Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.

Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

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 present application describes deuterium-enriched larotaxel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: A novel dioxetane compound is provided having a cationically polymerizable oxetane group, which compound is excellent in compatibility with a liquid crystalline compound and a non-liquid crystalline compound. An optical film is also provided with excellent liquid crystal orientation retention properties and mechanical strength, produced by aligning a composition of the dioxetane compound and a cationically polymerizable compound in a liquid crystal orientation and fixing the liquid crystal orientation by polymerization. Further, a liquid crystal display device is provided with the optical film.

Abstract: The present application describes deuterium-enriched paclitaxel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention relates to pharmaceutical compositions comprising anhydrous(2R,3S)4-acetoxy-2-a-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I)(docetaxel) and 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1,7?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il (2R, 3S)3-benzoylamino-2-hydroxy-3-phenylpropionate (II) (paclitaxel), methods for treating neoplastic tumors using anhydrous docetaxel and paclitaxel, and a process for the preparation of the anhydrous docetaxel and paclitaxel.

Abstract: To provide an adamantane derivative, a compound having an adamantane skeleton, compositions containing them that can provide a cured product having excellent optical properties such as transparency and light resistance, long-term heat resistance and electric characteristics such as dielectric permittivity, and optical electronic members using the compositions. An adamantane derivative represented by the general formula (I), a compound with an adamantane skeleton represented by the general formula (VII) or (VIII), compositions containing them, and optical electronic members using the resin compositions.

Abstract: The present invention relates to a new process for the preparation of 9-dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9-dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7-position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II.

Abstract: A general process for the functionalization at the 14-position of 13-ketobaccatin derivatives of formula I to give derivatives of formula II wherein the substituents are as defined in the disclosure. The conversion of compounds of formula II in compounds of formula III, wherein the substituents are as defined in the disclosure, is also described.

Abstract: Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in 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 is also included. A method for inducing cell death in 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 is included as well.

Abstract: The invention concerns novel 1,2-dioxetane derivatives of general formula (I) as defined in the description, capable of emitting a detectable luminescent signal, their use in a method for detecting and/or quantizing a physical, chemical or biological, in particular enzymatic, phenomenon, as well as a kit for implementing said method.

Abstract: This invention is directed to a method for the preparation of docetaxel having an amorphous, anhydrous crystalline, or hydrated crystalline structure. In accordance with the invention, highly pure amorphous, anhydrous crystalline, or hydrated crystalline docetaxel can be produced with a high yield by using a solvent precipitation method, colloid formation method, etc.

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 is directed to novel compounds according to formulae wherein R1, R2, R3 and R4 are as defined herein. The invention also discloses methods of preparation, pharmaceutical compositions, and methods of disease treatment utilizing pharmaceutical compositions comprising these compounds. The compounds of this invention are novel therapeutic agents for the treatment of cancer, diabetes, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

Abstract: Novel conjugates of docetaxel and novel docetaxel immunogens derived from the 7 and 10 positions of docetaxel and monoclonal antibodies generated by these docetaxel linked immunogens are useful in immunoassays for the quantification and monitoring of docetaxel in biological fluids.

Abstract: Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.

Abstract: The present invention relates to a process for the preparation of synthetic taxanes, which protects C(7)-OH with lanthanon compounds. Its advantages are simple process and firm & reliable binding. Moreover, no C(7)-acylated taxanes are produced in the subsequent steps, and hydrolysis of C(2?)-ester groups in acylated products becomes readily controllable. In the process for the preparation of synthetic taxanes, tetrahydrofuran is used in the present invention as a medium for acylation, which not only achieves the same effects as pyridine, but also avoids odor, so as to solve the problem regarding the extremely high requirements for the place of production. The present invention can be used for the preparation of not only semi-synthetic taxane using natural taxanes as raw material, but also full-synthetic taxane.

Abstract: Novel conjugates of docetaxel and novel docetaxel immunogens derived from the 7 and 10 positions of docetaxel and monoclonal antibodies generated by these docetaxel linked immunogens are useful in immunoassays for the quantification and monitoring of docetaxel in biological fluids.

Abstract: A process is provided for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. Also described is a process for the preparation of Docetaxel starting from the compound of formula (I).

Abstract: The present application relates to new taxane analogs, pharmaceutical compositions comprising such analogs and methods of treating cancer comprising such compositions. The compounds according to the present application have the general formula: wherein R1 and R2 are each selected from H, alkyl, alkenyl or aryl; R3 is hydroxyl or OP1; R4 is OH or R7COO; R7 is alkyl, alkenyl or aryl, R8 and R9 are each independently selected from H, alkyl or alkenyl. The compounds of the present application may particularly be 9,10-?,?-OH taxane analogs that are formed by a process starting with a standard taxane as the starting 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 invention is based on the discovery that certain well-defined compounds derived from pentacyclopentadecane dimethanol are useful components in adhesive formulations. In particular, the invention compounds described herein provide high Tg values and low shrinkage. Compounds of the invention are useful as adhesives for use in the semiconductor packaging industry.

Abstract: The present invention generally relates to at least one precursor compound and derivatives thereof, a process for preparing a taxane, and a baccatin derivative.

Abstract: A surface-treating agent for forming a resist pattern, includes: a compound represented by formula (1) as defined in the specification, wherein the surface-treating agent is used in a step between a formation of a first resist pattern on a first resist film and a formation of a second resist film on the first resist pattern to form a second resist pattern, and a pattern-forming method uses the surface-treating agent.

Abstract: The invention discloses novel secotaxane derivatives of general formula 1, having cytotoxic activity, which can be administered through the injective or oral route, for the therapy of tumors.

Abstract: Disclosed is an oxetane-containing vinyl ether compound including one or more aromatic or non-aromatic carbocycles and/or two or more vinyl ether structures, such as a compound of Formula: wherein Ring Z1 is non-aromatic carbocycle; Ra is vinyl group of Formula: wherein each of R1, R2, and R3 is hydrogen or C1-C4 alkyl; Wa is single bond or organic group having a valence of (m+1); X1 is, for example, hydrocarbon; “m” and “q” are each 1 or 2; and “p” is 0 to 5. Also disclosed is an alicyclic epoxy-containing vinyl ether compound of Formula: wherein Ring Z2 is non-aromatic carbocycle; Rb is vinyl group of Formula: wherein R4, R5 and R6 are each hydrogen or C1-C4 alkyl; Wb is single bond or organic group having a valence of (r+1); Rc and Rd are hydrogen or alkyl; and “r” and “s” are 1 or 2.

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: Paclitaxel is separated from a mixture containing cephalomannin by column chromatography on silica gel using a solvent mixture containing methyl isobutyl ketone and a less polar solvent as the mobile phase. The less polar solvent can be a (C5-C8) aliphatic hydrocarbon, a (C6-C8) aromatic hydrocarbon, a (C1-C4) dialkyl ether or their mixtures.

Abstract: The invention concerns a method for preparing paclitaxel characterized in that it consists in starting with 10-deacety)-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 invention relates to a process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. The invention also discloses a process for the preparation of Docetaxel starting from said compound of formula (I).

Abstract: The invention concerns a method for preparing docetaxel from paclitaxel, including the following steps: a) deacylating paclitaxel, b) protecting the free hydroxy functions, in 7-, 10- and 2?-position respectively, c) debenzoylating the amine in 3?-position, into a primary amine derived for 10-deacetylbaccatine whereof the hydroxy functions in 7-, 10- and 2?-position are protected, d) functionalizing the amine with a t-butoxycarbonyl In radical to obtain a docetaxel derivative of general formula (I), wherein: X represents protecting radicals or hydrogen atoms, then, if required, e) releasing the initially protected hydroxy functions to obtain docetaxel.

Abstract: Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a link, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in 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 is included as well.

Abstract: Monodisperse macromolecular conjugate compositions of a peptidic carrier irreversibly or reversibly conjugated with one or more effectors and one or more therapeutic agents, wherein at least one effector or therapeutic agent is attached to a pendant reactive group on said peptidic carrier via a water-soluble polymer. Monodispersity is obtained through the use of orthogonal and separate conjugation reactions.

Abstract: Provided are a liquid-crystal compound and a liquid-crystal composition containing the compound, of which the advantages are that they show nematic hybrid orientation on a rubbed TAC substrate, they are polymerizable in open air and they readily give a polymer having a high degree of polymerization even when exposed to a relatively small total quantity of light. The films formed by photopolymerizing them keep nematic hybrid orientation. The compound is represented by formula (1): wherein R1 is a hydrogen or an alkyl; R2 is a hydrogen, —OCF3, etc.; A1 is a 1,4-phenylene, etc.; A2 and A3 are independently a 1,4-cyclohexylene, a 1,4-phenylene, etc.; X1 is a single bond, —O—, etc.; X2 and X3 are independently a single bond, —COO—, —C?C—, —CONH—, etc.; m is an integer of from 0 to 20; and n is 1 or 0.

Abstract: The invention relates to a process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel, a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. The invention also discloses a process for the preparation of Docetaxel starting from said compound of formula (I).

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

Abstract: Included within the scope of the present invention are potent taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in 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 is also included. A method for inducing cell death in 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 is included as well.

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: 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.

Abstract: The compound (1) or (2), a composition containing the compound and a polymer obtained by polymerizing the composition. R1 is fluorine, cyano, alkyl, and so forth; R2 is hydrogen, alkyl, and so forth; R3 and R4 are independently hydrogen, fluorine, alkyl, and so forth; A is 1,4-cyclohexylene, 1,4-phenylene, and so forth; X is a single bond, —COO—, —OCO—, and so forth; P is alkylene and so forth; m and n are independently 0, 1 or 2.

Abstract: The invention provides conjugates of fatty acids and anticancer agents useful in treating cancer, and compositions and formulations thereof. Methods for using the conjugates also are provided.

Abstract: Disclosed are compounds that inhibit proteasomic activity in cells. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly cell proliferative conditions, such as cancer and inflammatory conditions.

Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.

Abstract: The present invention provides processes for the production of paclitaxel. Paclitaxel 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 paclitaxel.

Abstract: A medicament to decrease the adverse events of Olistat, an oral lipase inhibitor, arranged in combination with Olistat, comprising: an emulsifier, a bowel relaxant and one or more chelating agents to absorb and mechanically agitate non-digested fats.

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: This invention describes a process for the production of ANHYDROUS active pharmaceutical ingredients (APIs); a process for the preparation of HYDRATED active pharmaceutical ingredients, a process for the preparation of sterile and stable injectable solutions, and their use, more specifically, APIs which are taxane derivatives, especially (2R,3S) 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I); 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1, 7?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-benzoylamino-2-hydroxy-3-phenylpropionate (II), and particularly 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate tri-hydrate (III).

Abstract: A method to prepare Docetaxel trihydrate using the mixture of acetone and water, which provides the product with good stability, less experiment time, less exposal to light, and avoids purity decreasing. The process is simple and easy to operate.

Abstract: A process for the preparation of taxane derivatives by reacting 10-deacetylbaccatin III protected at the 7-and 1-positions with trichloroacetyl groups with a compound of formula and subsequent removal of the protective groups and hydrolysis of the oxazolidine ring.