Abstract: Reagents suitable for the modification of a bioactive species for the purpose of incorporating one or more phenyldiboronic acid (PDBA) moieties for subsequent conjugation to a different (or the same) bioactive species having one or more pendant boronic compound complexing moieties of the general formula of General Formula I,
wherein group R is a reactive electrophilic or nucleophilic moiety suitable for reaction of the PDBA reagent with a bioactive species. Group Z is a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length. Group Q is a linkage that includes one of amide, ether and thioether moieties.
Type:
Grant
Filed:
July 25, 2000
Date of Patent:
October 8, 2002
Assignee:
Prolinx, Inc.
Inventors:
Mark L. Stolowitz, Edward A. Kesicki, Kevin P. Lund, Karin A. Hughes
Abstract: The present invention relates to new pyranoside derivatives of general formula I, processes for preparing them as well as their use as medicaments.
Type:
Application
Filed:
October 23, 2001
Publication date:
September 12, 2002
Inventors:
Ralf Anderskewitz, Kurt Schromm, Franz Birke, Hans Michael Jennewein
Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
July 30, 2002
Assignee:
Massachusetts Institute of Technology
Inventors:
Stephen L. Buchwald, Obadiah J. Plante, Peter H. Seeberger
Abstract: Embodiments include reagents to modify a bioactive species for incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different or same bioactive species having pendant phenylboronic acid moieties of General Formula I,
wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R2 is selected from one of H and OH moieties, and wherein group R3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH2)n and CH2O(CH2CH2O)n2, wherein n is an integer of from 1 to 5, and wherein n2 is an integer of from 1 to 4. Group Z2 and Z3 is a spacer and need not be the same.
Type:
Grant
Filed:
August 29, 2000
Date of Patent:
July 2, 2002
Assignee:
Prolinx, Inc.
Inventors:
Clarence N. Ahlem, Robert J. Kaiser, Kevin P. Lund, Mark L. Stolowitz
Abstract: The present invention relates to derivatives of phosphorylated carbohydrates and pharmaceutical compositions comprising as a pharmaceutically active ingredient at least one of these compounds.
Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.
Type:
Application
Filed:
December 8, 2000
Publication date:
September 27, 2001
Applicant:
University of Kansas
Inventors:
Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
Abstract: The invention concerns a new lipoteichoic acid which can be isolated from the new Streptococcus sp DSM 8747. The new LTA is called LTA-T. It has a lipid anchor, which is a galacto-furanosyl-beta-1-3-glycerol with different rests of fatty acids esterified in the two adjacent hydroxy groups in the glycerol moiety and a non-glycosylated, linear, unbranched GroP chain with an unusual short hydrophilic GroP chain. The hydrophilic backbone consists of only 10 glycerophosphate units esterified with D-alanine in an extent of 30%. The invention further concerns a pharmaceutical composition with the new LTA-T, optionally together with a monokine and/or hyaluronidase, a method of treating cancer comprising administration of an antitumor effective amount thereof, a method of producing the new compound and the new pharmaceutical composition, two degradation products of the new LTA-T and their use, and the new Streptococcus strain from which the new compound can be isolated.
Abstract: Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein.