Abstract: The invention relates to a method for preparing an ester, by admixing a compound having the structure I or IV:
with a base and an alcohol to produce an ester, wherein the alcohol is a precursor to Taxol and its analogs. The present invention also relates to compounds having the structure I and IV and methods of main them therefor. The invention also relates to the esterification of an alcohol by adding an alkoxide to a compound having the structure, VII:
The invention further relates to compounds having the structure I, IV, and VII and methods of making them therefor. The invention further relates to alcohols, and in particular, alcohols that are synthetic precursors to Taxol and analogs thereof.
Type:
Grant
Filed:
August 25, 2000
Date of Patent:
June 4, 2002
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Hariharan Venkatesan, Laura Captain, Michael V. Voronkov, James P. Snyder, Marcus A. Schestopol
Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
Type:
Application
Filed:
August 10, 2001
Publication date:
April 25, 2002
Applicant:
GPI NIL HOLDINGS, INC.
Inventors:
Gregory S. Hamilton, Jai-He Li, Wei Huang
Abstract:
The invention relates to compounds of formula (I), wherein the symbols have the meanings indicated in the specification. The inventive compounds exhibit dramatic antiarrhythmic proprieties and contain a cardioprotective compound. They can preventively inhibit or strongly reduce pathophysiologic processes upon occurrence of ischemic injuries, especially ischemic cardiac arrhythmia. Said compounds also exhibit a strong inhibiting effect on cellular proliferation.
Type:
Grant
Filed:
January 17, 2001
Date of Patent:
April 16, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Stefan Petry
Abstract:
The invention relates to compounds of formula (I), wherein the symbols have the meanings indicated in the specification. The inventive compounds exhibit dramatic antiarrhythmic proprieties and contain a cardioprotective compound. They can preventively inhibit or strongly reduce pathophysiologic processes upon occurrence of ischemic injuries, especially ischemic cardiac arrhythmia. Said compounds also exhibit a strong inhibiting effect on cellular proliferation.
Type:
Grant
Filed:
January 18, 2001
Date of Patent:
April 9, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Stefan Petry, Andreas Weichert
Abstract: A process for the production of 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid starting from meso-2,3-bis(benzylamino)-succinic acid dialkali metal salt is described. This process includes reacting meso-2,3-bis(benzylamino)-succinic acid dialkali metal salt with triphosgene in a two-phase solvent system consisting of an aqueous alkali hydroxide solution and an organic solvent at a temperature not exceeding about 50° C. and converting the 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid dialkali metal salt, which results therefrom and which is present in the aqueous phase, into the desired 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid by acidification. The product is an important intermediate in the multi-stage process for the manufacture of biotin (vitamin H).
Abstract: A compound of the formula:
is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Type:
Grant
Filed:
February 23, 2000
Date of Patent:
November 6, 2001
Assignee:
Abbott Laboratories
Inventors:
Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
Abstract: Ureins are obtained by reaction, in basic medium, between an N&ohgr;-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
October 30, 2001
Assignee:
Solvay, S.A.
Inventors:
Roland Callens, Georges Blondeel, Marc Anteunis, Frank Becu
Abstract: The present invention is directed to a process for the production of 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid and of 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid anhydride, starting from meso-2,3-bis(benzylamino)succinic acid dialkali metal salt. The process involves reacting meso-2,3-bis(benzylamino)succinic acid dialkali metal salt with phenyl chloroformate in a monophasic solvent system consisting of an about 2:1 to 1:1 mixture of a water-miscible ether and an aqueous alkali metal hydroxide solution, at a temperature not exceeding about 40° C.
Type:
Grant
Filed:
February 9, 2001
Date of Patent:
September 18, 2001
Assignee:
Roche Vitamins Inc.
Inventors:
Juergen Fleckenstein, Bernd Kraemer, Joachim Veits
Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula:
and where m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.