Abstract: The invention relates to a compound having the formula I ##STR1## wherein R.sup.1 is hydroxy, (1-6C)alkoxy or NR.sup.4 R.sup.5, R.sup.4 and R.sup.5 being independently hydrogen, (1-6C)alkyl, (3-7C)cycloalkyl, (2-6C)alkenyl, (4-6C)aryl or (5-7C)aralkyl, the aryl groups of which may be optionally substituted with halogen, (1-6C)alkyl or (1-6C)alkoxy;R.sup.2 is a halo atom, (1-8C)acyloxy, --O--C(O)--O-(1-6C)alkyl, --O--C(O)--O-(5-7C)aralkyl, --SR.sup.6, --S(O)R.sup.6, --SeR.sup.6 or --Se(O)R.sup.6, R.sup.6 being (1-6C)alkyl or (4-6C)aryl; andR.sup.3 is --Si(R.sup.7).sub.3, R.sup.7 being independently (1-6C)alkyl or (4-6C)aryl. The compounds of the invention may be used as protective groups or as linkers in solid phase organic chemistry.
Abstract: Novel metal binding ligands are disclosed that may be coupled to peptides for use in methods of diagnosis and therapy. Peptides containing the ligands are produced using a method wherein ligand introduction or cyclization can be conducted at any point during the synthesis of the peptide. Such peptide derivatives are readily labeled with radiometals, such as isotopes of rhenium or technetium, while retaining their ability to tightly bind specific peptide receptors.
Abstract: The invention relates to the combination of hydroxyamines with nucleic acid binding motifs to generate molecules and libraries of molecules targeting specific nucleic acid sequences. In particular, a series of libraries are constructed which contain hydroxyamine functionalities that are attached to various template backbones which display varying degrees of molecular recognition to phosphodiesters and varying degrees of sequence specific recognition to nucleic acids.
Type:
Grant
Filed:
January 13, 1998
Date of Patent:
September 19, 2000
Assignee:
The Scripps Research Institute
Inventors:
Chi-Huey Wong, Martin Hendrix, Phil Alper, E. Scott Priestley
Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.
Type:
Grant
Filed:
October 20, 1999
Date of Patent:
July 25, 2000
Assignee:
Pharmacopeia, Inc.
Inventors:
Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.
Type:
Grant
Filed:
March 16, 1998
Date of Patent:
December 28, 1999
Assignee:
Pharmacopeia, Inc.
Inventors:
Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu