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WO/2002/040036A1 |
Drugs efficacious in preventing and treating endometriosis and uterine myoma are disclosed. The preventives or remedies for endometriosis and uterine myoma contain macrolide antibiotics as the active ingredient.
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WO/2002/038577A2 |
An extended release pharmaceutical composition comprised of an erythromycin derivative and non-polymer material for providing for extended release, in particular, a member selected from the group consisting of clays, long chain hydrocarb...
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WO/2002/036601A2 |
The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of can...
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WO/2002/036612A1 |
The invention concerns agents with anti-bacterial activity and methods and intermediates for their production. The present invention further concerns the use of such agents for the treatment of bacterial infections in animals, including ...
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WO/2002/036602A1 |
Pyrazole-O-glycoside derivatives represented by the formulae (i) and (ii), which are useful as diabetes remedies.
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WO/2002/032917A1 |
The present invention relates to a compound of formula (I) wherein R¿1? is hydrogen or together with R¿2? is oxo; R¿2? represents hydroxy, OC(O)XR¿7?, OC(O)NHXR¿7? or R¿2? together with R¿1? is an oxo group; R¿3? is hydrogen or a...
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WO/2002/032919A2 |
Compounds having formula (I) are useful for treating bacterial infections while avoiding the concomitant liability of gastrointestinal intolerance. Compositions containing the compounds and methods of treatment using the compounds are al...
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WO/2002/032233A2 |
The use of aivlosin, as much or as a pharmacologically acceptable (non-toxic) derivative such as an acid addition salt, for the preparation of a veterinary medicament for the treatment or prophylaxis of diseases and infections of pigs an...
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WO/2002/032918A2 |
The present invention includes compounds of the formula wherein: X is hydrogen or halide; R?2¿ is hydrogen, acyl, or a hydroxy protecting group; R?6¿ is hydrogen, hydroxyl, or -OR?a¿ wherein R?a¿ is a substituted or unsubstituted moi...
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WO/2002/032916A2 |
The present invention provides novel sixteen-membered macrolide compounds that are useful as anti-infective agents or as intermediates thereto. The present invention also provides methods for the preparation of these compounds, and metho...
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WO/2002/030943A1 |
Form E crystals of N-demethyl-N isopropyl-12-methoxy-11 -oxo-8,9-anhydroerythromycin A-6,9-hemiacetal fumarate produced by treating form E crystals of N-demethyl-N-isopropyl -12-methoxy-11-oxo-8,9-anhydroerythromycin A-6,9-hemiacetal fum...
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WO/2002/026220A2 |
Compounds according to formula (I): T¿1?-L-T¿2?, wherein T¿1? is a taxoid group, preferably of Formula (II): wherein R¿1? is C¿6?H¿5?; R¿2? is O; L is a linking group; and T¿2? is a substituent selected from the group consisting ...
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WO/2002/026753A1 |
Erythromycin derivatives of the following general formula or their salts, which exhibit excellent antimicrobial activities against atypical acid-fast microorganisms and are useful as antimicrobial agents, wherein R?1¿ and R?2¿ are each...
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WO/2002/022847A1 |
A process for producing purified anthocyanidin glucoside characterized by comprising cleaving the rhamnose end of anthocyanidin rutinoside with rhamnosidase, converting the anthocyanidin rutinoside component into anthocyanidin glucoside ...
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WO/2002/017909A1 |
The present invention relates to a therapeutic agent of osteoporosis which comprises an active ingredient of quercetin derivatives. The quercetin derivatives of the invention can be practically applied for the treatment and prevention of...
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WO/2002/018403A1 |
A process for producing a fumaric acid salt of a compound represented by the general formula (II) (wherein R¿1? represents hydrogen or lower alkyl; and R¿2? represents lower alkyl) which comprises converting a compound represented by t...
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WO/2002/015842A2 |
The present invention provides a stable form of azithromycin derivatives that act as antibiotics. These compounds are in anhydrous form and have increased stability over the hydrated forms.
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WO/2002/016380A1 |
The invention provides new macrolides antibiotics of formula (I) with improved biological properties and improved stability formula (I): wherein R?1¿ is hydrogen, cyano, -S(L)¿m?R?2¿, -S(O)(L)¿m?R?2¿, or -S(O)¿2?(L)¿m?R?2¿; L rep...
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WO/2002/014338A1 |
Pseudoerythromycin derivatives represented by the general formula [I] and serving as novel anti-inflammatory agents having decreased antibacterial activities and increased anti-inflammatory activities: [I] wherein R¿1? and R¿2 ?are eac...
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WO2000069875A9 |
A compound having the formula selected from the group consisting of a compound of formula (I), a compound of formula (II), and a compound of formula (III) as well as pharmaceutically acceptable salts, esters, solvates, metabolites, and p...
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WO/2002/013834A1 |
Novel nocathiacin derivatives have been prepared by both biotransformation and chemical methods. A novel nocathiacin derivative, nocathiacin IV, was prepared by either incubation of protease from Streptomyces griseus (Sigma, Cat# P5147) ...
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WO/2002/014251A1 |
The invention concerns a method for obtaining extracts based on polyphenol compounds contained in cocoa, characterised in that it consists in: using fresh beans, which have not been pre-treated or defatted, said fresh beans whereof their...
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WO/2002/013836A1 |
Preventive or therapeutic drugs for cancers containing as the active ingredient cyanidin compounds of the general formula (I): (I) (wherein R is H, -$g(b)-D-glucopyranoside, or 6-malonyl-$g(b)-D- glucopyranoside) The cyanidin compounds a...
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WO/2002/014339A1 |
A method of introducing a 6-position substituent into a 6,9-cyclic acetal of a 5-O-desosaminylerythronolide derivative, characterized by cleaving the cyclic acetal selectively at the 9-position C-O bond; and a process for efficiently syn...
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WO/2002/012259A1 |
The invention relates to erythromycin 2'-proprionate dedecyl sulfanate (salt) represented by general formula (I), a process for its preparation, pharmaceutical composition comprising this compound and its use as antibiotics.
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WO/2002/012256A1 |
The present invention relates to a novel process for the preparation of acarbose. Said process comprises the steps of: 1) acidifying a fermentation broth containing an acarbose; 2) removing particulates from the fermentation broth; 3) ad...
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WO/2002/012248A1 |
Compounds represented by the general formula (I) or salts thereof wherein -X---Y- is -CH=CH-, -CH¿2?-CH¿2?-, or the like; the symbol ---- between R?1¿ and the 4'-position carbon atom represents a single bond or a double bond; and the ...
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WO/2002/012261A1 |
Compounds of the general formula (I) or salts thereof, exhibiting antiparasitic activities wherein -X---Y- is -CH=CH- or the like; the symbol ---- between R?2¿ and the 5-position carbon atom is a single bond or a double bond; R?1¿ is l...
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WO/2002/012260A1 |
A macrolide antibiotic of formula (I) wherein the variables are defined as described herein.
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WO/2002/009699A2 |
The present invention relates to methods of treating conditions and/or symptoms related to common cold of the upper and/or lower respiratory tract and/or eyes. In particular the invention relates to the methods of treating conditions and...
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WO/2002/009640A2 |
The present invention provides a stable form of azithromycin derivatives that act as antibiotics. These compound are in anhydrous form and have increased stability over the hydrated forms.
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WO/2002/010144A1 |
The invention relates to an improved method for preparing 7,16-deoxy-2-aza-10-O-cladinosil-12-O-desosaminil-4,5-dihydr
oxi-6-ethyl-3,5,9,11,13,15-hexamethylbicycle[11.2.1]hexa-dec
a-1(2)-en-8-ona from erythromycin A, wherein said compoun...
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WO/2002/010148A1 |
The present invention relates to novel coumarin derivatives of formula (I) wherein: X= O or S; n= zero, 1, 2, 3 or 4; R¿5? and R¿6?, which can be the same or different, are optionally unsaturated C¿1?-C¿4? alkyl groups, or together w...
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WO/2002/010181A1 |
The improved form of azitromycin monohydrate of lower hydroscopicity and greater density and hardness that presents values of: apparent filling density not lower than 0.35 g/ml; and apparent knocked density not lower than 0.50 g/ml. The ...
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WO/2002/000663A2 |
A novel class of antitumour compounds has been recognised based on the isolation from a new marine microbe, strain PO13-046, belonging to the genus $m(f)i$m(g)Actinomadura sp.$m(f)/i$m(g)), of a compound designated IB-00208. The class of...
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WO/2001/097778A2 |
Parenteral compositions of oil-coated-Amphotericin B in structured-emulsion form, having LD¿50? of atleast 400mg/kg in mice and process for making the same have been described. The process essentially requires dispersing Amphotericin B ...
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WO2000066602A9 |
The present invention relates to derivatives of 3-deoxy desmycosin of formula (I), wherein, starting from triply protected desmycosin, there are performed an oxidation at C-3 in the first step and then, optionally, a hydrogenation of dou...
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WO/2001/092341A1 |
This invention provides an hexaglucal compounds of formula (III), which is a new kind of bio-pesticide. And also provides the processes for preparing them, which include the regioselective reaction of compounds presented by formula (I) a...
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WO/2001/091758A1 |
The present invention provides two new classes of polyene macrolide amide derivatives useful for treating or preventing fungal infections. The new polyene macrolide amide derivatives exhibit antifungal activity and are more water-soluble...
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WO/2001/092281A1 |
The invention concerns a method for preparing a compound of general formula (I) by reducing amination of a corresponding (4'')-carbonyl derivative. The invention is characterised in that it consists in: bringing said (4'')-carbonyl deriv...
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WO/2001/087911A1 |
A method is disclosed for identifying compound defined by pharmacophores which compound affect protein-protein interactions. The method involves determining functional residues of at least one protein of a protein-protein interaction of ...
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WO/2001/087309A1 |
Coumermycin analogs of general formula I: wherein X, a linking group, is selected from the group consisting of alkyl, aryl, diaryl, substituted alkyl, substituted aryl, alkyl with hereroatoms in the chain, heteroaryl, cyclic and bicyclic...
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WO/2001/087912A1 |
The invention relates to a polymorphic form of azithromycin dihydrate (9-desoxo-9a-aza-9a-methyl-9a-homoerythromycin A) showing endothermy in differential scanning calorimetry (DSC) at 139° C, when recorded in an open aluminum crucible ...
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WO/2001/087807A2 |
The present invention relates to a cost effective and industrially advantageous process for the selective methylation of a hydroxy group at the 6 position of erythromycin A derivatives.
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WO/2001/083448A2 |
Chemotherapy of malignant tumors is seriously restricted by the fact that available cytostatics are often not capable of differentiating between normal and malignant tissue. The aim of the invention is therefore to improve the selectivit...
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WO/2001/081358A1 |
Methods for treating or preventing bacterial or protozoal infections in mammals by administering a single dose of an antibiotic composition comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are disclosed. ...
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WO/2001/079244A1 |
Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA (V), wherein, Ring 1 comprises a cyclic or heterocyclic ring, or aryl or heteroaryl ring, all of said rings comprising 4 to 8 carbon atoms, a...
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WO/2001/079245A1 |
The invention relates to flavone and isoflavone glycoside derivatives of general formula (I): [A¿1?-C(=O)O]¿m?-[X-O-Z]-[O-C(=O)-A¿2?]¿n? (I), wherein [X-O-Z] represents a flavone or isoflavone glycoside structure, wherein X represent...
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WO/2001/079520A1 |
The present invention relates to hybrid glycosylated products, and in particular, to natural products such as polyketides and glycopeptides, and to processes for their preparation. The invention is particularly concerned with recombinant...
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WO/2001/077134A2 |
Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
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