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WO/2005/030150A2 |
9, 10-&agr ,&agr -OH taxane compounds and a process for their production.
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WO/2005/028462A1 |
The invention relates to dimethoxy docetaxel acetone solvate or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propio
nate of 4-acetoxy-2$g(a)-benzoyloxy-5?,20-epoxy-1-hydroxy-7$g(b),10$
g(b)-dimethoxy-9-oxo-tax-11-ene-13$g(a)-yle...
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WO/2005/026140A1 |
The present invention relates to processes for preparing crystalline forms of orlistat, which is tetrahydrolipstatin. More particularly, it relates to processes for preparing crystalline forms of orlistat, referred to as 'Form I' and 'Fo...
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WO/2005/016904A1 |
A process is provided for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs which includes the steps of converting paclitaxel into a C-7 acylprotected paclitaxel employing an electrophilic protecting group, such as benzoyloxyca...
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WO/2005/016340A1 |
The invention relates to a method of treating with furanone derivatives and the pharmaceutically acceptable salts thereof, one or more conditions of the skin, in particular regulating skin condition, regulating signs of skin aging, treat...
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WO/2005/007639A1 |
A process for obtaining substantially pure tetrahydrolipstatin (Orlistat) by a) extraction of a water miscible layer containing lipstatin with a water immiscible solvent, b) concentration of the water immiscible layer, c) extraction of t...
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WO/2005/005404A1 |
The invention provides cyclic fluorine compounds represented by the general formula (1): (1) (wherein R1 is halogeno; and R2 and R3 are each hydrogen or a hydrocarbon group which is a straight-chain, branched, or cyclic C1-25 hydrocarbon...
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WO/2005/005403A2 |
The present invention relates to a process for the preparation of diastereomerically and enantiomerically pure oxetan-2-ones. The present invention also relates to a process for the preparation of ester derivatives of oxetan-2-ones. The ...
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WO/2004/106314A1 |
A process for efficiently and easily producing an oxetane ring-containing biphenyl compound represented by the following general formula (2) through a single reaction step. It comprises reacting a 3-hydroxymethyloxetane compound represen...
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WO/2004/101541A1 |
These compounds contain an oxetane functionality and a styrenic functionality. The oxetane functionality is homopolymerizable in reactions that undergo cationic or anionic ring opening, and the styrenic is polymerizable with compounds su...
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WO/2004/101542A1 |
These compounds contain an oxetane functionality and a cinnamyl functionality. The oxetane functionality is homopolymerizable in reactions that can undergo cationic or anionic ring opening, and the cinnamyl functionality is polymerizable...
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WO/2004/099167A1 |
The present invention relates to a process for the preparation of docetaxel trihydrate, characterized in that anhydrous docetaxel is crystallized from a mixture of water and acetone. The procedure is simplified, avoiding the product to e...
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WO/2004/096786A1 |
A novel fluorinated cyclic compound which has an oxacyclopentane or oxacyclobutane structure derived from a norbornadiene compound and hexafluoroacetone and which may be represented by the following formula (1) or (2); a fluoropolymer ob...
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WO/2004/092151A1 |
The invention relates to a method for production of 4,10β-diacetoxy-2&agr -benzoyloxy-5β,20-epoxy-1,13&agr -dihydroxy-9-oxo-19-norcyclopropa[g]tax-11-ene from 4-acetoxy-2&agr -benzoyloxy-5β,20- epoxy-1,13&agr -dihydroxy-9-oxo-7β-trif...
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WO/2004/089923A1 |
The present invention pertains to a process for the carbonylation of an epoxide by reacting it with carbon monoxide in the presence of a catalyst system containing two components, wherein the first component is a source of one or more me...
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WO/2004/083176A2 |
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 c...
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WO/2004/080987A1 |
It is intended to provide an industrially advantageous process for producing an oxetane compound whereby a 3-halo-1-propanol represented by the following general formula (1) can be cyclized by eliminating a hydrogen halide at a high yiel...
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WO/2004/076435A1 |
Disclosed is a process for the extraction and purification of Paclitaxel from a natural source of taxanes containing Paclitaxel, which comprises the steps of: a) washing with deionized or pure water, a raw material comprising Paclitaxel,...
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WO/2004/074810A2 |
Methods and compound useful for detecting a source of hydrogen peroxide are disclosed wherein a signalling compound of the formula (I) is reacted with peroxide. Sig is a non-polymeric organic group, B is a boron atom, and each R is indep...
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WO/2004/068930A2 |
This invention relates to methods and compositions for preparing compounds using a benzoylating agent essentially free of ring chlorination. In one alternative embodiment, the present invention relates to methods and compositions for pre...
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WO/2004/065346A1 |
Processes for the production of compounds (IV) and (VIII) and (-)-tetrahydrolipstatin (XI), characterized by subjecting a compound (III) to diastereo-selective reduction to obtain a compound (IV), subjecting the compound (IV) to hexenyla...
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WO/2004/063211A1 |
The invention relates to new carbohydrate derivatives of paclitaxel and docetaxel with increased solubility in water as compared to the parent compounds, paclitaxel and docetaxel. These derivatives are produced from naturally occurring p...
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WO/2004/060626A1 |
A process of making Yew pellets from Yew tree material is disclosed herein. The process comprising the steps of (i) adding from about 1% to about 20% w/w water to the Yew tree material; and (ii) compressing the Yew tree material in a die...
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WO/2004/056790A1 |
The method for production of the semi-finished products useful in synthesis of Paclitaxel with the generalized formula (2), characterized in that phenyl isoserine derivatives, or mixtures of their epimerides with various configurations o...
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WO/2004/041161A2 |
The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine...
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WO/2004/037211A2 |
This invention relates to compounds that are metabolites of 3'-tert-butyl-3'-N-tert-butyloxycarbonyl-4-deacetyl -3'-dephenyl-3'-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel. The compounds of the invention are useful as therapeutic agents.
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WO/2004/033442A2 |
Disclosed are compounds of formula having utility as intermediates in the preparation of paclitaxel, taxotere and analogs thereof, and intermediates thereof.
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WO/2004/026230A2 |
Methods of preparing amino acid-substituted taxanes such as: (4 of Fig. 1) using selected blocked amino acids are disclosed. After coupling of the blocked amino acid to the taxane, deprotection is carried out with about an equimolar amou...
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WO/2004/024706A2 |
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 formu...
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WO2002083067A9 |
A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically do...
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WO/2004/014960A2 |
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, othe...
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WO/2004/013096A2 |
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 a...
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WO/2004/013093A2 |
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 ce...
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WO/2004/012860A1 |
The invention relates to the production of lactones by means of the catalytic carbonylation of oxiranes. According to the invention, the catalyst used is a catalyst system consisting of a) at least one cobalt compound as component A, and...
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WO/2004/007473A1 |
A process for making paclitaxel comprises: (a) acetylating 10-deacetyl baccatin-III at the C-10 position in the presence of a tertiary amine base to give baccatin-III; (b) protecting baccatin-III at the C-7 position by reacting baccatin-...
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WO/2004/003102A2 |
The invention relates to new polymerizable, luminescent compounds of formula I wherein R1, R2, Q and L1 have the meanings given in claim 1. Furthermore the invention relates to polymerizable mixtures containing compounds according to the...
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WO/2004/003212A1 |
The present invention provides a novel method for producing lipstatin, by solid substrate fermentation by culturing microorganisms.
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WO/2004/000922A1 |
A phosphate ester composition of-low acidity achieved by treating the phosphate ester of high acidity with an oxetane compound. The phosphate ester can be represented by the formula (I), where Ar is an aryl or alkaryl group, R is an aryl...
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WO/2003/097625A1 |
A cytotoxic agent comprising one or more polyethylene glycol-containing taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more polyethylen...
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WO/2003/097566A1 |
Disclosed is a method for producing dialkyl diketenes by reacting long-chain fatty acid chlorides with tertiary amines without using any solvent. The transformation of the initial substances is carried out in the presence of a catalyst d...
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WO/2003/087077A1 |
A process for the preparation of N-debenzoylpaclitaxel (I) through esterification of 7-protected baccatin III with a carboxylic acid reactive derivative of general formula (II), and elimination of the ester-protecting groups in acid cond...
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WO/2003/087079A1 |
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.
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WO/2003/086394A1 |
The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containin...
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WO/2003/087078A1 |
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 inv...
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WO/2003/080587A1 |
There are provided stable labelled taxanes, characterized in that the isotopes are present in the benzoyloxy group at the C-2 position. More particularly, one or more of the hydrogen or carbon atoms of the benzoyl residue at the C-2 posi...
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WO/2003/064403A1 |
Furanone derivatives and the pharmaceutically acceptable salts thereof have cytoprotective activity and protective activity for neuroinflammation, and neurodegenerative disorders&semi they are useful in the treatment of stroke, cerebral ...
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WO/2003/064423A1 |
The present invention refers to chemical compounds of formula (I): (Formula I)&semi as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R4 have the significance given in claim 1. They can be used in t...
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WO/2003/057250A1 |
The invention relates to a therapeutic system comprising (i) a radiolabelled antibody, which binds selectively to polymorphic epithelial mucin (PEM) such as the monoclonal antibody HMFG−1, and (ii) a chemotherapeutic agent, such as Tax...
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WO/2003/057685A1 |
The present invention provides compounds having formula (I) (and pharmaceutically acceptable derivatives thereof): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wh...
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WO/2003/057683A1 |
Alpha-methylenelactones are produced from butyrolactone and valerolactone by the addition of formaldehyde in a supercritical fluid in the presence of a catalyst and a phase transfer agent.
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