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WO/2001/002413A1 |
The invention provides compounds of formula (II), wherein R is -H or -CO-CH=CH-COOH, and pharmaceutically acceptable salts and esters thereof. Processes for the preparation of the compounds, pharmaceutical compositions containing them, a...
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WO/2001/002414A1 |
This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R) -13- [[2,6-dideoxy-3-C-methyl- 3-O-methyl- 4-C- [(propylamino)methyl] -$g(a)-L-ribo-hexopryanosyl] oxy] -2-ethyl-3,4,10- trihydroxy- 3...
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WO/2001/000640A1 |
Azithromycin in the form of a stable monohydrate and processes for the preparation of azithromycin in the form of an, e.g. stable, monohydrate.
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WO/2001/000582A1 |
The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed co...
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WO/2000/078764A1 |
A process is provided for the manufacture of morphine-6-glucuronide and related compounds of the general structure shown in Formula (1), wherein optionally substituted morphine is conjugated with an optionally substituted member of a new...
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WO/2000/078773A2 |
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4'-substituted 9-oxime erythromycin derivatives with an alkylating agent in the pr...
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WO/2000/078772A2 |
Methods of treating a microbial infection comprising administering to a patient in need of such treatment are disclosed. In one aspect the method comprises administering to a patient in need of such treatment a therapeutically effective ...
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WO/2000/078323A1 |
A use of Icariin in preparing the medicine for preventing and treating sexual disorder and vasoconstrictive diseases.
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WO/2000/077016A1 |
The invention relates to derivatives of 4'-demycarosyl-8a-aza-8a-homotylosin of formula (I) wherein R represents CHO, CH(OCH¿3?)¿2?) or CH¿2?N[CH¿2?(C¿6?H¿5?)]¿2?, R?1¿ represents H or C¿1?-C¿3? acyl, R?2¿ represents OR?6¿ an...
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WO/2000/077017A1 |
This invention relates to novel amorphous form of 6-0-methylerythromycin A (Clarithromycin), to a process for the preparation thereof and to a composition containing it.
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WO/2000/075156A1 |
The invention relates to a novel 6-O-carbamate ketolide compound or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, to a composition comprising the compound and a suitable carrier, a method of preparing the compoun...
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WO/2000/073317A1 |
Compounds represented by general formula (I) or salts thereof: wherein R?$g(a)¿ is C¿1? C¿10? alkyl, C¿3?-C¿10? alkenyl, C¿7?-C¿15? aralkyl, quinolinylalkyl, quinolinylalkenyl, C¿2?-C¿10? alkylcarbonyl, C¿7?-C¿15? aralkylcarbo...
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WO/2000/071557A1 |
The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?17¿, R?f¿, A, X, and Y are as defined herein. The invention also re...
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WO/2000/069874A1 |
Novel crystalline forms of a compound of formula (1) are disclosed. Also disclosed are pharmaceutical compositions comprising theses forms, and methods of their preparation and use.
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WO/2000/068413A1 |
Fermentattion of Nocardia sp- ATCC-202099 in the presence of a halogen- or hydroxy-substituted tryptophan precursor yields a novel corresponding halogen- or hydroxy-substituted nocathiacin compound which has broad spectrum antibiotic act...
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WO/2000/066603A1 |
The invention relates to halo derivatives of 9a-$i(N)-($i(N')-arylcarbamoyl)- and 9a-$i(N)-($i(N')- arylthiocarbamoyl) -9- deoxo-9a-aza-9a-homoerythromycin A of general formula (I) wherein R has the meaning of a substituted aryl group of...
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WO/2000/064484A2 |
Conjugates of a hydrophobic moiety, such as a lipid, linked through a cleavable dithiobenzyl linkage to a therapeutic agent are described. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of the...
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WO/2000/063361A2 |
A multiple-plasmid system for heterologous expression of polyketides facilitates combinatorial biosynthesis. The method can be extended to any modular polyketide synthase (PKS) or non-ribosomal peptide synthase (NRPS) and has the potenti...
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WO/2000/063224A2 |
Compounds of formula (1), (2) or (3), wherein R¿a? is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); ...
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WO/2000/062783A2 |
A series of ketolide antibacterials in the macrolide family of formula (a), intermediates used in their manufacture and pharmaceutical compositions containing them. The compounds are erythromycin analogues useful in the treatment of bact...
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WO/2000/063223A1 |
The invention relates to novel 15-membered 8a- and 9a-lactams from the class of 6-$i(O)-methyl-erythromycin A of general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wh...
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WO/2000/063225A2 |
Compounds of formula (1), (2) or (3) or the 10,11-anhydro forms thereof, wherein R¿a? is H or OH; R¿b? is H or halogen; R¿c? is H or a protecting group; R¿d? is methyl; unsubstituted alkyl(3-10C); substituted alkyl(1-10C); substitute...
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WO/2000/063222A2 |
Compounds of formula (I); wherein R¿1? = alkyl, alkenyl or alkynyl, O-alkyl, O-alkenyl or optionally substituted, optionally interrupted O-alkynyl; R¿2? = hydrogen or halogen; R¿3? = hydrogen, alkyl or halogen; R¿4?= NHR' or NHOR'', ...
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WO/2000/061593A1 |
Erythromycin derivatives of general formula (1) or salts of the same, extremely useful as antimicrobial agents: wherein R is H or lower alkyl; R?1¿ is alkyl, cycloalkyl, (cycloalkyl)alkyl, aralkyl, or -(CH¿2?)¿n?-X-R?4¿; R?2¿ is H o...
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WO/2000/061549A2 |
Compounds or their salts of general formula (I): A-(B) wherein A = R-T¿1?-, wherein R is the drug radical and T¿1? = (CO)¿t? or (X)¿t'?, wherein X = O, S, NR¿1C?, R¿1C? is H or an alkyl having from 1 to 5 carbon atoms, or a free va...
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WO/2000/059889A1 |
$g(a)-Substituted carboxylic acid derivatives represented by general formula (I), pharmacologically acceptable salts of the same, or pharmacologically acceptable esters or amides thereof, which are useful as therapeutic and/or preventive...
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WO/2000/058327A1 |
A method for reducing imidate intermediates arising from Beckmann stereospecific rearrangement of a compound of general formula (II), characterized in that said intermediates are not isolated from the pyridine-based reaction medium and a...
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WO/2000/058328A2 |
The invention relates to novel avermectin derivatives of formula (I), in which R?1¿, R?2¿, R?3¿ and R?4¿ have the meanings defined in the description. The invention also relates to various methods for producing them, to agents contai...
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WO/2000/058326A2 |
The invention relates to a method for the production of etoposide wherein 2,3 - diphenoxyacetyl -1-O-triethylsilyl -$g(b)-D- glucopyranoside is condensed with 4'-phenoxyacetyl-4'-demethylepipodophyllotoxine.
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WO/2000/057888A1 |
Food compositions for preventing type I allergy which contain as the active ingredient kaempferol-3-glucoside; medicinal compositions for preventing and treating type I allergy which contain as the active ingredient kaempferol-3-glucosid...
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WO/2000/057866A2 |
The topical application of an azalide antibiotic such as azithromycin to the eye is useful in treating or preventing ocular infections. In one embodiment, the azalide antibiotic is supplied to the eye in a depot for sustained release. A ...
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WO/2000/058324A1 |
The present invention relates to a method for the production of 4'-demethyl -4'- phosphate-2',3' -bispentafluorophenoxyacetyl - 4',6'-ethylidene - $g(b)-D-glucoside epipodophyllotoxin, characterized in that 2,3-bis pentafluorophenoxyacet...
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WO/2000/057889A1 |
Skin preparations for external use which contain chromanol glycosides represented by general formula (1) wherein R?1¿, R?2¿, R?3¿ and R?4¿ are the same or different and each represents hydrogen or lower alkyl; R?5¿ represents hydrog...
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WO/2000/056746A2 |
A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds $i(via) the key intermediate of general formula (III), wherein R¿4? and R¿5? are, for instance, sulfonates and R¿7? is, for instanc...
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WO/2000/055167A1 |
Compounds represented by general formula (I) and reagents for activity measurement of N-acetylglucosaminidase (NAG) containing the same, wherein R?1¿ is hydrogen, lower alkoxy, or NHCOCH¿3?; and R?2¿ is lower alkoxy or NHCOCH¿3?.
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WO/2000/055168A1 |
The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same. These macrolides are substituted on the 6-O-position with X'-Y'-Z', wherei...
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WO/2000/053169A2 |
The present invention provides a method of inhibiting binding of a chaperone protein with its client protein or client polypeptide. This method comprises contacting coumarin or a coumarin derivative with a chaperone protein, such that th...
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WO/2000/050434A1 |
Malto-oligosaccharide derivatives represented by general formula (1); hydrates or physiologically acceptable salts thereof; and $g(a)-amylase inhibitors or preventive or therapeutic agents for hyperglycemia including diabetes, containing...
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WO/2000/047596A1 |
A method for purifying a red fruit extract containing anthocyanides wherein said extract is taken up with an aqueous solution, the aqueous solution is subsequently cooled to a homogeneous temperature below 15 °C, the permeate thus obtai...
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WO/2000/047597A1 |
Avermectin derivatives represented by general formula (I) or salts thereof: wherein -X---Y- is -CH=CH-, -CH¿2?-C(=O)-, -CH¿2?-CH¿2?-, or -CH¿2?-CH(R?13¿)-, for example, (1) when -X---Y- is -CH=CH-, R?1¿ is (R?11¿) (R?12¿)C [where...
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WO/2000/044761A2 |
This invention relates to compounds of formula (1) and to pharmaceutically acceptable salts and solvates thereof wherein X?1¿, X?2¿, R?2¿, R?8¿, R?9¿, R?10¿ and R?11¿ are as defined herein. The compounds of formula (1) are antibac...
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WO/2000/044762A1 |
Novel compounds represented by the general formula (I) or salts thereof, which are reduced in toxicity and improved in anticancer activity as compared with known carcinostatic anthracycline derivatives (I), (wherein A is methyl or CF¿3?...
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WO1999064033A9 |
This invention relates to novel multibinding compounds that bind to the enzyme phosphodiesterase V (PDE V) and modulate its activity. The compounds of this invention comprise 2-10 PDE V modulator (particularly inhibitor) ligands covalent...
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WO1999064048A9 |
Disclosed are multibinding compounds which inhibit the enzyme HIV reverse transcriptase, an enzyme which catalyzes the conversion of viral RNA to single stranded DNA. The multibinding compounds of this invention containing from 2 to 10 l...
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WO/2000/042055A2 |
3'-Des-dimethylamino-9-oxyimino macrolides of formula (I) endowed with anti-inflammatory activity and their pharmaceutical use are described.
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WO/2000/042047A1 |
The invention relates to compounds of general formula (I), wherein R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6?, R¿7? and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advanta...
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WO/2000/042056A1 |
The invention concerns a method for regioselective preparation of a compound of general formula (I) by regioselective displacement with a nitrogenous nucleophile of the activated alcohol function in position 4'' of a corresponding deriva...
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WO/2000/040589A2 |
The invention relates to novel compounds from the class of the macrolide antibiotic oleandomycin of general formula (I).
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WO/2000/039141A1 |
The application relates to the design and synthesis of novel hexasaccharides of general formula (I), wherein: each R is independently selected from hydrogen, an alkyl or substituted alkyl group, an acyl or substituted acyl group, a phosp...
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WO/2000/039142A1 |
The present invention relates to a new erythromycin A 9-oxime compound which can be effectively used as intermediates for the preparation of erythromycin A oxime compound, a process for preparing the same and a process for preparing 6-O-...
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