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WO/2001/064649A1 |
A process for preparing 1,8-naphthalimide by reacting 1,8-naphthalic anhydride with ammonia in an aqueous solution under atmospheric pressure at 60 to 100 °C.
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WO/2001/064647A1 |
Compounds of the general formula (I) wherein R?10¿ means saturated 4 to 7 membered ring containing one or two nitrogen atom(s) connecting through the nitrogen atom and optionally substituted by a C¿1-4? alkyl group or a satured 4 to 7 ...
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WO/2001/064645A2 |
The invention provides a compound of formula (I), wherein A, Ra, Rb, R¿1? to R¿5?, m and t are as defined as disclosed, or a pharmaceutically acceptable salt or ester thereof, useful as alpha-2 antagonist. The compounds I can be used f...
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WO/2001/062736A1 |
This invention is directed to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R?1¿, R?2¿, and R?3¿ are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions con...
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WO/2001/058488A1 |
It is found out that inducible NO synthase (i-NOS) is efficacious against Sjoegren's syndrome. Based on this finding, remedies and/preventives for Sjoegren's syndrome containing i-NOS inhibitors as the active ingredient are developed. As...
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WO/2001/058875A2 |
The invention concerns substituted 1,2,3,4- tetrahydroquinoline-2-carboxylic acid derivatives, a method for the production of said derivatives, their use in the production of medicaments and medicaments containing said compounds.
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WO/2001/051471A1 |
The invention relates to substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of the general formula (1), wherein the groups R?1¿, R?2¿, R?3¿, R?3'¿, R?4¿, R?5¿, R?6¿, X and A are defined as per the description and claims,...
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WO/2001/051470A1 |
N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-...
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WO/2001/049292A1 |
A pharmaceutical formulation for the prolonged-release oral mucosal administration of apomorpine which comprises a therapeutically effective amount of apomorphine or a pharmaceutically acceptable salt or pro-drug thereof in combination w...
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WO/2001/047892A1 |
This invention provides compounds of formula (1) which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.
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WO/2001/047893A1 |
There is provided compounds of formula (I), wherein R?1¿, R?2¿, R?3¿ and R?a¿ to R?h¿ have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricu...
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WO/2001/042207A2 |
Novel methods for the treatment and/or prevention of ileus. The methods may comprise administering to a patient an effective amount of a peripheral mu opioid antagonist compound. Preferred compounds for use in the methods include piperid...
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WO/2001/042219A2 |
This invention provides a novel class of substituted 6(5H) phenanthridinone compounds. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereo...
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WO1999064041A9 |
Disclosed are novel multi-binding compounds (agents) which bind to NMDA receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors, thereby modulating the biological processes and/...
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WO/2001/034209A1 |
Ligands for nAChRs are provided based on various derivatives of methyllycaconitine (MLA) such as radiolabeled MLA, and MLA containing a fluorimetric marker group and their use in imaging for detection of Alzheimer's and other CNS disease...
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WO/2001/030333A2 |
The invention includes tissue factor (TF) blocking compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such compounds. Compounds of the invention are particularly useful for treating...
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WO/2001/027086A1 |
Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and drug compositions containing the derivatives or the salts.
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WO/2001/027099A2 |
Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a g...
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WO/2001/017972A2 |
The invention relates to novel compounds of formula (I), wherein the substituents have the significance cited in claim (1) and the agronomically compatible salts, isomers and enantiomers of said compound, which are suitable for use as he...
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WO/2001/017356A1 |
An antimicrobial polymer, characterised in that it carries a covalently bound chromophoric marker. The antimicrobial polymer is preferably a cationic antimicrobial polymer, especially a poly(hexamethylenebiguanide). Also claimed are comp...
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WO/2001/016109A1 |
The invention relates to rylene dyes of the general formula (I), wherein the variables have the following meanings: R represents hydrogen; optionally substituted C¿1?-C¿30? alkyl-C¿5?-C¿8?-cycloalkyl, aryl or hetaryl; R'represents op...
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WO/2001/014328A2 |
Compounds of Formula (I) are antagonists of VLA-4 and/or $g(a)4$g(b)7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical ...
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WO/2001/014380A1 |
The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, having activity toward trk kinase, platelet derived growth factor receptor (PDGFR) kinase, vascular endothelial g...
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WO/2001/014375A1 |
A compound of formula (I) wherein Ring A is imidazol[1,2a]pyrid-3-yl or pyrazolo[2,3a]pyrid-3-yl; R?2¿ is as defined within; m is 0-5; wherein the values of R?2¿ may be the same or different; R?1¿ is as defined within; n is 0 to 2, wh...
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WO/2001/010840A1 |
The invention relates to quaternized azafluorenones of formula (I) in which: R?1¿, R?2¿, R?3¿ and R?4¿ represent a hydrogen atom, a halogen atom, a C¿1?-C¿4? alkyl group, a C¿1?-C¿4? alkoxy group or a C¿1?-C¿4? hydroxyalkoxy gr...
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WO/2001/005765A1 |
Compounds (I) R and R¿1? independently = H or C¿1?-C¿4? alkyl or together = (CH¿2?)¿2-6?, n=0 or 1, ...... is a single or a double bond, A=CO or CH¿2?, A¿1? represents a CO or CH¿2? or CH, each R¿3? independently = H or C¿1?-CÂ...
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WO/2001/004094A1 |
A process for the preparation of ipidacrine (I) (9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta[b]quinoline), which comprises reacting diphosphorus pentaoxide with a trialkyl phosphate and a hydroxyl compound in a hydrocarbon solvent to the...
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WO/2001/004124A1 |
This invention provides novel oxathiepino[6,5-b]dihydropyridines. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharm...
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WO/2000/078768A1 |
Compounds having formula (I) are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
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WO/2000/078722A1 |
A process for preparing selectively compound (I), (1S, 5S, 6R, 7R)-2-aza-7-chloro-5-methyl-3-oxobicyclo[4.1.0]-heptane, by preparing compound (II) from compound (V) through compound (III) via a series of reactions and crystallizing the o...
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WO/2000/077002A1 |
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R?1¿, R?5¿, R?6a¿, R?6b¿, R?7¿, R?8¿, R?9¿, X, b, k, m, and n, and the d...
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WO/2000/077010A2 |
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R?1¿, R?5¿, R?6a¿, R?6b¿, R?7¿, R?8¿, R?9¿, X, b, k, m, and n, and the d...
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WO/2000/077001A1 |
The present invention is directed to certain novel compounds represented by structural Formula (I): or pharmaceutically acceptable salt forms thereof, wherein R?1¿, R?5¿, R?6a¿, R?6b¿, R?7¿, R?8¿, R?9¿, X, b, k, m, and n, and the ...
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WO/2000/077005A1 |
The invention relates to novel naphthopyran-type compounds having a lactam-type 6-membered ring annelated in position C¿5?-C¿6?. These compounds have formula (I). These compounds (I) have interesting photochromic properties. The invent...
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WO/2000/075141A1 |
The invention concerns metal chelates of amides of formula (I) wherein R represents formula (II), for use in medical imaging.
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WO/2000/075236A1 |
Extended rhodamine compounds exhibiting favorable fluorescence characteristics having structure (I) or (II) are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having structure (I...
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WO/2000/075116A2 |
A tricyclic compound of Formula (I): wherein: R?1¿ is hydrogen or hydroxy; R?2¿ is hydrogen or hydroxy; or R?1¿ and R?2¿ together are oxygen; A is a bond, CH¿2?, CH CH¿3?, CH¿2? CH¿2? or C(CH¿3?)¿2?; R?3¿ and R?4¿ are the sam...
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WO/2000/074678A1 |
Therapeutic and/or preventive agents for pain, hyperalgesia or allodynia, containing as the active ingredient fused-piperidine compounds of general formula (I), acid addition salts thereof or hydrates of both: wherein each symbol is as d...
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WO/2000/072801A2 |
The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as alphaV integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors...
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WO/2000/071518A2 |
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate rece...
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WO/2000/069416A1 |
Three pharmaceutical compositions are described: slow-release transdermal patches, sublingual/chewable tablets, and sprays based on apocodeine (APC) and/or its derivatives, for the treatment of male impotence and for the stimulation of m...
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WO/2000/069822A1 |
Compounds of the formula (I): B-X-(CH¿2?)¿m?-CR?1¿R?2¿-(CH¿2?)¿n?-CO-Y, in which X is S(O)¿1-2?, Y is OH or NHOH, and the other variables are as defined in the claims, have therapeutic utility as inhibitors of metalloproteinases, ...
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WO/2000/069829A1 |
The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75?NTR¿ common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve grow...
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WO/2000/069828A1 |
The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75?NTR¿ common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve grow...
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WO/2000/069862A2 |
Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically: R?1¿ is an amidomethylene group or an a...
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WO/2000/066528A2 |
Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.
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WO/2000/066583A1 |
This invention provides compounds of formula (I) having structure (a) wherein A'' is a diavalent moiety selected from the group (a, b, c) which are useful as inhibitors of protein tyrosine kinase.
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WO/2000/064986A1 |
The invention relates to the use of carbopyronine compounds of general formula (I) as marker groups in methods for detecting analytes. The invention also relates to novel carbopyronine compounds and to a method for producing same.
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WO/2000/063172A1 |
Compounds represented by the general formula (I) or salts thereof; and pharmaceutical preparations, particularly hair tonics, containing the compounds or salts as the active ingredient, wherein R?1¿ and R?2¿ are each independently an o...
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WO/2000/063179A1 |
Neurotrophin potentiators which contain 6(5H)-phenanthridinone derivatives of general formula (I) or pharmacologically acceptable salts thereof and are useful as preventive or therapeutic drugs for nerve degeneration diseases: wherein R1...
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