatory, anti-allergic, cox-2 inhibitors, etc. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable.

Abstract: The disclosure includes hydroxamic compounds of Formula I: (Formula I) wherein Z, L, R1, R2, and R3 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.

Abstract: The invention defines a nonwoven membrane for the controlled and sustained release of a therapeutic or cosmetic active agent in the area of the body to be treated. This nonwoven membrane comprises one single type of biocompatible electrospun nanofibers and microparticles of at least one therapeutic or cosmetic active agent which are entangled between the nanofibers, the active agent having a low water solubility.

Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice for treating pancreatic cancer.

Abstract: The present invention provides new ceramide analogs indicated as the compounds of formula (II). These novel analogs exhibit a significant anti cancerous effect and are therefore provided as a pharmaceutical composition for treating cell proliferative diseases, neurodegenerative disorders, metabolism-associated conditions, infectious diseases, and immune-related disorders. The invention further provides combined compositions and kits combining the novel ceramide analogs of formula (II) with an additional therapeutic agent.

Abstract: The present invention provides pharmaceutical compositions comprising a vinca alkaloid of formula (I): or a pharmaceutically acceptable salt (or hydrate) thereof, wherein each of R1, R2, R3, and R4 is as defined and described herein, wherein said formulations are useful for the topical treatment of actinic keratosis.

Abstract: A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one, is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) with surprisingly superior efficacy and pharmacodynamic properties in vitro and in vivo. Also provided are pharmaceutical compositions including the compound and methods of use of the compound in treating cancer and tumors in vivo, as well as inhibiting glycolytic flux and PFKFB3 enzymatic activity in cells.

Abstract: Methods for treating a patient using therapeutic spinal neuromodulation and associated devices, systems, and methods are disclosed herein. One aspect of the present technology is directed to methods including modulating nerves of one or more targeted organs proximate one or more dorsal root ganglia, stellate ganglia, vertebral ganglia, or cervical ganglia of the nerves using an intravascularly-positioned therapeutic element. One or more measurable physiological parameters corresponding to at least one condition associated with sympathetic activity in the targeted organs and/or central sympathetic activity in the patient can thereby be reduced.

Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 40 weight percent of a therapeutic agent and about 10 to about 90 weight percent a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa or the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa.

Abstract: Disclosed in the present invention is a pharmaceutical composition, comprising a weight ratio of 1:120 to 1:1000 of camptothecin compound of formula I and ?-cyclodextrin or derivatives thereof, and an acidic buffer to adjust the pH=3.5-6.0. The composition can be used to treat solid tumours, such as melanoma, pancreatic cancer, hepatoma etc. The pharmaceutical composition of the present invention is miscible with a water-miscible co-solvent system in any proportion, and can be used as an intravenous infusion solvent, and has no obvious hemolysis or vascular stimulation; the pharmaceutical composition has a better tumour inhibiting rate than solubilisation of surfactants.

Abstract: The present invention is related to the field of pharmaceutical compositions for the treatment of various disease states, particularly neoplastic diseases and autoimmune diseases. It especially relates to the oral application of bendamustine and its derivatives. The invention further relates to a process for preparing a pharmaceutical composition which comprises bendamustine and its derivatives prepared by hot melt extrusion using pharmaceutically acceptable excipients. The invention also relates to such pharmaceutical compositions and hot melt extrudates.

Abstract: The present invention relates to the method of pre-preparing pharmaceutical compositions for therapeutic uses, particularly pre-preparing medications for treating patients (e.g., cancer patients and the like) by intravenous infusion.

Abstract: A chemotherapy agent or a pharmaceutical composition including chemotherapy agent and artificial cerebrospinal fluid, wherein the chemotherapy agent at a concentration of between 0.01 mg/ml and 0.

Abstract: Provided herein are 3-dimensional drug-eluting materials comprising biodegradable polymer(s), one or more bioactive agents and entrapped air. Various embodiments of the methods and compositions described herein are based, in part, on the discovery of hydrophobic doping agents that can be used in the manufacture of polymeric drug delivery compositions that permit the encapsulation of air, thereby permitting tunable drug release via controlled air removal. Such compositions are particularly useful for delivering therapeutically effective doses of one or more bioactive agents to a subject over an extended period of time (e.g., days, weeks, or months).

Abstract: Oral dosage compositions for drugs normally given intravenously such as Paclitaxel, containing a plant sterol to enhance solubility and a small intestine efflux inhibitor to prevent P-glycoprotein from being a barrier to absorption.

Abstract: The invention provides novel amphiphilic drug-drug conjugates useful as cancer therapeutics, and compositions and methods thereof.

Abstract: A liposome comprising bilayer and inner water phase is disclosed. Said inner water phase may contain sulfobutyl ether cyclodextrin and an active compound.

Abstract: An amphiphilic block copolymer is disclosed. The amphiphilic block copolymer includes one or more hydrophilic polymers, one or more hydrophobic polymer, and one or more zwitterions. The invention also provides a nanoparticle and carrier including the amphiphilic block copolymer for delivery of water insoluble drugs, growth factors, genes, or water insoluble cosmetic substances.

Abstract: A 10?-fluoro-vinca alkaloid compound or its pharmaceutically acceptable salt is disclosed, as are methods of its preparation and use. A disclosed 10?-fluoro-vinca alkaloid compound has better cytotoxic potency against leukemia and cancer cell lines, and is about 8-times more cytotoxic to a multiple drug resistant cancer cell line than is a parental 10?-unsubstituted vinca alkaloid.

Abstract: A method and evaluation kit are provided, in which a high-capacity urate transporter is identified to assist in the early treatment and prevention of urate transport-related disease and inflammation-related disease. The method can include a step for detecting variations in genes that encode ABCG2 protein. When a subject has an SNP of V12M, R113X, Q126X, Q141K, F208S, G268R, E334X, S441N, L447V, S486N, F506SfsX4, R575X, and/or C608X, it can be concluded that the subject has a factor that is capable of inducing urate transport failure, or a state or disease attributable to that failure. When a subject has an SNP of V12M, it can be concluded that, unlike the other SNPs, there is a possibility that the subject does not possess such a factor because, although this variation itself does not lead to a change in urate transport capability, said variation is related to linkage disequilibrium with other SNPs.

Abstract: Compositions and methods are provided that enhance cognition in a human to which the composition is orally administered. Remarkably, clinical studies have proven that contemplated compositions achieved the desired effects using a minimal number of active ingredients at or near threshold active dosages, wherein such compositions almost exclusively comprise huperzine A, vinpocetine or rhodiola, and acetyl-L-carnitine, and optionally further include alpha lipoic acid, rhodiola, and biotin.