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7576127 |
Aromatic prodrugs of propofol, compositions and uses thereof
Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof...
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7569720 |
Compounds
This invention relates to newly identified ester-linked gemini surfactant compounds, to the use of such compounds and to their production. The invention also relates to the use of the ester-linked...
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7563930 |
Crystal forms of Cinacalcet HCI and processes for their preparation
Provided are crystalline forms of Cinacalet HCl and processes for their preparation.
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7473796 |
Cytotoxic agents comprising new maytansinoids
New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of...
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7439383 |
Sodium channel blockers
The present invention is directed to novel phenytoin derivative compounds and the use of such compounds as sodium channel blockers. Such compositions have utility as anti-cancer agents and can be...
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7419970 |
Cosmetic compositions comprising N-acylamino amides
The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing,...
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7405320 |
Therapeutic and diagnostic conjugates for use with multispecific antibodies
Disclosed are compounds that include two or more haptens conjugated by a spacer or a carrier. The haptens may include diethylenetriaminepentaacetate (DTPA), histimine-succinyl-glutamine (HSG), or...
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7393967 |
Process for the preparation of cinacalcet base
Provided is a process for preparing cinacalcet, (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naph
thalenemethane amine.
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7294735 |
Purification of cinacalcet
Isolated cinacalcet carbamate, processes for the preparation thereof, and processes for the use of cinacalcet carbamate as a reference marker and standard are provided. Also provided are cinacalcet...
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7288670 |
Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using 3,3-dimethylbutyraldehyde precursors
N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester is produced by hydrogenation of L-α-aspartyl-L-phenylalanine 1-methyl ester and 3,3-dimethylbutyraldehyde produced in situ by...
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7253299 |
Process for purifying n2-(1(s)-ethoxycarbonyl-3-phenylpropyl)-n6-thifluoroacetyl-l-lysine
A process for purifying N 2 -(1(S)-ethoxycarbonyl-3-phenylpropyl)-N 6 -trifluoroacetyl-L-lysine which comprises subjecting N 2 -(1(S)-ethoxycarbonyl-3-phenylpropyl)-N 6 -trifluoroacetyl-L-lysine...
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7183317 |
Compounds and methods to increase plasma HDL cholesterol levels and improve HDL functionality
It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may...
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7135587 |
Urea and urethane derivatives as integrin inhibitors
Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5′, X, Y, B, m, n and o are as defined in Patent Claim 1 , and physiologically acceptable salts or solvates...
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7115296 |
N-alkylaspartyl amide derivative and sweetening agent
The present invention relates to a novel N-alkylaspartyl amide derivative, a salt form thereof, a sweetening agent containing the same and a sweetened food or drink containing the N-alkylaspartyl...
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7037939 |
Compound and derivative of gabapentin
The present invention relates to a compound represented as formula (I):
wherein
A is R2-N(R3R4),
wherein Ar is a substituted or unsubstituted phenyl group, m is an integer between 0...
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6992207 |
Melphalan derivatives and their use as cancer chemotherapeutic drugs
The invention refers to new alkylating di- and tripeptides based on a melphalan unit, and one or two additional amino acids or amino acid derivatives, which can be used in the treatment of...
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6989384 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula:
where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds,...
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6989461 |
Catalyst for asymmetric (transfer) hydrogenation
Catalyst for the asymmetric (transfer) hydrogenation represented by the formula ML a X b S c , where M is a transition metal, to be chosen from rhodium and ruthenium, and X is a counter ion and S...
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6972340 |
Selective protein tyrosine phosphatatase inhibitors
Compounds of formula (I)
or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the...
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6949557 |
Hydroanthracene based compounds as anticancer agents
The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing...
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6888022 |
Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions...
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6849649 |
N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally...
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6849648 |
Phenylene alkyne matrix metalloproteinase inhibitors
A compound of Formula I
or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G 1 , G 2 , and B are as defined in the application, are selective inhibitors of...
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6849757 |
Antiangiogenic drug to treat cancer, arthritis and retinopathy
Compounds having Formula I
or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The...
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6844448 |
Main-group metal-based asymmetric catalysts and applications thereof
The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive π-bond of a substrate. The chiral, non-racemic catalysts of the present...
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6841183 |
Process for producing aspartame derivatives, process for purifying aspartame derivatives, production intermediates, and process for producing production intermediates
N-[N-[3-(2-hydroxy-substituted phenyl)propyl]-L-α-aspartyl]-L-phenylalanine 1-methyl ester derivatives, which are useful as sweeteners, may be conveniently produced by subjecting a...
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6838574 |
Dicarba-closo-dodecarborane derivatives
A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I):
wherein R 1 represents a...
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6831193 |
Trisubstituted-N-&lsqb (1S)-1,2,3,4-Tetrahydro-1-naphthalenyl&rsqb benzamides which inhibit P2X3 and P2X2/3 containing receptors
Compounds of formula (I) are novel P2X 3 and P2X 2 /P2X 3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
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6806381 |
Process for the preparation of aniline-derived thyroid receptor ligands
Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
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6803383 |
Inhibition of angiogenesis and tumor growth
Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.
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6794531 |
Process for production of aspartyl dipeptide ester derivative, novel production intermediate therefor, and process for production thereof
The present invention relates to a method of manufacturing aspartyl dipeptide ester compounds, which can be used as sweeteners, and aldehydes that can be used in the manufacturing processes.
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6784309 |
Method for the purification of N-&lsqb N-(3,3-dimethylbutyl)-L-α-aspartyl&rsqb -L-phenylalanine 1-methyl ester
This invention relates to the purification of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester by slurrying a mixture containing...
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6770778 |
N-(4-substituted phenyl)-anthranilic acid hydroxamate esters
The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.
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6761922 |
Sweetener compositions containing aspartyl dipeptide ester compounds
The present invention provides solid and liquid sweetening compositions with a high intensity sweetness containing aspartyl dipeptide ester compounds, processing of making the aspartyl dipeptide...
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6699463 |
Photostable cationic organic sunscreen compounds with antioxidant properties and compositions obtained therefrom
Compounds of Formula I Each R is independently linear or branched C 1 to C 8 alkyl, or linear or branched C 1 to C 8 alkoxy or one R is H and the other R is linear or branched C 1 to C 8 ...
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6689902 |
Arylpropyl aldehyde derivatives, processes for producing the same, and methods of using the same
3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group....
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6677360 |
Biphenyl and biphenyl-analogous compounds as integrin antagonists
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of...
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6657073 |
Crystallization of α-L-aspartyl-L-phenylalanine methyl ester
The present invention provides a novel process for the crystallization of α-L-aspartyl-L-phenylalanine methyl ester crystals wherein initial nucleation and initial crystal growth is conducted in a...
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6652901 |
Sweetener compositions and uses thereof
The present invention provides compositions containing one or more aspartyl dipeptide derivatives represented by formulas (1) and/or (2) mixed with another high intensity sweetner, such Aspartame,...
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6649784 |
Aspartyl dipeptide ester derivatives and sweeteners
Aspartyl dipeptide ester derivatives, such as a N-[N-[3-(3,4-dihydroxyphenyl)-3-methylbutyl]-L-α-aspartyl]-
L-phenylalanine 1-methyl ester, or salts thereof, having a high degree of sweetness...
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6649587 |
Polyamine analog conjugates and quinone conjugates as therapies for cancers and prostate diseases
Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as...
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6646137 |
Non-peptide GnRH agents
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X 1 , X 2 , Y, and Z are defined variables: Such compounds...
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6630600 |
3-aryl propionic acid derivatives and analogs
Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions...
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6613933 |
Process for separating and purifying aspartame and a derivative thereof
A process for easily and efficiently separating aspartame (APM) from N-[N-(3,3-dimethylbutyl)-L-(α-aspartyl]-L-phenylalanine methyl ester (APM derivative), and thus separating and purifying the...
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6610729 |
Hydroxamic acid derivatives and medicinal utilization thereof
The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a...
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6583177 |
Leukotriene B4 antagonist compounds and method for treatment
Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of...
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6569636 |
Assay for modulators of metallo-enzyme activity
An assay is disclosed for determining whether a test compound modulates the activity of an enzyme having a metallated active site. The assay method employs a comparison of the binding ability of...
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6559334 |
Polymers chromatographic separation of enantiomers
The invention relates to novel optically active polymerizable dipeptides, to the process for the preparation thereof, to the polymerization thereof and to the use of the polymers as adsorbents for...
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6509491 |
Aminohydroxylation of olefins in the presence of acetamide
The present invention is a process to prepare on of a phenylisoserine ester of the formula (II) φ—CH(NH—CO—CH 3 )—CH(OH)—CO—O—R 1 with reduced amount of diol by-product by the use...
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6495693 |
N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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