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| Number | Title | Issue Date |
| 7425560 | Thioxanthine 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 |
| 7423041 | A1 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 |
| 7247639 | A1 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 |
| 7202252 | Aadenosine 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 |
| 7074923 | Process 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 |
| 6649600 | Adenosine 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 |
| 6605600 | Adenosine 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 |
| 6518425 | Method 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 |
| 6437125 | Process 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 |
| 6413975 | Purine 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 |
| 6333331 | Substituted 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 |
| 6268373 | Trisubstituted 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 |
| 6258809 | 6-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 |
| 6252075 | Process 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 |
| 6248746 | 3-(arylalkyl) xanthines With the above and other objects in view, the present invention comprises compounds having the general formula (I): ##STR1## wherein: R1 is a C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, C... | 06/19/2001 |
| 6245910 | Process for producing purine derivatives Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of natural purine nucleosides obtained through fermentation or... | 06/12/2001 |
| 6183711 | Apatite-forming-systems: methods and products Methods comprise contacting apatite-forming-systems with partially alkylated xanthines. The methods include pharmaceutical applications of partially alkylated xanthines to mitigate the effects of hard tissue diseases. Products comprise apatite formed from... | 02/06/2001 |
| 6124288 | Xanthines and their therapeutic use The subject invention concerns a compound of the formula (i): ##STR1## in which Q represents heteroaryl or heterocyclo optionally substituted with one or more substituents selected from the group consisting of C1-6 alkyl (optionally substi... | 09/26/2000 |
| 6090816 | Aryl thioxanthines Disclosed are compounds having the formulae: ##STR1## wherein: Q3,Q6a,Q6b and Q8 are independently a bond, C1-8 alkylene, C2-8 alkenylene and C2-6 alkynylene, and R3, ... | 07/18/2000 |
| 6087497 | Process for producing purine derivatives 9-Substituted purine derivatives of formula (4) ##STR1## are prepared by debenzylating a compound of formula (3): ##STR2##... | 07/11/2000 |
| 6083954 | Method of treating cystic fibrosis The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I, which ... | 07/04/2000 |
| 6066641 | Aryl thioxanthines The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q3 R3 and Q8 R8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with reg... | 05/23/2000 |
| 6025361 | Trisubstituted thioxanthines Disclosed are compounds of formula (I), wherein R1, R3 and R8 are independently alkyl, aryl or aralkyl, and R2 is selected from the group consisting of S and O, R6 is selected from the group consistin... | 02/15/2000 |
| 5994361 | Substituted purinyl derivatives with immunomodulating activity The present invention comprises a compound of formula I: ##STR1## R1 of Formula I is substituted amino represented by formula NR5 R6 wherein R5 and R6 are independently selected from the group co... | 11/30/1999 |
| 5977119 | Trisubstituted thioxanthines Disclosed are compounds of the formula: ##STR1## wherein R1, R3 and R8 are independently alkyl, aryl or aralkyl, and R2 is selected from the group consisting of S and O, R6 is selected from the g... | 11/02/1999 |
| 5942617 | Process 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... | 08/24/1999 |
| 5919426 | Products of apatite-forming-systems Products comprise apatite formed from apatite-forming-systems contacted with partially alkylated xanthines.... | 07/06/1999 |
| 5919789 | Xanthines and their therapeutic use Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase.... | 07/06/1999 |
| 5877179 | Xanthines for identifying CFTR--binding compounds useful for activating chloride conductance in animal cells The present invention provides novel compounds and pharmaceutical compositions comprising such compounds useful for treating cystic fibrosis cells, wherein such compounds have the formula ##STR1## wherein (a) R1 and R3 are methy... | 03/02/1999 |
| 5861405 | S-substituted 1,3,7-trialkyl-xanthine derivatives The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1#... | 01/19/1999 |
| 5831092 | Process for producing purine derivatives Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of natural purine nucleosides obtained through fermentation or... | 11/03/1998 |
| 5821366 | Xanthines and their therapeutic use 1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition.... | 10/13/1998 |
| 5770595 | Oxime substituted therapeutic compounds Oxime-substituted compounds are preferably cyclic or heterocyclic compounds. The oxime-substituted compounds and pharmaceutical compositions thereof have the formula: CORE MOIETY--(R)j including resolved enantiomers (both syn and anti forms) and/or ... | 06/23/1998 |
| 5756735 | Xanthine derivatives The present invention relates to novel xanthine derivatives of the formula (I) which are selectively antagonistic to an adenosine A2 receptor, and pharmaceutically acceptable salts thereof. Formula (I): ##STR1## In the formula, R1 | 05/26/1998 |
| 5734052 | 8-substituted xanthines as selective adenosine receptor agents Xanthine derivatives having general structure (I) including the (R) and (S) enantiomers and racemic mixtures thereof, and the pharmaceutically acceptable salts thereof, wherein R1 and R2 are each independently (C1 -C4... | 03/31/1998 |
| 5719279 | Asymmetrically substituted xanthines Xanthine derivatives of formula ##STR1## wherein R1 is hydrogen, alkyl or alkynyl, R2 is different and is alkyl, alkynyl, phenyl-alkylene, phenyl alkenylene, cycloalkyl, inter alia, R3 is cycloalkyl, phenyl, norbornane, in... | 02/17/1998 |
| 5688947 | Production of purines via reductive formylation In order to produce a purine of the general formula (I), ##STR1## in which R1 and R2 can be the same or different and denote H, OH, SH, NH2, N-(di)-alkyl, halogen, O-alkyl, S-alkyl, alkyl or aryl and alkyl represents ... | 11/18/1997 |
| 5674998 | C-4' modified adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo2,3-d!pyrimidine and pyrazolo3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside ... | 10/07/1997 |
| 5675005 | Process for preparing xanthine derivatives, in particular 1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine This invention relates to a process for preparing xanthine derivatives of formula I: ##STR1## characterized in that a uracil derivative of formula A or B ##STR2## is dissolved in a suitable organic-aqueous solvent and cyclized in the presen... | 10/07/1997 |
| 5545627 | Irreversible inhibitors of adenosine receptors Irreversible ligands for adenosine receptors are derived from agonist and antagonist functionalized congeners which contain electrophilic acylating and alkylating groups for reaction at nucleophilic residues of adenosine receptors. The ligands are based o... | 08/13/1996 |
