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8119614 |
Substitution derivatives of N6-benzyladenosine, methods of their preparation, their use for preparation of drugs, cosmetic preparations and growth regulators, pharmaceutical preparations, cosmetic preparations and growth regulators containing these compounds
The invention concerns novel substitution derivatives of N6-benzyladenosine having anticancer, mitotic, immunosuppressive and antisenescent properties for plant, animal and human cells. This...
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7915232 |
4′-substituted nucleoside derivatives as inhibitors of HCV RNA replication
The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof which...
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7807653 |
Nucleotide mimics and their prodrugs
The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or...
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7772198 |
CFTR channel modulators
The invention concerns pharmaceutical formulas designed for the treatment of diseases related to CFTR channel dysfunction, such as cystic fibrosis, asthma or diarrhoea. These formulas contain a...
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7741473 |
Process for the preparation of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles
The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles (Formula I). The process...
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7737127 |
2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
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7732424 |
Purine derivatives and methods of use thereof
The present invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's core body temperature, protecting an...
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7696181 |
Partial and full agonists of A1 adenosine receptors
Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, myocardial...
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7691825 |
Adenosine A2B receptor agonists
The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions...
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7605143 |
2-propynyl adenosine analogs with modified 5′-ribose groups having A2A agonist activity
The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described herein.
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7544794 |
Method for sequencing DNA and RNA by synthesis
This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, this invention relates...
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7511133 |
Adenosine A3 receptor agonists
The compounds of the following formula: wherein Ar, R and R1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the 5′ p...
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7479485 |
Method of treating arrhythmias
Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor...
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7423144 |
Purine Derivatives as adenosine A1 receptor agonists and methods of use thereof
The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's...
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7414036 |
Compounds useful as A3 adenosine receptor agonists
Adenosine analogue-type A3 receptor agonists having the formula wherein D is N or CH; E is O; X1 is a group of the formula —CR20R2 1-CYCLE, where R20 and R21 are the same or different and are H, F...
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7342003 |
Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs
Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected...
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7300923 |
Partial and full agonists of A1 adenosine receptors
Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular...
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7265111 |
Adenosine analogues and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I) wherein X is selected from the group consisting of wherein n and p are independently 0, 1, 2, or 3, provided that n+p...
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7238676 |
Purine derivatives
The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of,...
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7217815 |
2-beta -modified-6-substituted adenosine analogs and their use as antiviral agents
Various 2′-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and c...
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7214665 |
2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
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7199127 |
Purine nucleosides
Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following...
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7189706 |
C2,5′-disubstituted and N6,C2,5′-trisubstituted adenosine derivatives and pharmaceutical compositions containing them
The present invention concerns novel C2,5′-disubstituted and N6,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent ade...
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7163928 |
Partial and full agonists of A1 adenosine receptors
Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and...
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7157440 |
Partial and full agonists of A1 adenosine receptors
Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and...
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7084127 |
C2,5′-disubstituted and N6, C2,5′-trisubstituted adenosine derivatives and their different uses
The present invention concerns novel C2,5′-disubstituted and N6′,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adeno...
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7022727 |
Crystalline drug form
The present invention relates to a crystalline form of...
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6995148 |
Adenosine cyclic ketals: novel adenosine analogues for pharmacotherapy
The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor...
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6903079 |
Nucleoside compounds and compositions thereof
The invention provides a novel class of substituted nucleoside derivatives having the formula: A-Z1-L-Z2-G wherein: A and G are connected via Z1 and Z2 respectively, to a linker, L; and A is:...
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6740644 |
Chemical compounds
A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents...
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6642210 |
2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
N-pyrazole substituted 2-adenosine compounds and methods for using the compounds as A2A-adenosine receptor agonists useful to stimulate mammalian coronary vasodilation for therapeutic purposes and...
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6596858 |
Process for the production of 2-halo-6-aminopurine derivatives
A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific...
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6576619 |
Orally active A1 adenosine receptor agonists
Esters of N6-oxa, thia, thioxa and azacycloalkyl substituted adenosine derivatives having the following formula; wherein the compounds are selective adenosine type 1 receptor agonists that are...
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6576620 |
Method of identifying partial adenosine A1 receptor agonists
The present invention provides a method for identifying partial adenosine A1 receptor agonists that are useful in the treatment of arrhythmias. Partial adenosine A1 receptor agonists and methods...
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RE38090 |
3′-substituted nucleoside derivative
The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents a l...
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6531589 |
Base protecting groups and synthons for oligonucleotide synthesis
The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under more mild conditions than existing methods. The invention further...
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6500946 |
Methods for producing nucleoside derivatives and intermediates therefor
Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even...
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6498241 |
2-deoxy-isoguanosines isosteric analogues and isoguanosine derivatives as well as their synthesis
2′-Deoxyisoguanosine, isosteric analogues and isoguanosine derivatives of formulae I-V, processes for their production via compounds of the general formulae a or b and reaction with aroyl i...
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6440948 |
Thiophene A2A receptor agonists
2-(3-,4-(substituted)-5-alkylthienyl)adenosines and the 5′-uronic acid amide analogues thereof having the following formula: are disclosed herein. Additionally disclosed are medicinal methods of t...
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6407076 |
Adenosine analogues and related method of treatment
A compound of formula (I) wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms; and salts and solvates thereof, in...
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6403567 |
N-pyrazole A2A adenosine receptor agonists
2-adenosine N-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic...
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6355787 |
Purine nucleoside modifications by palladium catalyzed methods and compounds produced
This invention discloses a method for the preparation of 2′-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the n...
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6326359 |
Adenosine A2A receptor agonists as antiinflammatory agents
The present invention provides compounds of formula (I): ##STR1##and pharmaceutically acceptable salts and solvates thereof, together with processes for the preparation of, compositions containing,...
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6294522 |
N6 heterocyclic 8-modified adenosine derivatives
N6 heterocyclic 8 modified adenosine derivatives that are selective, partial or full adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity,...
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6271212 |
Prodrug azide compositions and compounds
Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and...
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6221851 |
Pharmaceutical therapy for congestive heart failure
The present invention is directed to reduce elevated levels of tumor necrosis factor-alpha (TNF-α) found in a failing heart. The present invention is directed to a composition and method of ...
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RE37077 |
Adenosine derivatives and pharmaceutical composition thereof
The present invention relates to novel adenosine derivatives having the formula (I): ##STR1##wherein R is a lower alkyl group; R' is hydrogen or a lower alkyl group; X is a cycloalkyl group, an...
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6187914 |
Nucleoside derivatives, and their use in oligonucleotide synthesis
The invention relates to nucleoside derivatives bearing electrolabile protector groupings and their use in an oligonucleotide synthesis method comprising at least one step of electronic deprotection.
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6093807 |
Sugar-modified 7-deaza-7-substituted oligonucleotides
Functionalized nucleomonomers and oligonucleotides are provided which have increased nuclease resistance and enhanced binding affinity to target DNA or RNA molecules. The oligonucleotides of the...
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6015797 |
Adenosinergic agonist containing pharmaceutical composition with analgesic activity
The object of the present invention is a pharmaceutical composition, which comprises, as active principle, a combination of an adenosinergic agonist and a compound selected from the opiates,...
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