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WO/1995/012593A1 |
A novel 5-0-pyrimidyl-2,3-dideoxy-1-thio-D-furanoside derivative represented by general formula (I) or an L-isomer thereof, wherein X represents hydrogen, fluorine or azide group; R1 represents C1-C4 alkyl; R2 represents hydrogen, methyl...
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WO/1995/010525A1 |
There is disclosed a novel form of avermectin compounds wherein the avermectin compounds are crystallized as alcohol solvates to greatly enhance stability of the avermectin drug during long-term storage. The avermectin compounds have uti...
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WO/1995/009863A1 |
Intermediates and a process for preparing doramectin, the compound of formula (I), semisynthetically from by-product in the fermentation procedure which also yields the compound of formula (I). The intermediates prepared by the process o...
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WO/1995/009601A1 |
This invention relates to methods for treatment of adult periodontitis in a human or other animal subject, comprising administering to the subject having such disease a safe and effective amount of azithromycin. This invention also relat...
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WO/1995/008918A1 |
The present invention provides a method of preparing an improved antifungal composition containing an antifungal compound of the polyene type such as natamycin wherein the antifungal compound is incorporated into the composition in a for...
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WO/1995/007914A1 |
The present invention relates to novel amino glycoside salts of sucrose-octa-O-sulfonic acid having the general formula (I): ([sucrose-octa-O-sulfonic acid8-]-[R-(NH3+)x]y-Mzn+), wherein (x . y) + (z . n) = 8, x . y N|[4 x . y 8], N is t...
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WO/1995/006057A1 |
A novel galactosylmoranoline derivative represented by general formula [I], which is an intermediate for a sialyl-Lewis sugar chain derivative useful as a medicine, wherein R1 represents C1-C20 alkyl, C10 or lower alkenyl, C10 or lower a...
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WO/1995/005390A1 |
The most thermodynamically stable crystalline form of the benzoic acid salt of 4"-deoxy-4"-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.
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WO/1995/004746A1 |
Antiparasitic avermectin derivatives of formula (I), where the broken line represents an optional bond, R1 and R4 being absent when this bond is present, R1 and R4 are independently H, OH, halo, oximino, or an organic radical, R2, R6 and...
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WO/1995/003419A1 |
A process for separating a natural B avermectin from a natural avermectin containing fermentation broth by using an aqueous precipitation. The process comprises extracting natural avermectins from the fermentation broth with a water misc...
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WO/1995/003317A1 |
Novel antiparasitic compounds of formula (I), wherein the broken line represents an optional bond, R1 and R4 being absent when this bond is present, R1, R3, R4 are independently H, OH, halo, mercapto, oxo, oximino, or an organic radical,...
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WO/1995/003316A2 |
Novel glycosides containing novel leaving groups, pyridyloxy, pyrimidyloxy, methoxypyridyloxy, pyridyl carbonate and pyridyl thiocarbonate are utilized in many fertile syntheses of glycosides, disaccharides, trisaccharides, oligosacchari...
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WO/1995/002594A1 |
The present invention relates to amide derivatives of formula (I) or (II) of 19-carboxy-19-deformyl 16-membered ring macrolide antibiotics rosaramicin, repromicin, tylosin, 5-O-mycaminosyltylonolide, 4-deoxy-O-mycaminosyltylonolide, desm...
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WO/1995/001794A1 |
Antibacterial compounds having formula (II) and pharmaceutically acceptable salts thereof, wherein Y is selected form (a), (b), and (c) and X is selected from the group consisting of -C(O)-, -C(S)-, CH2-, -CH2CH2- and -C(CH3)2-; also dis...
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WO/1995/001361A1 |
A novel galactosylmoranoline derivative represented by general formula (I), wherein R1 represents optionally unsaturated C1-C18 acyl, aryloxycarbonyl, alkyloxycarbonyl or aralkyloxycarbonyl; R2 represents hydroxy or acetamido; R3 and R4 ...
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WO/1994/029328A1 |
Antiparasitic compounds of formula (I) where the broken lines between the 3-4 and 4-5 positions represent optional bonds and either (i) the 3-4 optional bond is present; the 4-5 optional bond is absent, R7 is absent and R6 is halogen ato...
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WO/1994/028910A1 |
Compounds of this invention are 5,6-dideoxy, 5-amino derivatives of idose and 6-deoxy, 6-amino derivatives of glucose which exhibit immunomodulatory, anti-inflammatory, and anti-proliferative activity. Methods of preparation, pharmaceuti...
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WO/1994/028419A1 |
An immobilised complex of one or more labelled carbohydrates.
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WO/1994/028008A1 |
Fluorescent tagging compounds of formula (I), wherein A is a member selected from the group consisting of an aromatic ring, a heteroaromatic ring, and a heterocyclic ring, and R is a linking moiety having from 1 to 20 carbon atoms, optio...
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WO/1994/027614A1 |
Acetals of podophyllotoxin-beta-D-glucopyranoside or of 4'-demethylpodophyllotoxin-beta-D-glucopyranoside having general formula (I) wherein R is OH or OCH3, and R' is an alkyl, aryl or heterocyclic residue, are used for the preparation ...
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WO/1994/026113A2 |
There is disclosed a topical formulation containing glycols, glycerides, or their derivatives, an avermectin compound (active ingredient) and optionally a polymeric material which has been discovered to provide superior efficacy against ...
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WO/1994/026758A1 |
A compound having formula (III). Also, a process of making azithromycin comprising reducing the compound of formula (III) and N-methylating the reduced product.
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WO/1994/025566A1 |
The present invention relates to the field of microorganisms and antibiotics. In particular, it relates to a new mutant strain and the method for mutagenizing breeding thereof, and the use of the new strain to produce a single ingredient...
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WO/1994/024145A1 |
Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and have significant applications for the treatment or prevention o...
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WO/1994/023582A1 |
An adenoviral vector including a DNA sequence encoding a lung surfactant protein. The adenoviral vector may be a replication deficient adenoviral vector which is free of at least the majority of the E1 and E3 DNA sequences. Such vectors ...
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WO/1994/022884A1 |
A "mirror" amide cord factor of "mirror" thioester cord factor having generic formula (I) wherein T is nitrogen or sulphur and when T is nitrogen, R1 is an alkyl or alkoxy having 8 to 90 carbon atoms, 11 to 191 hydrogen atoms, and 0 to 1...
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WO/1994/021269A1 |
The invention concerns drugs for the treatment of retrovirus infections, the drugs containing bacteria-free and protein-free extracts of Escherichia coli, optionally with the addition of extracts of green or yellow leaves of Ginkgo biloba.
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WO/1994/021657A1 |
The present invention relates to C-20 olefin derivatives of 16-membered ring macrolide antibiotics repromicin, rosaramicin, 5-mycaminosyltylonolide, desmycosin, lactenocin, O-demethyllactenocin, 4'-deoxymycaminosyltylonolide and 23-deoxy...
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WO/1994/020061A2 |
The invention disclosed relates to a process for the production of polyketide pigmented antibiotics, from Streptomyces venezuelae ISP5230 (ATCC no. 10712), and to novel polyketide pigmented antibiotics. The novel compounds have structura...
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WO/1994/020518A1 |
New A83543 components, including fermentation products A83543K, A83543O, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones o...
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WO/1994/020627A1 |
The present invention provides a method for identifying or selecting from a population of eukaryotic cells cultivated on or in a medium containing at least one compound, cells which have a metabolic advantage as a result of having being ...
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WO/1994/019360A1 |
The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage...
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WO/1994/017088A1 |
A novel macrolide antibiotic having a potent antimicrobial activity, represented by general formula (1), which is produced by introducing a specified aryloxy or alkyloxy group into the 3-position of a 5-O-desosaminylerythronolide derivat...
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WO/1994/015617A1 |
This invention relates to 8a-aza and 9a-aza macrolide antibiotics which are useful in the therapy of bacterial infections in mammal. The process for preparing these antibiotics is also described.
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WO/1994/015944A1 |
Antiparasitic compounds of formula (I) wherein the broken line at the 22-23 position represents an optional bond and either this bond is present and R1 is absent or this bond is absent and R1 is H, OH, oxo or oximino optionally substitut...
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WO/1994/014830A1 |
An antiparasitic compound of formula (I), (II) or (III) wherein R is selected from a variety of organic groups, the broken line represents an optional double bond, R1 is H, OH, -O-alkyl or optionally substituted oximino, and R2 and R3 ar...
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WO/1994/014829A1 |
Compound of the general formula (I) in which R' is a hydrogen atom or a radical R and R is an acyl residue. The invention also concerns a process for the preparation of said compound, the use of said compound as a drug and in the prepara...
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WO/1994/014849A1 |
Highly sulfated oligosaccharides in the form of hexasaccharide and octasaccharide compounds which have antiproliferative activity with respect to smooth muscle cells are useful in treatment of coditions characterized by unwanted smooth m...
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WO/1994/011382A1 |
Tricyclic heteronaphthoquinone derivatives, that have antineoplastic activity, are disclosed, together with processes for their synthesis. Some of these anti-neoplastics compounds have a saccharide moiety. Some members of this structural...
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WO/1994/011376A1 |
Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of general structure (I), wherein E is H, CO2R, CONH2, CONHR, CONR2, acyl, or CN; X is H, OH, or OR; R1, R2, R3 and R4 are independently the same o...
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WO/1994/010185A1 |
A compound represented by general formula (I) or a salt thereof, each being orally administrable because of being excellent in the effect of promoting gastrointestinal movement and extremely reduced in the extent of decomposition by the ...
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WO/1994/006438A1 |
Nucleoside analogues such as ribofuranosyl-beta-D-pyrrolopyrimidine compounds and ribofuranosyl pyrrolopyrimidine N-oxide compounds and pharmaceutically acceptable salts and mixtures thereof. Compositions comprising these compounds and p...
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WO/1994/005678A1 |
Compounds comprising a first aromatic ring linked to a xylose via a hydroxyl, thio, hydrocarbon, or amino substituent to form a beta-D-xyloside linkage and a second aromatic ring fused to the first ring are useful primers for the biosynt...
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WO/1994/005683A1 |
A rokitamycin monohydrate crystal (hereinafter referred to as "RKM hydrate") represented by formula (1), and a process for producing RKM hydrate by crystallizing rokitamycin from the acidic aqueous solution thereof. The novel RKM hydrate...
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WO/1994/005152A1 |
Triterpenoid acid derivatives have been found to have structures similar to natural ligands to the extent that these derivatives bind to natural selectin receptors including endothelial leukocyte adhesion molecule-1 (ELAM-1) and leukocyt...
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WO/1994/004547A1 |
A novel nicotine derivative represented by general formula (1) wherein R represents a hexose or a dihexose; and (a) represents (S)-(-)-3-(1-methyl-2-pyrrolidinyl)-2-pyridyl, (R)-(+)-3-(1-methyl-2-pyrrolidinyl)-2-pyridyl, (S)-(-)-5-(1-met...
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WO/1994/002496A1 |
The present invention relates to derivatives of 16-membered ring macrolide antibiotics rosaramicin, repromicin, 5-mycaminosyltylonolide, desmycosin, lactenocin, O-demethyllactenocin, cirramycin A1, and 23-deoxymycaminosyltylonolide, whic...
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WO/1993/024509A1 |
A compound represented by general formula [I] or a salt thereof, being extremely reduced in the decomposability by gastric juice as compared with other known erythromycin derivatives and having an excellent activity of promoting the move...
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WO/1993/023431A1 |
The present invention provides mutant proteins of steroid hormone receptors. These mutant proteins are useful in methods of distinguishing a steroid hormone receptor antagonist from a steroid hormone receptor agonist. The present inventi...
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WO/1993/023046A1 |
An enantiomer of a fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The enantiomeric compounds have DNA-cleaving,...
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