Abstract: In one aspect, the disclosure relates to pharmaceutical compositions comprising 2?-deoxycytidine analogs, oral and other dosage formulations containing the same, and methods of making the same. In another aspect, the disclosure relates to methods of treating hematological disorders and diseases associated with abnormal cell proliferation using the same. In a still further aspect, the disclosure relates to kits comprising 2?-deoxycytidine analogs useful for treating hematological disorders and diseases associated with abnormal cell proliferation. In still another aspect, the disclosure relates to methods for increasing fetal hemoglobin levels in a subject. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Abstract: This invention provides herbal compositions useful for increasing the therapeutic index of chemotherapeutic compounds. This invention also provides methods useful for improving the quality of life of an individual undergoing chemotherapy. Furthermore, this invention improves the treatment of disease by increasing the therapeutic index of chemotherapy drugs by administering the herbal composition PHY906 to a mammal undergoing such chemotherapy.

Abstract: Provided are a liposome composition which has a practically required long-term preservation stability, and which has a release rate of a drug on the order of several tens of hours due to releasability of a drug being able to be suitably controlled by rendering an inner water phase hyper-osmotic; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which the content of cholesterols is 10 mol % to 35 mol % with respect to the total amount of lipid components in the liposome composition, and each of the liposomes encapsulates a drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase.

Abstract: The present disclosure relates to a novel nucleoside or nucleotide derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating viral infection-associated diseases, containing the same as an active ingredient.

Abstract: Nanocrystals, compositions, and methods that aid particle transport in mucus are provided. In some embodiments, the compositions and methods involve making mucus-penetrating particles (MPP) without any polymeric carriers, or with minimal use of polymeric carriers. The compositions and methods may include, in some embodiments, modifying the surface coatings of particles formed of pharmaceutical agents that have a low water solubility. Such methods and compositions can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for administration routes involving the particles passing through a mucosal barrier.

Abstract: This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.

Abstract: The disclosure relates to methods for pain management in the perioperative context, particularly through the use of the DNA methylation status of the human OPRM1 gene as a biomarker for increased susceptibility to perioperative pain, and related methods and compositions.

Abstract: A method of improving both motor function and cognitive function of healthy human subjects through administration of citicoline or its salt in high dosage or low dosage for a period of time, resulting in improved motor function and cognitive function.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:

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

Abstract: Methods for treating BCL-2 inhibitor-resistant cancer in subjects using an MCL-1 inhibitor as well as compositions associated with the same are disclosed.

Abstract: Provided are medical uses and methods for targeting cancer stem cells employing ProTide compounds, particularly in the prevention or treatment of cancer. The ProTide may be other than one selected from the group consisting of NUC-1031, a ProTide derived from cordycepin, and a ProTide derived from 8-chloroadenosine. The medical uses and methods for targeting cancer stem cells are particularly useful in the treatment of relapsed or refractory cancer in human patients. Also provided are methods of selecting patients who will benefit from prevention or treatment of cancer through the medical uses or methods of treatment of the invention.

Abstract: This invention relates to methods and compositions for administering an effective amount of a CDA substrate drug and an effective amount of cedazuridine. In particular, the invention relates to methods for treating cancer, inhibiting degradation of a CDA substrate drug, and reducing DNA methylation in a subject in need thereof comprising administering an effective amount of a CDA substrate drug and an effective amount of cedazuridine.

Abstract: The present disclosure provides methods, pharmaceutical compositions, dosing regimens, and kits comprising 4,4?-trans-dihydroxystilbene (DHS), including methods of treating cancer in a subject and methods of decreasing or reversing resistance to a DNA damaging agent in a subject.

Abstract: Compositions and method are therefore disclosed for treating chronic obstructive pulmonary disease (COPD) and/or pulmonary fibrosis (PF). In particular, disclosed a composition that contains one, two, or more cytidine diphosphate (CDP)-conjugated phospholipid precursors selected from the group consisting of CDP-choline, CDP-ethanolamine, and CDP-diacylglycerol in a pharmaceutically acceptable carrier for use in treating COPD and/or PF.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with immunomodulating agents and auris pressure modulators. In these methods, the auris compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of the immunomodulating and/or auris pressure modulating compositions and formulations onto the auris media and/or auris interna target areas, or via perfusion into the auris media and/or auris interna structures.

Abstract: Disclosed herein are compounds useful for treating and/or preventing HIV infections and the transmission of HIV from an infected subject.

Abstract: Provided relates to conjugates including cytarabine and an amino acid for use in the treatment of cancer. Further, the subject matter relates to conjugates of cytarabine and aspartic acid for use in the treatment of hematological cancers in medically compromised patients.

Abstract: The present disclosure relates to the injection composition containing acetaminophen, the injection composition comprising acetaminophen mixed in 0.01˜5 wt %, a solubilizer mixed in 0.01˜10 wt %, a toxicity inhibitor mixed in 0.05˜5 wt %, an isotonic agent mixed in 0.1˜10 wt %, an antioxidant mixed in 0.001˜5 wt %, and the balance sterile purified water for injection.

Abstract: Compositions and method are therefore disclosed for treating ARDS. In particular, disclosed a composition that contains one, two, or more cytidine diphosphate (CDP)-conjugated precursors selected from the group consisting of CDP-choline, CDP-ethanolamine, and CDP-diacylglycerol (CDP-DAG) in a pharmaceutically acceptable carrier for use in treating ARDS.

Abstract: The present disclosure provides a method of treating a neurodegenerative disorder, the method comprising administering a DNA methyltransferase inhibitor.

Abstract: The disclosure relates to compositions and methods for treatment, such as inducing regression or inhibiting growth, of tumors in a patient such as a human. Use of gemcitabine, including in self-emulsifying orally administered dosage forms for these purposes is described. Gemcitabine is orally administered in a metronomic manner, which involves repeatedly administering a therapeutic amount of gemcitabine, being a fraction of the maximum tolerated dose, over an extended period of time, preferably on a non-interrupted schedule of weeks, months, or indefinitely.

Abstract: Provided herein are compounds of formula I, 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 a method for inhibiting myeloid-derived suppressor cells or treating cancer comprising administering a pharmaceutical composition containing decitabine or its pharmaceutically acceptable salt as an active ingredient. The decitabine suppresses creation of a cell population of myeloid-derived suppressor cells (MDSC) created in spleen and bone marrow in tumorigenic mice and induces apoptosis of the MDSC cell population. Therefore, the decitabine may be useful as agents for treating MDSC-related diseases and anticancer immunotherapy, or an anticancer supplement.

Abstract: The present invention provides pharmaceutical compounds and methods for preventing, ameliorating, or treating a mitochondrial disease by administering such compounds to a subject in need thereof. In some cases, the subject suffers from a mitochondrial disease or is predisposed to having a mitochondrial disease. The mitochondrial disease includes those associated with impairments to mitochondrial oxidative phosphorylation that can lead to vision loss or blindness.

Abstract: Nanocrystals, compositions, and methods that aid particle transport in mucus are provided. In some embodiments, the compositions and methods involve making mucus-penetrating particles (MPP) without any polymeric carriers, or with minimal use of polymeric carriers. The compositions and methods may include, in some embodiments, modifying the surface coatings of particles formed of pharmaceutical agents that have a low water solubility. Such methods and compositions can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for administration routes involving the particles passing through a mucosal barrier.

Abstract: This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Abstract: This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.

Abstract: Disclosed is a combination of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate (chemical name: 2?-Deoxy-2?,2?-difluoro-D-cytidine-5?-O-[phenyl (benzoxy-L-alaninyl)]phosphate) (NUC-1031) and a platinum-based anticancer agent selected from carboplatin, dicycloplatin, oxaliplatin, satraplatin and nedaplatin. The combinations are useful in the treatment of cancer and particularly ovarian cancer.

Abstract: The invention relates to compounds and compositions for modulation of nicotinamide adenine dinucleotide (NAD+). The invention also relates to methods of making such compounds and compositions. The invention relates to pharmaceutical compositions containing one or more NAD+ modulating compounds as a first ingredient in combination with one or more active pharmaceutical ingredients. Further, the invention relates to methods of using such compounds or compositions to promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and/or improving cell and tissue survival.

Abstract: Embodiments of compositions and methods for the treatment of blood disorders and malignancies in a subject are described herein. In one embodiment, a composition for the treatment of a blood disorder or a malignancy in a subject comprises decitabine, tetrahydrouridine, and an excipient. In another embodiment, a method for the treatment of a blood disorder or a malignancy in a subject comprises the oral administration of a composition comprising decitabine and tetrahydrouridine. In some examples, the composition may be administered 1-3 times weekly.

Abstract: The present invention provides mutual prodrugs comprising anti-cancer nucleosides and short chain fatty acids; methods for production of the mutual prodrugs; methods of treatment comprising administration of the mutual prodrugs; and pharmaceutical compositions comprising the mutual prodrugs. Further, the mutual prodrugs of the present invention can be used as therapeutic agents for the treatment of cancer diseases and conditions.

Abstract: Provided herein are stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride, and pharmaceutical compositions and uses thereof. The stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, for increasing insulin sensitivity in a subject, or to treat or prevent a skin condition. The compounds have general formulas (I) or (II): wherein R1 is —C(?O)—X—(C2-C18 straight chain or branched) alkyl or —C(?O)—X—(C2-C18 straight chain or branched) alkenyl; each R2 is independently selected from hydrogen, and a —C(O)—X—(C1-C18 straight chain or branched) alkyl or a —C(O)—X—(C2-C18 straight chain or branched) alkenyl; and X is a covalent bond or O.

Abstract: Rediced genome or native K12 strain E. coli bacteria comprising expression vectors encoding a recombinant CRM197 protein and their use in the production of CRM 197 is provided. The CRM 197 protein may be fused to a signal sequence that directs the expressed CRM197 protein to the periplasm of the E. coli host.

Abstract: Disclosed herein are derivatives of nucleobase analogs. The disclosed compounds have a nucleobase moiety and an omega-3 polyunsaturated fatty acid moiety, including pharmaceutically acceptable salt or prodrug thereof. Methods of using these compounds for the treatment of cancers such as pancreatic cancer are also disclosed.

Abstract: This invention relates to processes for preparing a JAK1 inhibitor having Formula Ia: as well as new forms of the inhibitor.

Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.

Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: The present invention relates to the use of ceranib-2 molecule in the treatment of lung cancer and breast cancer. At the same time, the present invention also describes the in vitro studies made by the inventors in this direction.

Abstract: To provide a marker for determining sensitivity to an anti-cancer agent, which can determine whether or not a patient has a therapeutic response to the anti-cancer agent, and cancer therapeutic means employing the marker.

Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.

Abstract: This present invention relates to pharmaceutical compositions comprising cyclophosphamide alone and/or in combination with one or more pharmaceutical active ingredients and one or more pharmaceutically acceptable excipients wherein the cyclophosphamide has D90 particle size less than 100 microns.

Abstract: Provided herein are solid forms comprising (a) 4-amino-1-?-D-ribofuranosyl-1,3,5-triazin-2(1H)-one and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.

Abstract: Described herein are oral abuse deterrent pharmaceutical compositions, methods for making the same, and methods for treating pain by administering the pharmaceutical composition to a subject in need thereof. In particular, an oral abuse deterrent pharmaceutical composition comprising a soft capsule and a controlled release matrix comprising oxycodone are described.

Abstract: The present disclosure relates to the compound of Formula I: Also disclosed are pharmaceutical compositions comprising the compound of Formula I, methods of using the compound of Formula I and/or compositions comprising the compound of Formula I for the treatment of HCV.

Abstract: The present invention relates to a process of preparing a stable pharmaceutical composition of compounds which are susceptible to hydrolysis comprising a. Addition of required quantity of pharmaceutically acceptable lyophilization excipients optionally in Water for Injection in a formulation vessel; b. Addition of organic solvent to form a appropriate proportion of aqueous and organic solvent; c. Maintaining the temperature of the formulation vessel from the range ?5±1° C. to ?5±3° C.; d. Addition of required quantity of compound susceptible to hydrolysis to form a solution and lyophilizing the solution.

Abstract: Described herein are oral abuse deterrent pharmaceutical compositions, methods for making the same, and methods for treating pain by administering the pharmaceutical composition to a subject in need thereof. In particular, an oral abuse deterrent pharmaceutical composition comprising a soft capsule and a controlled release matrix comprising oxycodone are described.

Abstract: The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers. The compounds that useful for treating a neoplasm in mammalian subjects. The cytidine derivative dimer has the following general formula (I): where R1 is C1-C10 alkyl, C1-C10 substituted alkyl, —(CH2)n-Ph, or substituted —(CH2)n-Ph; R2 is C1-C10 alkyl, C1-C10 substituted alkyl, —(CH2)n-Ph, or substituted —(CH2)n-Ph; R3 is hydrogen, alkoxycarbonyl or substituted alkoxycarbonyl; R4 is hydrogen, alkoxycarbonyl or substituted alkoxycarbonyl; and R5 is —(CH2)n—, substituted —(CH2)n—, or —(CH2)n—X1—X2—, X1 being O or S, and X2 being —(CH2)n-Ph, pyrimidyl, pyranyl, imidazolyl, pyrazinyl, or pyridyl. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.