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WO/2000/003705A1 |
Ophthalmic formulations containing as an active ingredient 11-(3-dimethylaminopropylidene) -6,11-dihydrodibenz[b,e]oxepin-2-acetic acid or a pharmaceutically acceptable salt thereof are useful for inhibiting cytokine release (e.g., IL-6 ...
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WO/2000/003976A1 |
The invention relates to novel imidamide derivatives of formula (I), wherein R, R?1¿, R?2¿ and R?3¿ have the meaning mentioned in the description. The invention also relates to a method of production and to the use of said derivatives...
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WO/2000/001381A1 |
The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new...
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WO/2000/000489A2 |
Disclosed are compounds of formula (I) or the pharmaceutically acceptable acid addition salts thereof, wherein: R¿1?, R¿2?, R¿3?, R¿4? and R¿5? are the same or different and represent hydrogen, halogen, C¿1?-C¿6? alkyl, C¿1?-C¿6...
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WO/2000/000485A1 |
The invention relates to new epothilon derivatives of general formula (I) where the substituents Y, Z, R?1a¿, R?1b¿, R?2a¿, R?2b¿, R?3¿, R?4a¿, R?4b¿, D-E, R?5¿, R?6¿, R?25¿, R?7¿, R?8¿ et X have the meaning given in the desc...
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WO/1999/067192A2 |
This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and $g(a),$g(b)-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds us...
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WO/1999/067252A2 |
The invention relates to epothilone analog represented by formula (I) wherein (i) R¿2? is absent or oxygen; 'a' can be either a single or double bond; 'b' can be either absent or a single bond; and 'c' can be either absent or a single b...
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WO/1999/061599A2 |
Recombinant DNA compounds that encode all or a portion of the narbonolide polyketide synthase are used to express recombinant polyketide synthase genes in host cells for the production of narbonolide, narbonolide derivatives, and polyket...
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WO/1999/055690A1 |
This invention relates to guanidine derivatives of formula (I) wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising...
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WO/1999/055689A1 |
Compounds represented by general formula (I) which show a tyrosine kinase inhibitory activity or salts thereof, wherein R?1¿ and R?2¿ represent each hydrogen, alkanoyl, etc.; Y represents optionally substituted alkylene; R?3¿ represen...
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WO/1999/054319A1 |
The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.
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WO/1999/054318A1 |
The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.
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WO/1999/043649A1 |
The invention relates to new arylphenyl-substituted cyclic keto-enols of the formula (I), where X is halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkyl sulfinyl, alkyl sulfonyl, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro,...
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WO/1999/043653A1 |
The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Als...
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WO/1999/040047A1 |
The invention relates to methods for preparing macrocyclic products with 9 or more ring atoms by ring-closing diine metathesis of suitable diine substrates. The diine substrates can be converted into cycloakynes or into cycloalkadiines b...
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WO/1999/037651A1 |
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by s...
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WO/1999/037619A1 |
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by s...
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WO/1999/034806A1 |
This invention provides novel compounds derived from a marine sponge, $i(Adocia sp.), that specifically modulate kinesin activity by targeting the kinesin motor domain and mimicking the activity of a microtubule. The compounds act as pot...
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WO/1999/033819A1 |
$g(e)-Caprolactone which less discolors upon heating, has a purity of 99.8 wt.% or higher, and gives under given conditions a gas chromatogram showing that the total concentration of ingredients (low-boiling ingredients) having a retenti...
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WO/1999/032468A1 |
This invention is provide a compound of formula (I) wherein R?1¿ is an optionally substituted 5- to 6-membered ring; W is a divalent group of formula (a) or (b) wherein the ring A is an optionally substituted 5- to 6-membered aromatic r...
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WO/1999/032100A2 |
This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of formula (I) wherein R?1¿ is an optionally substituted 5- to 6-membered ring; W is a divalent group of formula (a) or (b) where...
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WO/1999/028311A1 |
Novel 6-O-alkyl derivatives of erythronolide B are provided. A process for the preparation of 6-O-alkyl derivatives of erythronolide B using erythromycin B is also provided. A process for preparing 6-O-alkyl derivatives of erythromycin C...
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WO/1999/024397A1 |
A compound of formula (I) wherein R?1¿ is a carboxy group or a protected carboxy group, R?2¿ is a hydrogen atom, a hydroxy group or a protected hydroxy group, R?3¿ is a hydrogen atom, a hydroxy group or a protected hydroxy group, in a...
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WO1999001124A9 |
The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same...
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WO/1999/020274A1 |
The compounds of formula (I) are useful as immunosuppressive agents.
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WO/1999/015129A2 |
Selective inhibitors of the cPLA¿2? enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have general formula (i), where (R?1¿), p, D, Y, Z, R?a¿, R?b¿ ...
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WO/1999/009976A1 |
Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first-pass effect.
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WO/1999/007692A2 |
The invention relates to new epothilone derivatives of the general formula (I), in which the substituents Y, Z, R?2a¿, R?2b¿, R?4a¿, R?4b¿, D-E, R?5¿, R?6¿, R?7¿, R?8¿ and X have the meanings assigned to them in the description. ...
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WO/1999/005136A1 |
The present invention provides a compound of formula (I), wherein R?1¿ and R?2¿ are the same or different and are independently H, C¿1?-C¿6? straight-chain or branched-chain saturated or unsaturated alkyl, aryl, R?6¿CH¿...
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WO/1999/003824A1 |
Alkoxyimino-substituted bicyclic derivatives or salts thereof both having excellent disease control and insect pest control effects. The derivatives are represented by formula (I) wherein R?1¿ is, e.g., hydrogen, C¿1-6? alkyl, C¿1-6? ...
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WO/1999/002514A2 |
The present invention relates to compounds of formula (V).
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WO/1998/056752A1 |
Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsyc...
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WO/1998/055475A1 |
This invention relatess to guanidine derivatives of formula (I), wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprisi...
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WO/1998/049315A2 |
Combinatorial libraries of polyketides can be obtained by suitable manipulation of a host modular polyketide synthase gene cluster such as that which encodes the PKS for erythromycin. The combinatorial library is useful as a source of ph...
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WO/1998/047891A1 |
Cyclic products are prepared by selective olefin metathesis of bifunctional or polyfunctional substrates in the presence of one or several homogeneous or heterogeneous metathesis catalysts in a reaction medium. The invention is character...
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WO/1998/046587A1 |
Tricyclic compounds of general formula (I) and pharmacologically acceptable salts thereof, which are useful for the treatment of pollakiuria and enuresis, wherein R?1� is hydrogen, substituted or unsubstituted lower alkyl or the like; ...
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WO/1998/038192A1 |
Disclosed are epothilones with a modified side chain.
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WO/1998/033498A1 |
Disclosed are methods of treating a mammal suffering from cognitive dysfunction. The method comprises administering a therapeutically effective amount of Breflate or a Breflate derivative, as described herein. Also disclosed are methods ...
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WO/1998/029376A1 |
This invention is directed to processes for the solid-phase synthesis of aldehydes, ketones, oximes, amines and hydroxamic acid compounds and to polymeric hydroxylamine resin compounds useful therefor.
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WO/1998/025606A1 |
Novel derivatives of benzodioxole, benzofuran, 2,3-dihydrobenzofuran, and benzodioxane are useful as melatonergic agents.
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WO/1998/025929A1 |
Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the inducti...
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WO/1998/023767A1 |
A novel antibiotic useful as a remedy for fungal infectious diseases, i.e. antibiotic TKR 459 represented by formula (I) and pharmacologically acceptable salts thereof.
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WO/1998/018780A1 |
Radicicol derivatives having an antityrosine kinase activity and represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R?1� and R?2� are the same or different and each represents hydrogen, alkanoyl...
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WO/1998/016519A1 |
[$g(v)-(2,3-Dihydro-1-benzoxepin-4-yl)alkyl]amine derivatives represented by general formula (I), and salts and N-oxide derivatives thereof; a process for the preparation of them; and medicinal compositions containing the same as formula...
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WO/1998/015515A1 |
A method for preparing an aryl ether compound is provided in which an alcohol is reacted with an aromatic compound in the presence of a base, and a transition metal catalyst to form an aryl ether.
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WO/1998/012175A1 |
Fluorinated prostaglandin derivatives represented by general formula (1) or salts thereof; and medicines containing the same as the active ingredient, particularly ones to be used for preventing or treating eye diseases. In said formula ...
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WO/1998/005638A2 |
New phenyl-substituted cyclic ketoenols are disclosed having the formula (I), in which Het stands for one of the groups (1), (2), (3) and (4), in which A, B, D, G, X and Z have the meanings given in the description. Also disclosed are se...
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WO/1998/001164A1 |
Herein described are radiolabeled compounds useful to image D4 receptors $i(in vivo), of formula (I), wherein X?1� is selected from NH, O and S; X?2� is selected from CH and N; Z is selected from iodide, cyano, nitro, tri(loweralkyl)...
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WO/1997/046511A1 |
Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsyc...
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WO/1997/045422A1 |
Acid addition salts of 10-aminoaliphatyl-dibenz[b,f]oxepines of formula (I), wherein alk signifies a divalent, aliphatic radical, R represents an amino group, either unsubstituted or mono- or di-substituted by monovalent aliphatic and/or...
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