Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

Abstract: The present invention provides a chemical compound having the structure being one selected from a group consisting of wherein R1 is one selected from a group consisting of COOCH3, COOCH2Ph, CONHCH(CH3)2 and CONHC6H5, R2 is one selected from a group consisting of H, CH3 and CH(CH3)2, R3 is one selected from a group consisting of H, CH3, CH(CH3)2 and CH2Ph, and R4 is one of CH(CH3)2 and C6H5.

Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.

Abstract: A photoacid generator compound has the formula (I): [A-(CHR1)p]k-(L)-(CH2)m—(C(R2)2)n—SO3?Z+??(I) wherein A is a substituted or unsubstituted, monocyclic, polycyclic, or fused polycyclic C5 or greater cycloaliphatic group optionally comprising O, S, N, F, or a combination comprising at least one of the foregoing, R1 is H, a single bond, or a substituted or unsubstituted C1-30 alkyl group, wherein when R1 is a single bond, R1 is covalently bonded to a carbon atom of A, each R2 is independently H, F, or C1-4 fluoroalkyl, wherein at least one R2 is not hydrogen, L is a linking group comprising a sulfonate group, a sulfonamide group, or a C1-30 sulfonate or sulfonamide-containing group, Z is an organic or inorganic cation, p is an integer of 0 to 10,k is 1 or 2, m is an integer of 0 or greater, and n is an integer of 1 or greater.

Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.

Abstract: The present invention describes a method for the stimulation of the natural defense and the induction of resistance to diseases in plants by simultaneous activation of genes related to the route of the salicylic acid, the jasmonic acid/ethylene and the hypersensitive response. The invention also includes the use of brassinosteroids for the preventive and curative treatment against plant diseases caused by pathogens. In addition, includes a method for the prevention and treatment of the Huanglongbing disease in citrus.

Abstract: Disclosed are a novel resorcyclic acid lactone compound with inhibitory activity against protein kinases, a pharmaceutically acceptable salt thereof, a method for the synthesis thereof, and a pharmaceutical composition for the treatment and prevention of various cancer diseases comprising the same as an active ingredient. The novel resorcyclic acid lactone compound is useful as a therapeutic for cancer diseases, especially blood cancer, inter alia, acute myeloid leukemia (AML).

Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.

Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.

Abstract: A resist composition, a method of forming a resist pattern using the resist composition, a novel polymeric compound and a compound useful as a monomer for the polymeric compound, the resist composition including a base component (A) that exhibits changed solubility in a developing solution under action of acid and an acid generator component (B) that generates acid upon exposure, the base component (A) containing a resin component (A0) including a structural unit (a0) represented by general formula (a0) shown below in which A represents a divalent linking group; and R1 represents a hydrogen atom or a hydrocarbon group of 1 to 6 carbon atoms which may have a substituent.

Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV), wherein R1-R12 are as defined herein.

Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.

Abstract: Provided herein compounds, compositions and methods useful for the treatment of malaria for a subject in need thereof, including compounds of Formula (I), Formula (II), Formula (III), Formula (IV), and Formula (V).

Abstract: A compound represented by the following formula (I), wherein R1 is a hydrogen atom, a halogen atom, a methyl group or a trifluoromethyl group.

Abstract: The invention discloses biologically active ingredient(s) selected from 7-hydroxyfrullanolide, its analogs, the ex-tract(s) and fraction(s) standardized to 7-hydroxyfrullanolide or its analogs or both or mixtures thereof or their composition(s) for the prevention, control and treatment of one or more obesity, overweight, metabolic syndrome, diabetes and other metabolic disorders or for producing lean body mass in a warm blooded animal in need thereof.

Abstract: A photoacid generator compound has the formula (I): [A-(CHR1)p]k-(L)-(CH2)m—(C(R2)2)n—SO3?Z+??(I) wherein A is a substituted or unsubstituted, monocyclic, polycyclic, or fused polycyclic C5 or greater cycloaliphatic group optionally comprising O, S, N, F, or a combination comprising at least one of the foregoing, R1 is H, a single bond, or a substituted or unsubstituted C1-30 alkyl group, wherein when R1 is a single bond, R1 is covalently bonded to a carbon atom of A, each R2 is independently H, F, or C1-4 fluoroalkyl, wherein at least one R2 is not hydrogen, L is a linking group comprising a sulfonate group, a sulfonamide group, or a C1-30 sulfonate or sulfonamide-containing group, Z is an organic or inorganic cation, p is an integer of 0 to 10, k is 1 or 2, m is an integer of 0 or greater, and n is an integer of 1 or greater.

Abstract: The present invention provides a chemical compound having the structure being one selected from a group consisting of wherein R1 is one selected from a group consisting of COOCH3, COOCH2Ph, CONHCH(CH3)2 and CONHC6H5, R2 is one selected from a group consisting of H, CH3 and CH(CH3)2, R3 is one selected from a group consisting of H, CH3, CH(CH3)2 and CH2Ph, and R4 is one of CH(CH3)2 and C6H5.

Abstract: This invention is directed to methods of treating solid tumor cancers, particularly refractory cancers by administration of a drug capable of inhibiting mTOR and/or inhibiting an efflux pump and/or inhibiting HIF-1? and VEGF, the drug in particular being selected from the group consisting of sirolimus, everolimus, zotarolimus, tacrolimus, iolimus A9, deforolimus, AP23572, tacrolimus, temsirolimus, pimecrolimus, novolimus, 40-O-(3-hydroxypropyl), 40-O-[2-(2-hydroxy)ethoxy]ethyl-rapamycin and 40-O-tetrazolylrapamycin, the drug being administered along with a chemotherapeutic agent and/or radiation therapy.

Abstract: A homoadamantane derivative represented by the following formula (I): wherein R1 and R2 are independently a hydrogen atom or a linear, branched or cyclic hydrocarbon group having 1 to 6 carbon atoms, x is a hydroxyl group or a halogen atom, and n and m are independently an integer of 0 to 3, provided that n and m are not simultaneously 0.

Abstract: The present invention provides a chemical compound having the structure being one selected from a group consisting of wherein R1 is one selected from a group consisting of COOCH3, COOCH2Ph, CONHCH(CH3)2 and CONHC6H5, R2 is one selected from a group consisting of H, CH3 and CH(CH3)2, R3 is one selected from a group consisting of H, CH3, CH(CH3)2 and CH2Ph, and R4 is one of CH(CH3)2 and C6H5.

Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.

Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.

Abstract: [Problem to be Solved] An immunostimulant highly safe and administrable for a long period of time as well as a pharmaceutical composition containing the immunostimulant as an active ingredient and drink or food products for immunostimulation are developed and provided. [Solution] An immunostimulant containing a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient is provided. R1 is a hydrogen atom or a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms, R2 to R5 are independently a hydrogen atom, or a substituted or unsubstituted lower alkyl or lower acyl group, X is —(CH2)2—, —(CH2)3—, —(CH2)4—, —CO—CH2—, —CO—(CH2)2—, —CO—(CH2)3—, —CH2—CO—CH2—, —CO—O—CH2—, —CO—O—(CH2)2—, —O—CO—CH2—, —O—CO—(CH2)2—, —CH2—O—CH2—, —CH2—O—(CH2)2—, —O—CH2—, —O—(CH2)2—, —O—(CH2)3—, —NHY—CO—CH2—, —NHYCO—(CH2)2—, —CO—NHY—CH2— or —CO—NHY—(CH2)2—, Y herein is a hydrogen atom or a lower alkyl group.

Abstract: New lactone-containing photoacid generator compounds (“PAGs”) and photoresist compositions that comprise such PAG compounds are provided.

Abstract: A resist composition including a base component (A) which exhibits changed solubility in an alkali developing solution under action of acid and an acid-generator component (B) which generates acid upon exposure, the acid-generator component (B) including an acid generator (B1) represented by general formula (b1-1) [in the formula, Y0 represents an alkylene group of 1 to 4 carbon atoms or a fluorinated alkylene group, R0 represents an alkyl group, an alkoxy group, a halogen atom, a halogenated alkyl group, a hydroxy group or an oxygen atom (?O); p represents 0 or 1; and Z+ represents an organic cation.

Abstract: The present invention provides a composition having anti-Helicobacter pylori activity and the composition contains ovatodiolide with effective dosage to inhibit Helicobacter pylori growth or ovatodiolide related substances and its acceptable carrier. The present invention also provides a method for treating ovatodiolide to produce a composition for killing Helicobacter pylori. The present invention also provides an application of ovatodiolide to produce pharmaceuticals for curing gastric ulcers. The ovatodiolide isolated from natural material extract has been confirmed able to inhibit the growth of Helicobacter pylori or to kill Helicobacter pylori. The ovatodiolide can be used in various industries related to the inhibiting or killing of Helicobacter pylori with few side effects and is easy to obtain with low cost.

Abstract: Provided are formulations containing brassinosteroids or their derivatives for treating androgen-associated conditions, such as prostate problems. Particularly formulations comprising at least one brassinosteroid or a derivative thereof are provided for treating benign prostatic hyperplasia or androgenic alopecia.

Abstract: Provided herein compounds, compositions and methods useful for the treatment of malaria for a subject in need thereof, including compounds of Formula (I), Formula (II), Formula (III), Formula (IV), and Formula (V).

Abstract: Several ursolic acid derivatives and pharmaceutical compositions thereof are provided. The ursolic acid derivatives and the pharmaceutical compositions thereof have at least one of an anticancer and an anti-inflammatory effects. A method for increasing a reactive oxygen species in a cell is also provided. The method comprises a step of providing the cell with a pharmaceutical composition including an ursolic acid derivative.

Abstract: The present invention relates to an esterification catalyst composition that includes a zirconium compound and a method for producing an ester compound, which includes the steps of esterifying alcohol and carboxylic acid compounds by using the same, and it may be applied to a mass synthesis process.

Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV), wherein R1-R12 are as defined herein.

Abstract: The present invention provides a chemical compound having the structure being one selected from a group consisting of wherein R1 is one selected from a group consisting of COOCH3, COOCH2Ph, CONHCH(CH3)2 and CONHC6H5, R2 is one selected from a group consisting of H, CH3 and CH(CH3)2, R3 is one selected from a group consisting of H, CH3, CH(CH3)2 and CH2Ph, and R4 is one of CH(CH3)2 and C6H5.

Abstract: The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH2 or O—CH2 group, R2 is hydrogen or hydroxyl, R3 is hydroxyl, R24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo, especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids.

Abstract: The present invention relates to a process for preparing mumbaistatin derivatives (I), where the anthraquinone skeleton is constructed via a Diels-Alder reaction and the central methylene bridge via a transition metal-catalyzed reaction, and to the intermediates used in this process.

Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.

Abstract: The invention describes a process for making compound (2), comprising the step of cyclising diene (3). Compound (2) may be aigialomycin D or a derivative thereof or may be elaborated to make aigialomycin D or derivative thereof. Furthermore compound (2) or derivative thereof can be used in treating cancer or malaria or a microbial infection.

Abstract: Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.

Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The present invention relates to a process for preparing mumbaistatin derivatives (I), where the anthraquinone skeleton is constructed via a Diels-Alder reaction and the central methylene bridge via a transition metal-catalyzed reaction, and to the intermediates used in this process.

Abstract: The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: Described are amino substituted hydroxyphenyl benzophenone derivatives of formula (I), wherein R1, and R2 independently from each other are; C1-C20alkyl; C2-C20-alkenyl; C3-C10cycloalkyl; C3-C10cycloalkenyl; or R1, and R2 together with the linking nitrogen atom form a 5- or 6-membered heterocyclic ring; n1 is a number from 1 to 4; when n1=1, R3 is a saturated or unsaturated heterocyclic radical; hydroxy-C1-C5alkyl; cyclohexyl optionally substituted with one or more C1-C5alkyl; phenyl optionally substituted with a heterocyclic radical, aminocarbonyl or C1-C5alkylcarboxy; when n1 is 2, R3 is an alkylene-, cycloalkylene- or alkenylene radical which is optionally substituted by a carbonyl- or carboxy group; o R3 together with A forms a bivalent radical of the formula (Ia), wherein n2 is a number from 1 to 3; when n1 is 3, R3 is an alkanetriyl radical; when n1 is 4, R3 is an alkanetetrayl radical; A is —O—; or —N(R5)—; and R5 is hydrogen; C1-C5alkyl; or hydroxy-C1-C5alkyl.

Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein Ro-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.

Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Abstract: Alpha-methylenelactone is produced from butyrolactone and valerolactone by the addition of formaldehyde in a supercritical fluid.

Abstract: The present invention relates to derivatives of 9-keto spinosyns, which are substituted by a ?N—(O, NH or NRx)—Ry moiety in the C-9 position, to methods for their manufacture, and to their use for controlling animal pests.

Abstract: The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein R0–R4, Z, X, A—B, D—E, G—J, and K—L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.

Abstract: An object of the present invention is to provide a novel monomer compound having a lactone structure which gives polymers having more excellent feature as resist material, etc. The present invention relates to a compound represented by the following formula [1]: wherein R1 and R2 are an alkyl group; R3 and R4 are each independently hydrogen atom or an alkyl group; R5 is hydrogen atom, acryloyl group or methacryloyl group; and X is a methylene group which may have an alkyl group or an ethylene group which may have an alkyl group. The present invention provides a compound having a lactone structure which gives a polymer having more excellent feature particularly as a resist material and also provides a hydroxy lactone being useful as a material, etc. therefor.

Abstract: Disclosed herein is a novel norbornene, acrylate or methacrylate monomer as a photoresist monomer containing an oxepan-2-one group. Further disclosed are photoresist compositions comprising a polymer prepared from the monomer, methods for preparing the photoresist compositions, and methods for forming photoresist patterns using the photoresist compositions.