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Class 536/27.13 - Bicyclic ring system consisting of the N-hetero ring fused to another hetero ring (e.g., 2-azaadenines, 6-azaadenines, etc.)


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the N-hetero ring is part of a bicyclic
No. of patents: 136
Last issue date: 04/10/2012


1        
NumberTitleIssue Date
8153781Dendrimer conjugates of agonists and antagonists of the GPCR superfamily
Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A1 aden...
04/10/2012
8114986Analogous compounds of 6-thioguanosine triphosphate, their use in medical fields and processes for their preparation
The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or differen...
02/14/2012
7897759Metabolically stable puromycin analogs
Disclosed are structurally modified, metabolically stable nucleosides having antitumor activity wherein the formation of toxic metabolites is blocked and antimicrobial activity. The disclosure further relates to pharmaceutical compositions comprising one or more dis...
03/01/2011
7863438Stable salt of 3′-phosphoadenosine 5′-phosphosulfate
The present invention provides a stable salt of 3′-phosphoadenosine 5′-phosphosulfate (PAPS) and a production method therefor. The present invention is directed to a stable salt of PAPS (amine salt), which is formed between PAPS and an amine compound, and...
01/04/2011
7563887Universal nucleobase analogs
This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that can bind to nucleic acids, including compositions and processes that by doing so have use in the capture, detection and sequencing of nuc...
07/21/2009
7563886Nucleoside releasing functional unit through oxidation and process for producing oligonucleotide containing thereof
A method of easily releasing a useful substance bonded to oligonucleotide without impairing a target nucleic acid; and a novel base therefore. A nucleoside of nucleotide (oligonucleotide containing thereof) represented by the formula (I)
07/21/2009
7429571Therapeutic furopyrimidines and thienopyrimidines
The invention provides compounds of formula I, II, and III as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula I, II, and ...
09/30/2008
7419963Indole antiviral compositions and methods
The present invention provides novel chemical compounds, and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as...
09/02/2008
7399754N-quinoline or isoquinoline substituted purine derivatives
Novel compound having the following formula: wherein W represents a hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C3-6 cycloalkyl, or an optionally substituted C1-6
07/15/2008
7393954Process for the production of pentostatin aglycone and pentostatin
A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates. ...
07/01/2008
7368437Bicyclic heterocycles, processes for their preparation and their use as herbicides and pharmaceutical agents
Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or pharmacology as, for example, active compounds for crop protection or ph...
05/06/2008
73210333-B-D-ribofuranosylthiazolo [4,5-] pyrimidine nucleosides and uses thereof
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compou...
01/22/2008
7321828System of components for preparing oligonucleotides
Interative, preferably computer based iterative processes for generating synthetic compounds with desired physical, chemical and/or bioactive properties, i.e., active compounds, are provided. During iterations of the processes, a target nucleic acid sequence is prov...
01/22/2008
7282581Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof
The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to Z...
10/16/2007
7273933Methods for synthesis of oligonucleotides
Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether s...
09/25/2007
7227017Process for the preparation of phosphorothioate oligonucleotides
A process for the synthesis of phosphorothioate oligonucleotides is provided which comprises assembling an oligonucleotide bound to a solid support in the presence of acetonitrile; prior to cleaving the oligonucleotide from the solid support removing the acetonitril...
06/05/2007
72178152-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 combinatorial library approaches. Contemplated compounds are particula...
05/15/2007
7202224Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RN...
04/10/2007
7202223Nucleoside compounds for treating viral infections
Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula I as follows: wherein, e...
04/10/2007
7192932Use of immunomodulating agents
Pharmaceutical compositions useful for treating immunosuppressive disease and containing compounds capable of inhibiting cAMP-dependent protein kinase A (PKA) as well as use of the same, are described. ...
03/20/2007
7169916Chloral-free DCA in oligonucleotide synthesis
A process of manufacturing oligonucleotides includes a 5′-deblocking step in which the 5-blocking group is removed with dichloroacetic acid that is essentially free of chloral. The process is useful for making oligonucleotides that are substantially free of chlora...
01/30/2007
7163928Partial and full agonists of Aadenosine 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 myocardial infarction. ...
01/16/2007
7157440Partial 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 myocardial infarction. ...
01/02/2007
7144868Nucleoside compounds for treating viral infections
Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula I as follows: wherein, e...
12/05/2006
7125855Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RN...
10/24/2006
7101994Process for preparing substituted benzimidazole compounds
The invention relates to new methods of preparing substituted benzimidazole compounds, such as 2-bromo-5,6-dichlorobenzimidazole, which are useful in the preparation of compounds having antiviral activity. ...
09/05/2006
7074917Method for purifying 5′ -protected 2′ -deoxypurine nucleosides
A method for efficiently purifying 5′ protected 2′-deoxypurine nucleosides, efficient production of which has previously been difficult. Impurities can be separated by obtaining the 5′ protected 2′-deoxypurine nucleoside as an inclusion crystal including a s...
07/11/2006
7071199Kinase inhibitors as therapeutic agents
The present application is directed to a compound of Formula (I) as defined herein which are useful as kinase inhibitors. ...
07/04/2006
7071173Antiviral methods employing double esters of 2′, 3′-dideoxy-3′-fluoroguanosine
A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig ...
07/04/2006
70453099-substituted adenine derivatives as prodrug regulators of cell and tissue function
The present invention relates to 9-substituted adenine derivatives represented by formula (I) wherein W is selected from the group consisting of H, halogen, azido and amino group; X is selected from the group consistin...
05/16/2006
7019135Anti-viral pyrimidine nucleoside analogues
Compounds of the general formula (I) are described wherein R, R′, R″, Q, T, T′, T″, T″′, W, X, and Z are as defined in the specification. Compounds according to the invention preferably display potent anti-...
03/28/2006
7002006Protection of nucleosides
A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected nucleoside. In some embodiments of the inventive method, an optionally su...
02/21/2006
6974803Pharmaceutical combination
The present invention relates to a combination comprising (a) an adenosine A2a receptor agonist as defined herein and (b) an adrenergic β2 receptor agonist, for simultaneous, sequential or separate administration by the inhaled route in the treatment of ...
12/13/2005
6958214Polymorphic kinase anchor proteins and nucleic acids encoding the same
Polymorphic A-kinase anchor proteins (AKAPs) and nucleic acids encoding the proteins are provided herein. Methods of detecting polymorphic AKAPs and nucleic acids encoding the AKAPs, and kits for use in the detection methods are also provided. Further provided herei...
10/25/2005
6949640Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy...
09/27/2005
6949639Oligonucleotide labeling reactants and their use
The invention relates to a novel labeling reactant of formula (I) suitable for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support t...
09/27/2005
69242713-β-D-ribofuranosylthiazolo[4-5-d]pyridimine nucleosides and uses thereof
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compou...
08/02/2005
6914148Guanidinium functionalized intermediates
The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic,...
07/05/2005
6794502Methods for removing dimethoxytrityl groups from oligonucleotides
The present invention discloses improved methods for oligonucleotide synthesis and purification. In the methods of the invention, a half-life is determined for deprotection of the 5′-OH protecting group at the 5′-terminus of an oligonucleotide post-synthesis. Th...
09/21/2004
6777395Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase of hepatitis C virus
The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RN...
08/17/2004
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