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| Number | Title | Issue Date |
| 7786301 | 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... | 08/31/2010 |
| 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 |
| 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 |
| 7335655 | 8-heteroaryl xanthine adenosine Areceptor antagonists The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, ox... | 02/26/2008 |
| 7317017 | Aadenosine 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 |
| 7312223 | Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. ... | 12/25/2007 |
| 7307166 | Oxpurine 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 |
| 7304070 | Aadenosine 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 |
| 7268141 | Xanthine 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: | 09/11/2007 |
| 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 |
| 7235538 | Heterocyclic 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 |
| 7205403 | 8-Heteroaryl xanthine adenosine Areceptor antagonists The present invention relates generally to compounds of the formula (I): wherein: X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected f... | 04/17/2007 |
| 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 |
| 7192962 | Xanthine 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 |
| 7192952 | Heterocyclic compounds that are inhibitors of the enzyme DPP-IV The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that a... | 03/20/2007 |
| 7135475 | Amide substituted xanthine derivatives The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specificat... | 11/14/2006 |
| 7125993 | Aadenosine 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 |
| 7122545 | Imidazo-benzothiazoles The invention relates to 2-imidazo-benzothiazoles of general formula wherein R1, R2, R3, R4, R5, R6, R7, R′, R″, X, R′″ and n a... | 10/17/2006 |
| 7105665 | Aadenosine 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 |
| 7098216 | Thiazolopyrimidines useful as TNFα inhibitors The invention provides derivatives of thiazolo[4,5-d1]pyrimidine and their use as inhibitors of proinflammatory cytokines. ... | 08/29/2006 |
| 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 |
| 7074798 | Xanthine derivative and DPPIV inhibitor The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula: wherein, m is 0 or 1; n is 0; R3... | 07/11/2006 |
| 7019136 | 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,... | 03/28/2006 |
| 7005430 | Fused purine derivatives A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C═O or N═C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a sub... | 02/28/2006 |
| 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 |
| 6977300 | A2B 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 |
| 6930101 | Thiazolopyrimidines useful as TNFα inhibitors The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines. ... | 08/16/2005 |
| 6869947 | Heterocyclic compounds that are inhibitors of the enzyme DPP-IV The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that a... | 03/22/2005 |
| 6825349 | A2B 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 |
| 6815446 | Selective antagonists of A2B adenosine receptors A compound of the following formula: wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The compounds of formula (I) ma... | 11/09/2004 |
| 6806270 | Selective antagonists of A2B adenosine receptors A compound of the following formula: wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The compounds of formula (I) ma... | 10/19/2004 |
| 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 |
| 6653312 | Amidine derivatives, their preparation and application as medicines and pharmaceutical compositions containing same Amidine compounds of the formula ##STR1## wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.... | 11/25/2003 |
| 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 |
| 6608069 | Phenyl 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 |
| 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 |
| 6600044 | Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucl... | 07/29/2003 |
| 6583283 | Polymorphic forms of cipamfylline This invention relates to novel crystalline polymorphic forms, Form I, II and IV of Cipamfylline, methods of preparation, and use thereof in the treatment of PDE4 and TNF mediated diseases. Cipamfylline is 1,3-di-cyclopropylmethyl-8-amino xanthine, and is... | 06/24/2003 |
| 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 |
| 6495687 | A1 adenosine receptor antagonists A compound useful as an A1 adenosine receptor antagonist has the formula: ##STR1## wherein R1 is selected from the group consisting of C1 -C8 alkyl; R2 is of the formula: ##STR2## R3 i... | 12/17/2002 |
