Abstract: The main aim of the invention is to provide a polymerizable compound that is excellent in the stability of a liquid crystal phase, a polymerizable liquid crystal composition, and an anisotropic polymer in which the optical anisotropy can be adjusted and a uniform orientation is excellent. An anisotropic polymer having a uniform orientation formed by polymerization of a paint film that was prepared by application of a polymerizable liquid crystal composition including a compound represented by formula (1) having a benzyl ester moiety in the minor axis direction of the molecule to a supporting substrate; wherein at least one of Ra is a polymerizable group, A is a divalent cyclic-structure group, B is phenyl that may have a substituent, Y and Z are a single bond or alkylene, and m and n are an integer from 0 to 5.

Abstract: A new process for preparing a compound of Formula V, wherein P is a hydroxy protecting group and R is acetyl, said process including the steps of: i) selectively deacetylating the 10-hydroxy group of 9-dihydro-13-acetylbaccatin III with N,N-dimethylethylenediamine to produce 9-dihydro-10-deacetyl-13-acetyl-baccatin III; ii) concomitantly protecting 7-hydroxy and 10-hydroxy groups of the reaction product of step i); and iii) oxidizing the 9-hydroxy group of the reaction product of step ii) with an oxidizing agent to produce the compound of formula V.

Abstract: The present application relates to novel 3-phenylpropionic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.

Abstract: The invention provides a compound represented by formula (1). In the formula (1), R1 is hydrogen, methyl or ethyl; X1 is a single bond, —O— or —OCO—; X2 is a single bond, —O—, —COO— or —OCO—; A1 and A2 are each independently a divalent aromatic ring or a divalent cyclohexane ring, and in these rings, arbitrary hydrogen may be replaced by halogen, alkyl having 1 to 3 carbons or halogenated alkyl having 1 to 3 carbons; Z1 is independently a single bond, —O—, —S—, —COO—, —OCO—, —CH2O—, —OCH2—, —CH?CH—COO—, —OCO—CH?CH—, —CH2CH2—COO—, —OCO—CH2CH2—, —CON(R)— or —N(R)CO—; R is hydrogen or methyl; Y is a terpenoid residue or a steroid residue; m is an integer from 0 to 20; and n is an integer from 0 to 3.

Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.

Abstract: Processes for the preparation of docetaxel and paclitaxel or analogs from 9-dihydro-13-acetylbaccatin III via key intermediates (4), (5), (6), (6?), (8) and (8?) or via intermediate (12) as well as processes for the preparation of said intermediates are disclosed. Said processes involve, in particular, oxidation of the hydroxy group at C-10, reaction with side chain precursors and intramolecular isomerisation of the oxo at C-10 to produce the 9-oxo isomer. Paclitaxel and docetaxel are useful in the treatment of cancer. Formulae (I), (II), (III).

Abstract: Provided are a polymerizable group-containing and fluorine-containing adamantane derivative capable of affording a cured product having good heat resistance, good mechanical properties such as surface hardness and a low refractive index, a resin composition containing such a polymerizable group-containing adamantane derivative, and a fluorine-containing adamantane derivative which is useful as a reaction intermediate used for the production of the polymerizable group-containing and fluorine-containing adamantane derivative. Specifically provided are a fluorine-containing adamantane derivative represented by the general formula (I) below, a polymerizable group-containing and fluorine-containing adamantane derivative represented by the general formula (II) below, and a resin composition containing such a polymerizable group-containing and fluorine-containing adamantane derivative.

Abstract: The present disclosure relates to processes for the preparation of taxane derivatives with improved purity and enhanced stability. The taxane derivatives prepared according to the processes described herein are useful for the preparation of pharmaceutical compositions.

Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.

Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).

Abstract: A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2?, C-7 and C-10 positions and introducing a t-Boc group at the nitrogen of the amide group at the C-3? position in paclitaxel and subsequently conversion to docetaxel, and derivatives used therein.

Abstract: Disclosed herein are compounds and compositions including a polyglycerol nanocarrier, a therapeutic agent or imaging agent, and optionally a targeting agent. In certain aspects the disclosed compounds include biocompatible hyperbranched polymer nanocarriers. Such compounds and compositions are useful for the targeted delivery of antitumor agents and imaging agents to tumors in vivo. Methods are also disclosed for detecting and treating such tumors.

Abstract: The present invention provides an oxetane compound represented by the following formula (1), and a active energy ray-curable composition including the oxetane compound as a polymerizable monomer.

Abstract: A stereoselective synthesis of novel ?-lactam dimers as useful precursors for the preparation of paclitaxel, docetaxel, and analogues thereof. More particularly, the new ?-lactams are prepared from readily available and enantiomerically pure chiral auxiliaries. The ?-lactams are then reacted with a suitably protected taxane to produce diastereomerically enriched side chain-bearing taxanes. Finally, the chiral auxiliary is cleaved and protecting groups are removed to provide the desired taxane.

Abstract: This invention is directed to a method for isolating and/or purifying one or more taxanes from materials comprising taxanes. In one embodiment, the method comprises the steps of: (a) treating a taxane containing material with an amino containing material attached to a solid matrix, such as a polyethyleneimine-bonded silica chromatographic resin; (b) eluting the desired taxane compound from the resin; and (c) recovering the eluted taxane compound.

Abstract: A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediates.

Abstract: The present invention discloses cephalomannine derivatives of general formula (I), a process for preparation of such cephalomannine derivatives, a composition containing such compounds, and use of said compounds in the manufacture of a medicament for the treatment of tumors, especially multidrug resistant tumors.

Abstract: This invention is directed to a method for efficiently separating and purifying 13-dehydroxybaccatin III and 10-deacetylpaclitaxel with a high purity of 90% or higher purity, preferably 99.5% or higher purity, from taxane-containing materials such as Taxus species, and the thusly obtained highly pure 13-dehydroxybaccatin III and 10-deacetylpaclitaxel can be used as semi-synthetic precursors of paclitaxel and/or docetaxel that are anticancer agents.

Abstract: The invention provides a process for preparing a cell-binding agent chemically coupled to a drug. The process comprises covalently attaching a linker to a cell-binding agent, a purification step, conjugating a drug to the cell-binding agent and a subsequent purification step.

Abstract: A method for synthesizing carbon nanotube drug carriers and the carbon nanotube drug carriers are disclosed. Initially, carbon nanotubes, nitric acid, and sulfuric acid are mixed to oxidize carbon nanotubes in a first mixture. The oxidized carbon nanotubes are then extracted from the first mixture. The oxidized carbon nanotubes and monohydrated citric acid are mixed to synthesize carbon nanotubes grafted with poly(citric acid) in a second mixture. The carbon nanotubes grafted with poly(citric acid) are then extracted from the second mixture. The carbon nanotubes grafted with poly(citric acid) and 4-(dimethylamino)pyridine are dissolved in anhydrous dimethylformamide in a third mixture. Next, a mixture that comprises a drug is added to the third mixture to synthesize the carbon nanotubes grafted with poly(citric acid) and the drug in a fourth mixture. Then, the carbon nanotubes grafted with poly(citric acid) and the drug are extracted from the fourth mixture.

Abstract: The present invention relates to a novel method of preparing a taxane derivative having an anti-tumor and anti-leukemia activity, and intermediates used therein.

Abstract: ?-Cyanoacrylates of the formula I, where: R1 is ORa wherein Ra is hydrogen, substituted alkyl, branched alkyl, branched alkenyl, cycloloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; is NRbRc wherein Rb is hydrogen, alkyl which may be substituted, alkenyl, alkynyl; Rc is hydrogen, alkyl which may be substituted alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; or Rb and Rc form an alkandiyl-chain which may be substituted; or is SRd wherein Rd is hydrogen, alkyl which may be substituted, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; R2 is alkyl which may be substituted; is alkenyl or alkynyl; R3 is alkyl may be substituted; is alkenyl or alkynyl; R4 is hydrogen, halogen, cyano or alkyl; and their agriculturally useful salts, processes and intermediates for their preparation; and the use of these compounds or of compositions comprising these compounds for controlling undesirable plants are described.

Abstract: The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. The present invention also disclosed intermediates of docetaxel and methods for preparation thereof.

Abstract: A semisynthetic route has been provided in the preparation of docetaxel and paclitaxel. This new process involves the conversion of 9-dihydro-13-acetylbaccatin III to docetaxel and paclitaxel by the step of converting 9-dihydro-13-acetylbaccatin III into 7-O-triethylsilyl-9,10-diketobaccatin III, and adding docetaxel and paclitaxel side chain precursors, respectively, to form a new class of taxane intermediates, such as 7-O-triethylsilyl-9,10-diketodocetaxel and 7-O-triethylsilyl-9,10-diketopaclitaxeltaxel. These new intermediates then by a series reduction, acetylation of the 10-hydroxyl position for paclitaxel and finally deprotection to yield docetaxel and paclitaxel, the most important anti-cancer drugs.

Abstract: The invention relates to a water-dispersible derivative of a therapeutic agent having a low water solubility that comprises at least one molecule of said agent covalently bonded to at least one molecule of a hydrocarbon derivative having a squalenic structure or the like. The invention further relates to corresponding nanoparticles.

Abstract: A process is provided for the semi-synthesis and isolation of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis and isolation of 10-deacetylbaccatin III, the semi-synthesis of a mixture of 10-deacetylbaccatin III and baccatin III, and protected derivatives thereof, from a mixture of taxanes.

Abstract: The invention relates to a second-generation-fatty acid conjugate and pharmaceutical compositions thereof. The second-generation-fatty acid conjugate are useful in the treatment of cancer in a human in need thereof.

Abstract: The invention provides conjugates of fatty alcohols and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparation of the fatty alcohols-pharmaceutical agent conjugates are provided.

Abstract: Novel organic compounds are described and claimed which may in particular be useful in the treatment of diseases being triggered by the (human) autoimmune system.

Abstract: Provided are dendritic nano-antioxidant compounds according to Formula I, which may further comprise active agents covalently or non-covalently attached. Further provided are compositions comprising the disclosed compounds. Also disclosed are cosmetic compositions and dietary supplements comprising the compounds according to Formula I. The invention additionally provides methods of reducing free radicals or oxidative stress in a cell, a method of treating a subject, and a method of treating a condition comprising administering the compounds according to Formula I.

Abstract: The present invention relates to Y-shape branched PEG derivatives of formulae (I) to (IV). The present invention also relates to conjugates of these Y-shape derivatives and drug molecules, pharmaceutical compositions comprising those conjugates.

Abstract: Lipophilic di(anticancer drug) compounds, compositions that include the compounds, and methods for treating a cell proliferative disease using the compounds.

Abstract: This invention relates to the treatment of cancer using anti-cancer agents, such as doxorubicin or paclitaxel, in combination with antibody-interleukin 2 (IL2) conjugates which target tenascin-C.

Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: This invention relates to novel compounds with ester linkage(s) capped with either electron deficient olefinic linkage(s) or group(s) or reactive functional groups (termed herein as “active methylene reagents”), and curable compositions prepared therefrom.

Abstract: Processes for preparing substantially pure docetaxel, new crystalline forms of docetaxel and processes for preparation thereof, processes for preparing docetaxel trihydrate, and pharmaceutical compositions comprising docetaxel.

Abstract: A process and device for the precipitation of an organic compound comprising the steps: (a) providing a first stream comprising an organic compound and a solvent for the organic compound; (b) providing a second stream comprising an anti-solvent for the organic compound; (c) providing a third stream comprising a second stabilising agent; (d) intermixing the first and second streams to form a precipitate of the organic compound in particulate form; and (e) following step (d), intermixing the third stream with the intermixed first and second streams containing the precipitated organic compound in particulate form wherein the first and/or the second stream comprises a first stabilising agent.

Abstract: The present invention relates to a trisoxetane compound represented by the following formula (1): wherein each of R1 and R3's represents a hydrogen atom or an alkyl group having 1 to 6 carbon atom(s); R2 represents a divalent aliphatic chained organic group having 0 to 16 carbon atom(s); and A represents a carbon atom or a trivalent organic group derived from a cycloalkane having 3 to 12 carbon atoms; a process for producing the same; and an optical waveguide including the same.

Abstract: The present invention discloses a curable polycyclic compound represented by the following formula (1): {wherein A is a di- to hexa-valent group derived from a polycyclic hydrocarbon compound; R1 is an alkyl group of 1 to 4 carbon atoms, a perfluoroalkyl group of 1 to 4 carbon atoms, or a fluorine atom; n is an integer of 0 to 2; m is an integer of 2 to 4; and Y is a group represented by the following formula (2) or (3): (wherein R2, R3, R5 and R6 are each independently a hydrogen atom, a fluorine atom or an alkyl group of 1 to 4 carbon atoms; R4 is a methyl group or an ethyl group; and p and q are each independently an integer of 0 to 4)}.

Abstract: Disclosed is a 3-ethyloxethane compound having a hydroxyl group which is represented by the following general formula (1). (1) (In the formula, A represents an alkylene group having 3-5 carbon atoms which may have an ether bond or an alkylene group having 3-5 carbon atoms which may be substituted by a hydroxyl group.) The 3-ethyloxethane compound having a hydroxyl group can be produced by reacting a 3-ethyloxethane compound represented by the general formula (2) below, a diol compound represented by the general formula (3) below and a base. (2) (In the formula, X represents a leaving group.) (3) (In the formula, A is as defined above.

Abstract: An adhesive is provided containing at least one synthetic polymer with receptor sites that enable the selective capture or release of a target molecule. A polymer is synthesized by polymerizing and cross-linking a functional monomer or functional copolymers in the presence of a target or template molecule allowing for reversible interactions between the polymer and the target molecule. The target molecule may be extracted from the polymer creating receptor sites complimentary to the target molecule. Alternatively, the target molecule may remain in the polymer network and be controllably released. The molecularly imprinted polymer is formulated into an adhesive. The adhesive can be used as a component in an in-vitro diagnostic device to release template molecules or to capture target molecules in vacated receptor sites in the synthetic polymer.

Abstract: The present invention relates to taxane analogs for the treatment of cancer having the general formula: wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R3 is hydroxyl or OP1; R4 and R5 are each hydroxyl or R7COO; R6 is hydroxyl, OP2, R7COO, or an ether functionality; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 and P2 are each hydroxyl protecting groups; R8 and R9 are each selected from H, alkyl group, olefinic or aromatic group. The present invention is also directed to production methods and intermediates useful in the formation of these new taxane analogs. The methods may begin with a starting compound, such as paclitaxel or docetaxel, which is converted into a taxane analog through various intermediate compounds.

Abstract: The present invention provides crystalline polymorphs of docetaxel and processes for preparing them, a method for preparing amorphous docetaxel, and a process for preparing docetaxel.

Abstract: Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.

Abstract: A compound of the formula (I): wherein each symbol is as defined in the description, a salt s thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonist activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.

Abstract: The present invention relates to a trisoxetane compound represented by the following formula (1): wherein R1 and R3 to R8 are the same or different and each represents a hydrogen atom or an alkyl group having 1 to 6 carbon atom(s) with the proviso that at least one of R3 to R8 is an alkyl group having 1 to 6 carbon atom(s); R2 represents a divalent aliphatic chained organic group having 0 to 16 carbon atom(s); and R9's each represents a hydrogen atom or an alkyl group having 1 to 6 carbon atom(s), a process for producing the same, and an optical waveguide including the same.

Abstract: A 4,9-bis(glycidyloxy)diamantane and a 4,9-bis[(3-ethyloxetane-3-yl)methyloxy]diamantane are novel curable diamantane compounds, and cured bodies thereof are useful as encapsulants exhibiting excellent light resistance and heat resistance, and can be favorably used, for example, as encapsulants for near ultraviolet LEDs and white LEDs.

Abstract: The present invention relates to a novel method for preparing docetaxel having anti-tumor and anti-leukemia activity, and intermediates useful for preparing docetaxel.

Abstract: The present invention provides a stable anhydrous crystalline docetaxel which has anti-tumor and anti-leukemia activity, and method for the preparation thereof.

Abstract: Disclosed are water-soluble compositions of gemcitabine and docetaxel formed by conjugating the gemcitabine or docetaxel to a water-soluble polymer such as N-2-hydroxypropyl methacrylamide (HPMA). Also disclosed are methods of using the compositions of the invention for the treatment of cancer.