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WO/1998/050377A1 |
The invention relates to 2-benzoyl-cyclohexane-1,3 diones of formula (I) wherein the substituents have the following meanings: R?1�, R?2� stands for hydrogen, mercapto, nitro, halogen, cyano, rhodano, C�1?-C�6? alkyl, C�1?-C�...
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WO/1998/050379A1 |
4-benzoyl-pyrazoles having the formula (I) are disclosed, in which the substituents have the following meanings: R?1�, R?2� stand for hydrogen, mercapto, nitro, halogen, cyano, rhodano, C�1?-C�6?-alkyl, halogenated C�1?-C�6?-...
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WO/1998/047360A1 |
The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/1998/043946A1 |
Processes for preparing compounds of the formula (I) are described: P?1�OOC-CH(OH)-CHR?1�-CONH-Z wherein P?1� is hydrogen or a protecting group, Z is a group -CHR?2�COOP?2� or -CHR?2�CONR?3�R?4� wherein P?2� is hydrogen...
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WO/1998/038862A1 |
The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/1998/037765A1 |
The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/1998/033788A1 |
A compound of formula (I), wherein W is -NHOH or -OH, R�1? is either free or protected hydroxymethyl or mercaptomethyl or derivatives thereof, R�2? is free or protected hydroxy, R�3? and R�4? is an organic group, R�5? is hydrog...
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WO/1998/032718A1 |
The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and...
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WO/1998/030553A1 |
The present invention is directed to novel taxoids possessing strong reversing activities for drug-resistance associated with anti-cancer agents, the preparation of these reversal agents and pharmaceutical compositions thereof. The new t...
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WO/1998/028288A1 |
The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/1998/024427A2 |
The present invention provides methods for treating or preventing inflammatory diseases such as psoriasis or multiple sclerosis, comprising the step of delivering to the site of inflammation an anti-microtubule agent, or analogue or deri...
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WO/1998/022451A1 |
Substituted taxol derivatives of general formula (I) having an antitumor activity, wherein R?6� is optionally substituted alkyl, alkenyl or alkynyl; and R?5� is methyl, or together with R?4� forms a three-membered ring, provided th...
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WO/1998/019989A1 |
Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided as well as synthetic processes and intermediates used in their preparation. Dioxetanes further substituted ...
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WO/1998/017656A1 |
The present invention relates to a new taxane having the structure as in Formula (I), and its analogues as depicted in Formula (II) and Formula (III). The invention includes novel semi-synthetic and isolation methods for the preparation ...
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WO/1998/014187A1 |
The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/1998/013359A1 |
This invention concerns ultramicroemulsions of spontaneously dispersible concentrate with new esters of baccatin-III and 14-OH-10-deacetylbaccatin-III, the taxane esters themselves , processes for its production and for its processing in...
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WO/1998/013360A1 |
A method for producing paclitaxel is accomplished by first esterifying C-7-CBZ baccatin III with a C3'-N-CBZ-C2'-O-protected (2R, 3S)-3-phenylisoserine side chain to form a first intermediate. Next, the carbobenzyloxy groups at C-7 and a...
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WO/1998/008833A1 |
This invention provides a novel series of taxane derivatives which are characterized by the C3' nitrogen bearing one or two sulfur substituents. The new derivatives are antitumor agents useful in the treatment of such cancers as ovarian,...
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WO/1998/008832A1 |
The present invention relates to a process for preparing paclitaxel represented by formula (1) characterized in that: (a) an oxazolidine derivative represented by formula (2) or its salt in which X represents halogen, is coupled with a 7...
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WO/1998/007712A1 |
This invention relates to an improved method for isolating taxanes by using a preparative scale technique amenable to commercial production. This method provides high yields of known taxanes in addition to new taxanes.
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WO/1998/007713A1 |
The present invention is directed to compositions of formula (I) wherein D is a residue of biologically active moiety; X is an electron withdrawing group; Y and Y' are independently O or S; $i((n)) is zero (0) or a positive integer, pref...
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WO/1998/004539A1 |
Oxygenic heterocyclic derivatives of general formula (I), salts thereof, and solvates or hydrates of those [wherein R?1� is formula (II) (wherein R?4� is C�11?-C�20? alkyl or the like) or the like; R?2� is C�1?-C�10? alkyl ...
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WO/1998/002427A1 |
A method of acylating 10-deacetylbaccatin III at the C-10 position over the C-7 hydroxy position thereof to produce baccatin III is accomplished first by dissolving 10-deacetylbaccatin III in an anhydrous ether solvent, such as tetrahydr...
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WO/1998/002426A1 |
Taxane derivatives of general formula (1) and drugs containing the same wherein at least either of X and Y is -CO-A-B (wherein A is a single bond, alkylenecarbonyl or the like, and B is optionally substituted piperidono or the like); and...
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WO/1998/001130A1 |
Remedies for ischemic disease which contain as the active ingredient oxygen-containing heterocyclic derivatives represented by general formula (I), wherein R?1� represents (a), (b) or (c), (whereing R?4� represents alkyl, aryl or cyc...
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WO/1998/001435A1 |
The invention discloses a method for the selective monoacylation of hydroxy taxanes using a methylene iminium salt.
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WO/1997/046232A1 |
The present invention concerns novel paclitaxels derivatives, their use as antitumor agents, and pharmaceutical formulations.
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WO/1997/044336A1 |
The invention provides taxanes that are conjugates of cis-docosahexaenoic acid and paclitaxel. The conjugates are useful in treating cancer.
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WO/1997/042948A1 |
The present invention concerns the novel compound 7-O-methoxymethyl paclitaxel, its use as an antitumor agent and pharmaceutical compositions containing the novel compound.
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WO/1997/042181A1 |
1-Deoxybaccatin III, 1-deoxytaxol and 1-deoxy taxol analogs and method for the preparation thereof.
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WO/1997/042167A1 |
The present invention includes processes to prepare commercially important taxols (X) from substituted amino-3-phenyl (2R, 3S) isoserinates (II). In addition processes to prepare the substituted amino-3-phenyl (2R, 3S) insoserinates (II)...
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WO/1997/034866A1 |
A method of producing docetaxel comprises the esterification of C7, C10 di-CBZ 10-deacetyl baccatin III and an N-CBZ C2'-protected 3-phenyl isoserine side chain wherein C2' is protected by a hydrogenatable benzyl-type protecting group. T...
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WO/1997/032869A1 |
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/1997/032578A1 |
This invention relates to a taxoid of formula (I), wherein R1 is a C3-C5 alkyl or alkenyl or trifluoromethyl radical; R2 is a C3-C5 branched alkyl radical; R3 and R4 are independently selected from hydrogen and hydroxyl protecting groups...
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WO/1997/031911A1 |
C7, C10 di-CBZ 10-deacetyl Baccatin III of formula (1) provides an intermediate for the production of docetaxel. A method of producing this C7, C10 di-CBZ 10-deacetyl Baccatin III is provided. Here, 10-deacetyl Baccatin III is acylated w...
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WO/1997/031073A1 |
The invention pertains to a coating composition comprising a first compound comprising at least one bicyclo- or spiro-orthoester group and a second compound comprising at least two hydroxyl-reactive groups. The invention also comprises a...
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WO/1997/030352A1 |
The present invention provides new sources of taxanes and other metabolites from members of the order Coniferales that are not in the genus Taxus.
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WO/1997/029098A1 |
The present invention provides novel paclitaxel analogs, specifically 2", 3" side-chain halogenated cephalomannines, which show strong in vitro and in vivo paclitaxel-like efficacy in a variety of tumors.
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WO/1997/028156A1 |
There are described taxanes of general formula (I), wherein Sk may be (i), R1 may be hydrogen or C1-C10 acyl, R2 may be 'alpha'-OH or 'beta'-OH, R3 may be C1-C10 alkyl, X-substituted phenyl, C1-C10 alkoxy, X may be hydrogen, halogen, -N3...
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WO/1997/024345A1 |
This invention concerns a method for selective protection of 7-hydroxyl baccatin derivatives using substituted alkoxycarbonyl groups more encumbered than trichloroethoxycarbonyl, the intermediates obtained, and their use in the preparati...
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WO/1997/023472A1 |
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/1997/023473A1 |
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/1997/021695A1 |
A 4,10'beta'-diacetoxy-2'alpha'-benzoyloxy-5'beta',20-epoxy-1-
hydroxy-9-oxo-19-nor-cyclopropa[g]tax-11-ene-13'alpha'-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropion
ate dihydrate, and the preparation thereof by crystalli...
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WO/1997/021801A2 |
A process for producing phytochemicals from plant cell cultures is provided. That process includes the step of culturing plant cells that produce a particular phytochemical in a multi-phase culture medium that includes an aqueous phase a...
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WO/1997/021696A1 |
A novel process for extraction, isolation and separation of taxanes, particularly paclitaxel, from natural sources such as bark, needles and twigs from Taxus species, tissue cultures, and fungi is described, wherein the taxanes are separ...
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WO/1997/019938A1 |
Intensively fluorescent derivatives have been synthesized from a substance used at present as anticancer (chemotherapy) agent, against ovarian and mammal tumors, and other tumors. Said derivatives enable to visualize the cellular target ...
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WO/1997/019050A1 |
Compounds of formula (I) wherein R1, R2, R3, R4, X are as defined in the specification and are prepared by elimination of one of the groups X1 and X2 from a compound of formula (II) wherein X1 and X2 each independently represent a carbox...
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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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