Abstract: It is intended to provide a natural biodegradable material having both properties of biodegradability and mechanical strength; a biodegradable film or container produced from the natural biodegradable material; a binder for producing the biodegradable material; and a method for producing these. A natural polymeric substance which has a cellulose-like property of having hydroxy group which is not present in a petroleum-derived polymeric compound, and which moreover has a polypropylene-like structure is obtained by the steps of using a cereal starch such as Kaoliang starch as a culture raw material, adding a microorganism belonging to the genus Bacillus to the raw material to conduct a culture, and recovering a viscous polymeric substance. A biodegradable material having biodegradability comparable to that of cellulose and also having a mechanical strength property of polypropylene can be obtained by using the natural polymeric substance as a binder and mixing starch and/or shell powder thereto.

Abstract: A method for obtaining a taxane by which a taxane is isolated from a growth medium, such as soil, pumice, perlite, rocks, and/or gravel in which a taxane-producing plant has grown. A method for obtaining a taxane by which a taxane is isolated from water effluent from plantings of living plants (e.g. a yew tree) that produce a taxane have grown in a growth medium, such as soil, pumice, perlite, rocks, and/or gravel.

Abstract: A polymerizable liquid crystal compound that has a wide liquid crystal phase temperature range and has a sterol ferulate skeleton, and a liquid crystal composition containing the compound are provided. A polymer that is excellent in various characteristics, and a molded article having optical anisotropy produced with the polymer are obtained with the polymerizable liquid crystal compound. The compound is represented by formula (1): wherein R represents a sterol moiety derived from vegetable organisms; P represents one of polymerizable groups represented by formulae (P1) to (P8); X, Z, X0 and Z0 each represent a bonding group; and A represents a divalent group having a cyclic structure.

Abstract: Chemotherapeutic conjugates of a peptide substrate to a phosphoramide chemotherapeutic agent in which a peptide substrate is covalently linked to the chemotherapeutic agent by a linker with an aminoarylmethyl or aminoheteroaryl moiety, wherein the linking of the peptide to the chemotherapeutic agent inhibits the cytotoxic activity of the chemotherapeutic agent, the peptide is a substrate for proteolytic cleavage by a tumor-specific enzyme; and the linker is capable of undergoing 1,6-elimination in vivo upon cleavage of the peptide substrate. Methods for synthesizing and methods of using the conjugates are also disclosed.

Abstract: The application provides a process for the preparation of taxane derivatives and intermediates useful in such processes.

Abstract: Optoelectronic materials are provided that are bistable organic tautomeric compositions that intraconvert dithio or diseleno carbamate esters and cyclic 1,3-dithia- or -diselena-2-iminium salts of ?-conjugated bis-anthracenyl compounds. Specifically disclosed are compounds having the formula: where X is sulfur or selenium; where the R and R1 groups are alkyl or alkyl that together form a ring of carbon atoms; where An is the anion of a strong acid; and where the Z element is a chiral ring-completing system of atoms that changes chirality on tautomerization. These molecules are in themselves molecular-sized optoelectronic switching devices.

Abstract: A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3? and an isopropoxycarbamate substituent at C3?.

Abstract: A polymerizable liquid crystal compound is represented by the following formula (1): P-Sp1-L1-M1-L2-Sp2-Ox ??(1) wherein P represents a polymerizable group; one of Sp1 and Sp2 represents a branched alkylene group, or an alkylene group containing, in the chain thereof, at least one divalent linking group selected from the group consisting of —O—, —C?C— and —S—; the other of Sp1 and Sp2 represents a straight chain alkylene group; each of L1 and L2 independently represents a divalent linking group; M1 represents a mesogenic group; and Ox represents a substituent containing an oxetanyl group.

Abstract: The present invention provides processes for the production of polycyclic fused ring compounds. The polycyclic fused ring compounds are produced by protecting a polycyclic fused ring polyol with a bridging silicon-based protecting group and attaching a suitable side chain. Polycyclic fused ring compounds and intermediate compounds are also described.

Abstract: The invention relates to novel cytotoxic agents comprising taxanes and their therapeutic use as a result of delivering the taxanes to a specific cell population in a targeted fashion by chemically linking the taxane to a cell binding agent.

Abstract: Anbydrous crystalline form of docetaxel and process of making anhydrous docetaxel and docetaxel trihydrate are provided.

Abstract: The present invention relates to an oxetane compound containing a (meth)acryloyl group represented by formula (1) having a high copolymerizability with compounds containing a (meth)acryloyl group, and to a production method of an oxetane compound containing a (meth)acryloyl group which is characterized by reacting an isocyanate compound having a (meth)acryloyl group represented by formula (5) with an oxetane compound containing a hydroxyl group represented by formula (6). (In the formula, R1 represents a hydrogen atom or a methyl group, A represents —OR2— or a bond, R2 represents a divalent hydrocarbon group which may contain an oxygen atom in the main chain, R3 represents a linear or branched alkylene group having 1 to 6 carbon atoms, and R4 represents a linear or branched alkyl group having 1 to 6 carbon atoms.

Abstract: This invention relates to an improved semi-synthetic process for the preparation of taxane derivatives like paclitaxel, docetaxel, canadensol and its derivatives, the process, which has shorten reaction route, simple procedure, high yield and low materials cost, therefore facilitates the commercial manufacture of these derivatives.

Abstract: Disclosed are coated metal oxide nanoparticles comprising a metal oxide nanoparticle having a surface; and ligands attached to the metal oxide nanoparticle surface. Also disclosed are phosphonic acid compounds comprising the structure Gn-R-Xn, wherein G is a terminal group; wherein R is a bridging group; wherein X is a phosphonic acid group; and wherein each n is, independently, 1, 2, or 3. Also disclosed are methods for preparing and using coated metal oxide nanoparticles. Also disclosed are nanocomposite compositions comprising a polymer; and a coated metal oxide nanoparticle dispersed within the polymer. Also disclosed are articles, films, and capacitors comprising a coated metal oxide nanoparticle or a nanocomposite composition. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.

Abstract: Provided herein is a straightforward and efficient method for covalently attaching a polyethylene glycol polymer to an active agent.

Abstract: An object of the present invention is to provide an organic electronic material that can be easily formed into a multilayer structure. A further object of the present invention is to provide an organic electronic device and an organic EL device that exhibit a better emission efficiency and a better emission lifetime than heretofore achieved. In order to achieve these objects, an organic electronic material is provided, the material includes a polymer or oligomer that has at least one polymerizable substituent and a hole-transporting repeat unit.

Abstract: Taxanes having an ethyl ester or cyclopropyl ester substituent at C(10), a keto substituent at C(9), a hydroxy substituent at C(7), a thienyl substituent at C(3?) and a cyclobutyloxycarbamate or cyclopentyloxycarbamate substituent at C(3?), pharmaceutical compositions comprising such taxanes, methods of treatment and administration, and methods of preparation of medicaments comprising the taxanes.

Abstract: A process for the precipitation of an organic compound comprising mixing simultaneously introduced streams of a solution and a precipitation agent in a chamber using a mechanical stirrer in the presence of an amphiphilic polymer. The process may be operated in a continuous manner and is particularly useful for providing low solubility organic compounds (e.g. pharmaceuticals) in readily dispersible, nano-sized particulate form up to manufacturing scale.

Abstract: The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.

Abstract: The present invention is related to a thermal extract of a plant material and methods of extraction thereof. The method of producing a thermal extract from a plant starting material by means of a thermal extraction of the starting material wherein the improvement consists in requiring smaller amounts of costly and/or toxic organic solvents for the extraction and partitioning steps.

Abstract: A paclitaxel intermediate of formula 1: wherein R1 is acetyl, R2 is tert-butyloxycarbonyl (BOC), R3 and R4 are phenyl and R5 is 1-ethoxyethyl, is provided. Also provided are processes for preparing taxane intermediates of formula 1 comprising reacting a compound of formula 2 with a compound of formula 3 wherein, R1, R2 and R5 are independently a hydroxyl protecting group; R3 is phenyl, substituted phenyl, a straight or branched alkyl containing 1 to 12 carbon atoms, alkenyl containing 2 to 12 carbon atoms, cycloalkyl containing 4 to 15 carbon atoms, cycloalkenyl or an R6—O— group in which R6 is: phenyl, substituted phenyl group, a C1-C8 straight or branched alkyl, a C2-C8 straight or branched alkenyl group, a C3-C8 straight or branched alkynyl, a C3-C7 cycloalkyl, C4-C7 cycloalkenyl, a C7-C11 bicycloalkyl substituent, or a saturated or unsaturated nitrogen; and R4 is phenyl or a substituted phenyl group.

Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.

Abstract: New anhydrous crystalline form of docetaxel and process of making anhydrous docetaxel and docetaxel trihydrate are provided.

Abstract: A surfactant comprising a polyether segment including at least one pendant alkoxyfluoroalkyl group, and a cationic substituent defined by one of the formulae: or the substituted derivatives thereof.

Abstract: The invention relates to methods and compositions for converting taxane amides to paclitaxel or other taxanes. In one alternative embodiment, the present invention comprises; (i) selectively protecting at least one OH group of a taxane amide; (ii) contacting the taxane amide with a transition metal compound to reduce the amide; (iii) contacting the reduced amide with an agent capable of substantially removing the transition metal; (iv) contacting the reduced amide with a hydrolyzing amount of acid to form a taxane amine salt in solution; (v) adding a sufficient amount of solvent to solidify the amine salt; and (vi) converting the taxane amine salt into paclitaxel or other taxanes.

Abstract: Provided is a production process by which a novel alicyclic oxetane compound which has an oxetane ring, has excellent light transmission in the near ultraviolet region, and is useful as a cationically polymerizable monomer can be easily obtained. The production process which is for obtaining an alicyclic oxetane compound includes subjecting an aromatic oxetane compound to nuclear hydrogenation in high-pressure hydrogen in the presence of a hydrogenation catalyst. For example, when 4,4?-bis[(3-ethyloxetan-3-yl)methoxymethyl]biphenyl is used as the aromatic oxetane compound, 4,4?-bis[(3-ethyloxetan-3-yl)methoxymethyl]bicyclohexyl is obtained as the alicyclic oxetane compound.

Abstract: The invention relates to taxanes and to novel cytotoxic agents comprising taxanes and their therapeutic use as a result of delivering the taxanes to a specific cell population in a targeted fashion by chemically linking the taxane to a cell binding agent.

Abstract: The invention provides low molecular weight or polymeric organic materials in which at least one hydrogen atom is replaced by a group of the formula (A) where R is alkyl group, alkoxyalkyl group, alkoxy group, thioalkoxy group, aryl group or alkenyl group, in each of which one or more hydrogen atoms may be replaced and one or more nonadjacent carbon atoms may be replaced. Z is —O—, —S—, —CO—, —COO—, —O—CO— or a bivalent group —(CR1R2)n— in which R1 and R2 are hydrogen, alkyl, alkoxy, alkoxyalkyl or thioalkoxy group, aryl or alkenyl, in each of which one or more hydrogen atoms may be replaced and one or more nonadjacent carbon atoms may be replaced, and n is an integer from 1 to 20. X is a bivalent group —(CR1R2)n— and, with the proviso that the number of these A groups is limited by the maximum number of available substitutable hydrogen atoms.

Abstract: The present invention provides polymeric delivery systems including hindered ester moieties. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3? and an isopropoxycarbamate substituent at C3?.

Abstract: A process is provided for the semi-synthesis of taxane intermediates and aziridine analogues of cephalomannine and baccatin III intermediates, and the conversion of such intermediates and analogues to paclitaxel and docetaxel.

Abstract: Novel conjugates of taxol and novel taxol immunogens derived from the 9 and 7 positions of taxol and monoclonal antibodies generated by these taxol linked immunogens are useful in immunoassays for the quantification and monitoring of taxol in biological fluids.

Abstract: A pharmaceutical formulation of taxane intended to be administered to mammals, preferably humans, comprises two compositions combined prior to being administered, forming a transparent solution free from precipitates, in which the compositions comprise a solid composition of lyophilized taxane, free from tensoactives, oils, polymers, solubility enhancers, preservatives and excipients; and a solubilizing composition of the lyophilized taxane solid composition that comprises at least one tensoactive. This formulation is free from polysorbate 80 and polyoxyethylated castor oil. A procedure is provided for the preparation of the solid composition by means of the lyophilization of taxane in a lyophilizing organic solvent. A kit for the injectable formulation of taxane comprises a prefilled syringe. Also a pharmaceutical taxane solution for perfusion, free from organic solvent, is provided.

Abstract: Paclitaxel is isolated by a process including normal phase chromatography using a polyamide stationary phase and a mixture containing a dialkyl ketone and a less polar solvent as a mobile phase. Suitable dialkyl ketones include acetone or methyl isobutyl ketone. Suitable less polar co-solvents include a (C5-C8) aliphatic hydrocarbon, a (C6-C8) aromatic hydrocarbon, a (C1-C4) dialkyl ether or their mixtures.

Abstract: The present invention provides a process for production of an anticancer taxoid brevifoliol of the formula I from plants belonging to the genus Taxus by first extracting the dried and pulverized leaves of the plant with an alcohol preferably at a temperature in the range of 20-40° C. and then. concentrating the solvent to obtain an alcoholic extract. The alcoholic extract obtained is then adsorbed with an adsorbent and the resulting adsorbed material is then dried at a temperature ranging from 20-50° C. for 4-48 hours. The dried adsorbed material is then extracted with a combination of an aliphatic solvent and a chlorinated solvent successively and concentrated to obtain a residue. The residue is subjected to gross fractionation using column chromatography such as silica gel, florosil and silicic acid followed by chromatography with a suitable adsorbent to get brevifoliol.

Abstract: Heterocycles, e.g., epoxides, are carbonylated at low pressure with high percentage conversion to cyclic, ring expanded products using the catalyst where L is tetrahydrofuran (THF).

Abstract: The invention concerns a method for preparing paclitaxel characterized in that it consists in starting with 10-deacetyl-baccatine in accordance with a “one-pot” reaction including the following three steps: a) protecting the hydroxy radical in position 7 of 10-deacetylbaccatine with a silylated radical, then b) acetylating the hydroxy radical in position 10, c) optionally crystallizing the resulting baccatine III derivative, followed by condensation of (4S,5R)-3-N-benzoyl-2RS-methoxy-4-phenyl-1,3-oxazolidine-5-carboxylic acid, by esterifying in position 13 the acetylated 10-baccatine III derivative previously obtained, then opening the oxazolidine of the cyclic side chain and simultaneously releasing the hydroxy radical in position 7.

Abstract: The present invention relates to a process is provided for the conversion of 9-dihydro-13-acetylbaccatin to 10-deacetylbaccatin III. The process includes four specific interrelated steps. The first step involves protecting the 7-hydroxyl group of 9-dihydro-13-acetylbaccatin and converting that 7-hydroxyl-protected 9-dihydro-13-acetylbaccatin to 7, 13-diacetyl-9-dihydrobaccatin III. The second step involves reacting that 7, 13-diacetyl-9-dihydrobaccatin III with 4-methylmorpholine N-oxide in a suitable solvent and oxidizing that reaction product to yield 7, 13-diacetylbaccatin. The third step involves deacetylating that 7, 13-diacetyl-9-dihydrobaccatin III to yield 7-acetylbaccatin III. The fourth and final step involves converting that 7-acetylbaccatin III to 10-deacetylbaccatin III.

Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

Abstract: The present invention provides processes for the production of docetaxel. Docetaxel is produced by protecting the C(7) and the C(10) hydroxy groups of 10-DAB with a bridging silicon-based protecting group. The resulting 7,10-protected 10-DAB derivative is then derivatized and deprotected to form docetaxel.

Abstract: The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds. More particularly, the present embodiments disclosed herein relate to novel side chains, that when coupled to a taxane, are useful for the synthesis of pharmaceutically useful taxanes. Methods of forming the novel side chains and coupling them to hindered alcohols, namely taxanes resulting in useful esters are also disclosed. Various taxanes compounds are known to exhibit anti-tumor activity.

Abstract: The present invention relates to 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 provides an adamantane derivative that can provide a cured product having excellent optical properties such as transparency and lightfastness, long-term heat resistance, and electric characteristics such as permittivity, and an epoxy resin having an adamantane skeleton, a resin composition comprising them, and an optical electronic member using the resin composition. The adamantane derivative is represented by general formula (I). The epoxy resin having an adamantane skeleton is represented by general formula (V) or (VI). The resin composition comprises them. The optical electronic member uses the resin composition.

Abstract: Disclosed is an adamantane derivative which enables to obtain a cured product which is excellent in optical characteristics such as transparency and light resistance, long-term heat resistance, and electrical characteristics such as dielectric constant. Also disclosed are a resin composition containing such an adamantane derivative, and a sealing agent for electronic circuits and an optoelectronic member respectively using those. Specifically disclosed are an adamantane derivative represented by the general formula (I) below, a resin composition containing such an adamantane derivative, a sealing agent for electronic circuits and an optoelectronic member respectively using such a resin composition, and an adhesive of those.

Abstract: The invention provides a medical device comprising a hydrophobic analog of a medicament known to inhibit cell proliferation and migration. The invention also provides a method of treating a narrowing in a body passageway comprising placing an implantable medical device comprising a hydrophobic analog of a medicament known to inhibit cell proliferation and migration. The medicaments can be incorporated within or coated on the device. The invention further provides hydrophobic analogs of medicaments known to inhibit cell proliferation and migration.

Abstract: The invention relates to fluorinated second generation taxoid compounds, pharmaceutical formulations thereof, and their use for inhibiting the growth of cancer cells in a mammal.

Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: An oxetane-containing compound, a photoresist composition including the same, a method of preparing patterns using the photoresist composition, and an inkjet print head including polymerization products of the oxetane-containing compound.