Laurence Melnick - Watertown MA, US Donald Heefner - Hudson MA, US
International Classification:
C12Q001/00 C12Q001/70 G01N033/53
US Classification:
435/004000, 435/005000, 435/007100
Abstract:
Methods and gene regulator fusion proteins are disclosed utilizing a bacterial reporter system to quickly and easily identify mutations of a target protein, such as a protease, that confer resistance to a chemotherapeutic agent directed against that target protein.
In Vitro Method For Predicting The Evolutionary Response Of A Protein To A Drug Targeted Thereagainst
Inhibitory drug combinations targeted against a protein and first-generation, drug- resistant mutants of the protein. In a preferred embodiment, a combination of drugs that inhibits the activity of a protein and all first-generation, drug-resistant mutants of the protein is identified by determining in vitro the identity of each distinct, first-generation, drug-resistant mutant form of a protein that may arise in vivo in response to a first drug targeted thereagainst, wherein the distinct, first-generation, drug-resistant mutants contain a limited number of resistance-conferring mutations, and then determining in vitro the identity of one or more auxiliary drugs that inhibit all of the first-generation, drug-resistant mutants of the protein, wherein the first drug and the one or more auxiliary drugs represent the combination of drugs.
D-Amino Acid Oxidase Inhibitors For Learning And Memory
Donald Heefner - Hudson MA, US Mark Currie - Sterling MA, US Richard Rossi - Norton MA, US Charles Zepp - Hardwick MA, US
Assignee:
SEPRACOR INC. - Marlborough MA
International Classification:
A61K031/473 A61K031/404 A61K031/401 A61K031/34
US Classification:
514/419000, 514/423000, 514/461000, 514/290000
Abstract:
Methods and pharmaceutical compositions which inhibit the activity of D-amino acid oxidase (DAO) are disclosed. Inhibition of DAO improves memory, learning and cognition in individuals suffering from neurodegenerative diseases such as Alzheimer's, Huntington's or Parkinson's diseases; the methods and pharmaceutical compositions which inhibit the activity of DAO also improve cognitive dysfunctions associated with aging and improve catatonic schizophrenia. Several genera of heterocycle-2-carboxylic acids are disclosed as DAO inhibitors.
Compositions And Methods For Treating Or Preventing Hearing Impairment
Charles Zepp - Hardwick MA, US Donald Heefner - Waynesboro PA, US Paul Rubin - Sudbury MA, US Mark Currie - Sterling MA, US
Assignee:
Sepracor, Inc. - Marlborough MA
International Classification:
A61K038/17
US Classification:
514012000
Abstract:
Ototoxic side-effects have either limited the application of an important group of antibiotics, aminoglycoside antibiotics, or have added further burden to those who have to resort to platinum-containing antineoplastic agents to treat life-threatening tumors. The present invention discloses pharmaceutical compositions that prevent or treat the ototoxic side-effects of aminoglycoside antibiotics and platinum-containing antineoplastic agents. The otoprotective compositions disclosed herein can also be used to treat noise induced hearing loss.
Edward W. Foster - Loveland CO Dale C. Gyure - Fort Collins CO Donald L. Heefner - Longmont CO Craig A. Weaver - Louisville CO Michael J. Yarus - Boulder CO Linda A. Burdzinski - Boulder CO
Assignee:
Zeagen, Inc. - Broomfield CO
International Classification:
C12N 116 C12N 1500 C12P 1500
US Classification:
435255
Abstract:
Strains of yeast of the species Candida famata are disclosed which can produce 10 grams of riboflavin per liter in 6 days, and in particular, strains identified by ATCC Accession Nos. 20849 and 20850. Riboflavin yields of more than 20 grams per liter in 200 hours have been achieved. Strains of the present invention have increased sensitivity to iron inhibition of flavinogenesis and have enhanced riboflavin production per cell at increased iron concentrations in the fermentation medium.
Method Of Preparing Optically Pure Precursors Of Paroxetine
Charles M. Zepp - Berlin MA Yun Gao - Framingham MA Donald L. Heefner - Hudson MA
Assignee:
Sepracor, Inc. - Marlborough MA
International Classification:
C07D21122
US Classification:
546240
Abstract:
A biocatalytic method of preparing optically pure precursors of paroxetine and a method of preparing paroxetine therefrom are disclosed. A racemic trans ester precursor compound of paroxetine is first prepared. The racemic trans ester precursor compound comprises a mixture of (3S,4R) and (3R,4S) enantiomers. The (3R,4S) enantiomer is hydrolyzed biocatalytically to the corresponding (3R,4S)-trans carboxylic acid or alternatively, the (3S,4R) enantiomer is biocatalytically hydrolyzed the to (3S,4R)-trans carboxylic acid in a reaction catalyzed by a isolated enzyme or a microorganism. In the first instance, the unhydrolyzed (3S,4R) enantiomer is separated from the (3R,4S)-trans carboxylic acid, whereas in the second instance the (3S,4R)-trans carboxylic acid is separated from the unhydrolyzed (3R,4S) enantiomer. The (3S,4R) enantiomer obtained following the selective hydrolysis is reduced to form a (-)-trans-(3S,4R) primary alcohol precursor of paroxetine. Paroxetine is then formed from the (-)-trans-(3S,4R) primary alcohol precursor.
Asymmetric Grignard Synthesis With Cyclic 1,2 Aminoalcohols
Chris Hugh Senanayake - Shrewsbury MA Roger P. Bakale - Shrewsbury MA Qun Kevin Fang - Wellesley MA Paul Timothy Grover - Marlborough MA Donald L. Heefner - Hudson MA Richard F. Rossi - Norton MA Stephen Alan Wald - Sudbury MA
Assignee:
Sepracor Inc. - Marlborough MA
International Classification:
C07D26308
US Classification:
435195
Abstract:
Processes for preparing a single enantiomer of an. alpha. ,. alpha. -disubstituted-. alpha. -hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.
Method For Producing Riboflavin With Candida Famata
Donald L. Heefner - Longmont CO Craig A. Weaver - Louisville CO Michael J. Yarus - Boulder CO Linda A. Burdzinski - Boulder CO
Assignee:
ZeaGen, Inc. - Broomfield CO
International Classification:
C12P 0500 C12N 1165 C12N 1500 C12N 138
US Classification:
435 66
Abstract:
Strains of yeast of the species Candida famata are disclosed which can produce 10 grams of riboflavin per liter in 6 days, and in particular, strains identified by ATCC Accession Nos. 20849 and 20850. Riboflavin yields of more than 20 grams per liter in 200 hours have been achieved. Strains of the present invention have increased sensitivity to iron inhibition of flavinogenesis and have enhanced riboflavin production per cell at increased iron concentrations in the fermentation medium. The invention also is directed toward a process for selecting improved microorganisms which are resistant to inhibition of growth by depleted medium. Such selected mircoorganisms are then tested for riboflavin overproduction. The present invention is also directed toward a selection process in which mutated microorganisms are cultured in the presence of tubercidin, a purine analog. Mutant strains resistant to tubercidin are then tested for riboflavin over-production.
License Records
Donald L Heefner
Address:
Waynesboro, PA 17268
License #:
MV020755L - Expired
Category:
Vehicle Board
Type:
Vehicle Salesperson
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