Abstract: A chemical compound having the formula: ##STR1## wherein P.sub.1 is a hydroxyl protecting group, R.sub.1 may be H or electron withdrawing group, R.sub.2 may be H or electron withdrawing group, R.sub.3 may be H or electron withdrawing group, R.sub.4 may be H or electron withdrawing group, R.sub.5 may be H or electron withdrawing group, R.sub.6 may be an alkyl group, an olefinic group, an aromatic group, Ph, PhCH.sub.2, an O-alkyl group, an O-olefinic group, an O-aromatic group, O--Ph, or O--CH.sub.2 Ph.
Type:
Grant
Filed:
June 21, 1999
Date of Patent:
October 24, 2000
Assignee:
NaPro BioTherapeutics, Inc.
Inventors:
Madhavi C. Chander, James D. McChesney, Jan Zygmunt
Abstract: An antitumor compound of formula (5) ##STR1## and also provided by the present invention is a method of preparing a compound of formula (5) whereby diesterification of the alcohol groups located at the 2' and 7 positions of paclitaxel is followed by the hydrolysis of the 2' hexanoate group resulting in 7-hexanoyltaxol.
Type:
Grant
Filed:
April 10, 1998
Date of Patent:
October 24, 2000
Assignee:
Hauser, Inc.
Inventors:
Christopher K. Murray, Qun Y. Zheng, Sagar R. Shakya
Abstract: A method of isolating paclitaxel from pactitaxel-containing material that includes the steps of obtaining an acetone mixture of the paclitaxel-containing material, then mixing the acetone mixture with an aqueous solvent to form an aqueous supernatant and a precipitate, wherein the precipitate contains at least 3-times higher paclitaxel content than the paclitaxel extract. The acetone/water precipitation step provides a high yield of highly pure paclitaxel that is suitable for industrial scale isolation using conventional normal-phase silica chromatography steps, and the preparation of pharmaceutical compositions containing paclitaxel.
Type:
Grant
Filed:
December 30, 1998
Date of Patent:
October 24, 2000
Assignee:
Phytogen Life Sciences, Incorporated
Inventors:
Samuel Siang Kiang Foo, Yili Bai, Martin Ehlert
Abstract: The invention provides for a purified glycidyl ester product prepared from neo acids wherein said ester product is recovered as a light fraction from a glycidyl ester reaction product composition that has been subjected to conditions of temperature and vacuum in a thin film, short pass distillation evaporator, said purified glycidyl ester product further characterized that its polymerizable reaction product with methacrylic acid has a higher effective glass transition temperature as compared with the polymerizable reaction product with methacrylic acid of said glycidyl ester reaction product composition prior to purification.
Type:
Grant
Filed:
November 10, 1997
Date of Patent:
October 24, 2000
Assignee:
Exxon Chemical Patents Inc.
Inventors:
Richard William Ryan, Gerald G. McGlamery, Jr., Ralph Martin Kowalik, Michael J. Keenan
Abstract: A compound of formula IV ##STR1## wherein G is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl or Ar;Ar is an aromatic or heteroaromatic group or a substituted aromatic or heteroaromatic group;R.sup.1 is halo, SR, OR, amino, mono or di-(C.sub.1 -C.sub.6 -alkyl)amino, tri (C.sub.1 -C.sub.6 -alkyl)ammonium, C.sub.1 -C.sub.6 -alkylthio, di(C.sub.1 -C.sub.6 -alkyl)sulfonium, C.sub.1 -C.sub.6 -alkylsulfonyl, or C.sub.1 -C.sub.6 -alkylphosphonyl;R.sup.2 is OH or SH; orR.sup.1 and R.sup.2 taken together form a second bond or together form an epoxide, aziridine, episulfide, or cyclopropyl ring;R is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl or Ar;R.sup.3 is C.sub.1 -C.sub.6 alkyl;R.sup.4 and R.sup.5 are H; orR.sup.4 and R.sup.5 taken together form a second bond;R.sup.24 is a leaving group; andR.sup.26 is an alcohol protecting group;X is O, NH or (C1-C3 alkyl)N--.
Type:
Grant
Filed:
July 2, 1999
Date of Patent:
October 17, 2000
Assignees:
Eli Lilly and Company, Wayne State University, University of Hawaii
Abstract: Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.
Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted alkyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring.
Type:
Grant
Filed:
March 26, 1999
Date of Patent:
October 3, 2000
Assignee:
Enzon, Inc.
Inventors:
Richard B. Greenwald, Annapurna Pendri, Hong Zhao
Abstract: Epoxy resins which are diglycidyl ethers of tetrabromobisphenol A having a crystalline structure and in particulate form have an epoxy equivalent weight between 320 and 380 g/eq and a chlorine content that is smaller than 0.3%.
Abstract: A method for producing silasesquioxane metal complexes of the formula (II)((R.sup.1 SiO.sub.1,5).sub.n (R.sup.2a SiO.sub.1,5).sub.m ((B).sub.q (O).sub.r)).sub.u (M).sub.v (Y).sub.win which R.sup.1 represents C.sub.5 -C.sub.10 -cycloalkyl, norbornyl or adamantyl; R.sup.2a represents oxygen; B represents H, OH, halogen, alkoxy, SiR.sup.3.sub.y in which R.sup.3 can be C.sub.1 -C.sub.4 alkyl, aryl or substituted silyl groups, and y represents 2 or 3, and R.sup.1 and R.sup.3 can be functionalized; M represents metals of the 4.sup.th to 7.sup.th subgroups of the periodic system of elements; Y represents C.sub.1 -C.sub.20 alkyl or aryl groups devoid of beta-hydrogen, silyl, alkoxy, OH, halogen, oxo, imido, fluorenyl, indenyl, cyclopentadienyl, in which the individual ligands can be substituted; n=6 or 7; m=0 or 1; q=0-2; r=0-2; u=1-4; v=1-4; w=0-12, in which a metal compound of the 4.sup.th to 7.sup.th subgroups of the periodic system of elements and at least one silasesquioxane compound of the formula (I)(R.sup.
Type:
Grant
Filed:
October 18, 1999
Date of Patent:
October 3, 2000
Assignee:
Solvay Deutschland GmbH
Inventors:
Rutger Anthony Van Santen, Hendrikus Cornesis Louis Abbenhuis, Martinus Lambertus Wilhelmus Vorstenbosch
Abstract: A process for selective monoacylation of 10-deacetylbaccatin III, or a derivative thereof in positions C-2 and C-4 possessing free hydroxyl groups in positions C-7 and C-10, using a methyleneiminium salt.
Abstract: In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.
Type:
Grant
Filed:
December 16, 1997
Date of Patent:
October 3, 2000
Assignee:
G. D. Searle & Co.
Inventors:
Chin Liu, John S. Ng, James R. Behling, Arthur L. Campbell
Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a .beta.-lactam.
Abstract: Process for the production of drospirenone (6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-3-oxo-17.alpha.-pregn-4-ene-21, 17-carbolactone, DRSP) (1) and 7.alpha.-(3-hydroxy-1-propyl)-6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-5.beta.-androstane-3.beta., 5, 17.beta.-triol (ZK 92836) and 6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-5.beta.-hydroxy-3-oxo-17.alpha.-androstane-21, 17-carbolactone (ZK 90965) as intermediate products of the process.
Abstract: The invention relates to a method for separating a gaseous mixture comprising formaldehyde and trioxane, wherein at least some of the formaldehyde and the trioxane are dissolved from the mixture in a alcohol-containing liquid and the trioxane is crystallized from the solution thus obtained and is separated.
Type:
Grant
Filed:
July 23, 1999
Date of Patent:
September 19, 2000
Assignee:
Ticona GmbH
Inventors:
Hagen Kniep, Christine Meister, Elke Schweers, Ioannis Nicolaou, Dirk Scheid
Abstract: This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.
Type:
Grant
Filed:
November 27, 1996
Date of Patent:
September 12, 2000
Assignee:
The Liposome Company, Inc.
Inventors:
Eric Mayhew, J. Craig Franklin, Suresh Bhatia, Paul A. Harmon, Andrew S. Janoff
Abstract: A .beta.-phenylisoserine derivative of general formula (I): ##STR1## in the form of a salt or an ester, in which Ar represent an aryl radical, R represents a phenyl or naphthyl or a O--R.sub.1 radical and G.sub.1 represents --CH.sub.2 --Ph radical; and a method of using the same for making taxane derivatives.
Type:
Grant
Filed:
November 10, 1997
Date of Patent:
September 5, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Noel Denis, Andrew-Elliot Greene, Alice Kanazawa
Abstract: Highly active and selective epoxidation catalysts are prepared by combining high surface area silica support or the like, having surface area greater than 1100 m.sup.2 /g, with a titanium source. The titanium source is a non-oxygenated hydrocarbon solution of a titanium halide or a vapor stream of titanium tetrachloride. The impregnated support it then calcined at an elevated temperature (preferably, in a substantially oxygen-free atmosphere), and, optionally, reacted with water and/or silylated. The resulting materials are highly active heterogeneous epoxidation catalysts for the reaction of olefins to with organic hydroperoxides.
Type:
Grant
Filed:
September 28, 1999
Date of Patent:
September 5, 2000
Assignee:
Arco Chemical Technology, L.P.
Inventors:
Yuan-Zhang Han, Edrick Morales, Robert G. Gastinger, Kevin M. Carroll
Abstract: The present invention provides novel haloenol lactones that are effective as active site inhibitors of cholesterol esterase. By inhibiting cholesterol esterase the inhibitors of the present invention provide a new approach to the treatment of hypercholesterolemia through limiting the bioavailability of dietary cholesterol.
Abstract: A catalyst for the production of ethylene oxide by the vapor phase oxidation of ethylene under specific conditions such that an amount of chlorine suffered to adhere thereto is not more than 2 mol % per mol of silver after the duration of the reaction caused under the specific conditions has totalled 240 hours from the start of the reaction, a silver catalyst for the production of ethylene oxide which incorporates therein an organic nitrogen compound, methods for the production of the catalysts mentioned above, and a method for the production of ethylene oxide by the gaseous-phase oxidation of ethylene with a molecular oxygen-containing gas in the presence of such a catalyst.