Abstract: A preparation containing a chlorogenic acid crystal form. The crystal form is an orthorhombic crystal system, a space group is P212121, cell parameters are as follows: a=7.7291(2)?, b=10.9808(2)?, c=36.5334(7)?, ?=?=?=90.00°, Z=8, and a cell volume is 3100.65(11)?3. The content of the chlorogenic acid crystal form in the preparation is 10-5000 mg/g. The preparation is advantageous to bioavailability, and can be used for preparing medicines for treating tumor, psoriasis and other immune system diseases, resisting oxidation, protecting liver and gallbladder, treating cardiovascular diseases, and resisting viruses.

Abstract: This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, palbociclib (Ibrance), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; and/or HER2-positive; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Abstract: The present disclosure provides a compound represented by Formula (I) and a pharmaceutically acceptable salt which are effective as a dopamine reuptake inhibitor and a method of using the compound: wherein X is independently halo, alkyl, alkoxy or nitro; m is 0, 1, 2, 3 or 4; n is 1 or 2; R1 and R2 are independently H— or alkyl; R3 is H—, alkyl or aralkyl; and R4 is H— or aryl.

Abstract: Application of Derivatives of Clostridium ghonii, especially in the application of Derivatives of Clostridium ghonii MW-DCG-HNCv-18 in preparation of medicines for treating non-small cell lung carcinoma. It also discloses a medicine combining the Derivatives of Clostridium ghonii MW-DCG-HNCv-18 strain with Docetaxel as the active ingredients. According to the invention, the MW-DCG-HNCv-18 strain is found to have specific inhibition effect on non-small cell lung carcinoma for the first time, the inhibition effect on the non-small cell lung carcinoma is significantly superior to that of other known similar strains, and through screening, the MW-DCG-HNCv-18 strain is found to have more prominent inhibition effect on non-small cell lung carcinoma when combined with Docetaxel injection.

Abstract: Provided herein are novel agents that modulate AhR activity for use in therapeutic compositions and methods thereof for inhibiting cancer cell proliferation and tumor cell invasion and metastasis. The agents comprise AhR inhibitors or non-constitutive AhR agonists of Formula (I) and (II) for the inhibition of cancer cell growth and parameters that characterize tumor metastasis, such as tumor cell invasiveness.

Abstract: A method for treating diarrhea induced by a chemotherapy agent by administering a carboxylesterase 2 (CES2) inhibitor, i.e., hesperetin, naringenin, or 2?,4?-dihydroxychalcone. Also disclosed is a method for treating cancer by administering a chemotherapy agent together with hesperetin, naringenin, or 2?,4?-dihydroxychalcone. Furthermore, a composition for treating cancer is provided, the composition containing a chemotherapy agent and hesperetin, naringenin, or 2?,4?-dihydroxychalcone.

Abstract: The present invention is directed to compositions comprising physiologically active phenolic compounds and methods for making and using the same. In particular embodiments, the compositions described herein include suspension formulations including a physiologically active phenolic compound provided as a nanoparticulate material and dispersed within an edible lipid.

Abstract: Clostridium difficile infects and kills 30,000-40,000 people a year in the United States. Provided herein are methods to inhibit growth and reduce the spread of C. difficile using puupehenone, a natural marine product that is excreted from some species of sponges and coral as a defense mechanism.

Abstract: A composition comprising 7-hydroxymatairesinol (HMR), or a stereoisomer, salt, complex, adduct or derivative thereof, or an extract containing them for preventing, alleviating or ameliorating the metabolic syndrome conditions.

Abstract: The present invention provides a crystalline Form A of Compound 1, also referred to as Granaticin B, and pharmaceutically compositions thereof. The present invention also provides methods of treating a microbial infection, or a disease, disorder, or condition associated with abnormal cellular proliferation, using crystalline Form A of Compound 1 or pharmaceutical compositions thereof.

Abstract: Described herein are antimicrobial compounds identified via a high-throughput inhibitor screen of the in vitro activity of MipZ, which is an ATPase that regulates division site placement in Caulobacter crescentus. The compounds and their analogs are active against bacterial membranes and thus represent a novel class of antimicrobial compounds. The antimicrobial compounds are effective against both actively growing bacterial cells as well as bacterial cells in the stationary phase. The antimicrobial compounds are also effective against bacteria in biofilms.

Abstract: EHT extract including a mixture of late eluting tryptamides and early eluting tryptamides in a weight ratio of at least about 7:1 late eluting tryptamides:early eluting tryptamides, wherein the EHT extract includes at least 30% eicosanoyl-5-hydroxytryptamide, based on the total weight of the tryptamides in the EHT extract.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: Disclosed are solid state forms of Eluxadoline, processes for their preparations, compositions comprising them and their medical use. The present invention also encompasses solid state forms of Eluxadoline for use in the preparation of other solid state forms of Eluxadoline, particularly form alpha.

Abstract: The present invention relates to novel compounds of formula (I) suitable e.g. as therapeutic agents for use in the treatment of mammalian disease and in particular to novel therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. The present invention also relates to processes for making said agents.

Abstract: The present disclosure discusses crystalline forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridine-3-yl]-1H-imidazole-2-carboxamide.

Abstract: Provided are low-volume, safe for injection formulations of dantrolene yielding significant advantages over the currently approved and marketed dantrolene for malignant hyperthermia (MH) threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. The low volume, safe for injection formulations of dantrolene have significant advantages over currently used approaches to the prevention and treatment of pumphead, and other neurological, cognitive and motor dysfunction incident to iatrogenically or trauma induced situations of altered blood flow, including those incurred during surgical procedures involving CPB or related procedures, as well as those incurred during non-normothermic episodes caused iatrogenically or by disease.

Abstract: The invention relates to antibacterial compounds of formula I wherein M is one of the groups MA, MB and MC represented below wherein R1, MA, MB and MC are as defined in the specification; and to salts thereof.

Abstract: The present invention is directed to methods of treating, preventing, and/or ameliorating fibrosis syndrome, and in particular cardiac fibrosis, by administration of a therapeutically effective amount of ifetroban, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a pharmaceutical composition for the treatment of primary biliary cirrhosis (PBC), in which containing a therapeutically effective amount of (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy] butyric acid, a salt thereof, or a solvate thereof.

Abstract: It has now been discovered that p53 is a potent inhibitor of angiogenesis and arteriogenesis. Inhibition of p53 stimulates angiogenesis, arteriogenesis and improves perfusion in limbs. Therefore, methods are provided for treating diabetic-induced ischemia in a subject in need thereof comprising locally administering a therapeutically effective amount of one or more p53 molecule inhibitors or analogs and derivatives thereof to a site of ischemic tissue in the subject. Methods are provided for improving limb perfusion in a subject in need thereof comprising locally administering a therapeutically effective amount one or more p53 inhibitors together with a therapeutic agent or separately from the therapeutic agent to cells of a limb of a subject in need thereof.

Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:

Abstract: The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin. The instant application also provides methods for determining if a subject has a neurological condition or hepatic encephalopathy by determining the critical flicker frequency and/or the venous ammonia level of the subject at two or more time points. The invention further provides methods for treating these subjects.

Abstract: The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.

Abstract: The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.

Abstract: Small molecule inhibitor compounds for inhibiting Rac1 activity and their use for treating, preventing, or reducing the incidences of malignant and nonmalignant manifestations, e.g., plexiform neurofibromas that occur in subjects suffering from neurofibromatosis type 1 (NF1) are disclosed.

Abstract: The present application discloses a compound which is which activates Wnt/?-catenin signaling and thus treats or prevents diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.

Abstract: According to the present invention, there is provided a pharmaceutical composition for treating Philadelphia chromosome positive lymphocytic leukemia, including a thalidomide derivative and BCR-ABL tyrosine kinase inhibitor. According to the present invention there is also provided a method of treating Philadelphia chromosome positive lymphocytic leukemia, including administering a thalidomide derivative and a BCR-ABL tyrosine kinase inhibitor to a patient suffering from Philadelphia chromosome positive lymphocytic leukemia.

Abstract: This disclosure relates to managing conditioned fear and conditions induced by experiencing or witnessing an extreme traumatic event using neurokinin receptor antagonists. In certain embodiments, the disclosure relates to methods of treating or preventing conditioned fear comprising administering an effective about neurokinin 3 receptor antagonist to a subject in need thereof. In certain embodiments, the subject is diagnosed with Post-Traumatic Stress Disorder. In certain embodiments, the neurokinin 3 receptor antagonist is (R)—N-{{3-[1-Benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-methylacetamine or salts thereof.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of multiple myeloma.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.

Abstract: The invention relates to a composition comprising buprenorphine and a ? opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ c ma ? ? x ? ( BUP ) / EC 50 ] [ c ma ? ? x ? ( ANTAGONIST ) / IC 50 ] .

Abstract: The present invention provides a composition comprising an opioid agonist, and a polymer-antagonist conjugate. The polymer-antagonist conjugate preferably does not hydrolyze upon administration to a patient, and does not bind to the opioid receptors. The covalent bond between the polymer and the antagonist in the conjugate is broken over a defined period of time to release the antagonist into the formulation. The released antagonist attenuates the liking of the agonist, thereby eliminating the incentive to the diversion of the medicines.

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

Abstract: The present invention provides compounds of Formula (II) for the treatment of cancer, rheumatoid arthritis and other diseases.

Abstract: Described herein are methods for treating B cell proliferative disorders, in an individual in need thereof. The methods include administering to an individual in need thereof a Btk inhibitor (e.g., ibrutinib), in combination with a CDK4 inhibitor (e.g., palbociclib).

Abstract: The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with therapeutic agents that are inhibitors of mitosis (a mitotic inhibitor).

Abstract: Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.

Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.

Abstract: The invention provides immunoconjugates comprising anti-HER2 antibodies and methods of using the same.

Abstract: The present invention discloses scalarane sesterterpenoids represented by formula (I) and meroditerpenoid represented by formula (II), which are extracted from Carteriospongia sp. sponge: where R1 is —CH3 or —C2H5. The compounds of formula (I) can be used to be an anticancer, act as an inhibitor targeting to topoisomerase II and hsp90 and a pharmaceutical composition for anticancer.

Abstract: The invention relates to the field of male and/or female sexual dysfunction. The invention specifically relates to the use of testosterone and a 5-HT1A agonist.

Abstract: This invention provides new methods for a) identifying Cushing's Syndrome patients at high risk of developing hypokalemia during glucocorticoid receptor modulator (GRM) treatment, and b) for prophylactically treating such patients to prevent, or reduce the severity of, hypokalemia. Patients at such high risk may be identified prior to their developing hypokalemia. Such a patient may be an adult patient with endogenous Cushing's Syndrome having type 2 diabetes mellitus or glucose intolerance to control hyperglycemia secondary to hypercortisolism. Patients may be identified by an above-threshold level of ACTH or cortisol in a patient sample taken post-GRM administration or pre-GRM administration, respectively. Upon identifying such a patient prior to the development of low potassium, the present methods provide for prophylactically treating the patient by administration of one or more hypokalemia treatments concurrently with an increased dose of GRM or with an initial dose of GRM to prevent hypokalemia.

Abstract: The invention provides, inter alia, methods of treating a disorder characterized by excessive metakaryotic stem cell growth by a combination metakaryocidal therapy. Also encompassed by the present invention are preventative methods comprising the administration of a metakaryocidal or metakayrostatic therapeutic agent.

Abstract: The invention relates to a mixture of human milk oligosaccharides that consists essentially of: a) a component A which is 3-FL or DFL, a component B which is LNT, LNnT, LNFP-I or 2?-FL, a component C, which is LNFP-II when component B is LNT, or LNFP-III when component B is LNnT, or LNDFH-I when component B is LNFP-I, or DFL when component B is 2?-FL, and a component D, which is lactose when component A is 3-FL, or 2?-FL when component A is DFL, with the proviso that if component B is 2?-FL, then component A is 3-FL; or consists essentially of: b) 3-FL, a component E which is LNT, LNnT or LNFP-I, and a component F, which is LNFP-II when component E is LNT, or LNFP-III when component E is LNnT, or LNDFH-I when component E is LNFP-I, and to processes for producing them and their uses.

Abstract: Preparations of glycan therapeutics, pharmaceutical compositions and medical foods thereof, optionally comprising micronutrients, polyphenols, prebiotics, probiotics, or other agents are provided and methods of making same. Also provided are methods of using said gycan therapeutics, e.g. for the modulation of human gastrointestinal microbiota and to treat dysbioses.

Abstract: Disclosed are compositions, kits, and methods for treating cancer in a subject in need thereof. The compositions, kits, and methods may be used to treat a tumor in a subject in situ. The compositions, kits, and methods comprise or utilize cytotoxic particles, immune checkpoint inhibitors, and/or T-cell stimulatory agents.

Abstract: The methods and assays described herein relate to detection, diagnosis, and treatment of lung cancer, e.g., by detecting the level of expression of certain miRNAs described herein and/or by therapeutically increasing the level of those miRNAs.

Abstract: The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof.