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| Number | Title | Issue Date |
| 8173811 | Apoptosis promoters Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an ant... | 05/08/2012 |
| 7906649 | Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme ... | 03/15/2011 |
| 7601840 | Carboline derivatives useful in the inhibition of angiogenesis In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inh... | 10/13/2009 |
| 7417041 | Imidazopyrimidines as transforming growth factor (TGF) inhibitors Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of tran... | 08/26/2008 |
| 7338963 | Lactam-containing compounds and derivatives thereof as factor Xa inhibitors The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P—M—M4I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle ... | 03/04/2008 |
| 7265128 | 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 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 ... | 09/04/2007 |
| 7230100 | Stereoselective method for the preparation of nucleosides A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, c... | 06/12/2007 |
| 7226929 | Pyrrolidin-2-one derivatives as inhibitors of factor xa The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical con... | 06/05/2007 |
| 7205314 | Compounds for the treatment of dementia related diseases The present invention relates to new compounds of formula (I) wherein Y, P, R1, R2, R3, n, m are defined as in claim 1, a process for their preparation and new intermediates used therein, pharmaceutical composition containing ... | 04/17/2007 |
| 7179910 | 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c... | 02/20/2007 |
| 7074929 | Certain alkylene diamine-substituted heterocycles This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula II, IV, V, VII–IX and X... | 07/11/2006 |
| 7038053 | Process for imidazo[4,5-]pyridin-4-amines A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine and converting a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine to a 1H-imidazo[4,5-c]pyridin-4-amine. | 05/02/2006 |
| 6992188 | Substituted heterocyclic derivatives Corticotropin-releasing factor (CRF) antagonists having the formula wherein the dashed lines, A, B, D E, F, Z, G, R3, and R5 having the definitions set forth in the specification pharmaceutical com... | 01/31/2006 |
| 6984646 | Imidazopyridinones as p38 map kinase inhibitors The invention relates to imidazopyridinones of the formula wherein the groups R1, R2, R3, and R4 are as defined in claim 1, to the process for their preparation, to pharmaceu... | 01/10/2006 |
| 6875772 | [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1 | 04/05/2005 |
| 6867217 | Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety... | 03/15/2005 |
| 6673810 | Imidazo-heterobicycles as factor Xa inhibitors The present application describes imidazo-heterobicycles of formulas I and III: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, speci... | 01/06/2004 |
| 6610692 | Thrombin inhibitors Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N; d is CY3... | 08/26/2003 |
| 6569869 | Annulated azole derivatives useful as microbicidal agents Novel fused azole derivatives of the formula ##STR1## in which R1, R2, A and G are as defined in the description, and also their acid addition salts and metal salt complexes, a plurality of processes for preparing these substances and their us... | 05/27/2003 |
| 6525056 | Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders Corticotropin releasing factor (CRF) antagonists of Formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as wel... | 02/25/2003 |
| 6479506 | Triazolo-pyridine derivatives as ligands for GABA receptors Substituted or 6,7-ring fused 1,2,3-triazolo[4,5-b]pyridine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system.... | 11/12/2002 |
| 6458950 | Compounds and pharmaceutical compositions containing the same A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen,... | 10/01/2002 |
| 6413980 | Nitrogen containing heterobicycles as factor Xa inhibitors The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.... | 07/02/2002 |
| 6387922 | Annulated azole derivatives useful as microbicidal agents Novel fused azole derivatives of the formula ##STR1## in which R1, R2, A and G are as defined in the description, and also their acid addition salts and metal salt complexes, a plurality of processes for preparing these substances and their us... | 05/14/2002 |
| 6288078 | 6-azaindole compounds as 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 men an... | 09/11/2001 |
| 6245769 | Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders Corticotropin releasing factor (CRF) antagonists of Formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as wel... | 06/12/2001 |
| 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 |
| 6156766 | Benzamide compounds and pharmaceutical use thereof Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of... | 12/05/2000 |
| 6110931 | 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... | 08/29/2000 |
| 6046136 | Herbicidal heterocyclic N-oxides compounds This invention relates to novel optionally substituted heterocyclic N-oxide compounds of formula (I): ##STR1## wherein: R, R1, R2, R3, R4, R5, R6, R7, A, X, Z and m are defi... | 04/04/2000 |
| 6025366 | 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... | 02/15/2000 |
| 5912348 | Method of making arylamino triazolopyridines Method for making 4-arylamino-1-alkyl-1,2,3!triazolo4,5-c!pyridines by base-promoted isomerization of 7-alkylamino-3-aryl-1,2,3!triazolo4,5-b!pyridines.... | 06/15/1999 |
| 5910504 | Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula (I) wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one to four nitrogen a... | 06/08/1999 |
| 5874382 | Cyclic sulfonamide herbicides Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C1 -C3 alkyl); N(C1 -C3... | 02/23/1999 |
| 5846990 | Substituted biphenyl isoxazole sulfonamides Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, R3 and R4 are each directly bonded to a ring carbon and are each independently (a) hydrogen;... | 12/08/1998 |
| 5840894 | Preparation of 1,2,4-triazolium salts and 1,2,4-triazolines A process for the preparation of 1,2,4-triazolium salts Ia ##STR1## where R1, and R2 and R3 are C-organic radicals, it being possible for R2 and R3 to be connected to give a 5- to 8-membered ring... | 11/24/1998 |
| 5767141 | Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseases Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseases Propane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the pre... | 06/16/1998 |
| 5719170 | Substituted cyclohexanol esters, their use for treating diseases, and pharmaceutical preparations Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases ... | 02/17/1998 |
| 5679700 | Substituted phosphinic acid-containing peptidyl derivatives as antidegenerative agents Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, perio... | 10/21/1997 |
| 5641783 | Substituted amino alcohol compounds Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R1 and R2 are hy... | 06/24/1997 |
