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| Number | Title | Issue Date |
| 8183373 | Solid state forms of sitagliptin salts Crystalline forms of Sitagliptin salts, processes for preparing crystalline forms of Sitagliptin salts, and pharmaceutical compositions of Sitagliptin salts are provided. ... | 05/22/2012 |
| 8097724 | Process for the preparation of Sitagliptin A process for the preparation of a compound of formula (I) such as 2(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]-7(8H)-pyrazinyl]-1-(2,4,5-trifluorophenyl)-2-butanamine, or a salt thereof, in the anhydrous or hydrated form, either as a mixture ... | 01/17/2012 |
| 8058438 | Eszopiclone process Eszopiclone is prepared by reacting zopiclone with an enatiomerically pure di-p-toluoyl tartaric acid, recovering a solid salt, and reacting a solid salt with a base. Zopiclone is prepared by reacting 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]-... | 11/15/2011 |
| 8017772 | Substituted tetrahydropyrrolopyrazine compounds and the use thereof in the treatment and/or inhibition of pain Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I: processes for their preparation, pharmaceutical compositions comprising these compounds and the use of these compounds for the treatment and/or... | 09/13/2011 |
| 7989621 | Method for producing substituted imidazo[1,2-A]pyrazines of (s)-1-(3-(2-sec-butyl-6-(1h-indol-3-yl)-3-oxo-3,7-dihydroimadazo[1,2-a]pyrazin-8-yl)propyl)guanidine The present invention relates to a method for producing marine ostracod crustacean luciferin or a derivative thereof represented by a general formula (4), characterized by reacting a compound represented by a general formula (2) with a compound represented by a gene... | 08/02/2011 |
| 7968712 | Process for the resolution of zopiclone and intermediate compounds The present invention refers to a process for the resolution into one of its enantiomers of the racemate of compound of formula (I): which comprises separating said one of its enantiomers from a diastereoisomeric salt of fo... | 06/28/2011 |
| 7858788 | Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent. A compound represented by the formula: (wherein | 12/28/2010 |
| 7786304 | Process for the preparation of eszopiclone The invention relates to a process for making 6-(5-chloro-2-pyridinyl)-6,7-dihydro-7-oxo-5H-pyrrolo-[3,4-b]pyrazin-5-yl-4-methyl piperazine-1-carboxylate, also known as zopiclone. The invention further describes an effective method for resolving zopiclone into its e... | 08/31/2010 |
| 7772396 | Process for the resolution of zopiclone and intermediate compounds The present invention refers to a process for the resolution into one of its enantiomers of the racemate of compound of formula (I): which comprises separating said one of its enantiomers from a diastereoisomeric salt of fo... | 08/10/2010 |
| 7732603 | Organic compounds as agents for the treatment of aldosterone mediated conditions Compounds of formula I provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds ... | 06/08/2010 |
| 7732604 | Triazolopyrazine derivatives The invention relates to compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to p... | 06/08/2010 |
| 7626021 | Fused ring heterocycle kinase modulators The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity. ... | 12/01/2009 |
| 7476737 | Eszopiclone process Eszopiclone is prepared by reacting zopiclone with an enatiomerically pure di-p-toluoyl tartaric acid, recovering a solid salt, and reacting a solid salt with a base. Zopiclone is prepared by reacting 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]-... | 01/13/2009 |
| 7435731 | Substituted pyrazolo[3,4-d]pyrimadines and methods of using the same Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invent... | 10/14/2008 |
| 7432265 | Imidazopyrazines as cyclin dependent kinase inhibitors In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of pr... | 10/07/2008 |
| 7425629 | Stereoselective synthesis of certain trifluoromethyl-substituted alcohols A process for stereoselective synthesis of a compound of Formula (I) wherein R1, R2, R3, R4, and R5 are as described herein. ... | 09/16/2008 |
| 7420056 | Substituted bicyclic imidazo-3-ylamine compounds Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related metho... | 09/02/2008 |
| 7405217 | N-aroyl piperazine derivatives as orexin receptor antagonists This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ... | 07/29/2008 |
| 7405295 | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined h... | 07/29/2008 |
| 7405212 | Helix mimetics and composition and methods related thereto Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y,... | 07/29/2008 |
| 7393848 | Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds Compounds of Formula I and all pharmaceutically acceptable forms thereof, are described herein. The variables R1, R2, R3, Z2, and Q, shown in Formula I are defined herein.... | 07/01/2008 |
| 7390809 | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for diabetes The present invention is directed to compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme i... | 06/24/2008 |
| 7388011 | Substituted pyrazoles Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ... | 06/17/2008 |
| 7388019 | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV en... | 06/17/2008 |
| 7365196 | Sulphonamido-substituted bridged bicycloalkyl derivatives A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease. ... | 04/29/2008 |
| 7361656 | Prenyl transferase inhibitors A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH | 04/22/2008 |
| 7348326 | Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAreceptors Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are... | 03/25/2008 |
| 7348324 | Cyclic amine compounds as CCR5 antagonists A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic ... | 03/25/2008 |
| 7342012 | Inhibitors of αβmediated cell adhesion The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. ... | 03/11/2008 |
| 7326708 | Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non-insulin ... | 02/05/2008 |
| 7323484 | Farnesyl transferase inhibitors The present invention is directed to compounds of the formula wherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumor... | 01/29/2008 |
| 7323468 | Pyridopyrazines and the use thereof as kinase inhibitors The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations. | 01/29/2008 |
| 7288651 | Preparation of quinoxaline compounds Certain methods are disclosed that are useful in the preparation of CCK2 active amidophenyl-sulfonylamino-quinoxaline compounds of the formula: wherein R1, R2, Ra and Rb | 10/30/2007 |
| 7288545 | Piperazinedione compounds This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: | 10/30/2007 |
| 7276507 | Pyridopyrazines and the use thereof as kinase inhibitors The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations | 10/02/2007 |
| 7273868 | Pyrazine derivatives 1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, ... | 09/25/2007 |
| 7259161 | Compositions useful as inhibitors of JAK and other protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the inventio... | 08/21/2007 |
| 7259164 | Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pha... | 08/21/2007 |
| 7259250 | C-nitroso compounds and use thereof A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th... | 08/21/2007 |
| 7250417 | Arylmethyl triazolo- and imidazopyrazines as c-Met inhibitors The present invention relates to compounds of the Formulae (I)-(IV), wherein R1-R6, R11-R13, X and Y are defined herein, and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are t... | 07/31/2007 |
