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| Number | Title | Issue Date |
| 7820815 | Process for the preparation of chiral 8-(-3-aminopiperidin-1-yl) xanthines The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof | 10/26/2010 |
| 7407955 | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs t... | 08/05/2008 |
| 7361661 | 8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alken... | 04/22/2008 |
| 7358235 | Analogs of nitrobenzylthioinosine Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical composition... | 04/15/2008 |
| 7342006 | Substituted 8-heteroaryl xanthines Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents. ... | 03/11/2008 |
| 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 |
| 7148229 | Sulfonamide 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 |
| 7087599 | Estrogen receptor modulators The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a v... | 08/08/2006 |
| RE39056 | 4-Azasteroids for treatment of hyperandrogenic conditions Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula... | 04/04/2006 |
| 6998484 | Synthesis of purine locked nucleic acid analogues The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic ... | 02/14/2006 |
| 6919337 | 8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, ... | 07/19/2005 |
| 6911440 | Phthalazine derivatives for treating inflammatory diseases The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, ... | 06/28/2005 |
| 6774130 | Therapeutic 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 |
| 6774129 | Benzothieno[3,2-c]pyridines as α2 antagonists The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, ... | 08/10/2004 |
| 6723727 | Substituted 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 |
| 6686347 | Phthalazine derivatives for treating inflammatory diseases The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, ##STR1## the substituents ... | 02/03/2004 |
| 6664043 | Acridinium ester labels having hydrophilic modifiers The present invention is generally directed to detectable chemiluminescent acridinium ester labels having hydrophilic modifiers; to compositions, complexes and/or conjugates which include such labels; and to processes for performing bioanalytical assays f... | 12/16/2003 |
| 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 |
| 6573044 | Methods of using chemical libraries to search for new kinase inhibitors The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibit... | 06/03/2003 |
| 6562814 | 3-thioxo-[1,2,4]-oxadiazinan-5-one derivatives ##STR1## wherein R is alkyl, alkenyl, or alkynyl; R1 and R2 are each independently hydrogen alkyl, or aryl; and Ar is phenyl, indanyl, benzhydryl, or phenyl, substituted with one or more groups selected from the group consisting of halogen, al... | 05/13/2003 |
| 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 |
| 6514974 | Pyrido-, pyrimido-, pyridazo- and pyrazo- pyridazines having angiogenesis inhibiting activity The invention relates to compounds of formula I, ##STR1## wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* ##STR2## or (iii) together fo... | 02/04/2003 |
| 6495555 | Tricyclic Ɗ-3-piperidines as 댒-antagonists The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6 alkanediyl; n is 1 or 2; X1 is --... | 12/17/2002 |
| 6426350 | Benzothieno[3,2-c]pyridines as 댒 antagonists The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6 a... | 07/30/2002 |
| 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 |
| 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 |
| 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 |
| 6166019 | Piperazinyl pyrimidine dione compounds selective for adrenoceptors Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states.... | 12/26/2000 |
| 6159975 | Antagonists of gonadotropin releasing hormone There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both m... | 12/12/2000 |
| 6156757 | 1,2,3,4-tetrahydro-benzofuro[3,2-C]pyridine derivatives The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6 | 12/05/2000 |
| 6143744 | Sulfamide-metalloprotease inhibitors This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.... | 11/07/2000 |
| 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 |
| 6103730 | Amine substituted compounds Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula: CORE MOIETY--(R)j In these compounds, j is an integer from one to three; the core moiet... | 08/15/2000 |
| 6100271 | Therapeutic compounds containing xanthinyl Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula: CORE MOIETY --(R)j wherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R m... | 08/08/2000 |
| 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 |
| 6075029 | Xanthine modulators of metabolism of cellular P-450 A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These compounds generally are useful in affecting drug metabolism ... | 06/13/2000 |
| 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 |
| 6046207 | Benzopyranopyrrole and benzopyranopyridine -1 adrenergic compounds The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are -1 adrenergic antagonists and are useful in the treatment of BPH; also ... | 04/04/2000 |
| 6043228 | O6 -substituted guanine derivatives, a process for their preparation and their use in treating tumor cells O6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR', wherein X is O or S, R" and R"' are alkyl, or substituted derivatives thereof, R' is H, or alkyl or hydroxyalkyl R ... | 03/28/2000 |
