Abstract: Disclosed herein are compositions including a compound of formula (I) for treating cancer. Some embodiments relate to methods of treating cancer by co-administering a compound of formula (I) and one or more immune checkpoint inhibitor to a subject in need thereof. Some embodiments relate to methods of treating cancer by co-administering a compound of formula (I) and plinabulin to a subject in need thereof. Some embodiments relate to methods of providing co-stimulation of T-cell activation against cancer by co-administering a compound of formula (I), one or more immune checkpoint inhibitor.

Abstract: The present invention relates to a new bio-sourced vanillin and/or ethylvanillin, containing specific impurities. The invention further relates to a process for their preparations and the use of such compounds.

Abstract: The present invention relates to a skin conditioner comprising the compound represented with the general formula: (wherein, the symbols are the same as those defined in the text). Examples of active ingredients of the present invention include L-arginine and ethanolamine. These active ingredients can be acquired as chemical synthesis products, or they may also be acquired in the form of natural substances. Preferable examples of natural substances include substances containing L-arginine and/or ethanolamine obtained from rice. The skin conditioner as claimed in the present invention demonstrates remarkable effectiveness as an agent for the prevention and treatment of atopic dermatitis and as a skin moisture retention agent.

Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: Disclosed herein are compounds, compositions and methods for preventing and treating diseases such as intracerebral hemorrhage, cancer, or conditions associated with damaged cells, activated lymphocytes, or microbial products. The disclosed compounds are curcumin analogs. The curcumin analogs possess anti-inflammatory and antioxidant properties, which in part, reduce AP-1 and NF-?B activity.

Abstract: The invention relates to certain compounds, salts of these compounds and mixtures containing or consisting of two or more such compounds, two or more such salts or one or more such compounds and one or more such salts, each for use in a method for the prophylaxis and/or treatment of inflammation, in particular of inflammation of the skin.

Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.

Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.

Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I or a pharmaceutically acceptable salt thereof. In Formula I m is 0, 1, 2, 3 or 4; n is 0 or 1; m+n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are —CH2CH2—. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms.

Abstract: Suggested is a compound of the formula (X) or any salt of a compound of the formula (X) or any mixture containing or consisting of two or more different compounds of the formula (X), two or more different salts of compounds of the formula (X) or one or more different compounds of the formula (X) and one or more different salts of compounds of the formula (X), wherein for R1, R2 and R3 independently of one another in every compound of the formula (X) the following applies: R1 means hydrogen or methyl, R2 means an organic residue with 5 carbon atoms and one oxygen atom or none and R3 means an organic residue with 10 carbon atoms and one or more oxygen atoms, or R1 and R2 together with the carbon atoms in positions 4 and 5 and the oxygen atom bound to the carbon atom in position 4 form a ring and comprise 5 carbon atoms and one oxygen atom or none, and R3 means an organic residue with 10 carbon atoms and one or more oxygen atoms, for use in a method for the prophylaxis and/or treatment of inflammation.

Abstract: Provided is an anti-leishmanial compound represented by formula (1):

Abstract: The invention relates to certain compounds, salts of these compounds and mixtures containing or consisting of two or more such compounds, two or more such salts or one or more such compounds and one or more such salts, each for use in a method for the prophylaxis and/or treatment of inflammation, in particular of inflammation of the skin.

Abstract: Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R?C(0); —OC(O)— or —CH(OH)—; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction.

Abstract: The present invention concerns compositions and methods of extracting infectious pathogens from a volume of blood. In one embodiment, the method includes the steps of creating a fibrin aggregate confining the pathogens and introducing a fibrin lysis reagent to expose the pathogens for analysis. The present invention also concerns materials and methods for removing aurintricarboxylic acid (ATA) from a sample.

Abstract: Novel substrates for detection of activity of amyloid beta degrading enzyme, such as Neprilysin (NEP) and insulin degrading enzyme (IDE), associated with Alzheimer's disease, are provided. A quenched fluorogenic peptide substrate containing the first seven residues of the A?peptide plus a C-terminal Cys residue to detect neprilysin activity with a fluorophore attached to the C-terminal Cys and a quencher linked to the N-terminus of the peptide is disclosed. An assay system sensitive to endopeptidase activity of NEP and IDE, but insensitive to other A?-degrading enzymes is disclosed. Active compounds are identified by a cell-based assay system for high-throughput screening.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides.

Abstract: There is provided a novel loxoprofen derivative that has no side effect such as a gastrointestinal disorder and also has excellent anti-inflammatory and analgesic effects and is represented by the following formula (I) or (II): (wherein R1 and R2 each represent a halogen atom or a substituted or unsubstituted phenyl group) or a pharmacologically acceptable salt thereof. In the derivative, the halogen atom is selected from a chlorine atom, a bromine atom, a fluorine atom, and an iodine atom, and a substituent of the substituted phenyl group is a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkyl group, a lower alkylthio group, a lower alkoxy group, a nitro group, an amino group, or a carboxyl group.

Abstract: A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.

Abstract: The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.

Abstract: Disclosed are a serious of 2?,5?-dimethoxychalcone derivatives for treating cancer, wherein 2,5-dimethoxyacetophenone and methyl 4-formylbenzoate are condensed to form 4-carboxyl-2?,5?-dimethoxychalcone (compound 1), which is further reacted with alkyl halides or amines to synthesize the chalcone derivatives of compounds 2-17. In addition, 2,5-dimethoxyacetophenone is reacted with 5-formyl-2-thiophenecarboxylic acid to form compound 18 (3-(3-thiophene)carboxyl-1-(2,5-dimethoxyphenyl)prop-2-en-1-one). The synthesized 2?,5?-dimethoxychalcone derivatives can be acted as microtubule-targeted tubulin-polymerizing agents.

Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.

Abstract: The compound 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobutanoic acid (DPA) is synthesized from 1-[3-(2,6-Dimethylbenzyloxy)-phenyl]-ethanone (DPE) via the intermediate 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobulanoic acid ethyl ester (DPAE).

Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.

Abstract: Provided are the expression method of influenza virus polymerase PAc-PB1N complex, the co-crystallization method of the complex and the three-dimendional structure of the crystal of PAc-PB1N complex. Also provided are the compounds binding to the influenza virus polymerase PAc and the expression method of influenza virus polymerase PAN. The three-dimensional structure of the crystal of PAc-PB1N complex can be used for screening and designing the drug for the treatment of influenza.

Abstract: Novel pyruvate derivatives exhibiting outstanding neuroprotective effect, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions for prevention and treatment of brain disease including them as effective ingredient are provided.

Abstract: The invention relates to novel compounds of the formula (I) in which X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates 33 and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.

Abstract: A new tris(formylphenyl) of the following general formula and polynuclear phenol derived therefrom:

Abstract: This application describes quinone derivatives which target the redox site of Ape1/Ref1. Also included in the invention are pharmaceutical formulations containing the derivatives and therapeutic uses of the derivatives.

Abstract: Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.

Abstract: A lapping composition is presented, wherein that lapping composition is formed by mixing a solvent, a base, and a phenolic compound having structure I: wherein R1 is selected from the group consisting of —O?Mx+ wherein x is selected from the group consisting of 1, 2, and 3, —O—R3 wherein R3 is selected from the group consisting of alkyl, allyl, and phenyl, —N(R3R4) wherein R4 is selected from the group consisting of —H, alkyl, allyl, and phenyl, and —S—R3; and wherein R2 is selected from the group consisting of —O?Mx+ wherein x is selected from the group consisting of 1, 2, and 3, —O—R3 wherein R3 is selected from the group consisting of alkyl, allyl, and phenyl, —N(R3R4) wherein R4 is selected from the group consisting of —H, alkyl, allyl, and phenyl, and —S—R3.

Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.

Abstract: A novel tris(formylphenyl) according to the following general formula and polynuclear phenol derived therefrom, which are useful as a material for heat resistant materials, material for photosensitive resist compositions, epoxy resin material or hardener, developer or anti-fade agent for thermosensitive recording materials, or sterilizer, fungicide, antioxidant, etc: In the formula, Y represents a hydrogen atom or —R2COOR3 group, R2 represents a monocyclic or condensed cyclic aromatic hydrocarbon group with a carbon atom number of 6 to 15 or an aliphatic hydrocarbon group with a carbon atom number of 1 to 8 that may have in its main chain a monocyclic or condensed cyclic aromatic hydrocarbon group with a carbon atom number of 6 to 15, and R3 represents a hydrogen atom or alkyl group with a carbon atom number of 1 to 6. R1s may be the same or different and respectively represent a hydrogen atom, alkyl group with a carbon atom number of 1 to 8 or alkoxyl group with a carbon atom number of 1 to 8.

Abstract: The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products.

Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.

Abstract: Disclosed and described herein are compounds of the formula or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed and described.

Abstract: Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length.

Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Abstract: Diketoacids of Formula A are useful as inhibitors of viral polymerases. In particular hepatitis C virus RNA dependent RNA polymerase (HCV RdRp), hepatitis B virus polymerase (HBV pol) and reverse transcriptase of human immunodeficiency virus (HIV RT): The group R may be broadly chosen and is an organic moiety which contains 2 to 24 carbon atoms and includes an optionally cyclic or heterocyclic group in which the atom directly bonded to the adjacent carbonyl in the diketoacid is part of the ring structure.

Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are CH2; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR2, CO2R and OR.

Abstract: The present invention provides a novel bioactive compound 12-(2′-CARBOXY-5′-METHOXYPHENYL)-2,12-DIHYDROXY-DODECA-4-ONE “Sporotricolone”, mainly as acetylcholinesterase (AchE) inhibitor, along with a process for the isolation of said compound from fungus Sporotrichum species.

Abstract: This invention relates to novel aldehyde containing compounds and their uses as adjuvants and immunoeffectors.

Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.

Abstract: A &ohgr;-substituted phenyl-prostaglandin of formula (I), a process for the preparation thereof, a mediciament comprising it as active ingredient (all symbols have the same meaning as described in the specification). The compounds of the formula (I) bind strongly in PGE2 receptor (especially subtype EP4) and therefore are useful for the prophylaxis and/or treatment of immune diseases (autoimmune diseases (amyotrophic lateral sclerosis (ALS) etc.), post-transplantation graft rejection, etc.), asthma, abnormal bone formation, neurocyte death, pulmopathy, hepatopathy, etc. They are also related to sleeping disorders and platelet coagulations, and therefore they are also applicable to these diseases.

Abstract: The present invention relates to HIV integrase inhibitors of the formula wherein R1 and Z are as defined in the specification.

Abstract: Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.