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WO/2013/092941A1 |
Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds f...
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WO/2013/088335A1 |
The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β
-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbon
ylamino-2-hydroxy...
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WO/2013/090276A1 |
The present invention describes metal salen complexes having dianionic counterions. Such complexes can be readily precipitated and provide an economical method for the purification and isolation of the complexes, and are useful to prepar...
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WO/2013/080217A2 |
The present invention discloses Crystalline Forms of 4-acetoxy-2α-benzoyIoxy- 5β-20-epoxy-1-hydoxy-7β, 10β-dimethoxy-9-oxotan-11-en-13α-y1(2R,3S)-3-tert- butoxycarbony lamino-2-hydoxy-3-phenylpropionate, i.e Cabazitaxel, methods for...
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WO/2013/063894A1 |
The present invention belongs to the technical field of inorganic chemical synthesis, and relates to a method for modifying titanium silicon molecular sieves. The method is characterized in firstly pre-treating TS-1, then modifying the p...
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WO/2013/064538A1 |
The invention provides compounds of the formula (I): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally subs...
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WO/2013/063893A1 |
The present invention relates to the technical field of inorganic chemical synthesis, and relates to a process for modifying a titanium silicalite molecular sieve. The process is characterized by firstly pre-treating TS-1; then modifying...
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WO/2013/065070A1 |
An Amorphous Form of Cabazitaxel is disclosed. It is preferably characterized by an X-ray powder diffraction (XRD) pattern as depicted in Fig-1. It is prepared by (a) preparing a solution of Cabazitaxel in a suitable solvent and mixture ...
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WO/2013/059651A1 |
A compound having the formula (I) wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl g...
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WO/2013/056662A1 |
Provided is a novel taxane isoserine ester and a preparation method therefor, and the use of said novel taxane isoserine ester to prepare the anti-neoplastic drugs cabazitaxel, docetaxel and paclitaxel.
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WO/2013/057260A1 |
The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.
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WO/2013/054204A2 |
A novel process of making 7,10-dialkyl-10-DAB of formula (I) which is useful as a key intermediate for the preparation of cabazitaxel, comprises selective elaboration of positions 7 and 10 of 10-deacetylbaccatin III.
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WO/2013/034979A2 |
, The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.
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WO/2013/029723A1 |
The present invention provides novel photoactivatable paclitaxel derivatives wherein the C2 and C7 positions of the paclitaxel molecule are substituted with a photocleavable moiety such as a chromophore. Typically, the chromophore is sel...
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WO/2013/022960A1 |
Pharmaceutical formulations comprising cabazitaxel,, solubilizer, tocopherol polyethylene glycol succinate (TPGSF), one or more hydrotropes, optionally one or more agents having a pKa of about 3 to about.6, and optionally one or more ant...
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WO/2013/013504A1 |
The invention belongs to the medicinal technical field, and in particular relates to a tigecycline derivative of general formula (I), a pharmaceutically acceptable salt, precursor drug, solvate or isomer thereof, wherein R2a, R2b, R3, R4...
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WO/2013/005621A1 |
Provided is a palladium complex having high heat resistance and a high activity on a transvinylation reaction. This palladium complex is represented by formula (1). L1Pd(CH2COOR1)X (1) [In formula (1), L1 represents a bidentate ligand ha...
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WO/2013/000275A1 |
Disclosed are compounds as shown as general formula (I), derivatives and uses thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c and X have the definition as same as the description.
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WO/2012/172473A1 |
Compounds of the formula (I) wherein One of A1 and A2 is N-CH3 and the other is CH; R1 is C1-C6alkyl, C1-C6haloalkyl, C3-C6cycloalkyl or oxetan-3-yl, wherein C3-C6cycloalkyl is optionally substituted with one, two or three fluoro or with...
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WO/2012/169555A1 |
In order to manufacture an intermediate that makes it possible to obtain a cyclic alcohol compound stereoselectively, the method for manufacturing an oxetane compound according to the invention reacts a compound expressed by formula (I) ...
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WO/2012/160568A1 |
A crystalline form of docetaxel trihydrate designated as Form-VK and process for preparation thereof are provided. A substantially pure trihydrate crystalline product obtained by the process is also provided. The crystalline product of t...
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WO/2012/145361A1 |
The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical a...
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WO/2012/142117A1 |
The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention ...
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WO/2012/140300A1 |
The invention relates to compounds that are inhibitors of the enzyme carnitine palmitoyltransferase I (CPT I), to compounds that are inhibitors of gastric and/or pancreatic lipase, to the therapeutic uses of same, and to compositions and...
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WO/2012/133861A1 |
An amide compound represented by the formula (I): [wherein, R1, R2, R3, R4, R5, R6, R7, R8, X, W, r, n and Y are as defined in the description] has an excellent control effect on harmful arthropods.
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WO/2012/131698A1 |
Disclosed is a process of preparation of (2R,3S)-N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(P)-20-epoxy-l,2(a), 4,7(P), 10(β), 13(a)-hexa hydroxyl tax-l l-en-9-one 4-acetate 2-benzoate (docetaxel) and its trihydrat...
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WO/2012/119941A1 |
The invention relates to compounds of Formula (II) and their use in theraphy as peptidase inhibitors.
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WO/2012/116520A1 |
A method for preparing orlistat comprises following steps: (1) a reversal phase silica gel or a polymer resin is used as the filler for DAC preparative column, then an organic solvent and the filler are evenly mixed by stirring to obtain...
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WO/2012/115402A2 |
The present invention relates to a novel anhydrous crystalline form of docetaxel. The novel anhydrous crystalline form of docetaxel according to the present invention is significant since it solves drawbacks the prior art such as stabili...
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WO/2012/070015A9 |
The present invention relates to compounds which are inhibitors of the activity of Complex III of the mitochondrial electron transport chain and pharmaceutical compositions comprising said compounds alone or in combination with other act...
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WO/2012/089601A1 |
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
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WO/2012/085785A1 |
The present application relates to the pharmaceutical field, especially the field of combination and pharmaceutical compositions that comprise a lipase inhibitor and a phytoalexin and pharmaceutically acceptable vehicles or excipients; t...
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WO/2012/088433A1 |
The invention relates to (among other things) deuterated and/or fluorinated docetaxel and cabazitaxel and derivatives thereof, as well as compositions comprising each of the foregoing.
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WO/2012/088391A1 |
The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-pept...
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WO/2012/070437A1 |
[Problem] To provide a practical production method by which an optically active fluorine-containing oxeten, which can be an important intermediate for pharmaceuticals and agrochemicals, is able to be stably isolated. [Solution] This meth...
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WO/2012/029942A1 |
Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A represents a C6-10 arylene group or the like; R1a, R1b and R1c each independently represents a hydrogen atom, a halogen ...
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WO/2012/010296A1 |
The invention relates to a method for the production of L-carnitine, wherein a chiral β-lactone carnitine precursor is obtained by a [2+2] cycloaddition of ketene with an aldehyde X-CH2-CHO, wherein X is selected from CI, Br, I and trim...
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WO/2012/010297A1 |
The invention relates to a method for the production of L-carnitine, wherein a β- lactone, which is a 4-(halomethyl)oxetane-2-one, is converted into carnitine with trimethylamine (TMA), wherein the β-lactone is not subjected to a basic...
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WO/2012/006351A1 |
Methods for generating a chemiluminescent enzyme substrate in situ, in aqueous or other assay conditions. Also disclosed are methods to use the substrates to generate light, detect and/or quantify enzymes, antigens, and/or nucleic acids....
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WO/2012/004270A1 |
The invention relates to spirocyclically substituted 1,3-propane dioxide derivatives and to their physiologically compatible salts. The invention relates to compounds of formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, A and X have ...
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WO/2012/002140A1 |
The disclosed polymerizable liquid crystal compound is represented by General Formula (I). A1-A3 represent 1,4-phenylene groups, naphthalene-2,6-diyl groups, or alicyclic groups represented by General Formula (II) and at least one of A1-...
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WO/2011/147330A1 |
The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as showed by formula I. In detail, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a co...
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WO/2011/134067A1 |
There is provided novel amino acid molecules and processes for their preparation. There is also provided novel amino acid molecules and their use in processes for preparing the compounds that are useful for the synthesis of paclitaxel, a...
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WO/2011/132712A1 |
Provided is a novel compound that is useful as a medical drug in that said compound displays strong antimicrobial activity against gram-negative bacteria such as Pseudomonas aeruginosa and drug-resistant strains thereof, on the basis of ...
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WO/2011/124031A1 |
Conjugates of Paclitaxel or docetaxel and octreotide or Tyr3-octreotide and preparation methods thereof are provided. The conjugates have the activity of treating cancer, favorable cell-selectivity and water-solubility. Thus they are use...
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WO/2011/124578A1 |
The present invention relates to a method for preparing a lactone. The invention relates in particular to the preparation of butyrolactone, valerolactone and caprolactone. The method for preparing a lactone according to the invention is ...
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WO/2011/118672A1 |
Disclosed is a pharmaceutical product, particularly a pharmaceutical composition having a plasma kallikrein inhibition activity and is useful as a prophylactic or therapeutic agent for edemas (particularly hereditary vascular edema and c...
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WO/2011/100608A1 |
The patent application relates to a method of producing a monomer component from a genetically modified polyhydroxyalkanoate (PHA) biomass, wherein the biomass is heated in the presence of a catalyst to release a monomer component from t...
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WO/2011/087841A1 |
An oxolanyl compound-containing composition comprising specified amounts of the meso-isomer of one or more of the oxolanyl compounds of specified structure is provided. Also provided are methods for the use of such compositions as vinyl ...
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WO/2011/081373A2 |
A method for preparing highly pure anhydrous crystalline docetaxel is provided. The method for preparing highly pure anhydrous crystalline docetaxel enables preparation of anhydrous crystalline docetaxel that has purity of 99.5% or more,...
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