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WO/2001/077135A1 |
The present invention relates to a process for preparing 6-methyl erythromycin A. The present invention, for the methylation reaction, forms nitrogen oxide only at 3'-dimethylamino group by a suitable oxidizing agent thereby resulting in...
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WO/2001/076602A1 |
Apomorphine derivative compounds; pharmaceutically active compositions of apomorphine derivative compounds; and the use of apomorphine derivative compounds in methods for treating sexual dysfunction or for enhancing apormorphine effectiv...
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WO/2001/072763A1 |
The invention concerns a method for preparing 9-deoxo-8a-aza-(8a-alkyl)-8a-homoerythromycin A and its 8a-alkyl derivatives from 9-deoxo-9(Z)-hydroxyiminoerythromycin A via a Beckmann stereospecific rearrangement in a reaction medium usin...
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WO/2001/070758A1 |
A process for producing purified erythromycin from which erythromycin F has been removed. The process comprises using a combination of (i) an organic solvent and (ii) water or an aqueous solution of an inorganic substance and/or an organ...
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WO/2001/068662A1 |
High purity clarithromycin of Form II crystals can be easily prepared in a high yield by a process comprising the steps of: protecting the 9-oxime hydroxy group of erythromycin A 9-oxime or a salt thereof with a tropyl group and the 2'- ...
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WO/2001/068867A1 |
The complete sequence of the gene cluster for the monensin type I polyketide synthase, from S. cinnamonensis, is provided. Thus variant polyketides containing monensin-derived elements can be genetically engineered. Furthermore there are...
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WO/2001/064224A1 |
The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methy-2',4'-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime('S-MOP oxime'), and for converting protected s...
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WO/2001/064701A1 |
A simple and easy process for preparing pharmacologically useful flavonoids exhibiting effects of inhibiting aldose reductase, extinguishing active oxygen, inhibiting carcinogenesis promotion, counteracting inflammation, and so on. Speci...
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WO/2001/064700A1 |
A compound JK represented by the following general formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R is hydrogen or -CH¿3?). The compound has an excellent antibacterial effect on drug-resistant bacteria such...
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WO/2001/063539A2 |
The invention relates to novel methods for using macrolide anti-infective agents. The macrolide anti-infective agents demonstrate antibacterial activity against multi-drug resistant strains of bacteria and, in particular, methicillin-res...
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WO/2001/060833A2 |
The present invention provides novel macrolide compounds of the formulas (I, II, III or IV) wherein: R is hydroxyl or methoxy; R?1¿ is selected from the group consisting of hydrogen, hydroxyl, halide, NH¿2?, OR?9¿, (a, b, c, and d) wh...
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WO/2001/060390A1 |
New toralactone of general formula [A] extracted from seed of cassiae obtusifollia L. and its derivative, wherein R?3¿ is H or acyl of C¿2?-C¿4?, R?1¿, R?2¿ is identity or difference, independently H, saccharide group, acyl of C¿2?...
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WO/2001/060832A2 |
The invention relates to a compound of formula (I) wherein R¿1? is a sugar; R¿2? is -CH¿2?-O-(R¿7?)m, R¿7? representing a sugar, or R¿2? is -COOH; R¿3? is an epoxide-comprising group, C¿1?-C¿6?-alkyl or C¿2?-C¿6?-alkenyl, unsu...
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WO/2001/059126A2 |
The invention provides a nucleic acid molecule comprising: a nucleotide sequence as shown in SEQ ID No. 35; wherein said sequence preferably encodes or is complementary to a sequence encoding a nystatin PKS enzyme or a part thereof. Also...
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WO/2001/054691A1 |
Nitrate salts of antimicrobial agents for the preparation of antimicrobial medicaments, specifically antiviral, antifungal and antibacterial medicaments.
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WO/2001/055158A1 |
Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by addin...
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WO/2001/051059A1 |
The present invention relates to processes for converting clarithromycin Form I to clarithromycin Form II, which include slurrying clarithromycin the Form I in water. The present invention also relates to processes for the preparation of...
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WO/2001/051061A1 |
The present invention provides a new class of polyene macrolide derivatives useful for treating or preventing fungal infections. The new polyene macrolide derivatives exhibit surprisingly superior antifungal activity and water solubility...
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WO/2001/049699A1 |
Compounds of the formula (1), (1'), (2), (2'), (3), (3') (101), (102), or (103) wherein R¿a? is substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); subs...
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WO/2001/049697A1 |
This invention relates to a method for preparing azithromycin dihydrate from crude azithromycin by the gradual crystallization of azithromycin from acetone by the addition of a minimal amount of water to effect crystal formation is discl...
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WO/2001/047507A2 |
This invention relates to combinations of an abl-, PDGF-Receptor-and/or Kit receptor-tyrosine kinase inhibitor with an organic compound capable of binding to $g(a)¿1?-acidic glycoprotein (AGP), as well as to pharmaceutical preparations ...
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WO/2001/046211A1 |
The invention concerns a method for preparing 9-deoxo-9(Z)-hydroxyiminoerythromycin A of formula (I) wherein: starting with 9-deoxo-9(E)-hydroxyiminoerythromycin A by reaction with a base in water or a dialkylketone type water/solvent mi...
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WO1999063937A9 |
Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more prot...
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WO/2001/044262A1 |
The present invention relates to processes for converting clarithromycin Form 0 to clarithromycin Form II, which include slurrying clarithromycin the Form 0 in water. The present invention also relates to processes for the preparation of...
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WO/2001/044186A1 |
Compounds of general formula (1), prodrugs of the same, or pharmaceutically acceptable salts of both are useful as preventive or therapeutic drugs for disease due to increased sodium/proton exchange: (1) wherein R is an optionally substi...
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WO/2001/041775A2 |
Methylated procyanidins which include procyanidin monomers and their oligomers are useful in the modulation of inflammatory pathways, in the maintenance of the vascular health of a mammal and as an antibacterial treatment. They can be in...
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WO/2001/040242A2 |
The present invention relates to a novel 6-O-methylerythromycin A crystal form, a process for preparing the crystal form, and methods for using the crystal form to prepare a 6-O-methylerythromycin A crystal form II.
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WO/2001/040241A2 |
The present invention relates to 6-O-alkyl-2-nor-2-substituted ketolide compound or a derivative thereof, a composition comprising the compound and a suitable carrier, a method of preparing the compound, and a method of treatment and pre...
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WO/2001/038339A1 |
Antimitotic terpenoid compounds including sarcodictyin A and diterpenes such as eleutherobin may be obtained from organisms of the order Gorgonacea. Methods of obtaining or preparing such compounds are provided, as are novel antimitotic ...
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WO/2001/038340A1 |
Clarithromycin can be easily prepared by reacting erythromycin A N-oxide with a methylating agent to obtain 6-O-methylerythromycin A N-oxide; and treating 6-O-methylerythromycin A N-oxide obtained above with a reducing agent in a high yi...
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WO/2001/036434A1 |
Subject of the invention is a process for the preparation of a compound of formula (I) in which R¿1?-R¿9? represent, independently of each other hydrogen a substituent; m is 0, 1 or 2; n is 0, 1, 2 or 3; and the bonds marked with A, B,...
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WO/2001/036437A1 |
The invention concerns a 4-methyl-2-oxo-2H-1-benzopyran-7-yl 5-thio-$g(b)-d-xylopyranoside compound of formula (I) wherein: R represents a C¿1?-C¿5? alkyl group, which is linear, branched or cyclized, a mono-unsaturated C¿2?-C¿3? alk...
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WO/2001/030794A1 |
The invention concerns novel enzymatic substrates of general formula (I) wherein: X represents a nitrogen atom or a carbon atom substituted with a phenyl group, said phenyl group being optionally substituted in meta or para position; Y a...
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WO/2001/025246A2 |
The current invention relates to the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including human) origin. In particular, this invention pr...
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WO/2001/022971A1 |
Sebum production inhibitors which contain as the active ingredient compounds having glucuronic acid derivatives and glucosamine derivatives in the structure as represented by general formula (1) or pharmacologically acceptable salts ther...
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WO/2001/021608A2 |
Described are novel flavonoids of formula (I) wherein: A and E form together a C-C or C=C bond, R1, R2, R3, and R4 are chosen from: H, OH, and from the substituents, O(CH¿2?)¿n?-aromatic group, n=0-8, O(CH¿2?)¿n? N(CH¿3?)¿q? with n...
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WO/2001/019839A1 |
This invention provides tissue selective estrogens of formula (I) having structure (I) wherein: R¿1? and R¿2? are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl, (1) or (2); X is hyd...
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WO/2001/019840A1 |
Macrolide compounds produced by culturing Saccharopolyspora species LW107129 (NRRL 30141) have insecticidal and acaricidal activity and are useful intermediates for preparing spinosyn analogs.
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WO/2001/016147A1 |
Glucopyranosyloxypyrazole derivatives represented by general formula (I), which have an effect of inhibiting human SGLT2 activity and are useful as preventives or remedies for diabetes, complication of diabetes or obesity, or pharmacolog...
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WO/2001/016148A1 |
20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-substituents are peperidino optionally substituted with one or two methyl gro...
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WO/2001/014396A1 |
The present invention relates to a use of a flavonoid derived from citrus peels for inhibiting a collagen-induced platelet aggregation in a mammal.
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WO/2001/014397A1 |
Compounds of formula (I), formula (II), formula (III), and formula (IV) or pharmaceutically acceptable salts or prodrugs thereof, are antibacterial agents. Compositions containing the compounds, processes for making the compounds, synthe...
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WO/2001/014393A2 |
The invention relates to spherical telithromycin clusters and to a method for the production thereof characterized in that a telithromycin crystal suspension is prepared, said crystals are coated with a telithromycin insoluble phase whic...
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WO/2001/011963A1 |
The invention provides single-dose oral formulations for controlling an ectoparasite infestation on a companion animal for a prolonged time, said formulations comprising a spinosyn component, or a physiologically acceptable derivative or...
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WO/2001/010879A1 |
Novel erythromycin derivatives of general formula (1), characterized by an acyl group introduced at the 3-position, a cyclic carbamate structure fused at the 11- and 12-positions, and an aryl-substituted five-membered heterocycle, one of...
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WO/2001/010878A1 |
Novel erythromycin derivatives of general formula (1), characterized by an acyl group introduced at the 3-position, a cyclic carbamate structure fused at the 11- and 12-positions, and a five-membered heterocycle on the 11-position substi...
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WO/2001/010881A1 |
Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compo...
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WO/2001/010880A1 |
Novel erythromycin derivatives of general formula (1), characterized by an acyl group introduced at the 3-position, a cyclic carbamate structure fused at the 11- and 12-positions, and a fused ring composed of a five-membered nitrogenous ...
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WO1999064049A9 |
This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligan...
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WO/2001/003681A2 |
The invention provides the use of flavin compounds or coumarins, as well as 2-(3',4'-dibenzyloxy)-4,5,6-trimethoxy acetophenone or 3',4'-dibenzyloxy-2-hydroxy-4,5,6-trimethoxy dibenzoylmethane or derivatives thereof, more particularly ci...
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