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WO/2001/097618A2 |
The present invention provides the combined use of acryloyl distamycin derivatives, in particular $g(a)-bromo- and -$g(a)-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, antimicrotubule agents an...
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WO/2001/098286A1 |
The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or release...
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WO2000066602A9 |
The present invention relates to derivatives of 3-deoxy desmycosin of formula (I), wherein, starting from triply protected desmycosin, there are performed an oxidation at C-3 in the first step and then, optionally, a hydrogenation of dou...
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WO/2001/094328A1 |
The present invention relates to isotopically labeled analogs of taxane molecules, which are synthetically formed to have incorporated therein at a selected position a stable isotope of an element existing at the selected position in the...
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WO/2001/092245A1 |
The invention provides novel paclitaxel derivatives obtained by effecting modifications at C¿2'?, C¿3'? and/or C¿7? positions of paclitaxel, said derivatives being useful in inhibiting the growth of cancer of lung, breast, ovary, cerv...
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WO/2001/082859A2 |
The inventive method consists in extracting an active ingredient from a natural product. Oleoresins of the Pinus sibrica and/or Pinus cembra and/or Abies and/or Larix variety, from which a fraction of lambdoidic-diterpen acids is extract...
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WO/2001/083560A1 |
An antibody of the invention interacts with human DR5 to produce agonistic or antagonistic effects downstream of the receptor including inhibition of cell proliferation and apoptosis. Nucleic acid sequences and amino acid sequences of an...
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WO/2001/077094A1 |
The present invention relates to a compound named Percyquinnin which is obtainable by cultivation of the fungus ST 001837 (DMS 13303), and to its pharmaceutically acceptable salts. The present invention further relates to a process for t...
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WO/2001/074799A1 |
A process for preparing compounds (I) by radical addition of 3-(allyloxy)methyl-3-alkyloxetanes (1) with RfI, in formula (A), R is alkyl having 1 to 3 carbon atoms; and Rf is linear or branched fluoroalkyl having 1 to 18 carbon atoms. Th...
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WO/2001/074800A1 |
3-Fluoroalkoxymethyl-3-alkyloxetanes useful as intermediates of various fluorine-containing functional materials can be prepared by addition reaction of a 3-alkyloxetanemethanol with a fluoroolefin in the presence of an alkali.
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WO/2001/070718A1 |
The present invention concerns novel 7-deoxy taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/2001/070717A1 |
Novel methods and synthetic intermediates to prepare baccatin III and 10-deacetylbaccatin from readily available 9-dihydro-13-acetylbaccatin III are described. Selective protection and deprotection of the C-7 hydroxyl functionality provi...
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WO/2001/068089A1 |
N-Deacetyl-thiocolchicine and 10-deacetyl-baccatine III derivatives of formula (I) wherein R and n have the meanings specified in the disclosure, are valuable antitumoral drugs.
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WO/2001/068624A1 |
The present invention relates to a process for producing 10-deacetyl baccatin III from an acidic solution containing a spectrum of taxanes, which comprises contacting the acidic solution with a hydrazine hydrate, thereby to convert into ...
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WO/2001/066535A1 |
A process for obtaining paclitaxel and other taxanes from a source containing taxanes. The process involves extracting taxane compounds from the source into an organic solvent and passing this composition through a distribution chromatog...
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WO/2001/062753A1 |
Methods for isolating taxol and derivatives thereof with high purity are described. The methods include a supercritical fluid and a cosolvent extraction step, a liquid-liquid separation step, and a column chromatography step. An apparatu...
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WO/2001/057028A1 |
Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10) and a range of C(2), C(9), C(14), and side chain substituents.
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WO/2001/057030A1 |
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.
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WO/2001/057027A1 |
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.
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WO/2001/057029A1 |
Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range C(2), C(9), C(14), and side chain substituents.
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WO/2001/056564A1 |
Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
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WO/2001/057032A1 |
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.
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WO/2001/057031A1 |
Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
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WO/2001/057033A1 |
Taxanes 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.
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WO/2001/056565A1 |
The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations. The invention claims compounds of formula (I) and the use of compounds of formula (I) or pharmaceutical salts thereo...
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WO/2001/057013A1 |
The present invention is directed to various formulations of taxanes having improved solubility as compared to paclitaxel, particularly formulations of such taxane derivatives for oral or parenteral administration to a patient.
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WO/2001/057014A2 |
The present invention relates to a novel process for producing a $g(d)-lactone of the formula (I) using an acyl halide of the formula (1) wherein R?1¿, R?2¿, R?3¿ and X are described herein, as well as novel intermediates. In particul...
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WO/2001/055126A2 |
Compounds of the formula of claim 1 are disclosed as well as a method of preparation.
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WO/2001/053282A1 |
Novel derivatives obtained by oxidation, stereospecific reduction and esterification of baccatine III and the use thereof as antitumor, antiangiogenetic and anti-arthrosis agents. The compounds of the invention have cytotoxicity comparab...
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WO/2001/051476A2 |
A high yield, economical process for purifying taxanes from yew biomass is disclosed. The process does not require initial liquid:liquid portioning of the crude extract to separate highly polar substances. The organic solvent extract of ...
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WO/2001/038318A1 |
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 bindin...
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WO/2001/034589A1 |
The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a p...
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WO/2001/032669A1 |
This invention relates to novel oxetanone derivative compounds and processes for producing such derivatives that are useful as lipase inhibitors. Further the invention relates to processes for producing salts and for producing pharmaceut...
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WO/2001/032616A2 |
This invention relates to novel oxetanone derivative compounds and processes for producing such derivatives that are useful as lipase inhibitors. Further the invention relates to processes for producing salts and for producing pharmaceut...
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WO/2001/032670A1 |
This invention relates to novel oxetanone derivative compounds and processes for producing such derivatives that are useful as lipase inhibitors. Further the invention relates to processes for producing salts and for producing pharmaceut...
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WO/2001/030770A1 |
The present invention relates to a stereoselective synthetic method of oxazoline derivative. More particularly, it relates to a synthetic method of oxazoline derivative having the structure of formula (I), wherein R represents phenyl, be...
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WO/2001/027115A1 |
Novel Taxol derivatives having various substituents as represented by general formula (I) and being usable as antitumor compounds which can be orally administered.
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WO/2001/025223A1 |
The invention provides a method of stabilizing a taxane in a dispersed system, which method comprises exposing the taxane to a molecule which improves physical stability of the taxane in the dispersed system. By improving physical stabil...
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WO/2001/024926A1 |
A method of synthesizing an olefin epoxidation catalyst comprises the step of treating a porous crystalline aluminosilicate material having an X-ray diffraction pattern including d-spacing maxima at 12.4±0.25, 6.9±0.15, 3.57±0.07 and ...
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WO/2001/019810A1 |
The present invention relates to water-soluble esters of cephalomannine with poly-amino-acid or the salts thereof, especially the esters with poly-Glu or the alkali metal or alkaline earth metal salts of them and the esters with poly-Asp...
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WO/2001/015675A2 |
The present invention is based on the finding that docetaxel is significantly more active against hepatocellular carcinoma cells than paclitaxel at concentrations of up to 1$g(m)M. It accordingly provides the use of docetaxel, or a hydra...
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WO/2001/010856A1 |
A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.
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WO/2001/005871A1 |
This invention is directed to mono- and bis-substituted oxetane monomers having fluorinated alkoxymethylene side chains, hydroxy-terminated prepolymers derived from these mono- and bis-substituted oxetane monomers and tetrahydrofuran (TH...
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WO/2001/002407A2 |
A novel taxane derivative with anticancer activity, a process for its preparation and a process for the preparation of 14-$g(b)-hydroxy-1,14-carbonate-baccatine III and V derivatives 13-substituted by an isoserine residue.
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WO/2000/078707A1 |
New C-2 hydroxyl protected-N-Acyl (2R,3S)-3-phenylisoserine activated esters and method of making the same which are useful in semi-synthesis of paclitaxel.
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WO/2000/078741A2 |
A process for the extraction and purification of Paclitaxel from a natural source of taxanes. This process comprises the following steps: a) extracting with an organic solvent, a raw material comprising Paclitaxel from said natural sourc...
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WO/2000/073293A1 |
A process for the synthesis of paclitaxel from 10-deacetylbaccatin-III which is protected at the 7-position with a dialkylalkoxysilyl protecting group having the formula -Si(R)¿2?(OR').
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WO/2000/069840A1 |
Novel reaction conditions for the cleavage of silyl ethers from silyl protected taxane precursors to afford paclitaxel and paclitaxel analogues in high yield and quality are described. Paclitaxel is prepared from a taxane precursor by tr...
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WO/2000/068290A2 |
Poly(3-cyclopropyl-3-hydroxypropionates) (I) which are useful for the preparation of vinylcyclopropane and cyclopropylacetylene are disclosed. Methods for the preparation of a variety of intermediates obtained from (I) such as 3-cyclopro...
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WO/2000/053592A1 |
Osteogenesis promoters containing taxoids represented by general formula (I) in amounts effective for osteogenesis: wherein X and Y are each independently hydroxyl or a group convertible into hydroxyl $i(in vivo); R?1¿ is alkyl, alkenyl...
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