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Patent No. 6295668

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Class 544/267 - At 2- and 6-positions (e.g., theophyllines, etc.)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogens (i.e., oxygen, sulfur, selenium,
No. of patents: 258
Last issue date: 09/14/2010


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NumberTitleIssue Date
7795427Methods for inhibiting osteoclast differentiation, formation, or function and for increasing bone mass
The invention provides methods and compositions for modulating osteoclastogenesis and for treating bone diseases characterized by bone loss or a decrease in bone mass or density, by administering a compound or agent that modulates the adenosine A1 receptor, in parti...
09/14/2010
7425560Thioxanthine derivatives as myeloperoxidase inhibitors
There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for t...
09/16/2008
7423041A1 adenosine receptor antagonists
Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described. ...
09/09/2008
7317017Aadenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract dis...
01/08/2008
7307166Oxpurine nucleosides and their congeners, and acyl, derivatives thereof, for improvement of hematopoiesis
The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The invention also relates to methods of treating or preventing hematopoiet...
12/11/2007
7304070Aadenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract di...
12/04/2007
7247639A1 adenosine receptor antagonists
The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceut...
07/24/2007
7247721Materials and methods for binding nucleic acids to surfaces
Surfaces containing high purity silica (silicon dioxide) exhibit high loading potential for nucleic acids. Formulations containing nucleic acids and materials which mask the electrostatic interactions between the nucleic acids and surfaces are disclosed. By m...
07/24/2007
7235538Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3
06/26/2007
7229473Local delivery of rapamycin for treatment of proliferative sequelae associated with PTCA procedures, including delivery using a modified stent
Methods of preparing intravascular stents with a polymeric coating containing macrocyclic lactone (such as rapamycin or its analogs), stents and stent graphs with such coatings, and methods of treating a coronary artery with such devices. The macrocyclic lactone-bas...
06/12/2007
7223286Local delivery of rapamycin for treatment of proliferative sequelae associated with PTCA procedures, including delivery using a modified stent
Methods of preparing intravascular stents with a polymeric coating containing macrocyclic lactone (such as rapamycin or its analogs), stents and stent graphs with such coatings, and methods of treating a coronary artery with such devices. The macrocyclic lactone-bas...
05/29/2007
7217286Local delivery of rapamycin for treatment of proliferative sequelae associated with PTCA procedures, including delivery using a modified stent
Methods of preparing intravascular stents with a polymeric coating containing macrocyclic lactone (such as rapamycin or its analogs), stents and stent graphs with such coatings, and methods of treating a coronary artery with such devices. The macrocyclic lactone-bas...
05/15/2007
7202252Aadenosine receptor antagonists
Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described. ...
04/10/2007
7192962Xanthine phosphodiesterase V inhibitor polymorphs
Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those show...
03/20/2007
7148229Sulfonamide substituted xanthine derivatives
The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl sub...
12/12/2006
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
7125993Aadenosine receptor antagonists
Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the formula (3):
10/24/2006
7105665Aadenosine receptor antagonists
Disclosed are methods for making novel A2B adenosine receptor antagonists having the structure of formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastro...
09/12/2006
7074923Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof
A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to sy...
07/11/2006
7053096Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. ...
05/30/2006
6977300A2B adenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorder...
12/20/2005
6894040Xanthine phosphodiesterase V inhibitors
A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:
05/17/2005
6825349A2B adenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists compounds having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal trac...
11/30/2004
6821978Xanthine phosphodiesterase V inhibitors
A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:
11/23/2004
6787548Thienopyrimidines as phosphodiesterase inhibitors
Thienopyrimidines of the formula I and their physiologically acceptable salts, in which R1, R2 and X have the meanings indicated in claim 1, exhibit phosphodiesterase V inhibition and ...
09/07/2004
6780865Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. The disclosed compounds have a structure of formula I: ...
08/24/2004
6774130Therapeutic compounds for inhibiting interleukin-12 signaling and methods for using same
Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intrace...
08/10/2004
6734187Purine derivatives and medicaments comprising the same as active ingredient
Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl gr...
05/11/2004
6723727Substituted purine derivatives, processes for their preparation, their use, and compositions comprising them
The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their p...
04/20/2004
6693105Hydroxyl-containing compounds
Disclosed are therapeutic compounds having the formula: including resolved enantiomers, diastereomers, hydrates, salts, solvates or mixtures thereof where j is an integer from one to three. The core moiety is a bicyclic ring structure having at least one heter...
02/17/2004
6649600Adenosine receptor antagonists and methods of making and using the same
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be usefull in the prevention and/or treatment of n...
11/18/2003
6608069Phenyl xanthine derivatives
The present invention relates to novel compounds of formula (I): ##STR1## wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally co...
08/19/2003
6605600Adenosine receptor antagonists and methods of making and using the same
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of nu...
08/12/2003
6518425Method of manufacture of 1,3-oxathiolane nucleosides
Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the process...
02/11/2003
6437125Process for the production of purine derivatives
The invention provides a method of rearranging a compound of formula (I), wherein R and R' are selected independently from hydrogen and C1-12 alkyl; and R1 and R2 are selected independently from hydrogen, hydroxy, halo, C
08/20/2002
6413975Purine derivatives having phosphodiesterase iv inhibition activity
Disclosed are compounds of the formula: ##STR1## wherein R3, R6a, R6b and R8 are substituted as disclosed herein. The compounds are effective in effecting PDE IV inhibition in patients in need thereof....
07/02/2002
6333331Substituted O6-benzylguanines
The present invention provides AGT inactivating compounds such as substituted O6 -benzylguanines of the formula ##STR1## 7- or 9-substituted 8-aza-O6 -benzylguanines, 7,8-disubstituted O6 -benzylguanines, 7,9-disubstituted...
12/25/2001
6268373Trisubstituted thioxanthines
Disclosed is a compound selected from the group consisting of 1,3,8-triethyl-2,6-dithioxanthine; 1,3,8-triethyl-2-thioxanthine; 8-cyclopropyl-1-ethyl-3-(2-methyl-butyl)-6-thioxanthine; 1,3-diethyl-8-isopropyl-6-thioxanthine; 8-cyclopropyl-1,3-dipropy...
07/31/2001
62588096-aryloxy and arylthiopurines
Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: ...
07/10/2001
6252075Process for producing purine derivatives
A process for preparing 7-benzylpurine derivatives is provided. An acetylpurine nucleoside is reacted with a benzyl halide to benzylate the 7-position of the purine base, and an acid is then added to the reaction mixture to hydrolyze the glycoside bond. T...
06/26/2001
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