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WO/2002/017916A1 |
Disclosed are guanidine and biguanidine derivatives which have anti-viral and anti-bacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial me...
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WO/2002/016371A1 |
Crystals of 2-methyl-2-triazolylmethylpenam-3-carboxylic acid 1,1-dioxide diphenylmethyl ester. Even when allowed to stand for 1 year at 5 to 35°C, the crystals are stable and undergo substantially no decomposition or alteration. The cr...
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WO/2002/014325A1 |
Stable crystals of diphenylmethyl 2-methyl-2-triazolyl-methylpenam-3-carboxylate, which cause substantially no decomposition or deterioration even after allowing to stand at room temperature for one year. The crystals are produced by con...
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WO/2001/098518A2 |
The invention relates to a method for producing biologically active ingredients. Active ingredients comprising additional functional groups, a modified spectrum of activity and modified application properties can be obtained from medicam...
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WO/2001/092268A1 |
Process for drying amoxicillin (compositions), characterised in that a gas, which is inert towards amoxicillin (compositions) and having a relative humidity content which is greater than zero is used for drying.
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WO/2001/087299A1 |
The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is admin...
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WO/2001/085664A2 |
The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.
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WO/2001/079210A2 |
Highly crystalline, highly filterable sodium Cefoperazone in the form of needle crystal aggregates, obtainable by a process comprising the controlled addition of acetone to a solution of water/acetone/alcohols/sodium Cefoperazone at 20 $...
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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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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/2001/030783A1 |
Process for the preparation of a $g(b)-lactam antibiotic by acylation of a $g(b)-lactam nucleus with the aid of an acylating agent, use being made of a complexing agent, and the acylating agent containing L-isomer and an aldehyde being a...
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WO/2001/026691A1 |
Attempts are made to develop a widely applicable technique for developing granules for oral use which can be quickly disintegrated or dissolved in the oral cavity at the administration or in the dissolution or suspension step in using an...
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WO/2001/012584A2 |
Compounds or their salts of general formula (I): A$m(Y)B$m(Y)N(O)¿s? wherein: s is an integer equal to 1 or 2; A = R$m(Y)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 a...
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WO/2001/009135A1 |
An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an...
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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/2000/061537A2 |
Compounds or their salts having general formulas (I) and (II): wherein s is and integer equal to 1 or 2, preferably s = 2; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C¿...
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WO/2000/061115A2 |
Bacterial infections may be treated using a high dosage regimen of amoxycillin. Preferably, the dosage is provided by a bilayer tablet.
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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/2000/061541A2 |
Compounds or their salts having general formulas (I) and (II) wherein: s = is an integer equal to 1 or 2, preferably s = 2; b0 = 0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the descript...
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WO/2000/053207A1 |
The invention relates to novel biologically active compounds of fungi of the species $i(Ganoderma pfeifferi) DMS 13239, to methods of preparing same and to their use. From the fruit-body and mycelium of $i(Ganoderma pfeifferi) DMS 13239 ...
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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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WO/2000/043399A1 |
Compounds are provided having formulae (I) and (II) wherein n is 0 or 1 and when n=1, R is a 5 or 6 membered heterocyclic ring, hydroxy, halogen, oxo, carbamoyl, alkoxy, or disubstituted amino, when n=0, R is an ester, cyano or amide gro...
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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/2000/041478A2 |
The present invention describes novel agglomerates in crystalline form of $g(b)-lactam compounds. Furthermore, a process for the preparation of said agglomerates, wherein a solution or suspension of at least one $g(b)-lactam compound in ...
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WO/2000/037484A1 |
Process for the preparation of amido compounds in which an amino acid R¿1?R¿2?-C(NHR)-(CH¿2?)¿n?-COOH, where R¿1? and R¿2? represent an amino acid residue, n is 0 or 1 and R is H, alkyl or aryl, is in a solvent brought into contact...
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WO/2000/034289A1 |
A new synthesis of penicillanic sulfoxide acid ester is claimed. The synthesis starts with 6-amino penicillanic acid and proceeds through conversion to a bromide via diazotization, esterification, reduction of the bromide, and oxidation ...
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WO1999063988A9 |
Disclosed are multibinding compounds which inhibit nitric oxide synthases (NOSs), enzymes which form nitric oxide and L-citrulline from L-arginine. The multibinding compounds of this invention contain from 2 to 10 ligands covalently atta...
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WO1999064047A9 |
Novel compounds are disclosed, useful as antiviral agents.
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WO1999063929A9 |
Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compound...
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WO1999064054A9 |
Disclosed are multibinding compounds which inhibit topoisomerases which are essential enzymes in higher encaryotes for DNA replication and repair. The multibinding compounds of this invention containing from 2 to 10 ligands covalently at...
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WO/1999/064051A1 |
Novel multibinding compounds are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of inhibiting bacterial Type II DNA topoisomerase, thereby modulating the biol...
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WO/1999/063940A2 |
Disclosed are multibinding compounds which inhibit H?+¿/K?+¿-ATPase, an enzyme which is involved in the control of acid secretion in the stomach. The multibinding compounds of this invention containing from 2 to 10 ligands covalently a...
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WO/1999/064037A1 |
Novel multi-binding compounds are disclosed that modulate enzymatic processes. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to an enzyme, enzyme substrate o...
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WO/1999/062910A1 |
A novel process for preparing a crystalline alkali metal salt of amoxycillin is dislcosed.
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WO/1999/061448A1 |
The present invention relates to penem antibacterial agents in which the penem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. ...
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WO/1999/055709A1 |
A process to prepare a crystalline $g(b)-lactam compound by the addition of a base to an acidic solution of a $g(b)-lactam compound obtained by the addition of an acid to a solution or suspension of a $g(b)-lactam compound obtained by (a...
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WO/1999/055710A1 |
The invention relates to a method for crystallizing a $g(b)-lactam, wherein the $g(b)-lactam is crystallized from a nitric acid solution.
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WO/1999/052912A1 |
A process for producing a halogenated $g(b)-lactam compound represented by general formula (4), characterized by reacting a $g(b)-lactam-derived amino compound represented by general formula (1) with nitrous acid or a nitrite in the pres...
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WO/1999/052530A1 |
Antibacterial agents exerting excellent effects in preventing or treating respiratory mixed infection with two or more bacteria belonging to different genera selected from among $i(Streptococcus, Moraxella, Haemophilus, Klebsiella), etc....
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WO/1999/048895A1 |
The invention relates to a process for recovering 6-aminopenicillanic acid from a mother liquor, wherein 6-aminopenicillanic acid is extracted from the mother liquor with a recovery solution, which recovery solution is collected and re-u...
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WO/1999/042466A2 |
Compounds of formula (1a) or (1b) or (2a) or (2b) and the salts, esters and amides thereof wherein Z is S, SO, SO¿2? or O; each of R?1¿, R?2¿ and R?3¿ is independently substituted or unsubstituted alkyl (1-10C), substituted or unsubs...
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WO/1999/036098A1 |
An antibacterial composition for topical administration having a potent antibacterial effect over a broad range and a high safety and containing in a stable state penem antibiotics which are chemically unstable to hydrolysis, oxidation, ...
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WO/1999/033837A1 |
A method for preparing a $g(a)-oxolactam comprising, reacting a corresponding $g(a)-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding $g(a)-oxolactam.
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WO/1999/033838A1 |
Compounds of formula (I), wherein R?1¿ and R?2¿ are each independently hydrogen, (C¿1?-C¿10?)alkyl, (C¿3?-C¿8?)cycloalkyl, (C¿2?-C¿10?)alkenyl, (C¿2?-C¿10?)alkynyl, -COOR¿a?, -CONR¿b?R¿c?, cyano, -C(=O)R¿d?, -OR¿e?, aryl, ...
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WO/1999/032493A1 |
A process for purifying a solution of an ampicillin pro-drug, e.g. bacampicillin, or an acid addition salt thereof, which comprises a step wherein a crude solution thereof is subjected to an evaporation which is controlled by the evapora...
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WO/1999/028308A1 |
A group of reagents, as diisocyanates, dianhydrides, diacidchlorides, diepoxides, carbodiimides and the like are utilized to link a wide variety of antibiotic moieties, reacted two at a time with said reagents, the said antibiotic moieti...
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WO/1999/024441A1 |
A process for the crystallization of $g(b)-lactam compounds involving simultaneous addition of a solution of said $g(b)-lactam compound and a titrant to a crystallization vessel. In case of zwitterionic $g(b)-lactam compounds, the pH-val...
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WO/1999/015532A1 |
Process for recovery of a $g(b)-lactam antibiotic from a mixture containing $g(b)-lactam antibiotic and D-phenyl glycine (FG) in solution, with the mixture being brought to a pH between 3 and 8 at a temperature between -5 and 20 °C and ...
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WO/1999/015531A1 |
Process for recovery of a $g(b)-lactam antibiotic from a mixture containing $g(b)-lactam antibiotic and D-phenyl glycine (FG) in solution, with the mixture being brought to a pH between (3) and (8) at a concentration such that FG remains...
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WO/1999/003859A1 |
A compound of formula (I) wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H¿2? or F¿2?; A is N or C(R?2¿); G is N or C(R?3¿); D is N or C(R?4¿); with the proviso that no more than...
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