Abstract: Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided.

Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.

Abstract: Process for preparing tetrahydrofuran, 1,4-butanediol and/or gamma-butyrolactone by hydrogenation of 1,4-butynediol, wherein 1,4-butynediol is vaporized in a hydrogen-comprising gas stream and hydrogenated in gaseous form over at least one catalyst which comprises at least one of the elements of groups 7 to 11 of the Periodic Table of the Elements.

Abstract: Compositions capable of simultaneous two-photon absorption and higher order absorptivities are provided. Compounds having a donor-pi-donor or acceptor-pi-acceptor structure are of particular interest, where the donor is an electron donating group, acceptor is an electron accepting group, and pi is a pi bridge linking the donor and/or acceptor groups. The pi bridge may additionally be substituted with electron donating or withdrawing groups to alter the absorptive wavelength of the structure. Also disclosed are methods of generating an excited state of such compounds through optical stimulation with light using simultaneous absorption of photons of energies individually insufficient to achieve an excited state of the compound, but capable of doing so upon simultaneous absorption of two or more such photons. Applications employing such methods are also provided, including controlled polymerization achieved through focusing of the light source(s) used.

Abstract: Methods for the preparation of hexahydrofuro[2,3-b]furan-3-ol and especially its enantiomer (3R,3aS,6aR) hexahydrofuro[2,3-b]furan-3-ol, as well as certain novel intermediates for use in such methods are disclosed.

Abstract: The present invention provides methods and compositions for treating lung cancer by cyclohexenone compounds.

Abstract: A process for the purification of a crude liquid feed stream comprising 1,4-butanediol and a minor amount of 2-(4-hydroxybutoxy)-tetrahydrofuran and/or precursors thereof wherein the process comprises passing the crude feed in the presence of hydrogen in a reaction zone over a heterogeneous liquid tolerant copper catalyst in the liquid phase at hydrogenation conditions and recovering a purified stream of 1,4-butanediol having a lower amount of 2-(4-hydroxybutoxy)-tetrahydrofuran than the crude liquid feed stream.

Abstract: Disclosed is a method of preparing 3-hydroxytetrahydrofuran using cyclodehydration. More particularly, this invention relates to a method of preparing 3-hydroxytetrahydrofuran, including subjecting 1,2,4-butanetriol to cyclodehydration under reaction conditions of a reaction temperature of 30˜180° C. and reaction pressure of 5000 psig or less in the presence of a strong acid cation exchange resin catalyst having a sulfonic acid group as an exchange group. According to the method of this invention, 3-hydroxytetrahydrofuran can be economically prepared at higher yield and productivity than when using conventional methods.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: The invention provides a liquid crystal compound that has an excellent compatibility with other liquid crystal compounds and also has at least one of characteristics such as a high stability to heat, light or the like, a suitable refractive index anisotropy (?n), a low threshold voltage and a suitable dielectric anisotropy (??). A compound represented by formula (1). For example, R1 is alkyl having 1 to 10 carbons, R2 is halogen or alkenyl having 2 to 10 carbons; the ring A1, the ring A2 and the ring A3 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2 and Z3 are a single bond or alkylene having 1 to 4 carbons; G is —CH2— or —O—; and m is 1, and n and p is 0 or 1.

Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.

Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.

Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I): as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I). They are useful in the treatment of CNS disorders.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Abstract: Pyrazoloamides are provided which are phosphonate and phosphinate glucokinase activators that are useful in treating diabetes and related diseases and have the structure wherein is a pyrazoyl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R3(CH2)s, wherein R3 is aryl , s is 0, X is a bond; and n, Z, m, R4, R5, R6, and R7 are as defined herein; or a pharmaceutically acceptable salt thereof.

Abstract: A ?-butyrolactone compound as shown in Formula (I) and pharmaceutical composition thereof: wherein X?N, O, S, Se; and A and B are selected from substituents having the following formula: wherein R1, R2, R3, R4, and R5 are selected from a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, an amino group, an alkoxy group, and a nitro group. The ?-butyrolactone compound and pharmaceutical composition thereof butyrolactone have inhibitory effects on hepatoma, ovarian cancer, breast cancer, lung cancer, malignant glioblastoma or colorectal carcinoma, and are cytotoxic with high specificity to inhibit Paclitaxel-resistant tumor cells at later stage of chemotherapy without any damage on normal cells.

Abstract: The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y and CKE have the meanings given in the disclosure, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention further relates to selectively herbicidal compositions containing 2,4,6-phenyl-substituted cyclic ketoenols and a compound which improves crop plant tolerance.

Abstract: The present disclosure relates to methods of preparation of compounds resulting from the reaction of levulinic esters and epoxidized unsaturated fatty acid esters. The compounds are useful as renewable biomass-based plasticizers for a variety of polymers. Mono-, di- and tri-ketal adducts formed in a reaction between alkyl esters of levulinate and epoxidized unsaturated fatty acid esters derived from vegetable oils are also disclosed.

Abstract: The invention is drawn to a new class of isoeicosanoids that have been identified as products of the oxidation of docosahexaenoic acid (DHA). The invention provides compositions and methods related to the new class of molecules.

Abstract: The present invention is directed to cyclic ketal compounds of 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: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.

Abstract: The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.

Abstract: Glyceryl ether compounds prepared by the reaction of glycerol and olefin epoxides are disclosed. The compounds are renewable biomass-based surfactants useful as detergents and emulsifiers in formulations for cleaning, laundry, personal care, cosmetics, and industrial uses.

Abstract: A dissolution modification agent suitable for use in a photoresist composition including a polymer, a photoacid generator and casting solvent. The dissolution modification agent is insoluble in aqueous alkaline developer and inhibits dissolution of the polymer in the developer until acid is generated by the photoacid generator being exposed to actinic radiation, whereupon the dissolution modifying agent, at a suitable temperature, becomes soluble in the developer and allows the polymer to dissolve in the developer. The DMAs are glucosides, cholates, citrates and adamantanedicarboxylates protected with acid-labile ethoxyethyl, tetrahydrofuranyl, and angelicalactonyl groups.

Abstract: Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.

Abstract: The present invention provides ?-hydroxy benzeneacetic acid derivatives of the formula as defined in the specification which is a precursor indispensable for synthesis of compounds having two 5-membered lactone rings fused to central cyclohexa-1,4-diene nucleus, and a process of easily preparing the same. According to the preparation process of the present invention, the ?-hydroxy benzeneacetic acid derivative can be readily prepared at high purity and yield without using toxic materials or producing toxic by-products. Some novel compounds, synthesized by using such a ?-hydroxy benzeneacetic acid derivative, have excellent fastness properties, dye fixing rate and leveling property to general synthetic fiber materials such as polyester fibers and their blends with other fibers, especially to micro fibers, and also can be used as a coloring agent for plastic resins, color tonors, color filters, etc.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with tetradentate ligands having at least one amino or imino coordinating group and at least one phosphino coordinating group in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: The invention relates to the use of 5,5-dimethyl-3-ethyl-3,4-dihydrofuran-2-one (A), named “Noxolide” by the applicant, as an olfactory agent in perfumery, and also as a food flavouring. The invention also relates to a novel process for the preparation of 5,5-dimethyl-3-ethyl-3,4-dihydrofuran-2-one.

Abstract: Methods for the preparation of hexahydrofuro[2,3-b]furan-3-ol and especially its enantiomer (3R,3aS,6aR) hexahydrofuro[2,3-b]furan-3-ol, as well as certain novel intermediates for use in such methods.

Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required a-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Abstract: Silicon compounds having fluorinated hemiacetal structure are provided. Silicone resins having the same structure have an appropriate acidity to enable formation of a finer pattern by minimizing the pattern collapse by swelling, exhibit improved resistance to the etching used in the pattern transfer to an organic film, and are thus suited for use in resist compositions for the bilayer process.

Abstract: A compound represented by formula (I): [wherein, for example, X is a hydrogen atom or a halogen atom; R1 is a hydrogen atom; R2 is a hydrogen atom or a C1-4 alkyl group; R3 is —CHO or —COOH; and R4 is —CH?CH—(CH2)p—CH3 (wherein p is an integer of 1 to 12), —CH(OH)—(CH2)q—CH3 (wherein q is an integer of 1 to 13), —CH(OH)—CH2—CH(CH3)—(CH2)2—CH?C(CH3)2, —CH?CH—CH(CH3)—(CH2)3—CH(CH3)2, —(CH2)2—CH(CH3)—(CH2)3—CH(CH3)2 or —(CH2)8—CH3], an optical isomer thereof and a pharmaceutically acceptable salt thereof. These compounds have antitrypanosoma activity, and accordingly are useful as drugs for preventing or treating the diseases caused by trypanosoma.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: Fatty acid-based, pre-cure-derived biomaterials, methods of making the biomaterials, and methods of using them as drug delivery carriers are described. The fatty acid-derived biomaterials can be utilized alone or in combination with a medical device for the release and local delivery of one or more therapeutic agents. Methods of forming and tailoring the properties of said biomaterials and methods of using said biomaterials for treating injury in a mammal are also provided.

Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.

Abstract: The present invention is a process for the preparation of diphenylazetidinone derivatives of the formula (I) or forms thereof comprising the substituents X, R1 and/or R2 as defined herein. More specifically, the invention comprises methods for the preparation of these compounds by cyclization of certain ?-amino carboxamides or ?-amino carboxylic esters. These diphenylazetidinone compounds are useful in the treatment of high blood serum cholesterol levels and the maintenance of the reduced cholesterol levels achieved thereby.

Abstract: The present invention relates to a novel class of compounds mainly, leucinamide-amino-carboxylate derivatives of formula (I) wherein Y is CR1R2, O, S, —SO2, C=0 or NR9; Z is CR1R2, O, S, —SO2, C?O or NR9 and each G is independently a CR1CR2. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B and to pharmaceutical compositions thereof. These compounds are useful for treating and preventing cathepsin dependent conditions in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The present invention is directed to cyclic ketal compounds of 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: The present invention relates to processes for preparing biaryl ureas derivatives and analogs thereof. The invention also provides compounds useful as intermediates in the processes of the present invention. The process is useful for preparing compounds that inhibit IMPDH.

Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.

Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: To provide a functional molecule including a modified nucleotide unit having a substituent introduced to a base thereof, wherein the substituent is removably introduced to the base; a functional molecule synthesizing amidite that has a substituent removably introduced to its base and that is used for the manufacture of the functional molecule; and a target substance analysis method including: preparing a random pool of functional molecules using a functional molecule synthesizing amidite; screening a functional molecule having affinity for a target substance from the random pool; amplifying the functional molecules having affinity for the target substance, wherein the method further comprises, prior to the amplification step, removing a substituent from the functional molecule having affinity for the target substance.

Abstract: Disclosed is a method of preparing 3-hydroxytetrahydrofuran using cyclodehydration. More particularly, this invention relates to a method of preparing 3-hydroxytetrahydrofuran, including subjecting 1,2,4-butanetriol to cyclodehydration under reaction conditions of a reaction temperature of 30˜180° C. and reaction pressure of 5000 psig or less in the presence of a strong acid cation exchange resin catalyst having a sulfonic acid group as an exchange group. According to the method of this invention, 3-hydroxytetrahydrofuran can be economically prepared at higher yield and productivity than when using conventional methods.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.

Abstract: Herein described is a process for the preparation of 1-chloro-3,5-di-O-acyl-2-de-oxy-L-ribofuranoside derivatives of general formula (I) useful as intermediates in processes for preparing nucleotides of the L series having antiviral activity