Abstract: The invention provides conjugates of fatty acids and anticancer agents useful in treating cancer, and compositions and formulations thereof. Methods for using the conjugates also are provided.
Type:
Grant
Filed:
March 9, 1999
Date of Patent:
June 26, 2007
Assignee:
Luitpold Pharmaceuticals, Inc.,
Inventors:
Nigel L. Webb, Matthews O. Bradley, Forrest Anthony, Mark Fisher
Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reached with a ?-lactam.
Abstract: 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.
Type:
Grant
Filed:
May 21, 2003
Date of Patent:
June 6, 2006
Assignee:
Errant Gene Therapeutics, LLC
Inventors:
Hsuan-Yin Lan-Hargest, Robert J. Kaufman
Abstract: Bis-?-hydroxyethyl terephthalate having an optical density measured in a 10 wt % methanol solution at a measurement wavelength of 380 nm and a cell optical path length of 10 mm of 0.000 to 0.006. The present invention makes it clear that purified BHET having an optical density of 0.006 or less provides high-quality PET having excellent purity, whiteness and transparency.
Abstract: The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I) in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.
Type:
Grant
Filed:
December 2, 2002
Date of Patent:
February 14, 2006
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Yolande Lydia Lang, Bart Petrus Anna Maria Jozef Medaer, Georges Joseph Cornelius Hoornaert, Thierry Brossette, Frans Josef Cornelius Compernolle, Michel Joseph Maurice André Guillaume, Hua Mao, Tomasz Kozlecki
Abstract: A process for making optically pure (R) and (S) salbutamol comprises obtaining the (R) or (S) isomer of either salbutamol or a salbutamol precursor in substantially optically pure form by resolving a racemic or optically impure mixture of enantiomers of salbutamol or of said precursor with either (L) or (D) tartaric acid, and where necessary converting said isomer of said precursor into either (R or (S) salbutamol respectively; then optionally converting said optically pure (R) and/or (S) salbutamol into a pharmaceutically acceptable salt.
Type:
Grant
Filed:
December 10, 2001
Date of Patent:
February 7, 2006
Assignee:
Cipla Limited
Inventors:
Yusuf Khwaja Hamied, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. wherein x and y are integers independently selected from 0 or 1; and B is a bridging group *—(CR16R17)q—(CR18R19)r—(CR20R21)s—Lt—(CR22R23)u—(CR24R25)v—(CR26R27)w—, where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.
Type:
Grant
Filed:
April 27, 2004
Date of Patent:
January 17, 2006
Assignee:
FMC Corporation
Inventors:
George Theodoridis, Edward J. Barron, Dominic P. Suarez, Y. Larry Zhang, Ping Ding, David M. Roush, Stephen F. Donovan, Frank J. Zawacki, Walter H. Yeager, John W. Lyga, Daniel H. Cohen
Abstract: A process of making D-panthenyl triacetate which includes reacting D-panthenol with acetic anhydride in the presence of the catalyst polymer bound dimethylaminopyridine to form an exothermic mixture. The so-produced acetic acid, and the catalyst are removed from the exothermic mixture which is then neutralized with sodium hydroxide. Sodium acetate in the form of a solid is removed by filtration. The D-panthenyl triacetate is useful in cosmetic compositions.
Type:
Grant
Filed:
July 1, 2003
Date of Patent:
January 3, 2006
Assignee:
ISP Investments Inc.
Inventors:
Jon Kirk Smith, Zongzheng Liu, Murugappa Vedachalam, David Compton
Abstract: Process for preparing alkylaryl hydroperoxide containing product, which process comprises: (a) oxidation of an alkylaryl compound to obtain reaction product containing alkylaryl hydroperoxide, (b) contacting with water at least part of the alkylaryl hydroperoxide containing reaction product obtained in step (a) which reaction product contains less than 0.05 % wt of sodium, (c) separating the product of step (b) into a hydrocarbonaceous phase containing alkylaryl hydroperoxide and an aqueous phase, (d) optionally repeating process steps (b) and (c) one or more times, (e) contacting at least part of the hydrocarbonaceous phase containing alkylaryl hydroperoxide obtained in step (c) or (d) with olefin and catalyst to obtain alkylaryl hydroxide and oxirane compound, and (f) separating at least part of the oxirane compound from the alkylaryl hydroxide.
Type:
Grant
Filed:
January 14, 2004
Date of Patent:
December 13, 2005
Assignee:
Shell Oil Company
Inventors:
Antoon Paul Michael Kremers, Eduardus Petrus Simon Schouten, Cornelis Willem Adriaan Schram
Abstract: Large crystals of titanium silicalite or intergrowths of intergrown smaller crystals, having a mean particle size greater than 2 ?m, have been found catalytically effective at commercially reasonable rates for the epoxidation of olefins in the presence of hydrogen peroxide. Crystals synthesized with a silica source having a low sodium content exhibit high levels of production and selectivity. The crystals have a low attrition rate and are easily filterable from a product stream.
Type:
Grant
Filed:
September 20, 2002
Date of Patent:
November 1, 2005
Assignee:
Arco Chemical Technology, L.P.
Inventors:
Bernard Cooker, Wilson H. Onimus, Jennifer D. Jewson, Ralph M. Dessau
Abstract: A compound represented by the following Formula (I): (wherein A represents oxygen atom or —NR3— (R3 represents hydrogen atom or lower alkyl group); R1 represents nitro group, lower alkoxycarbonyl group, carbamoyl group unsubstituted or mono- or di-substituted by lower alkyl group, unprotected or protected hydroxyl group, unprotected or protected carboxyl group, lower alkyl group substituted by unprotected or protected hydroxyl group, or tetrazolyl group; and R2 represents hydrogen atom, cyano group or lower alkylsulfonyl group, provided that when A is —NR3—, it is excluded that R1 represents unprotected or protected hydroxyl group or lower alkyl group substituted by unprotected or protected hydroxyl group) or its salt, and method for producing the compound, and a pharmaceutical composition containing the compound as active ingredient.
Abstract: A fluorocompound denoted by general formula (1) below (wherein R1 denotes a substituted or unsubstituted alkyl group having a total of at least six carbon atoms, with R1 not being an alkyl group substituted with a fluorine atom; Rf denotes a perfluoroalkyl group having not more than six carbon atoms; either X1 or X2 denotes a hydrogen atom and the other denotes SO3M; M denotes a cation; and n denotes an integer of not less than 1) was disclosed. A silver halide photographic light-sensitive material having at least one layer comprising a light-sensitive silver halide emulsion layer on a support and comprising a compound denoted by general formula (1) above was also disclosed.
Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, C?O, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C?O, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, C?O, COOH, CH2F, CHF2 and CF3; such that: at least one of R1-R13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.
Abstract: A high yield, economical process for purifying taxanes from yew biomass is disclosed. The process does not require initial liquid:liquid portioning of the crude extract to separate highly polar substances. The organic solvent extract of the biomass is adsorbed onto and selectively desorbed from an adsorption resin to provide a taxane enriched eluate. Substantially pure individual taxanes may be further isolated from the eluate by hydrophobic-interaction chromatography.
Abstract: Process for the production of drospirenone (6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, DRSP) (1) and 7?-(3-hydroxy-1-propyl)-6?,7?; 15?,16?-dimethylene-5?-androstane-3?,5,17?-triol (ZK 92836) and 6?,7?; 15?,16?-dimethylene-5?-hydroxy-3-oxo-17?-androstane-21,17-carbolactone (ZK 90965) as intermediate products of the process.
Inventors:
Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Jr., Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
Abstract: Macrolide compounds produced by synthetic modification of factors produced by NRRL 30141 have insecticidal and acaricidal activity and are useful intermediates for preparing additional insecticidal and acaricidal compounds
Type:
Grant
Filed:
March 21, 2002
Date of Patent:
July 19, 2005
Assignee:
Dow AgroSciences LLC
Inventors:
Gary D. Crouse, Donald R. Hahn, Paul R. Graupner, Jeffrey R. Gilbert, Paul Lewer, Jesse L. Balcer
Abstract: Crystalline particles of escitalopram oxalate with a particle size of at least 40 ?m is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.
Type:
Grant
Filed:
March 31, 2003
Date of Patent:
July 12, 2005
Assignee:
H. Lundbeck A/S
Inventors:
Troels Volsgaard Christensen, Ken Liljegren, Michiel Onne Elema, Lene Andresen, Shashank Mahashabde, Sebastian P. Assenza