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Class 544/264 - Purines (including hydrogenated)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 366
Last issue date: 08/31/2010


1                    
NumberTitleIssue Date
7786300Process for preparation of entecavir and novel intermediates thereof via carbon-silicon oxidation
Processes for preparing entecavir and novel intermediates thereof using carbon-silicon oxidation. ...
08/31/2010
7511139Process for the preparation of entecavir and novel intermediates thereof via carbon-silicon oxidation
Processes for preparing entecavir and novel intermediates thereof using carbon-silicon oxidation. ...
03/31/2009
7468436Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers
A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (−)-2-hydroxymethyl-5-(5-f...
12/23/2008
7439359Small molecule compositions for binding to hsp90
Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with a...
10/21/2008
7432272Antiviral analogs
The application relates to 4′-substituted nucleoside derivatives of Formula I: wherein B and R1 have any of the values described in the application, as well as to compositions comprising such compounds, to meth...
10/07/2008
7427616Condensed pyridines and pyrimidines with tie2 (TEK) activity
A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms selected from O, N and S, and wherein the 5-membered ring containing G ...
09/23/2008
7407962Heteroaryl compounds useful as inhibitors or protein kinases
The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmac...
08/05/2008
73717372-substituted-6-trifluoromethyl purine derivatives with adenosine-Aantagonistic activity
The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful fo...
05/13/2008
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
7368086Functionalized fluorescent nanocrystals, and methods for their preparation and use
Functionalized fluorescent nanocrystal compositions and methods for making and using these compositions are disclosed. The compositions are fluorescent nanocrystals coated with at least one material. The coating material has chemical compounds or ligands with functi...
05/06/2008
7358273Inhibitors of caspases
The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and...
04/15/2008
7351827Substituted oxetanes, method of making, and method of use thereof
Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation...
04/01/2008
7335654Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
02/26/2008
7321035Process for producing 2,6-dihalogenopurine
A process for conveniently and efficiently preparing a 2,6-dihalogenopurine using an inexpensive starting material. A process for preparing a 2,6-dihalogenopurine, comprising treating a 2-amino-6-halogenopurine having a protective group at 7th position or...
01/22/2008
7317018Anti-inflammatory medicament
The use of adenosine-5′-triphosphate-2′,3′-dialdehyde (oATP) as a medicament useful for the treatment of inflammatory conditions is disclosed. ...
01/08/2008
731222921-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the ute...
12/25/2007
7307167Production method of 2,6-dihalopurine
By reacting the compound of the formula [Ia] or [Ib] with halosilane compound and an agent for diazo reaction, 2,6-dihalopurine of the formula [II] can be produced conveniently in a high yield and can be easily isolated, wherein each symbol is as defined in the spec...
12/11/2007
7300923Partial 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 tachycardia and atrial flutter, angina, and myocardial infa...
11/27/2007
7285288Inhibition of Bcl-2 protein expression by liposomal antisense oligodeoxynucleotides
The present invention provides novel compositions and methods for use in the treatment of Bcl-2-associated diseases like cancer, specifically, in the treatment of follicular lymphoma (FL). The compositions contain antisense oligonucleotides that hybridize to Bcl-2 n...
10/23/2007
7285558Pyrazolo[3,4-d]pyrimidines inhibiting infections
Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection. ...
10/23/2007
7271157Aadenosine receptor agonists
Disclosed is a synthesis suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonist having the structure of Formula I: wherein R is optionally subst...
09/18/2007
7256196Purine cytokine inhibitors
The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions c...
08/14/2007
7256275Methods, kits and compositions pertaining to combination oligomers and libraries for their preparation
This invention pertains to the field of combination oligomers, including the block synthesis of combination oligomers in the absence of a template, as well as related methods, kits, libraries and other compositions. ...
08/14/2007
7253154Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which m...
08/07/2007
7244847Benzimidazole compounds
The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods...
07/17/2007
7223879Ligands for metals and improved metal-catalyzed processes based thereon
One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. ...
05/29/2007
721772017-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uteru...
05/15/2007
7211667Antagonists of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of m...
05/01/2007
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
7189730Aadenosine receptor antagonists
Disclosed are novel A2A adenosine receptor antagonists of the formula: wherein: R1 is optionally substituted aryl or optionally substituted heteroaryl;
03/13/2007
7176312Kinase inhibitor scaffolds and methods for their preparation
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...
02/13/2007
7148226Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The ...
12/12/2006
71482234′-thio-L-xylo furanosyl nucleosides, precursors thereof, preparation and use thereof
Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or...
12/12/2006
7138399Alkoxypyridine-derivatives
The compounds of formula I in which R1 is 1–4C-alkoxy, A is 1–4C-alkylene, B represents 3H-imidazo[4,5-b]pyridin-2-yl, 3H-imidazo[4,5-b]pyridin-2-yl substituted by R2 and/or R3, 9H-purin-8-yl or 9H-purin-8-yl...
11/21/2006
7135564Reusable solid support for oligonucleotide synthesis
A reusable linker arm for solid support oligonucleotide synthesis, the linker arm comprising formula (a) wherein Z is a linker moiety and T is an organic radical. A method for adding one or more nucleosides on the linker arm is also described
11/14/2006
7129239Purine compounds and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. ...
10/31/2006
7102023Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries
One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention ...
09/05/2006
7098197Phosphonate compounds
The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and th...
08/29/2006
7094772Phosphonate compounds
The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and th...
08/22/2006
RE39112Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically...
05/30/2006
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