Abstract: The invention relates to a method for the production of a compound comprising a free hydroxyl group and a hydroxyl group which is protected by an ester function by enzymatic reaction, using a lipase EC 3.1.1.3. The invention also relates to the use of the resultant compound as an intermediate for the production of medicaments and pharmaceutical products.

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: The present invention provides novel fluorine-containing copolymers which comprise at least one fluorinated olefin, at least one polycyclic ethylenically unsaturated monomer with a fused 4-membered heterocyclic ring and, optionally, other components. The copolymers are useful for photoimaging compositions and, in particular, photoresist compositions (positive-working and/or negative-working) for imaging in the production of semiconductor devices. The copolymers are especially useful in photoresist compositions having high UV transparency (particularly at short wavelengths, e.g., 157 nm) which are useful as base resins in resists and potentially in many other applications.

Abstract: The present invention provides an ink composition comprising a compound having a fragment containing a cyclic ether group having at least one bicyclo or tricyclic substituent.

Abstract: A process for the preparation of 14?-hydroxy-baccatin III-1,14-carbonate useful for the preparation of novel taxane derivatives with antitumor activity.

Abstract: A novel semisynthetic route has been provided in the preparation of docetaxel and paclitaxel. This new process involves the conversion of 9-dihydro-13-acetylbaccatinIII 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 present invention relates to a method for producing a 2-hydroxypropyl-beta-cyclodextrin inclusion complex of taxol, said 2-hydroxypropyl-beta-cyclodextrin having a degree of substitution of 0.4 to about 0.9, wherein the method comprises admixing the 2-hydroxypropyl-beta-cyclodextrin with taxol at a molar ratio of 1-1000 times with respect to taxol. A second aspect of the invention relates to a method for improving the solubility of taxol, said method comprising: (i) dissolving taxol in ethanol; (ii) dissolving 2-hydroxypropyl-beta-cyclodextrin, having a degree of substitution of 0.4 to about 0.9, in water; (iii) admixing the solution from step (i) with the solution from step (ii) and stirring, shaking or heating. A third aspect of the invention provides a 2-hydroxypropyl-beta-cyclodextrin inclusion complex of taxol, wherein said 2-hydroxypropyl-beta-cyclodextrine has a degree of substitution of 0.4 to about 0.9.

Abstract: The invention includes compounds represented by Formula (1): wherein R1 is an alkyl having 1 to 20 carbon atoms; A1 and A2 are a 1,4-cyclohexylene or 1,4-phenylene; X is a single bond, —C?C—, —COO—, —OCO—, —CH?CH—COO— or —OCO—CH?CH—; P is an alkylene having 1 to 20 carbon atoms; and p and q are 0, 1 or 2.

Abstract: Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.

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 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 relates to new 3-methyl oxetanemethanol derivatives and their use as fragrance chemicals suitable for incorporation in fine fragrances, cosmetics, toiletries and related applications.

Abstract: This invention provides methods whereby taxol, baccatin III, and other taxol-like compounds, or taxanes, can be produced in very high yield from all known Taxus species, e.g., brevifolia, canadensis, cuspidata, baccata, globosa, floridana, wallichiana, media and chinensis. Particular modifications of culture conditions (i.e., media composition and operating modes) have been discovered to enhance the yield of various taxanes from cell culture of all species of Taxus. Particularly preferred enhancement agents include silver ion or complex, jasmonic acid (especially the methyl ester), auxin-related growth regulators, and inhibitors of the phenylpropanoid pathway, such as 3,4-methylenedioxy-6-nitrocinnamic acid. These enhancement agents may be used alone or in combination with one another or other yield-enhancing conditions. While the yield of taxanes from plant cell culture of T.

Abstract: This invention relates to methods for purification of paclitaxel from a paclitaxel-containing material. The method comprises the following steps: (a) extracting a paclitaxel-containing material with an organic solvent to obtain an extract, and concentrating the extract; (b) adding the concentrate with an organic solvent which is not mixed with water to separate an organic solvent phase and then concentrating; (c) subjecting the concentrate to normal phase chromatography to obtain an eluate; (d) dissolving the eluate in an acetone or dichloromethane followed by adding pentane or hexane to form a precipitate; and (e) subjecting the precipitate to high performance liquid chromatography. According to the method of the present invention, paclitaxel of over 99.5% purity can be easily obtained from a Taxus genus plant with a high yield.

Abstract: Taxanes having a methylcarbonate or ethylcarbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(13) side chain substituents.

Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.

Abstract: This invention relates to a process for preparation of taxanes comprising subjecting 7,10-diprotected intermediates 7-O-(2-haloacyl)baccatin III 6c or 7,10-O-di-(2-haloacyl)-10-deacetylbaccatin III 6b to a step of coupling with (4S,5R)-3-[(2-alkyl/aryl-2-trialkylsilyl)ethoxy-carbonyl]-4-aryl-2-substituted-1,3-oxazolidine-5-carboxylic acid 1 in the presence of a condensation agent, an activating agent and an aromatic hydrocarbon to obtain 7-O-[2-(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3(2-unsubstituted/substituted-2-trialkylsilyl)-ethoxycarbonyl-1,3-oxazolidinyl-5-carbonyl]baccatin III 7a or 7,10-di-O[2-(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3-(2-unsubstituted/substituted-2-trialkylsilyl)ethoxy-carbonyl-1,3-oxazolidinyl-5-carbonyl]-10-deacetylbaccatin III 7b; treating the coupled products 7-O-[2-(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3-(2-substituted-2-trialkylsilyl)ethoxy-carbonyl-1,3-oxazolidinyl-5-carbonyl]baccatin III 7a or 7,10-di-O-[2[(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3-(2-su

Abstract: This invention discloses and claims an acetone solvate of dimethoxydocetaxel or 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1-hydroxy-7?,10?-dimethoxy-9-oxotax-11-en-13?-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and its preparation by crystallization from an aqueous/acetone solution.

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: Compositions comprising a taxane having a carbamoyloxy 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: Compositions containing oxetane compounds having ester, amide, urea, carbamate, carbonate, or carbonyl functionality one carbon atom removed from the oxetane ring cure at high temperatures are suitable for use as underfill materials within a semiconductor package, particularly in applications using lead free solder electrical interconnections.

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

Abstract: The invention provides methods and compositions for reductively deoxygenating an amide group at a C-3? position of a taxane molecule followed by subsequent intra-molecular acyl migration of an acyl group to the C-3? position.

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 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: A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and the insertion of the phenylisoserine side chain onto the protected baccatin III from 9-dihydro-13-acetylbaccatin III to form the taxane derivatives, paclitaxel and docetaxel is disclosed.

Abstract: A process for synthesizing a C-7 protected baccatin III compound represented by formula (A), which comprises reacting a 10-deacetylbaccatin III compound represented by formula (B) with a protecting agent and an acylating agent in the presence of a secondary amine and a nitrogen-containing compound. Also, a process for synthesizing a C-7 protected 10-deacetylbaccatin III compound represented by formula (C), which comprises reacting a 10-deacetylbaccatin III compound represented by formula (B) with a protecting agent in the presence of a secondary amine and a nitrogen-containing compound. In both processes the nitrogen-containing compound is selected from a nitrogen-containing heterocycle or a trialkylamine. When the nitrogen-containing heterocycle is selected, it may be an unsubstituted or a substituted pyridine or an unsubstituted or a substituted pyrazine. When a trialkylamine is selected, it may be, for example, triethylamine or diisopropylethylamine.

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

Abstract: Texanes having a heterosubstituted acetate substituent at C(7), a hydroxy substitutent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

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: The invention provides methods and compositions for selectively acylating a specific hydroxyl group in a molecule of interest containing at least two unprotected secondary hydroxyl groups. Although the methods and compositions of the invention have general applicability, they are particularly useful in the selective acylation of taxane molecules.

Abstract: Novel ?-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling ?-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.

Abstract: This invention teaches a purification technology to extract an organic solution of paclitaxel by using a “Load and Lock Axial Compression Column” for industrial scale preparative high performance liquid chromatography. The “Load and Lock Axial Compression Column” is one in which a piston is used to pack and unpack the chromatography bed substantially to avoid voids therein, and to maintain bed compression during use. This effectively substantially prevents the formation of voids in the bed. The column can be packed with any packing material, including small particle size (e.g., about 10 ?m) media, and very high plate numbers are generated. The bed length can be adjusted by controlling the amount of packing material used to prepare the column.

Abstract: Disclosed is an oxetane compound represented by the following formula (I), (II), (III), (IV) or (V):

Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.

Abstract: A taxane having the formula: wherein X3 is furyl, X5 is t-butoxycarbonyl, Bz is benzoyl, and Ac is acetyl.

Abstract: A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or derivative thereof, and Z is —O— or —NH—, respectively, Y is a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups; and R2 is —CH?CH(W), —CH(OH)CH(OH)W, or —C(O)H, where W can be H, a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups.

Abstract: Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2-furyl, 2-thienyl; R1 is t-butoxycarbonyl or benzoyl; R2 is hydroxy; R3 is hydrogen or, together with R2, it forms the residue of a cyclic carbonate of formula: II with the proviso that when R3 is hydrogen, R is different from phenyl.

Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: This invention relates to a synergistic therapeutic combination of anti-cancer compounds which comprises a) a taxane, and b) a substance that binds to the epidermal growth factor receptor (EGFR) and blocks the ability of epidermal growth factor (EGF) to intitiate receptor activities which results in tumor growth inhibition, and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use.

Abstract: Liquid crystal films with excellent heat resistance and mechanical strength are provided.

Abstract: A 1,2-dioxetane derivative of the formula (I): wherein Ar is an aryl group which may have an alkyl group, an aryl group, a halogen atom, an alkoxyl group, a carboxyl group, a formyl group, an alkyl ester, an aryl ester, an alkylketone, an arylketone or a hetero ring bonded thereto, X is a substituent capable of labeling an organic compound or a biological molecule, or an ester, Y is a hydrogen atom, an acyl group or a group of the formula —Si(R4R5R6) (wherein each of R4, R5 and R6 which are independent of one another, is an alkyl group or an aryl group), Z is an alkyl group, an aryl group, an oxygen atom, a sulfur atom, a carbonyl group, —(CO)—O—, —O—(CO)—, —NH—, —NH—CO—, —CO—NH—, —OSi(R7R8)— (wherein each of R7 and R8 which are independent of each other, is an alkyl group or aryl group) or a group of the formula —(R9R10)SiO— (wherein each of R9 and R10 which are independent of each other, is an alkyl group or an aryl group), each of R1 and R2 is an alkyl group or an aryl group, and R3 is a spacer.

Abstract: The invention relates to new reactive mesogenic azulene derivatives, their use as semiconductors or charge transport materials, in optical, electro-optical or electronic devices like for example liquid crystal displays, optical films, organic field effect transistors (FET or OFET) for thin film transistor liquid crystal displays and integrated circuit devices such as RFID tags, electroluminescent devices in flat panel displays, and in photovoltaic and sensor devices, and to a field effect transistor, light emitting device or ID tag comprising the reactive mesogenic azulenes.

Abstract: Methods for obtaining paclitaxel from plants containing paclitaxel are disclosed. Plant material is first obtained from plants containing paclitaxel. Paclitaxel is then extracted from the plant material. Subsequently, paclitaxel is separated from the paclitaxel extract using a series of column chromatography separation steps to obtain at least one fraction containing paclitaxel. The paclitaxel in a fraction that is obtained from the final chromatography step is crystallized. Using these methods, high purity paclitaxel may be efficiently obtained from plants containing paclitaxel.

Abstract: Compounds having the formula: are disclosed. M1 and M2 are the same or different and are transition metal atoms or ions; Z2 and Z3, independently, are the atoms necessary to complete a 3–12 membered heterocyclic ring; Z1 is an alkylene or arylene group; Q1 and Q2 are the same or different and are electron withdrawing groups; L1 and L3, taken together, represent —O—CR13—O—; L2 and L4, taken together, represent —O—CR14—O—; and R13 and R14 are the same or different and are selected from the group consisting of alkyl groups and aryl groups or R13 and R14 represent alkylene or arylene groups that are directly or indirectly bonded to one another. Methods for making such compounds are also disclosed, as are intermediates which can be used in their preparation. Also disclosed are methods for carrying out C—H insertion reactions using bis-transition metal catalysts, such as the above compounds. Procedures for preparing d-threo methylphenidate, tolterodine, CDP-840, nominfensine, and sertraline, are described.

Abstract: A method for obtaining a taxane by which a taxane is isolated from a growth medium, such as soil, in which a taxane-producing plant has grown.

Abstract: The present invention provides a compound represented by formula (1) defined in the specification. The invention further provides a liquid crystal composition comprising at least two compounds, which at least one compound out of them is the above compound. The invention still further provides a polymer obtained by polymerizing the above composition, and uses of the polymer such as a molded article having an optical anisotropy, an optical compensation element, a wavelength functional plate, an optical element, and a liquid crystal display element comprising the polymer.

Abstract: A chemiluminescent system for detecting the presence of influenza virus in a biological fluid sample is provided. An influenza diagnostic kit is provided which includes (1) a sampling device for obtaining the biological fluid from a subject, (2) a chemiluminescent substrate material which, in the presence of influenza virus in the biological sample, will generate a chemiluminescent product that will produce detectable light, and (3) a means for detecting any generated light. A liquid sample containing the biological fluid, and preferably a diluent, are contacted with the an absorbent material containing the chemiluminescent substrate material. The substrate responds to neuraminidase activity intrinsic to influenza A and influenza B virus particles, such that when the substrate is in contact with influenza virus, the substrate is cleaved to yield a chemiluminescent product that then decomposes to produce light which can then be detected.

Abstract: A process for the preparation of 14 beta-hydroxy-1,4-carbonate-deacetylbaccatin III and intermediates useful for the preparation of novel taxan derivatives with antitumor activity are disclosed.

Abstract: Seco-baccatin III derivatives of formula: wherein R, R1-R4, R1 R?, R11 R?, and R111 R?? are disclosed herein; pharmaceutical compositions comprising seco-baccatin III derivative; and methods for treating cancer, arthritis, and inhibiting angiogenesis in an animal comprising administrating to a patient in need thereof a therapeutically effective amount of a seco-baccatin III derivative are disclosed.