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| Number | Title | Issue Date |
| 8183365 | Synthetic method for ceratamine A and B and analogs thereof Methods are provided for preparing compounds of the general formula (I) wherein X1 is an aryl hydrocarbon group optionally substituted with one or more groups independently selected from —R, —NH2, ... | 05/22/2012 |
| 7419975 | Organic compounds Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I ... | 09/02/2008 |
| 7384931 | Constrained compounds as CGRP-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodila... | 06/10/2008 |
| 7384930 | Constrained compounds as CGRP-receptor antagonists The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodila... | 06/10/2008 |
| 7323472 | 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof. ... | 01/29/2008 |
| 7307162 | Resolution of a narwedine amide derivative The present invention provides for an efficient method of effecting the resolution of a narwedine amide, and the synthesis of galantamine. ... | 12/11/2007 |
| 7238812 | Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic agents Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallerg... | 07/03/2007 |
| 7229985 | Amorphous substance of tricyclic triazolobenzazepine derivative Disclosed are 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H), 10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine, which has been rendered amorphous and possesses improved absorption and dissoluvability, and a pharmaceutical composition com... | 06/12/2007 |
| 7138408 | HIV integrase inhibitors, pharmaceutical compositions and methods for their use Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the a... | 11/21/2006 |
| 7009047 | Ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenylpropanoate], processes for its preparation and its use The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylenediamine in 2-propanol, and the use of etha... | 03/07/2006 |
| 7002009 | Crystalline tricyclic triazolobenzazepine derivative Disclosed are novel crystalline 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a pharmaceutical composition comprising the same. ... | 02/21/2006 |
| 6958330 | Polycyclic α-amino-ε-caprolactams and related compounds Disclosed are polycyclic α-amino-ε-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of β-amyloid peptide release and/or its synthesis. ... | 10/25/2005 |
| 6916805 | Quinoxalinones as serine protease inhibitors This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable co... | 07/12/2005 |
| 6693101 | v integrin receptor antagonists The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ... | 02/17/2004 |
| 6664249 | Bicyclic vasopressin agonists Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or --CH.dbd.CH--, R1 and R2 are independen... | 12/16/2003 |
| 6632943 | Process for production of optically active pyrroloazepine derivatives It is provided a method for preparing the pyrroloazepine derivatives, especially in optically active form useful as drugs, by low-priced and simple method and in industrial applicable scale, represented by the following formula (I): ##STR1## wher... | 10/14/2003 |
| 6610684 | Fused azepinone cyclin dependent kinase inhibitors A new class of cyclin dependent kinase inhibitors that also have antiproliferative activity in human tumor cell line assays are described. Most of these compounds satisfy the formula ##STR1## wherein A is oxygen or sulfur coupled to the right by a single ... | 08/26/2003 |
| 6602866 | Mercaptoacetylamide derivatives, a process for their preparation and their use This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds. The use of said compounds fo... | 08/05/2003 |
| 6559141 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid... | 05/06/2003 |
| 6544978 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid... | 04/08/2003 |
| 6541466 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid... | 04/01/2003 |
| 6528646 | Intermediates for the synthesis of debromohymenialdisine and process thereof The synthesis of C11 N5 marine sponge alkaloids (&#b1;)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that... | 03/04/2003 |
| 6514964 | Fused cycloheptane and fused azacycloheptane compounds and their methods of use The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as vଲ.sub.3... | 02/04/2003 |
| 6489473 | Pyrroloazepine derivatives A method of effecting serotonin-2-receptor antagonism in a mammal in need thereof, which entails administering to the mammal an effective amount of a compound of the formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein ring P,... | 12/03/2002 |
| 6486315 | Recrystallization processes Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.... | 11/26/2002 |
| 6423840 | Inhibitors of interleukin-1ଲ converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-1ଲ converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also rel... | 07/23/2002 |
| 6410526 | v integrin receptor antagonists The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors vଲ... | 06/25/2002 |
| 6407229 | Processes for the preparation of derivatives of 4a,5,9,10,11,12-hexahydro-6H-benzofuro-[3a,3,2-ef][2] benzazapine The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a,5,9,10,11,... | 06/18/2002 |
| 6372735 | Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as... | 04/16/2002 |
| 6348456 | Method of treating chemical dependency in mammals and a composition therefor An essentially pure noribogaine compound having the formula: ##STR1## wherein R is hydrogen or a hydrolyzable group of the formula: ##STR2## wherein X is an unsubstituted C1 -C12 group or a C1 -C12 group substit... | 02/19/2002 |
| 6340752 | Deprotection and recrystallization processes Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosph... | 01/22/2002 |
| 6313290 | Azolobenzazepine derivatives and compositions and method of use thereof The invention relates to azolobenzazepine derivatives of the formula I: ##STR1## wherein: X is O or S; R1, R2, R3 and R4 are independently hydrogen, perfluorolower-alkyl, halogen, nitro or cyano; and C together ... | 11/06/2001 |
| 6288073 | Acronycine derivatives, preparation method and pharmaceutical compositions A compound selected from those of formula (I): ##STR1## in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents h... | 09/11/2001 |
| 6281227 | Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/28/2001 |
| 6271371 | Oxidative process and products thereof The subject invention concerns a process for the preparation of a compound of formula (2), which comprises phenolic oxidation of a compound of formula (1) ##STR1## wherein X1 and X2 are independently selected from H or a protect... | 08/07/2001 |
| 6268369 | 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines This invention is directed to dihydropyrimidine compounds of the following formula: ##STR1## which are selective antagonists for human receptors. This invention is also related to uses of these compounds for lowering intraocular ... | 07/31/2001 |
| 6218376 | Uracil compounds as P2-purinoreceptor 7-transmembrane G-protein coupled receptor antagonists Compounds of formula I or salts thereof ##STR1## where for example Y is a group of the formula (i) ##STR2## and R1 is a group of formula (ii) ##STR3## are provided along with compositions containing them and processes for their preparation... | 04/17/2001 |
| 6211362 | Pyrroloazepine compounds Disclosed are pyrroloazepine compounds and their salts. These pyrroloazepine compounds are represented by the following formula: ##STR1## wherein the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is ... | 04/03/2001 |
| 6211361 | Method for making debromohymenialdisine and analogs thereof A method for making debromohymenialdisine (DBH) 2 and analogs thereof is described. One embodiment of the present method first comprises forming hymenin 4, and then converting hymenin into DBH 2 as described herein. One such embodiment first comprises pro... | 04/03/2001 |
| 6204261 | Inhibitors of interleukin-1ଲ Converting enzyme inhibitors The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: ##STR1## which compounds are inhibitors of interleukin-1beta converting enzyme.... | 03/20/2001 |
