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...that Charles Goodyear performed some of his experiments on rubber while in debtor's prison? He was there so often he referred to it as his "hotel". Chronically in debt because of poor business sense and ill health, Goodyear depended on the generosity of friends and family. Even after he unlocked the secret to vulcanizing rubber, he was unable to improve his financial situation. When he died, his estate was $200,000 in debt.

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Attorney: Lewis; Donald G.


Number of patents: 144
Last date: August 25, 2009

1        
NumberTitleIssue Date
7579366Epothilone derivatives and their synthesis and use
The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; ...
08/25/2009
7410998Inhibitors of NADH:ubiquinone oxidoreductase
Benzopyran-based inhibitors of NADH:ubiquinone oxidoreductase for inhibiting the growth of cancer cells. ...
08/12/2008
7408026Synthesis of proteins by native chemical ligation
Proteins of moderate size having native peptide backbones are produced by a method of native chemical ligation. Native chemical ligation employs a chemoselective reaction of two unprotected peptide segments to produce a transient thioester-linked intermediate. The t...
08/05/2008
7375234Copper-catalysed ligation of azides and acetylenes
A metal catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to give triazoles. In many instances, the reaction sequence regiospecifically ligates azides and terminal acetylenes to give only 1,4-disubstituted [1,2,3]-triazole...
05/20/2008
7358266Cyclopropyl and cyclobutyl epothilone analogs
The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and ...
04/15/2008
7351724Oxadiazole ketone inhibitors of fatty acid amide hydrolase
Certain oxadiazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the ...
04/01/2008
7348173Fatty-acid amide hydrolase
The soporific activity of cis-9,10-octadecenoamide and other soporific fatty acid primary amides is neutralized by hydrolysis in the presence of fatty-acid amide hydrolase (FAAH). Hydrolysis of cis-9,10-octadecenoamide by FAAH leads to the formation of oleic acid, a...
03/25/2008
7312361Inhibitors of transthyretin amyloid fibril formation
Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin. ...
12/25/2007
7288623Cyclic peptide tube
Cyclic homodetic peptides having a repeating D-L-chirality motif are shown to have a stable disk conformation with the amino acid side chains extending radially outward and the carbonyl and amino groups extending axially upward or downward. Such cyclic peptides can ...
10/30/2007
7250409Ningalin B analogs employable for reversing multidrug resistance
Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell line (HCT116/VM46), with respect to a variety of cytotoxic agents, e.g....
07/31/2007
7173137Epothilone analogs
Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of micro...
02/06/2007
7169930Analogs of epothilone
Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog wi...
01/30/2007
7135279D-enzyme compositions and methods of their use
D-enzyme compositions are described comprising an amino acid residue sequence that defines an polypeptide able to catalyze an enzymatic reaction. The D-enzyme has an amino acid residue sequence consisting essentially of D-amino acids ...
11/14/2006
7135578Iminocyclitol inhibitors of hexoaminidase and glycosidase
Designed imminocyclitols have potent inhibition activity with respect to hexoaminidases and glycosidases. ...
11/14/2006
7126006Glycoluril core molecules for combinatorial libraries
The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinato...
10/24/2006
7118856D-enzyme compositions and methods of their use
D-enzyme compositions are described comprising an amino acid residue sequence that defines an polypeptide able to catalyze an enzymatic reaction. The D-enzyme has an amino acid residue sequence consisting essentially of D-amino acids. ...
10/10/2006
7019131Programmable one-pot oligosaccharide synthesis
The reactivity of a number of p-methylphenyl thioglycoside (STol) donors which are either fully protected or have one hydroxyl group exposed has been quantitatively determined by HPLC in conjunction with the development of a broadly applicable approach for a facile ...
03/28/2006
7015321Synthesis of non-symmetrical sulfamides using burgess-type reagents
A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N′-differentiated sulfamides employs a wide range of amino alcohols and simple amines using Burgess-type reagents. This methodology extends the application and avail...
03/21/2006
6921810Bifunctional antibiotics
Bifunctional antibiotics that target both bacterial RNA and resistance-causing enzymes are disclosed. The A-site of bacterial 16S rRNA serves as the target site for most aminoglycoside antibiotics. Resistance to this class of antibiotics is frequently developed by m...
07/26/2005
6900238HIV protease inhibitors
Combinatorial libraries of HIV and FIV protease inhibitors are characterized by α-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or subs...
05/31/2005
6891043Inhibitors of fatty acid amide hydrolase
Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K1's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, ...
05/10/2005
6858649Selective potentiation of serotonin receptor subtypes
The selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A response to serotonin (5-HT) is achieved using analogs of oleamide. Selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A leads to a m...
02/22/2005
6852874Second cycle asymmetric dihydroxylation reaction
A process for catalyzing asymmetric dihydroxylations of olefins employs an Os(VI) complex as a catalytic intermediate in the formation of chiral vicinal diol products. The process requires a chiral bidentate ligand that favors diol formation in the “second cycle...
02/08/2005
6849398Use of encoded reaction cassette
A reaction cassette has been designed for the highly sensitive detection of the making and breaking of chemical bonds. The system may be employed as a companion device to be used in the search for antibody and other novel catalysts. The cassette also has important c...
02/01/2005
6803466HIV/FIV protease inhibitors having a small P3 residue
With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as FIV. Modifica...
10/12/2004
6774140Iminocyclitol inhibitors of hexoaminidase and glycosidase
Designed iminocylitols that have potent inhibition activity with respect to hexominidases and glycosides are disclosed. ...
08/10/2004
6734204Serotonin potentiation by oleamide analogs
Analogs related to oleamide are employed for potentiating the 5-HT2A and 5-HT1A responses to serotonin (5-HT). With respect to the potentiation of the 5-HT2A receptor response, it is disclosed that, of the naturally occurring fatty a...
05/11/2004
6664372Azatide peptidomimetics
Peptidomimetic azatides and combinatorial oligoazitide libraries are produced by means of a stepwise synthesis. Combinatorial library construction of this new biomimetic polymer provides a means to fabricate global peptidomimetic libraries....
12/16/2003
6660758Epothilone analogs
Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilizati...
12/09/2003
6653087Convergent synthesis of combinatorial library
Targeted C2-symmetric and unsymmetric chemical libraries for use in protein and receptor homodimerization and heterodimerization are constructed by solution phase methodologies. Exemplary libraries are prepared in a 60 to 10 sub-library format by symmetri...
11/25/2003
6642357Process for preparing modified proteins
Modified proteins are represented by the formula R-L-R', wherein R and R' are peptides or pseudopeptides linked to one another by linkage L. Linkage L may be either a thiol ester pseudopeptide backbone linkage or a selenol ester pseudopeptide backbone lin...
11/04/2003
6642035Synthesis of B-keto esters
ଲ-keto esters are prepared by way of a lipase-catalyzed transesterification. The synthetic methodology provides a simple scheme for the synthesis of optically active ଲ-keto esters that are useful building blocks and starting materials for natu...
11/04/2003
6573387Synthesis of ଱,ଲ-substituted amino amides, esters, and acids
଱,ଲ-Unsaturated amides and esters are converted to ଱,ଲ-substituted amino amides, esters, and acids. An ଱,ଲunsaturated amide or ester is first converted to an ଱,ଲ-hydroxysulfonamide or hydroxycarbamate amide ...
06/03/2003
6548530CBI analogs of CC-1065 and the duocarmycins
Analogs of the antitumor antibiotics CC-1065 and the duocarmycins incorporate the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) alkylation subunit. The CBI-based analogs have potent cytotoxic activity and are useful as efficacious antitumor com...
04/15/2003
6548279D-enzyme compositions and methods of their use
D-enzyme compositions are described comprising an amino acid residue sequence that defines an polypeptide able to catalyze an enzymatic reaction. The D-enzyme has an amino acid residue sequence consisting of D-amino acids and glycine....
04/15/2003
6531497Epothilone derivatives and their synthesis and use
The invention relates to epothilone analog represented by formula (I) wherein (i) R2 is absent or oxygen; "a" can be either a single or double bond; "b" can be either absent or a single bond; and "c" can be either absent or a single bond, with ...
03/11/2003
6495314Process for characterizing proteins
A protein signature analysis is obtained using a peptide ladder library. The molecular signature of a protein is defined to be that subsequence of amino acid positions within the protein which are essential for the protein to bind to a target molecule. Th...
12/17/2002
6486326iso-CBI and iso-CI analogs of CC-1065 duocarmycins
A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA bin...
11/26/2002
6476190Process for preparing modified proteins
Processes for the preparation of modified proteins comprising the coupling of a first peptide segment having a haloacyl group at the N-terminus thereof with a second peptide sequent having a carbonylthiol group at the C-terminus thereof are disclosed. Nov...
11/05/2002
6462193Hydroxyazepanes as inhibitors of glycosidase and HIV protease
Hydroxyazepanes display inhibitory activity with respect to glycosidase, with Ki values from-moderate to low micromolar range. Benzyl and 3,6-dibenzyl derivatives of hydroxyazepanes display inhibitory activity with respect to HIV protease. Thes...
10/08/2002
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