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| Number | Title | Issue Date |
| 8168826 | Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support The invention is directed to compounds and methods of synthesizing hydroxyethylamino amides and their use in treatment of aspartyl protease mediated diseases and conditions. ... | 05/01/2012 |
| 8039669 | Catalytic metathesis of secondary amides The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demon... | 10/18/2011 |
| 7642379 | Aminoacetonitrile derivatives and their use for controlling parasites on warm-blooded animals The invention relates to compounds of the general formula (I) wherein Ar, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, W, a, b, m, n, o and p are as defined in ... | 01/05/2010 |
| 7385085 | Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein. ... | 06/10/2008 |
| 7378448 | Diphenylether amide derivatives as opioid receptor antagonists A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3′, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mi... | 05/27/2008 |
| 7312360 | Substituted hydroxyethylamines Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds i... | 12/25/2007 |
| 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 |
| 7214715 | Compounds to treat Alzheimer's disease The present invention is substituted amines of formula (X) and of the formula (X′) useful in treating Alzheimer's disease and other similar diseases. ... | 05/08/2007 |
| 7166746 | N-bisaryl- and n-aryl-cycloakylidenyl-αhydroxy-and α-alkoxy acid amides The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12 | 01/23/2007 |
| 7041702 | Pharmaceutically active compounds and methods of use The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly usefu... | 05/09/2006 |
| 6936736 | Amide derivative A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1 is hydogen atom, optionally substituted alkyl, etc.; R2 and R | 08/30/2005 |
| 6855847 | Process for producing optically active amide from α β- unsaturated amide derivative in the presence of transition metal complex containing phosphine-phosphorane compound and transition metal A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an α,β-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is... | 02/15/2005 |
| 6670400 | Phenoxyethylamine derivatives having high affinity for the 5-HT1A receptor, preparation thereof, use thereof as drugs, and pharmaceutical compositions containing said derivatives Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhib... | 12/30/2003 |
| 6653321 | Naphthylsulfonic acids and related compounds as glucose uptake agonists Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptabl... | 11/25/2003 |
| 6506937 | Substituted benzenesulfonylureas and -thioureas-processes for their preparation and their use as pharmaceuticals Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto)alk(oxy)yl, E is O or S; Y is --[CR(3)2 ]n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alky... | 01/14/2003 |
| 6495576 | Aminal diones as potassium channel openers Compounds of formula (I) ##STR1## may be useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal... | 12/17/2002 |
| 6436925 | Substituted benzamides, their production and their use as cysteine protease inhibitors Benzamides of the formula I ##STR1## and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1 --C1 -... | 08/20/2002 |
| 6410749 | Process for the preparation of optically active amino alcohols Process for preparing optically active ଲ-amino alcohols represented by a general formula (2): Ra--C*H(OH)--C*H(Rb)--Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one memb... | 06/25/2002 |
| 6384080 | Anthranilic acid derivatives as inhibitors of the cGMP-phosphodiesterase Compounds of formula (I) ##STR1## where R1 is hydrogen; R2 is nitro, cyano or halo(lower)alkyl; R3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene gr... | 05/07/2002 |
| 6339157 | Synthesis of carboxamides from the catalyzed reaction of aldehydes and amines Aldehydes are catalytically combined with amines to form carboxamides in one step using an oxidant and a metal-ligand complex or metal/ligand composition.... | 01/15/2002 |
| 6323229 | N-acyl and N-aroyl aralkylamides A compound of the formula ##STR1## wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or... | 11/27/2001 |
| 6194612 | Template for solution phase synthesis of combination libraries This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this inven... | 02/27/2001 |
| 6194458 | Benzamide potassium channel inhibitors This invention relates to benzamide potassium channel inhibitors of general structural Formula I. ##STR1## The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and ... | 02/27/2001 |
| 6133315 | Amidino protease inhibitors Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R1 -R4, R6 -R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically ac... | 10/17/2000 |
| 6107511 | Process for the purification or isolation of (2S,3R)-1-halo-2-hydroxy-3-(protected amino)4-phenylthiobutanes or optical antipodes thereof The present invention has for its object to provide a commercially useful, expedient and efficient method for purification and isolation of an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1) or its enantiomer, which is capable of remov... | 08/22/2000 |
| 6090981 | Substituted benzenesulfonylureas and -thioureas--process for their preparation and their use as pharmaceuticals Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(ozy)yl, E is O or S; Y is --[CR(3)2 ]n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or ... | 07/18/2000 |
| 6054457 | Benzamide derivatives and their use as vasopressin antagonists This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower... | 04/25/2000 |
| 6018069 | 2-isoxazoline derivative and process for producing the same and process for producing related derivatives from the same A purified acid addition salt of a (2S, 3S, 5S)-2,5-diamino-1,6-diphenyl-3-hydroxyhexane, e.g., (2S, 3S, 5S)-2-tert-butoxycarbonylamino-3-hydroxy-5-amino-1,6-diphenylhexane, is obtained from its mixture, in an arbitrary ratio, with its (2S, 3S, 5R) s... | 01/25/2000 |
| 5998667 | Substituted biphenyl oxazolines The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R1 represents C1 -C6 -halogenoalkylthio and R2 represents hydrogen, or R1 and R2 together wi... | 12/07/1999 |
| 5985881 | Neurokinin antagonists The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing th... | 11/16/1999 |
| 5972939 | Cyclopentene derivatives useful as antagonists of the motilin receptor The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonis... | 10/26/1999 |
| 5939554 | Diarylaminopropanediol and diarylmethyl-oxazolidinone compounds A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form ... | 08/17/1999 |
| 5922771 | Benzocycloalkene compounds, their production and use A compound of the formula ##STR1## wherein R1 and R2 independently represent H or an optionally substituted hydrocarbon group; R3 represents an optionally substituted hydrocarbon group; R4 represents H or a... | 07/13/1999 |
| 5852007 | Cysteine and serine protease inhibitors containing D-amino acid at the P2 position, methods of making same, and methods of using same The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.... | 12/22/1998 |
| 5696123 | Neurokinin antagonists The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing th... | 12/09/1997 |
| 5693630 | Phenylethyl and phenylpropylamines Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain, m is 2 or 3, R1 is a hydrogen atom, or a straight or branched C1-4 alkyl group,... | 12/02/1997 |
| 5663437 | 2-(N-benzoylimino)-4, 4-diaminobiphenyl A new benzidine monomer composition containing an asymmetrically situated benzamide (iminobenzoyl) group: ##STR1## was prepared from the benzolyation reaction of 4,4'-dinitro-2-biphenylamine and benzoyl chloride, followed by catalytic hydrogenat... | 09/02/1997 |
| 5646329 | Cyclopropylamine derivatives 2-fluoro-cyclopropylamine is prepared in an advantageous manner by reacting an N-vinyl compound with a carbene of type FXC: (where X=chlorine or bromine) to give the corresponding cyclopropylamine derivative, replacing the radical X in this derivative by ... | 07/08/1997 |
| 5637753 | Process for the preparation of N-carbonylarylimines useful in the synthesis of therapeutically active taxoids A process for the preparation of N-carbonylarylimine of the general formula I: ##STR1## in which Ar represent an aryl radical and R represent a phenyl or t-butoxy radical, by desulphonating the compound of the general formula II. ##STR2## T... | 06/10/1997 |
| 5637121 | Poly(oxyalkylene) aromatic amides and fuel compositions containing the same Poly(oxyalkylene) aromatic amides having the formula: ##STR1## or a fuel-soluble salt thereof; wherein a is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group indepen... | 06/10/1997 |
