Patent EP0094844A2 successfully refreshed from Google Patents.
EP0094844A2
Expired / Lapsed
EP
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Drug-carrier conjugates
Assignee: University of California
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Filing: 1983-05-18
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Granted: —
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Expires: 2003-05-18
Abstract
Abstract Biologically active drugs, e.g. catecholamine hormones, are coupled to carrier molecules, e.g. monodisperse peptides to produce conjugate molecules. The conjugate molecules retain biological activity, but the pharmacokinetic, pharmacodynamic and/or potency properties of the drug is modified. The drug is coupled to the carrier via a spacer moiety which not only serves to covalently link the drug to the carrier, but also insulates the biologically active portion of the drug, i.e., the pharmacophore, from degradation during the coupling process. The carrier preferably consists of a monodisperse peptide in which the sequence of amino acid residues is carefully preselected and controlled.
Inventors
- 👤 Murray Goodman
- 👤 Neal Castagnoli
- 👤 Kenneth Alan Jacobson
- 👤 Kenneth Lloyd Melmon
- 👤 Roberto Pedro Rosenkranz
- 👤 Michael Stephen Velander
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-30 21:44
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0819; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61P; A61P25/00; A61P25/02; A61P9/00; A61P9/04; C07K5/06; C07K5/06008; C07K5/06078; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/28; Y10S930/29
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
66 words
A conjugate molecular composition comprising a carrier moiety and at least one drug molecule moiety containing a pharmacophore, each drug molecule moiety being covalently linked to the carrier moiety via a spacer grouping, the spacer grouping being linked to the carrier by reacted functional groups and to the drug molecule moiety by covalent attachment at a position on the drug molecule moiety remote from the pharmacophore.
Claim 2
Dependent Claim
66 words
A conjugate molecular composition comprising a carrier moiety and at least one drug molecule moiety containing a pharmacophore, each drug molecule moiety being covalently linked to the carrier moiety via a spacer grouping, the spacer grouping being linked to the carrier by reacted functional groups and to the drug molecule moiety by covalent attachment at a position on the drug molecule moiety remote from the pharmacophore.
Claim 3
Dependent Claim
25 words
A composition as claimed in claim 1 wherein said drug molecule moiety is a catecholamine, a beta- adrenergic drug, a sympathomimetic drug or an autacoid.
Claim 4
Dependent Claim
24 words
A composition as claimed in claim 1 or claim 2 wherein two or more drug molecule moieties are covalently linked to said carrier moiety.
Claim 5
Dependent Claim
19 words
A composition as claimed in any one of the preceding claims wherein the spacer grouping includes an alkyl chain.
Claim 6
Dependent Claim
20 words
A composition as claimed in claim 4 wherein the alkyl chain is a branched methylene chain containing 2-6 methylene groups.
Claim 7
Dependent Claim
27 words
A composition as claimed in claim 4 or claim 5 wherein said spacer grouping has an amide group attached thereto intermediate said alkyl chain and said carrier.
Claim 8
Dependent Claim
58 words
A composition as claimed in any one of claims 1 to 3 wherein the spacer grouping is a branched chain organic grouping one end of which is covalently linked to said drug molecule moiety and the other end of which is covalently linked to a functional group and the reacted functional group is covalently linked to said carrier.
Claim 9
Dependent Claim
27 words
A composition as claimed in any one of the preceding claims wherein the carrier moiety is a natural or synthetic peptide or protein, or a monoclonal antibody.
Claim 10
Dependent Claim
34 words
A composition as claimed in claim 8, wherein the carrier moiety is a peptide and an amino acid residue in said peptide is covalently linked to said spacer grouping via the reacted functional groups.
Claim 11
Dependent Claim
44 words
A composition as claimed in claim 8 or claim 9 wherein the carrier moiety is a monodisperse peptide. ll. A composition as claimed in any one of the preceding claims wherein the carrier moiety is a peptide whose amine and carboxyl ends are protected.
Claim 12
Dependent Claim
158 words
A composition as claimed in claim 1 having the general formula: where: A and B are oligopeptide blocks.wherein the amino acid residues are the same, or preselected sequences of amino acid residues; C is an amino acid residue functionalized for attachment to the drug molecule moiety ("DRUG"); S is a spacer grouping connecting the drug to reacted functional groups, Z, and wherein the spacer grouping includes a branched alkyl chain and wherein one end of said spacer grouping is covalently bound to the drug and the other end is covalently bound to said reacted functional groups and from thence to a side chain forming a portion, -Y', of amino acid residue C; X is an amine-blocking group, or a hydrogen atom; X' is a carboxyl-blocking group, or a hydrogen atom; Y is an amino acid residue side chain; a and b, which may be the same or different, represent zero or an integer; and m is an integer.
Claim 13
Dependent Claim
42 words
A composition as claimed in claim 12 wherein the blocks A and B and the amino acid residue, C, comprise a monodisperse peptide carrier for said drug, or wherein the peptide blocks comprise a protein, a monoclonal antibody or a naturally-occurring peptide.
Claim 14
Dependent Claim
16 words
A composition as claimed ih claim 12 wherein the peptide sequence of the carrier is: or
Claim 15
Independent Claim
71 words
A method for producing a composition as claimed in any one of the preceding claims comprising reacting at least one drug containing a pharmacophore with a functionalized spacer moiety to produce a drug congener in which said spacer moiety is linked to said drug at a position remote from the pharmacophore and reacting said congener with a carrier to link said congener covalently to said carrier via said functionalized spacer moiety.
Claim 16
Dependent Claim
27 words
A method as claimed in claim 15 wherein the drug is a catecholamine and the spacer moiety is linked to the amine containing grouping of said catecholamine.
Claim 17
Dependent Claim
63 words
A method for producing a composition as claimed in claim 10, comprising synthesizing a monodisperse peptide, linking a functionalized spacer moiety to at least one preselected amino acid residue on said peptide, and then reacting said peptide and its attached spacer moiety with a drug molecule to link said spacer moiety and thereby said peptide covalently to said drug to form said composition.
Claim 18
Dependent Claim
28 words
A method as claimed in claim 17 wherein the drug is a catecholamine and is linked to said spacer moiety and the peptide at the amine end thereof.
Claim 19
Dependent Claim
23 words
A method as claimed in claim 18 wherein the catecholamine is linked to said spacer moiety and peptide by a reductive amination reaction.
References Cited (Backward Citations)
No citation records indexed.
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