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| Number | Title | Issue Date |
| 8138346 | Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R | 03/20/2012 |
| 7629468 | Metabotropic glutamate receptor antagonists The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C | 12/08/2009 |
| 7375227 | Quinoline derivatives The invention relates to novel 1-pyridin-4-yl urea derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the com... | 05/20/2008 |
| 7368573 | Triamide-substituted heterobicyclic compounds This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the ... | 05/06/2008 |
| 7314939 | Compositions and methods for inhibiting TGF-β The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R... | 01/01/2008 |
| 7223774 | Benzamide 2-hydroxy-3-diaminoalkanes The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the... | 05/29/2007 |
| 7173135 | Substituted 3-cyanoquinolines as MEK inhibitors The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmac... | 02/06/2007 |
| 7173136 | 3-Cyano-quinoline derivatives The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmac... | 02/06/2007 |
| 7074933 | Urea and thiourea derivatives The invention is directed to a new class of quinolin-zene and z-exc chromen compounds that have been derivatized at the 6-position with a urea or this urea moet, and to then use as androgen antagonists. ... | 07/11/2006 |
| 7001913 | Aminopiperidine derivatives as antibacterials Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. ... | 02/21/2006 |
| 6930185 | Melanin-concentrating hormone antagonist A melanin-concentrating hormone antagonist comprising a compound of the formula (I): wherein Ar1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main c... | 08/16/2005 |
| 6881753 | Potassium channel inhibitors and method Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined... | 04/19/2005 |
| 6875764 | Urea and thiourea compounds useful for treatment of coccidiosis The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coc... | 04/05/2005 |
| 6818655 | Urotensin-II receptor antagonists The present invention relates to quinolines, pharmaceutical compositions containing them and their use as antagonists of urotensin II. ... | 11/16/2004 |
| 6613901 | 2-aminoalkylaminoquinolines as dopamine D4 ligands Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein: R1, R2, and R3 are as defined herein; R6 is hydrogen or C1 -C6 alkyl; and Q repr... | 09/02/2003 |
| 6602882 | Quinoline derivatives and their use as antibacterial agents Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.... | 08/05/2003 |
| 6495693 | N-(aryl/heteroaryl) amino acid derivatives, 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... | 12/17/2002 |
| 6482951 | Isoindolin-1-one glucokinase activators Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.... | 11/19/2002 |
| 6387926 | Inhibitors of farnesyl protein transferase Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment ... | 05/14/2002 |
| 6313141 | 2-aminoalkylaminoquinolines as dopamine D4 ligands Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: A represents an optionally substituted alkylene group of from 2-5 carbon atoms; W is COH or CH; Y and Z are nitrogen or CH; and R1, R2 | 11/06/2001 |
| 6281216 | 2-aminoquinoline derivatives having d4-agonistic activity The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, ... | 08/28/2001 |
| 6255323 | Cyanoguanidine compounds A cyanoguanidine compound of the following formula: ##STR1## is disclosed. A cyanoguanidine compound of the present invention possess a high specificity for tumor cells. Also disclosed are methods for preparing a cyanoguanidine compound.... | 07/03/2001 |
| 6174897 | Bis-(quinolyl)-diamines The present invention relates to bis-(quinolyl)-diamines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides a process for the preparation of the compounds of the formula ... | 01/16/2001 |
| 6103739 | Metalloproteinase inhibitors A compound of general formula (I), wherein X is a group of formula (II) or (III), R2, R1, R21, R3, R4, and R5 being as defined in the specification are matrix metalloproteinase inhibitors.... | 08/15/2000 |
| 5972945 | 2-aminoalkylaminoquinolines; dopamine receptor subtype specific ligands Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein: R1, R2, and R3 are as defined herein; R6 is hydrogen or C1 -C6 alkyl, and Q repres... | 10/26/1999 |
| 5958947 | DNA-affinic hypoxia selective cytotoxins Hypoxia selective cytotoxins having the structural formula ##STR1## wherein D, E, F and G, independently, are carbon or nitrogen, with the proviso that three or more of D, E, F and G are carbon; R1 and R2, independently, are sel... | 09/28/1999 |
| 5948791 | Quinoline derivatives for treating malaria The invention relates to novel quinoline derivatives and their therapeutic use against malaria.... | 09/07/1999 |
| 5866579 | Imidazole and imidazoline derivatives and uses thereof This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human 댒 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease... | 02/02/1999 |
| 5770734 | N-substituted-2-aminoquinolines useful for treating hypofunction of the cholinergic system R2 is H, alkyl of 1 to 6 carbon atoms, cyano, halo, nitro, amino or mono or dialkylamino in which the alkyl groups have 1 to 6 carbon atoms; R3 is H or alkyl of 1 to 6 carbon atoms; n is 1 to 5 and R4 and R5 taken with th... | 06/23/1998 |
| 5739134 | N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2h-benzopyran, dihydrobenzodioxin, benzodioxole, dihydrobenzodioxepin, or tetrahydrobenzoxepin)carboxamide derivatives N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing ... | 04/14/1998 |
| 5736557 | N,N-bis (quinolin-4-yl)-diamine derivatives, their preparation and their use as antimalarials Disclosed are N,N'-bis(quinolin-4-yl)diamine derivatives of general formula I wherein R1 signifies halogen or trifluoromethyl, R2 signifies hydrogen or halogen, A signifies cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3-diyl, cyclohe... | 04/07/1998 |
| 5698581 | Substituted N-heteroaroylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing them The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly sui... | 12/16/1997 |
| 5674894 | Amidine derivatives useful as platelet aggregation inhibitors and vasodilators The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.... | 10/07/1997 |
| 5596002 | Method of treating chloroquine-resistant malaria with aminoquinoline derivatives Novel aminoquinoline derivatives of the general formula ##STR1## are described. Also described are methods for the treatment of malaria pathogens, particularly chloroquine-resistance malaria pathogens with compounds of formula I or the pharmaceutical... | 01/21/1997 |
| 5508288 | Indole derivatives as 5HT1C antagonists A compound of formula (I) or a salt thereof: ##STR1## Wherein: P represents a quinoline or isoquinoline residue; R1 is hydrogen or C1-6 alkyl; R2, R3, R10, R11 are independently hydrog... | 04/16/1996 |
| 5476935 | Dyes for use in thermal dye transfer Dye-donor element for use according to thermal dye transfer comprising least one dye corresponding to the general formula (I): ##STR1## wherein Z is --CN, --COOR1 or --CONR2 R3 ; R1 is --H, (cyclo)alkyl, or... | 12/19/1995 |
| 5461049 | Amide tetrazole ACAT inhibitors Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R5, or --NR3 R4, where R2, R4, and R5 include alk... | 10/24/1995 |
| 5436338 | Heterocyclic formamidines useful as ultraviolet light absorbers Novel substituted heterocyclic formamidines are useful as ultraviolet light absorbers, the formamidines having the formula ##STR1## wherein: Ar represents a 2-thiazolyl, 2-pyridyl, 2- 4,6-dimethyl) pyrmidyl or a 4-(2-methyl)quinolyl group, and, R rep... | 07/25/1995 |
| 5399697 | N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R1 is thienyl, im... | 03/21/1995 |
| 5356903 | 1-cyclopropyl-4-pyridyl-quinolines Compounds of formula ##STR1## wherein; R1 is hydrogen, lower-alkyl, or trifluoromethyl; R2 is lower-alkyl, trifluoromethyl or CH2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino; R3 and R | 10/18/1994 |
