Monsanto Company

Hemagen/pfc

Errant Gene Therapeutics, LLC

Other

E.i. Dupont De Nemours and Company

Minnesota Mining and Manufacturing Company

Pfizer Corporation

Wellstat Therapeutics Corporation

Baxter Healthcare Inc.

E.i. Du Pont De Nmeours and Company

Circagen Pharmaceutical

Robert J Kaufman

John E Franz

Thomas J Richard

Hsuan-Yin Lan-Hargest

Norbert L Wiech

Ronald Joseph Brinker

Suzanne S Metz

Raymond C Grabiak

Andrew Jackson

Stephan M Brandstadter

Vicki Hedrick

E Bradley Edwards

John Chien

Vimal Sharma

Lawrence H Brannigan

Janet Boggs

Edward Norman

Thomas H Goodin

Richard M Flynn

George G Moore

Shalini Sharma

John Gregory Slatter

Gregory Leman

Reid W Von Borstel

Donald W Schoendorfer

Bruno Ameduri

David Dale Wirth

William P Cacheris

Kirvin L Hodge

Albert C Lee

Tony E Layton

John S Allen

George K Kostov

Richard A Stephens

Jason P Chinn

Ralph W Fuhrhop

The compound 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobutanoic acid (DPA) is synthesized from 1-[3-(2,6-Dimethylbenzyloxy)-phenyl]-ethanone (DPE) via the intermediate 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobulanoic acid ethyl ester (DPAE).

Synthesis of 4-[3-(2,6-dimethylbenzyloxy)phenyl]-4-oxobutanoic acid

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Histone deacetylase inhibitors

Production processes and systems are provided that include reacting halogenated compounds, dehalogenating compounds, reacting alcohol's, reacting olefins and a saturated compounds, reacting reactants having at least two &#x2014;CFgroups with reactants having cyclic groups, R-compositions such as R-intermediates, R-surfactants, R-monomers, R-monomer units, R-metal complexes, R-phosphate esters, R-glycols, R-urethanes, and or R-foam stabilizers. The Rportion can include at least two groups &#x2014;CFgroups, at least three &#x2014;CFgroups, and/or at least two &#x2014;CFgroups and at least two &#x2014;CHgroups. Detergents, emulsifiers, paints, adhesives, inks, wetting agents, foamers, and defoamers including the R-surfactant composition are provided. Acrylics, resins, and polymers are provided that include a R-monomer unit. Compositions are provided that include a substrate having a R-composition thereover. Aqueous Film Forming Foam ('AFFF') formulations are provided that can include R-surfactants and/or R-foam stabilizers are provided.

Production processes and systems, compositions, surfactants, monomer units, metal complexes, phosphate esters, glycols, aqueous film forming foams, and foam stabilizers

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-ketoepoxide group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or to stimulate hematopoietic cells ex vivo.

Histone deacetylase inhibitors based on alpha-ketoepoxide compounds

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy. Carboxylic acid-containing compounds having a terminal cyclic moiety, a carboxylic acid group, and a Chydrocarbon chain optionally containing at least one double bond, at least one triple bond, or at least one double bond and one triple bond linking the cyclic moiety and the carboxylic acid group are inhibitors of histone deacetylase.

R-compositions including surfactants, foam stabilizers, monomers, polymers, urethanes, intermediates, metal complexes, phosphate esters as well as telomerization methods are provided.

Production processes and systems, compositions, surfactants, monomer units, metal complexes, phosphate esters, glycols, aqueous film forming foams and foam stabilizers

Production processes and systems are provided that include reacting halogenated compounds, dehalogenating compounds, reacting alcohol's, reacting olefins and a saturated compounds, reacting reactants having at least two &#x2014;CFgroups with reactants having cyclic groups. R-compositions such as R-intermediates, R-surfactants, R-monomers, R-monomer units, R-metal complexes, R-phosphate esters, R-glycols, R-urethanes, and/or R-foam stabilizers. The Rportion can include at least two &#x2014;CFgroups, at least three &#x2014;CFgroups, and/or at least two &#x2014;CFgroups and at least two &#x2014;CH&#x2014; groups. Detergents, emulsifiers, paints, adhesives, inks, wetting agents, foamers, and defoamers including the R-surfactant composition are provided. Acrylics, resins, and polymers are provided that include a R-monomer unit. Compositions are provided that include a substrate having a R-composition thereover. Aqueous Film Forming Foam ('AFFF') formulations are provided that can include R-surfactants and/or R-foam stabilizers are provided.

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, genetic disorders, e.g. Huntington's disease and spinal muscular atrophy and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 2 or 3; q is 0 or 1; t is 0 or 1; Ris alkyl having from 1 to 3 carbon atoms; Ris hydrogen, halo, alkyl having from 1 to 3 atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and Ris hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when Ris hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I) 

Compounds for the treatment of metabolic disorders

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Novel 3,3-diphenylpropylamines of the formula and stereoisomers and physiologically acceptable acid addition salt thereof; wherein R, R, R, R, R, and Rare as defined herein; methods of use thereof; and pharmaceutical compositions thereof.

3,3-diphenylpropylamines useful in therapy

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Histone deacetylase inhibitors based on alpha-chalcogenmethylcarbonyl compounds

Growing community of inventors

University City, MO, United States of America

Robert J Kaufman