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WO/1997/016200A1 |
A biotransformation process for the production of hydroxylated derivatives of taxol and new derivatives of taxol and cephalomannine are described. A method for converting taxol to L-760,006 and L-760,007, and a method for converting ceph...
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WO/1997/015562A1 |
The present invention relates to new intermediaries for the hemisynthesis of taxanes and their preparation processes. It relates particularly to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine II...
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WO/1997/014954A1 |
Dioxetanes that can be triggered by bases are provided which can be used to detect bases in organic solvents, aqueous preparations and detect gaseous bases in the atmosphere. The dioxetanes can be used to detect the release of bases from...
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WO/1997/010234A1 |
Provided herein is a taxane having a hydrocarbon attached at the 2' and/or 7 positions, the hydrocarbon's alpha position being occupied by a "hydrolysis-promoting group" ("HPG"). Substitution of an HPG for the methylene unit ordinarly oc...
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WO/1997/009979A1 |
Taxanes containing electron-affinic radiosensitizing functional groups, their pharmaceutical preparations, and methods of making and using this new class of highly potent radiosensitizers of tumor cells.
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WO/1997/010233A1 |
The invention is in the field of biologically active compounds such as taxol-2'-adipate derivatives, derivatives of bergenin and erythromycin derivatives. Taxol-2'-adipate derivatives have anti-cancer activity analogous to taxol. Bergeni...
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WO/1997/007110A1 |
A process for the preparation of taxol and derivatives of taxol (I) is disclosed. The process involves reacting a 'beta'-alkoxycarbonylamino-phenylpropionic acid with a 13-hydroxy taxane to produce an ester of the taxane at C-13; and the...
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WO/1997/003061A1 |
A method for extracting and isolating 10-deacetylbaccatin III (tetraol) from yew leaves, comprising a first step of extracting yew leaves using a suitable protic solvent to give an aqueous extract, followed by a second step of extracting...
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WO/1997/003105A1 |
A method of producing cyclic oligomers of substituted oxiranes and oxetanes involves the slow addition to a solution of the ether in a relatively polar organic solvent such as dichloromethane or dichloroethane, of a stable protonic acid ...
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WO/1997/002236A1 |
Disclosed is a process for producing 'beta'-amino-'alpha'-hydroxycarboxylic acid derivatives of general formula (2R,3S)- or (2S,3R)-N-(X,Y)-3-amino-2-hydroxy-3-phenyl-propionic acid-Z of formula (I), e.g. of (2R,3S)-3-amino-2-hydroxy-3-p...
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WO/1997/000870A1 |
The invention refers to a process for the preparation of compounds of formula (I), wherein R1 is an aryl or heteroaryl group; R2 is hydrogen, arylcarbonyl, heteroarylcarbonyl or C1-C6 alkoxycarbonyl; R3 is hydrogen or acetyl; the process...
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WO/1996/040624A1 |
The invention relates to the semi-synthesis of taxol using a protected baccatin III backbone which is esterified with a suitably protected side chain acid to produce an intermediate that may thereafter be acylated and deprotected to prod...
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WO/1996/040666A1 |
A paclitaxel intermediate and a process of making the same via the condensation of a suitably protected side chain acid and a baccatin III derivative.
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WO/1996/040091A1 |
In accordance with the present invention, there are provided derivatives of chemotherapeutic agents (e.g., paclitaxel), which serve as bifunctional agents. Invention derivatives retain the antitumor activity of the parent compound, and, ...
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WO/1996/040667A1 |
A semi-synthesis of taxol using a protected baccatin III backbone which is esterified with a suitably protected side chain acid.
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WO/1996/038138A1 |
Novel taxoids are provided having enhanced water solubility and/or improved pharmacological properties as compared to paclitaxel. The subject taxoids comprise a functional group attached to a paclitaxel at the C-2' and/or C-7 position by...
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WO/1996/036622A1 |
The present invention relates to novel 10-deacetyl-14'beta'-hydroxybaccatine III derivatives. The novel derivatives, having cytotoxic and antitumour activity, are prepared from this synton after functionalization of the hydroxyls at 1-, ...
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WO/1996/034862A1 |
The present invention provides three basic routes for the total synthesis of taxol having the structure (I). The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermed...
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WO/1996/033998A1 |
Compounds represented by general formula (I) and having an antitumor effect and salts thereof: wherein R1 represents phenyl; R2 represents alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; R3 represents hydrogen, hydroxy, halogeno, alkoxy, ...
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WO/1996/034110A1 |
The present invention relates to a method for mass production of taxol by semi-continuous culture of Taxus genus plant with a high yield. According to the present invention, taxol can be prepared with a high yield, by employing semi-cont...
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WO/1996/032387A1 |
Novel taxoids of general formula (I), the preparation thereof, and pharmaceutical compositions containing same, are disclosed. In general formula (I), Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally...
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WO/1996/031493A1 |
Novel taxoids of general formula (I), wherein R is a substituted alkyl radical or an alkenyl, alkynyl, cycloalkyl, optionally substituted cycloalkenyl or phenyl radical, or an optionally aromatic 5- or 6-membered heterocyclic radical; an...
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WO/1996/030355A1 |
Novel taxoids of general formula (I), the preparation thereof, and pharmaceutical compositions containing same, are disclosed. In general formula (I), Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally...
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WO/1996/030356A1 |
Novel taxoids of general formula (I), the preparation thereof and pharmaceutical compositions containing them are described, wherein Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzo...
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WO/1996/029321A1 |
The present invention relates to novel derivatives of 10-deacetylbaccatine III and of 10-deacetyl-14'beta'-hydroxybaccatine III, having cytoxic and anti-tumoral activity. They are prepared starting from the so-called syntons or from othe...
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WO/1996/028435A1 |
An antitumor compound of formula (5), in which R = Ac or H, and R1 = R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R3 = H; R1 = R2 = R3 = H; R1 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R2 = R3 = H; R1 = R3 =...
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WO/1996/025408A1 |
An oxygen-containing heterocyclic derivative represented by general formula (I), a salt thereof, a solvate thereof or a hydrate thereof: wherein R1 represents hydrogen, A, B, etc., (wherein R8 represents C1-20 alkyl, aryl, etc); R2, R4 a...
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WO/1996/025510A1 |
Taxol, an antineoplastic drug, has shown cytotoxic activity against numerous malignant tumors including: breast cancer, colon cancer, ovarian cancer, and skin cancer. Taxol is found in many species of yew including: slow-growing Taxus br...
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WO/1996/023794A1 |
High molecular weight, water-soluble prodrugs of formula (I), wherein: D is a biologically active moiety; M is X or Q; X is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y'...
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WO/1996/023780A1 |
The invention relates to a process for converting Taxol A, B and C to Taxol primary amine which can then be easily and efficiently converted to Taxol A or docetaxel, thereby significantly increasing the yield of these products from bioma...
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WO/1996/023779A1 |
A novel taxol derivative having an antitumor effect and represented by formula (I), wherein R1 represents phenyl; R2 represents alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; R3 represents hydroxy, hydrogen or halogeno; R4 represents alk...
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WO/1996/022984A1 |
A method for preparing 4,10-diacetoxy-2'alpha'-benzoyloxy-5'beta',20-epoxy-1,7'beta
'-dihydroxy-9-oxo-tax-11-en-yl-13'alpha' (2R,3S)-3-benzoylamino-2-hydroxy-3-phenylpropionate trihydrate by crystallisation from a water/alcohol solution.
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WO/1996/021658A1 |
This invention provides a taxane derivative of formula (I), wherein a hydrophobic organic moiety is attached to a taxane. R and R1 is each independently H or a hydrophobic organic moiety, as long as at least one of R and R1 is not H. Att...
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WO/1996/021657A1 |
This application is directed to fluorinated oxetane monomers and methods for making the monomers. The mono-substituted fluorinated oxetane monomers having fluorinated alkoxymethylene side-chains are prepared in high yield by the reaction...
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WO/1996/014872A1 |
This invention provides inclusion complexes of Taxol {[2aR-[a'alpha',4'beta',4'alpha''beta',6'beta',9'alpha'('alp
ha'R*, 'beta'S*,) 11'alpha',12'alpha', 12a'alpha', 12b'alpha',]]-'beta'-(benzoylamino)-'alpha'-hydroxy-benzene-
propanoic a...
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WO/1996/014309A1 |
Taxane derivatives modified at 7-position of the taxane derivative skeleton (taxol numbering) of formula (I) wherein R1 is N3, CN, 1H-tetrazol-5-yl, or -NR7R8 and R2, R3, R4, R7 and R8 are organic residues, are endowed with antitumor act...
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WO/1996/014308A1 |
Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, Ra, Rb, Rc, R1, R2, R3 are appropriate organic residues can be antitumour agents.
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WO/1996/013495A1 |
This invention relates to a taxoid of formula (I), wherein R1 is a C3-C5 alkyl or alkenyl radical; R2 is a C3-C5 branched alkyl radical; R3 and R4 are independently selected from hydrogen and hydroxyl protecting groups including function...
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WO/1996/013494A1 |
Novel taxoids of general formulas (I) and (II), preparation thereof, and pharmaceutical compositions containing same. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy or alkoxyacetoxy and Rb is hydrogen, or Ra and Rb, tak...
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WO/1996/010060A1 |
The invention includes compositions of 1,2,2,3,3,4,4,4-octafluorobutane and bis(fluoromethyl) ether, 2,2,4,4-tetrafluorooxetane, 2,2,3,3-tetrafluorooxetane, 1-difluoromethoxy-1,1,2,2-tetrafluoroethane, 1-difluoromethoxy-1,2,2,2-tetrafluo...
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WO/1996/003395A1 |
Novel taxoids of general formula (I), wherein X is an oxygen or sulphur atom; Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl radical or a radical R2-O-CO- where R2 is an alkyl, ...
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WO/1996/003394A1 |
The present invention relates to novel derivatives obtained by oxidation and the stereospecific reduction of 10-deacetylbaccatine III, and successive esterification with a variously substituted isoserine chain to prepare taxol analogues....
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WO/1996/002527A1 |
The present invention relates to a highly selective method for the deacetylation and deacylation of taxol and taxanes compounds. Specifically, the present invention relates to a one step process wherein acyl groups located at the carbon ...
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WO/1996/001815A1 |
A method for preparing 4-acetoxy-2'alpha'-benzoyloxy-5'beta',20-epoxy-1,7'beta',10'
beta'-trihydroxy-9-oxo-tax-11-en-yl-13'alpha'(2R,3S)-3-tert-
butoxycarbonylamino-2-hydroxy-3-phenylpropionate trihydrate by crystallisation from a hydroa...
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WO/1996/000724A1 |
This invention provides 7-ether-taxol analogs of formula (I). The compounds of formula (I) are useful for the treatment of the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and maligna...
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WO/1996/000712A1 |
The present invention provides a process for the preparation of a compound of the formula (X) useful as precursor for the A-ring in taxanes wherein R', is an acyl R'' (a), in which R'' is linear, branched or cyclic alkyl group of 1 to 10...
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WO/1995/034613A1 |
A lubricating oil composition containing a compound represented by general formula (I) and having an excellent stability, wherein n represents an integer of 0 to 5; R1a represents CF2CF2H or H; and R2 to R7 represent each a C1-C100 aliph...
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WO/1995/033738A1 |
New taxoids having the general formula (I), preparation thereof and pharmaceutical compositions containing a product of general formula (I) wherein Z is a radical having general formula (II) which have remarkable antitumoral and antileuk...
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WO/1995/033740A1 |
A novel antitumor taxol derivative that is represented by general formula (I) has various substituents, and is modified with a carbon-carbon bond at the 10-position.
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WO/1995/033737A1 |
New taxoids having general formula (I), (II), preparation thereof and pharmaceutical compositions containing them. In the general formula (I), R is alkyl radical (1-6 carbon atoms), alkenyl (2-6 carbon atoms), alkynyl (2-6 carbon atoms),...
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