Abstract: Disclosed are indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.

Abstract: The allyl compound of the present invention is represented by general formula (?): wherein ring Z1 is a naphthalene ring, ring Z2 is a benzene ring or a naphthalene ring, X is a hydrogen atom or a monovalent substituent having 1 to 18 carbon atoms, R is each independently an alkyl group having 1 to 4 carbon atoms or a halogen atom, m is 1 or 2, n is each independently an integer of 0 to 5, and when m is 1, the ring Z1 and the ring Z2 are bonded to each other via an oxygen atom.

Abstract: The invention refers to compounds of general formula (I) wherein the variables take various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.

Abstract: The present invention relates to oxygen-substituted sterically hindered amines of the formulae I or II: (II), wherein, for example, F2, R3, R5, R6, R8, R9, R11, R12, R13, R14 are n-butyl: Z1 to Z10 are propoxy and R1, R4, R7, R10, R13 are 2,2,6,6-tetramethyl-1-propoxy-piperidin-4-yl. Compositions comprising compounds of formulae I or II and an organic material, which is susceptible to oxidative, thermal or light-induced degradation, are further disclosed. Optionally, further additives are contained.

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.

Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.

Abstract: There is provided a method for producing an epoxy compound having an epoxy ring bonded to a triazinetrione ring via a long chain alkylene group, an olefin compound having a specific structure is used to efficiently obtain an epoxy compound of which an olefin moiety is epoxidized in high yield. A method for producing an epoxy compound of Formula (2): including reacting a triolefin compound of the following Formula (1): (In the above-mentioned Formulae, R1 to R9 are each independently a hydrogen atom or a methyl group; and n1 to n3 are each independently an integer of 1 to 4) with hydrogen peroxide, a nitrile compound, and an alkaline substance in a solvent. The nitrile compound is an aliphatic nitrile compound or an aromatic nitrile compound. The alkaline substance is phosphate, carbonate, or an alkaline metal hydroxide.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: Compounds having PDE10A inhibitory activity and having general formula (I), or an isotope thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient.

Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

Abstract: The invention relates to a crystalline monohydrate of (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.13,7]decane dihydrogen citrate, compositions comprising such compound, and a process for preparing such compound.

Abstract: Methods employing chemiluminescent agents as therapeutically active agents in the treatment of proliferative disorders are disclosed. The chemiluminiscent agents are used in the disclosed method without a therapeutically effective amount of a photosensitizer. Novel chemiluminescent agents having the general formula: are also disclosed, wherein X, Y, Z, R3 and R5-R9 are as defined herein.

Abstract: The present invention relates to the cosmetic use, as agent for preventing and/or treating an aesthetic defect in the skin and/or its appendages that is associated with an imbalance in the differentiation and/or proliferation of the cells of an epidermis, of an effective amount of at least one compound represented by one of the general formulae, (Ia) or (Ib)

Abstract: The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as a factor D inhibitor for the treatment of ophthalmic diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein R1, R2, R3, R4, R5, R6, m, n, X and Y are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use for the treatment and prevention of diseases such as those associated with oxidative stress and inflammation.

Abstract: The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:

Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.

Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Abstract: Crystalline form, Form N-2, of N,Ndicyclopropyl-4-(1,5-dimethyl-1Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising Form N-2 of Compound I as well as a method of using the Form N-2 of Compound I in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.

Abstract: A reagent for carrying out a difluoromethylation reaction of unsaturated compounds and ring-nitrogen-containing aromatic compounds, a zinc difluoro-methanesulfinate, as well as a method for making the reagent and a method for its use are disclosed.

Abstract: The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.

Abstract: This document relates to compounds and compositions useful for treating cancers, such as brain and nervous system cancers.

Abstract: Stable crystalline forms of a compound represented by the formula (IA): an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.

Abstract: A method for producing a high-purity nitrogen-containing heterocyclic compound includes: a process (a) and a process (b): (a) a process of mixing a mixture containing a compound and as an impurity compound with a solvent and a metal salt, and (b) a process of obtaining a mixture in a solution state in which the content of the compound has decreased compared to that in the mixture in the process (a) by filtering a mixed solution obtained in the process (a), or a process of obtaining a mixture in which the content of the compound has decreased compared to that in the mixture in the process (a) by further evaporating the solvent or crystallizing following the filtering; (where R1 and R2 are each independently a hydrogen atom, a C1-6 alkyl group, etc., R3 is a hydrogen atom, a C1-6 alkyl group, etc., X is a hydrogen atom, etc.).

Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.

Abstract: Gold (I) hydroxide complexes of the form Z—Au—OH and digold complexes of the form Z—Au-(?OH)—Au—Z where groups Z are two electron donors are provided. The groups Z may be carbenes, for example nitrogen containing heterocyclic carbenes (NHCs), phosphines or phosphites. The complexes can be used as catalysts, for example in reactions such as hydration of nitriles, skeletal arrangement of enynes, alkoxycyclization of enynes, alkyne hydration, the Meyer-Shuster reaction, 3,3? rearrangement of allylic acetates, cyclization of propargylic acetates, Beckman rearrangements and hydroamination. The complexes can be used in medicine, for example in the treatment of cancer.

Abstract: The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.

Abstract: The present invention provides processes for preparing carbon-containing hydridosilanes, in which an optionally boron- or phosphorus-doped hydridosilane is reacted without catalyst and reducing agent with at least one carbon source selected from linear, branched or cyclic carbosilanes, halogenated hydrocarbons, carbenes, alkyl azides, diazomethane, dimethyl sulphate or alcohols, the carbon-containing hydridosilane oligomers obtainable by the process and the use thereof.

Abstract: An organosilicon compound having a hydrolyzable silyl group and a catechol group in the molecule is novel. When modified by surface treatment with an adhesive composition comprising the organosilicon compound, various inorganic materials such as glass and metals become tightly adherent to epoxy and other resins.

Abstract: Lithium diphenylphosphide solutions in a solvent, e.g., diethoxymethane (DEM), that are more stable than when tetrahydrofuran (THF) is used as a solvent. Methods of producing them are also disclosed.

Abstract: The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

Abstract: Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.

Abstract: Embodiments of the invention are directed to ONO pincer ligands that can be in a trianionic, protonated or protonated equivalent form. The ONO pincer ligand can be combined with a transition metal comprising compound to form an ONO pincer ligand comprising transition metal complex. By choice of the ONO pincer ligand structure, the steric and electronic properties of the transition metal complexes therefrom can be controlled. The ONO pincer ligands comprise a central nitrogen atom that is disubstituted with a pair of three atom comprising bridges where the three atoms are three sp2 hybridized carbons or the three atoms are a pair of sp2 hybridized carbons and an sp3 hybridized carbon or silicon.

Abstract: The invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom or a hydroxyl group; two R2 are the same or different and each is a hydrogen atom or a hydroxyl group; R3 is a hydrocarbon group having 8-14 carbon atoms, which optionally has substituent(s); and R4 is a hydrocarbon group having 18-24 carbon atoms, which optionally has substituent(s), or a salt thereof. The invention also provides a method of treating an autoimmune disease or suppressing immunity by administering the aforementioned compound or a salt thereof to a patient in need thereof.

Abstract: The invention features improved nucleic acids and methods for expression profiling of mRNAs, identifying and profiling of particular mRNA splice variants, and detecting mutations, deletions, or duplications of particular exons or other splice variants, e.g., alterations associated with a disease such as cancer, in a nucleic acid sample, e.g., a biological sample or a patient sample.

Abstract: Labeled reactant compositions, and particularly labeled nucleic acid reaction compositions that include structural components including double-stranded nucleic acids. In some embodiments, the structural components maintain potentially damaging labeling components sufficiently distal from the reactant portion of the molecule such that damaging effects of the label group on other reaction components, such as enzymes, are reduced, minimized and/or eliminated.

Abstract: The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.

Abstract: A method for the introduction of a labeling structure such as fluorescent molecules or a Raman tag to a compound is described. Imidazole functionalized resins or polymers are used to selectively immobilize phosphocompounds without protecting the carboxylic groups is described. Relying on the pKa difference between amines and hydrazides and carrying out the reaction in a slightly acidic buffer, all of the amines are protected by protonation while the hydrazides react with the phosphate imidazolide to form a phosphoramidate bond.

Abstract: An acyl dipeptide derivative represented by the formula (1): wherein an acyl group represented by R1—CO— is a saturated or unsaturated, straight or branched chain acyl group having 2-24 carbon atoms, R2 and R3 are each independently a hydrogen atom, an OH group or an OR5 group, R5 is a saturated or unsaturated, straight or branched chain hydrocarbon group having 1-6 carbon atoms, and R4 is a hydrogen atom, or a saturated or unsaturated, straight or branched chain hydrocarbon group having 1-6 carbon atoms, or a salt thereof has a superior antimicrobial effect, and a composition containing the compound is superior in the sensory feel.

Abstract: A short chain polypeptide having antioxidant activity is provided. The short chain polypeptide has 2 to 4 amino acids bonded to form a polypeptide chain having an amine-terminal end and a carboxyl terminal end; wherein a net charge of the short chain polypeptide is positive, the amino terminal amino acid is an amino acid selected from the group consisting of arginine, lysine and histidine, the polypeptide chain following from the amino terminus comprises a hydrophobic or neutral amino acid, and the polypeptide chain is free of an amino acid having a negatively charged side-chain group. A method to prepare a composition having antioxidant activity and a composition having antioxidant activity are also provided.

Abstract: Provided are small peptide fragments derived from the NF-?B p65 subunit and a pharmaceutical or cosmetic composition comprising the same. The peptides have a NF-?B inhibitory activity, through controlling the transcription-activation of NF-?B. The peptides inhibit the expressions of pro-inflammatory mediators, which are induced by NF-?B, and also inhibit the transmigration of leukocytes, thereby exhibiting an anti-inflammatory activity. Especially, the peptides have excellent inhibitory activities against dermatitis and skin aging. And also, the peptides inhibit base membrane invasion of cancer cells, thereby exhibiting an inhibitory activity against the growth and/or metastasis of cancer cells.

Abstract: Provided are anti-heparan sulfate peptides and methods that employ those peptides for the prevention or treatment of viral infections, including herpesviral infections such as ?-herpesviral, ?-herpesviral, and ?-herpesviral infections, which are exemplified by HSV-1. CMV, and HHV-8 viral infections, respectively. Peptides may comprise at least 10 amino acids of the amino acid sequences (SEQ?ID?NO:?2) XRXRXKXXRXRX, (SEQ?ID?NO:?8) XRXRXXKXRXRX, (SEQ?ID?NO:?4) XXRRRRXRRRXK, and/or (SEQ?ID?NO:?10) KXRRRXRRRRXX, wherein X represents any amino acid. In some embodiments, peptides comprise at least 10 amino acids of the sequence LRSRTKIIRIRH (SEQ ID NO: 1), HRIRIIKTRSRL (SEQ ID NO: 7), MPRRRRIRRRQK (SEQ ID NO: 3), and/or KQRRRIRRRRM (SEQ ID NO: 9).

Abstract: Disclosed are novel peptides comprising SEQ ID NO: 1 and modifications thereof, which are effective in blocking leukocyte recruitment. The disclosed peptides are useful for treating diseases associated with leukocyte recruitment for example inhibiting metastasis of a solid tumor to the liver and lungs and for treating sepsis. Also disclosed are methods of screening for compounds having the ability to block leukocyte recruitment.

Abstract: Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.

Abstract: The present invention provides novel n-alkenyl glycosides and glycoconjugates, n-alkyl glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycoconjugates as disclosed herein.