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WO/2000/009486A1 |
Compound of formula (I) or salts thereof or solvates thereof: wherein: R?1¿ is hydrogen, C¿1-6?alkyl (optionally substituted by hydroxy or C¿1-4?alkoxy), C¿1-6?alkenyl, C¿1-6?alkynyl, C¿1-6?alkylCO-, formyl, CF¿3?CO-or C¿1-6?alky...
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WO/2000/006545A1 |
Compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X?1¿ is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X?2Â...
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WO/2000/006531A2 |
Nitric acid esters and nitrate salts with medicines active in the respiratory system pathology treatment.
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WO/2000/006569A1 |
The present invention concerns novel substituted pyrazole derivatives of general formula (I), wherein R?1¿, R?2¿, R?3¿ and A have the indicated meaning. The invention also relates to a method for the production of said derivatives and...
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WO/2000/006167A1 |
Novel tricyclic compounds having structural formula (I) as disclosed herein having the natural steroidal trans-anti-trans relative configuration at the A, B, C ring structure are inhibitors of 5-alpha reductase. The inventive compounds a...
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WO/2000/006577A1 |
Thiazolo-, oxazolo- and selenazolo[4,5-c]quinoline-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, inclu...
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WO/2000/005215A1 |
A novel method for generating dianions using 3-methylpyridine-2-carboxylic acid derivatives of formula (V) or using their corresponding alkali metal salts of formula (VI), preferably from their lithium salt (Scheme 3) is described. The s...
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WO/2000/004020A1 |
Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1...
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WO/2000/002851A1 |
The present invention relates to compounds of formula (I), wherein A?1¿, A?2¿, R?1¿, R?2¿, R?3¿, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases,...
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WO/2000/001672A1 |
Naphthalimidobenzamide derivatives represented by general formula (1) or salts thereof; and drugs containing both as the active ingredient: (wherein R?1¿ is hydrogen or the like; Y is hydrogen or -CON(R?4¿)-A?2¿-X?2¿; R?2¿ and R?4¿...
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WO/2000/000472A1 |
The present invention relates to compounds of formula (I), of formula (II) or of formula (III) having pharmacological activity toward the 5-HT¿7? receptor. Pharmaceutical compositions and methods for their use in the treatment of CNS di...
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WO/1999/067231A1 |
Nitric acid salts with medicines having an antihypertensive activity.
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WO1999058500B1 |
The invention relates to a method for stereochemically controlled production of azacyclic compounds of general formula (I), whereby the substituents have the meaning cited in the description. The invention also relates to intermediate pr...
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WO/1999/067220A1 |
Disclosed are compounds which inhibit $g(b)-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits...
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WO/1999/065878A1 |
A process for preparing intermediates and benzoquinolin-3-one pharmaceuticals, such pharmaceuticals are effective in treating conditions consequent on 5$g(a)-reductase.
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WO/1999/066005A1 |
Chemiluminescent labeling compounds and chemiluminescent labeled conjugates are provided. The compounds comprise an acridan ring bearing an exocyclic double bond and further contain a labeling substituent which permits attachement to com...
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WO/1999/064042A1 |
Disclosed are novel multi-binding compounds (agents) which bind alpha-1A adrenergic receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological pro...
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WO/1999/063996A1 |
Disclosed are multibinding compounds which are agonists, partial agonists, inverse agonists or antagonists of the 5HT¿2? receptors, which are involved in neurological disorders. The multibinding compounds of this invention containing fr...
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WO/1999/064052A1 |
This invention relates to novel multibinding compounds that bind to leukotriene receptors and inhibit their activity. In particular, cysteinal leukotriene receptor antagonists and, most particularly leukotriene D¿4? receptor antagonist ...
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WO/1999/063944A2 |
Disclosed are novel multi-binding compounds (agents) which bind estrogen receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological processes/func...
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WO/1999/063993A1 |
Disclosed are multibinding compounds which are agonists, partial agonists, inverse agonists or antagonists of the D¿1? receptors, preferably, agonists of the D¿1? receptors, which are involved in neurological disorders. The multibindin...
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WO/1999/063999A1 |
This invention relates to novel multibinding compounds (agents) that are H1-histamine receptor antagonists and pharmaceutical compositions comprising such compounds. Accordingly, the multibinding compounds and pharmaceutical compositions...
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WO/1999/063930A2 |
This invention relates to novel multibinding compounds that bind to angiotensin (AT) receptors and modulate their activity. The compounds of this invention comprise 2-10 AT receptor ligands covalently connected by a linker or linkers, wh...
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WO/1999/064053A1 |
The present invention is directed to multibinding compounds which are $g(b)3-adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.
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WO/1999/061424A1 |
Novel substituted amino acids of formulae (I) to (VIII) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain...
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WO/1999/061444A2 |
This invention provides bicyclic heterocycles that are useful for treating cell proliferative disorders, such as cancer and restenosis, as well as angiogenesis and atherosclerosis. We have now discovered a group of bicyclic compounds tha...
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WO/1999/059973A1 |
A compound of formula (I) or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof; wherein: Y represents the atoms necessary to form a fused 5-to 6-membered, aromatic or non-...
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WO/1999/059976A1 |
The invention relates to a new method for preparing norbenzomorphane derivatives of general formula (1).
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WO/1999/059975A1 |
A compound of formula (I) or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein the compound of formula (I) is present in an amount that is effective as PARP inhib...
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WO/1999/058495A1 |
The invention concerns compounds of formula (I): R-A-R' wherein: A is as defined in the description; R represents a group (V), wherein R'¿a? and R''¿a? are as defined in the description, or R forms with A a cyclic structure as defined ...
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WO/1999/058496A1 |
The invention concerns compounds of formula (I): R-A-R' wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R?1¿, R?2¿, R?3¿, v and R?4¿ are as defined in the description; R' repr...
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WO1999043983A9 |
Polyhalide light-polarizing particles prepared by the process comprising reacting in a suitable liquid (i) elemental molecular iodine, (ii) an inorganic halide, with (iii) a substantially rigid polycyclic procursor compound, wherein: a) ...
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WO/1999/055680A1 |
Compounds of formula (I) and their pharmaceutically acceptable salts, wherein R?1¿, R?2¿, R?3¿ and Z are defined as in the specification, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such co...
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WO/1999/052876A1 |
The invention concerns azacycloalkane derivatives of general formula (I) wherein: R¿1? represents a hydrogen atom, hydroxyl, a C¿1?-C¿4? alkyl, a 1-C¿4? hydroxyalkyl, a C¿4?-C¿7? cycloalkyl, a C¿1?-C¿4? alkyloxy C¿1?-C¿4?alkyl ...
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WO/1999/052900A1 |
The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin ant...
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WO/1999/052907A1 |
The present invention relates to compounds of formula (I). These compounds are useful as psychotherapeutic agents.
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WO/1999/051579A1 |
The invention concerns fungicide compounds of general formula (I) and compositions containing them, wherein G is selected among the groups (G1) to (G9), the other substituents being such as defined in the description. The invention also ...
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WO/1999/048492A1 |
Compounds represented by general formula (1') and nociceptin antagonists containing the compounds [1'] as the active ingredient wherein R?2¿ represents optionally hydroxylated lower alkyl, amino, etc.; the ring B represents phenyl, thie...
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WO/1999/047521A1 |
The present invention concerns derivatives of general formula I (I' and I''), in which X represents a divalent radical of formula (a) or (b), R¿1?, R¿2?, R¿3?, and R¿4? represent, independently of each other, a hydrogen atom, a hydro...
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WO/1999/045925A1 |
The present invention relates to a class of nitrogen-containing heterocyclic compounds which bind to opioid receptors. The inventive compounds can be used to treat a variety of disease states which involve the opioid receptors.
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WO/1999/043670A1 |
Disclosed are compounds of formula (I) or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R¿1?, R¿2? and R¿3? represents hydrogen, halogen, hydroxy, alkoxy, alkyl, triflu...
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WO/1999/043661A2 |
Disclosed are compounds of Formula (a) or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, aryla...
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WO/1999/042105A1 |
A novel compound N-demethyl-sinomenine, a metabolite of the anti-arthritic alkaloid sinomenine, has been identified and characterized. The compound may be incorporated in a pharmaceutical composition and may be administered to patients f...
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WO/1999/042442A1 |
Compounds represented by general formula (I) or salts thereof having preventive and therapeutic effects on ischemic heart diseases, etc., and being useful as preventives/remedies for ischemic heart diseases such as heart infarction and a...
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WO/1999/040910A1 |
Compounds of general formula (I) wherein R¿4? is an ester or thioester group and R, R¿1?, R¿2?, and R¿3? are as specified in the description, inhibit intracellular Leukotriene A¿4? hydrolase activity and are therefore of value for t...
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WO/1999/041240A1 |
The invention relates to compounds of formula (I), their tautomeric and isomeric forms and physiologically compatible salts, wherein R?1¿ and R?2¿ independently mean a) hydrogen, b) C¿1?-C¿6?-alkyl, c) OR?8¿, d) NR?8¿R?9¿, e) CN, ...
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WO/1999/040070A1 |
Compounds represented by general formula (I) wherein Ar represents aryl or heteroaryl optionally substituted by halogeno, lower alkyl or lower alkoxy; R?1¿ represents optionally fluorinated C¿3-6? cycloalkyl; R?2¿ and R?4¿ represent ...
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WO/1999/040123A2 |
The invention relates to a method for producing aqueous polymer dispersions containing colorants by radical aqueous emulsion polymerisation of ethylenically unsaturated monomers in the presence of radical-forming initiators. At least a p...
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WO/1999/038869A1 |
This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of opioid compounds, particularly morphine a...
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WO/1999/038467A1 |
Sexual dysfunction in human females can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms. Administration of apomorphine increases nerve stimulated clitoral intracavern...
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