Abstract: The present disclosure relates to a class of JAK inhibitor compounds and uses thereof. Specifically, the present disclosure discloses a compound represented by formula (G), isotopically labeled compound thereof, or optical isomer thereof, geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof. The present disclosure also relates to the application of the compounds in medicine.

Abstract: Certain exemplary embodiments are directed to a biologically active composition of matter (and uses thereof) configured for targeted delivery of biotin to mitochondria, the composition comprising a first D-biotin conjugated to a water-soluble, cell-permeable, peptide sequence, wherein the peptide sequence is selected from a polypeptide group with an alternating aromatic-cationic motif.

Abstract: Provided are positively charged nanoparticles and use thereof. According to the nanoparticles of an aspect, cucurbituril may limit electrostatic attraction between a guest for cucurbituril and a metal salt, thereby generating nanoparticles with a uniform size. Accordingly, the nanoparticles may have an effect of being capable of efficient intracellular gene delivery.

Abstract: The present disclosure relates to a pharmaceutical composition for treating brain cancer containing an aldehyde inhibitor and an anticancer drug. Since there are many types of brain cancer and the boundary between brain cells and tumor cells in brain cancer is not clear, brain cancer is particularly difficult to treat. The pharmaceutical composition of the present disclosure may further contain a biguanide-based compound as needed, wherein the compound is preferably phenformin. The pharmaceutical composition of the present disclosure is very effective for the treatment and improvement of prognosis of brain cancer, and has remarkable effects of killing cancer cells and inhibiting cancer stem cell characteristics, compared to when each of the active ingredients is administered alone. Thus, it is expected that the pharmaceutical composition of the present disclosure will be widely used in the field of brain cancer treatment.

Abstract: Compositions include arginine and one or more unsaturated fatty acids. Methods for using such compositions can enhance cognitive function, reduce or prevent a decline of social interaction, reduce or prevent age-related behavioral changes, increase trainability, maintain optimal brain function, facilitate learning and memory, reduce memory loss, retard brain aging, prevent or treat strokes, and/or prevent or treat dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.

Abstract: Certain exemplary embodiments are directed to a biologically active composition of matter (and uses thereof) configured for targeted delivery of biotin to mitochondria, the composition comprising a first D-biotin conjugated to a water-soluble, cell-permeable, peptide sequence, wherein the peptide sequence is selected from a polypeptide group with an alternating aromatic-cationic motif.

Abstract: The present invention relates to a composition for stimulating muscle growth, repair and maintenance and the method of using the same. The present invention generally relates to compositions and methods for supporting muscle anabolism. The compositions described herein are pharmaceutical or nutritional compositions suitable for preserving muscle mass, strength, and/or function in a subject in need thereof. The compositions are based on a specially formulated mixture of essential amino acids (EAAs) and protein with additional components. Use of the compositions herein may prevent muscle atrophy associated with periods of rest, such as those following surgery, injury, inactivity and during recovery from disease.

Abstract: A formulation having excellent gastric protection properties comprises an active pharmaceutical ingredient and a waxy compound, dispersed in a pharmaceutically acceptable oily carrier. The formulation presents a palatable and stable oral dosage form which is particularly suitable for acid-sensitive active pharmaceutical ingredients, and which is also suitable for active pharmaceutical ingredients which are liable to cause stomach irritation.

Abstract: The present invention relates to novel fused bicyclic heterocycle derivatives of formula (I) in which Aa, Ab, Ac, Ad and Q have the meanings mentioned above, agrochemical formulations containing the compounds of formula (I) and their use as acaricides and/or insecticides for controlling animal pests, particularly arthropods and especially insects and arachnids.

Abstract: The present disclosure relates to substituted pyrrollo[3,4-D]imidazoles as JAK inhibitor compounds and uses thereof. Specifically, the present disclosure discloses a compound represented by formula (I), optical isomer thereof, geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof. The present disclosure also relates to the application of the compounds in the treatment of JAK-related diseases or disorders.

Abstract: The present invention in the field of cancer therapeutics is based on the finding (illustrated in FIG. 4) that when cannabinoids are administered to cancer cells after a chemotherapeutic agent has been administered, the combined treatment leads to lower cancer cell viability than administration of the chemotherapeutic agent alone. There is provided a pharmaceutical composition comprising a chemotherapeutic agent for use in the treatment of breast cancer, wherein said treatment comprises a first phase in which the chemotherapeutic agent is administered, and a subsequent second phase in which a cannabinoid is administered.

Abstract: A dispersion stabiliser precursor composition including one or more of cucurbituril, a variant or a derivative thereof, and one or more oil-in-water macromolecular amphiphilic emulsifier, wherein the composition is in the form of a free flowing powder; and an oil-in-water emulsion composition including one or more of cucurbituril, a variant or a derivative thereof, and one or more oil-in-water macromolecular amphiphilic emulsifier.

Abstract: The present invention provides a compound substituted with an excellent control effect against a harmful arthropod, which is represented by formula (I) Het-Q??(I) wherein Q represents a group represented by Q1, etc., Het represents a group represented by Het1, etc., R2 represents a C1-C6 alkyl group, etc., G1 represents a nitrogen atom or CR3a, G2 represents a nitrogen atom or CR3b, G3 represents a nitrogen atom or CR3c, G4 represents a nitrogen atom or CR3d, R3a, R3b, R3c, and R3d are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, etc., n represents 0, 1, or 2, T represents a C1-C10 chain hydrocarbon group substituted with one or more halogen atoms, etc., A2 represents a nitrogen atom or CR4a, A3 represents a nitrogen atom or CR4b, R4a and R4b are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, W1 represents an oxygen atom, etc., and R6 represents a C1-C6 chain hydrocarbon group, etc.

Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.

Abstract: The present invention relates to compounds of formula a process for their production and their use in electronic devices, especially electroluminescent devices. When used as host material for phasphorescent emitters in electroluminescent devices, the compounds of formula I may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.

Abstract: The present invention relates to compounds of formula I wherein L is a bond, a triple bond, —C(O)NH— or —NHC(O)—; R1 is phenyl or a five or six-membered heteroaryl group, optionally substituted by lower alkyl, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R2 is fluoro; R3 is fluoro or chloro; R4 is hydrogen, lower alkyl, halogen, lower alkyl substituted by hydroxy, S(O)2CH3, or is a five or six-membered heteroaryl group or a heterocycloalkyl group, which are optionally substituted by lower alkyl, hydroxy or ?O; R5 and R6 are both methyl and the dotted line is a bond, or R5 and R6 are both methyl and the dotted line is nothing, or one of R5 and R6 is hydrogen and the other is methyl, and the dotted line is nothing; or to a pharmaceutically acceptable salt or acid addition salt, to all possible tautomeric forms, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

Abstract: The invention relates to a method for the prognosis a person's susceptibility to environmental stress. The method includes: a step of determining the sequence for initiating the translation of at least one of the genes from the CCND family, and a step of quantifying the expression of the protein encoded by said gene, the translation initiation sequence of which was sequenced in the previous step, and comparing said expression with the expression level of said protein from a reference sample.

Abstract: A temozolomide compound according to formula (I) is described, wherein R1, L1, and X are defined herein. The temozolomide compound can be used to prepare polymers comprising temozolomide. Additionally, the polymers comprising temozolomide can be particularly useful in the treatment of certain diseases.

Abstract: Provided herein are compounds of formula (I) or formula (Ia) that inhibit tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease.

Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.

Abstract: The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.

Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.

Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of Rifaximin with high purity and yield. Particularly, the present invention relates to improved processes for the preparation of Rifaximin from Rifamycin O and S. More particularly the present invention relates to a process for the preparation of Rifaximin through 3-halorifamycin S. The present invention further relates to a novel polymorph of Rifaximin and process for its preparation.

Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 2, 8 and 12 (USP2 and USP8 and USP12) activity and methods for their use in treating cancers. The small molecule inhibitors of the invention are particularly useful in the treatment of non-small cell lung cancers that are resistant to tyrosine kinase inhibitors and in the treatment of prostate cancer that is resistant to AR inhibitor therapy.

Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.

Abstract: The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. (S)—N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide.

Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.

Abstract: This invention provides for compounds of the Formula II: wherein A, B, Het, R1, R2 and R3 are as described herein. These compounds are androgen receptor modulators useful for the treatment of androgen receptor-associated conditions.

Abstract: Disclosed are naphtho[2,3-f]quinoxaline compounds and pharmaceutical composition thereof. The compounds of the invention have been demonstrated as having analgesic effects and therefore may be applicable for use as a novel agent in relieving acute or chronic pain.

Abstract: The present invention concerns an injectable composition comprising a filler or a botulinum toxin and an adrenergic receptor agonist, and its use for diminishing, decreasing or avoiding skin reactions due to injection, specially redness, ecchymosis, bruising, bleeding, erythema, oedema, necrosis, ulceration, swelling and/or inflammation.

Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.

Abstract: The present invention relates to glioblastoma inhibiting compounds, in particular gambogic acid amid and derivatives thereof for the treatment of glioblastoma. Moreover, methods for determining whether a treatment with the compounds of the invention is suitable for a patient are disclosed.

Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.

Abstract: C. difficile infection (CDI) is the most common cause of antibiotic-associated diarrhea. Unfortunately, antibiotic therapy remains as the standard treatment for this antibiotic-induced disease and relapses are common. Antibiotic treatment typically is given for 10 to 14 days for initial or second episode of CDI. For recurrent episodes, more prolonged courses are recommended. It is disclosed herein that lower dose or shorter course of the antimicrobial treatment is sufficient to treat the disease and prevent recurrent disease by enabling a good immunologic response to infection, and perhaps also by better preserving normal flora, thus protecting against relapses or reinfection.

Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.

Abstract: The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients.

Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.

Abstract: The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy.

Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.

Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.

Abstract: Disclosed are solid dispersions comprising a compound having the formula: wherein the compound is dispersed within a polymer matrix formed by a pharmaceutically acceptable polymer, and further wherein the compound is substantially amorphous. Also disclosed are pharmaceutical compositions comprising the compound and methods of use for the compound.

Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.

Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and

Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.

Abstract: Hydroxytyrosol or olive juice containing hydroxytyrosol in combination with at least one of the compounds selected from the group consisting of: creatine, coenzyme Q10, resveratrol, caffeine, carnitine, B vitamins (B1, B2, B3, B5, B6, and/or B12) and ginseng (preferably: root) extract. can be used to maintain or increase mitochondrial biogenesis in cardiac muscle, skeletal muscles, and liver tissue.