US5094848A
Expired / Lapsed
US
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Cleavable diphosphate and amidated diphosphate linkers
Assignee: Poniard Pharmaceuticals Inc
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Filing: 1989-06-30
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Granted: 1992-03-10
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Expires: 2009-06-30
Abstract
Abstract The specificity of a pharmaceutical agent for a given site of action is increased by covalently bonding the agent via a diphosphate or amidated diphosphate bond to a targeting moiety, preferably a polypeptide specific for the site.
Inventors
- 👤 Diana I. Brixner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 08:44
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/10; A61K51/1093; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6889; A61K2121/00
Claims Analysis
Total Claims: 30
Claim 1
Independent Claim
77 words
A conjugate, useful for targeting of an active agent to a desired site, comprising an active agent cleavably linked to a moiety effective for targeting to said site, of the formula A--L.sup.1.sub.n --DP--L.sup.2 --polypeptide wherein DP is diphosphate, L 1 is a bridging spacer group, n is 0 or 1, A is an active agent or a portion thereof "polypeptide" is effective for targeting A to a desired site, and L 2 is an oligopeptide linking arm.
Claim 2
Dependent Claim
77 words
A conjugate, useful for targeting of an active agent to a desired site, comprising an active agent cleavably linked to a moiety effective for targeting to said site, of the formula A--L.sup.1.sub.n --DP--L.sup.2 --polypeptide wherein DP is diphosphate, L 1 is a bridging spacer group, n is 0 or 1, A is an active agent or a portion thereof "polypeptide" is effective for targeting A to a desired site, and L 2 is an oligopeptide linking arm.
Claim 3
Dependent Claim
24 words
A conjugate of claim 1, wherein the amino acid monomer of the oligopeptide L 2 which is linked to DP is serine or threonine.
Claim 4
Dependent Claim
14 words
A conjugate of claim 2, wherein L 2 is --Ser--GABA-- or a derivative thereof.
Claim 5
Dependent Claim
72 words
A conjugate, useful for targeting of an active agent to a desired site, comprising an active agent cleavably linked to a moiety effective for targeting to said site, of the formula A--L.sup.1.sub.n --DP--L.sup.2 --polypeptide wherein DP is diphosphate, n is 1, L 1 is a bridging spacer group containing about 2-10 atoms, A is an active agent or a portion thereof, and "polypeptide" is effective for targeting A to a desired site.
Claim 6
Dependent Claim
72 words
A conjugate, useful for targeting of an active agent to a desired site, comprising an active agent cleavably linked to a moiety effective for targeting to said site, of the formula A--L.sup.1.sub.n --DP--L.sup.2 --polypeptide wherein DP is diphosphate, n is 1, L 1 is a bridging spacer group containing about 2-10 atoms, A is an active agent or a portion thereof, and "polypeptide" is effective for targeting A to a desired site.
Claim 7
Dependent Claim
14 words
A conjugate of claim 4, wherein L 1 contains at least one peptide bond.
Claim 8
Dependent Claim
78 words
A conjugate, useful for targeting of an active agent to a desired site, comprising an active agent cleavably linked to a moiety effective for targeting to said site, of the formula A--L.sup.1.sub.n --DP(A)--L.sup.2 --polypeptide wherein DP(A) is amidated diphosphate, L 1 n is a bridging spacer group, n is 0 or 1, L 2 is a linking arm, A is an active agent or a portion thereof, and "polypeptide" is effective for targeting A to a desired site.
Claim 9
Dependent Claim
78 words
A conjugate, useful for targeting of an active agent to a desired site, comprising an active agent cleavably linked to a moiety effective for targeting to said site, of the formula A--L.sup.1.sub.n --DP(A)--L.sup.2 --polypeptide wherein DP(A) is amidated diphosphate, L 1 n is a bridging spacer group, n is 0 or 1, L 2 is a linking arm, A is an active agent or a portion thereof, and "polypeptide" is effective for targeting A to a desired site.
Claim 10
Dependent Claim
16 words
A conjugate of claim 6, wherein A is a radionuclide metal chelate or an anti-tumor agent.
Claim 11
Dependent Claim
32 words
A conjugate comprising at least two groups (A--L 1 n --DP--L 2 --) as defined in claim 1 bonded to a pharmacologically acceptable carrier polymer which is bonded to a targeting moiety.
Claim 12
Dependent Claim
30 words
A conjugate comprising at least two groups (A--L 1 n --DP(A)--L 2 --) as defined in claim 6 a pharmacologically acceptable carrier polymer which is bonded to a targeting moiety.
Claim 13
Dependent Claim
10 words
A conjugate of claim 8, wherein said polymer is dextran.
Claim 14
Dependent Claim
14 words
A conjugate of claim 1, wherein the polypeptide is a polyclonal or monoclonal antibody.
Claim 15
Dependent Claim
14 words
A conjugate of claim 4, wherein the polypeptide is a polyclonal or monoclonal antibody.
Claim 16
Dependent Claim
14 words
A conjugate of claim 6, wherein the polypeptide is a polyclonal or monoclonal antibody.
Claim 17
Dependent Claim
19 words
A conjugate of claim 11, wherein n is O and A or a monophosphorylated metabolite thereof is pharmacologically therapeutic.
Claim 18
Dependent Claim
24 words
A conjugate of claim 11, wherein n is O, A is Ara-C and the polypeptide is a monoclonal antibody of an immunospecific fragment thereof.
Claim 19
Dependent Claim
16 words
A conjugate of claim 11, wherein A is an antitumor agent or a radionuclide metal chelate.
Claim 20
Dependent Claim
16 words
A conjugate of claim 4, wherein A is an antitumor agent or a radionuclide metal chelate.
Claim 21
Dependent Claim
20 words
A pharmaceutical composition comprising a diagnostically or therapeutically effective amount of conjugate of claim 1 and a pharmaceutically acceptable carrier.
Claim 22
Dependent Claim
20 words
A pharmaceutical composition comprising a diagnostically or therapeutically effective amount of conjugate of claim 9 and a pharmaceutically acceptable carrier.
Claim 23
Dependent Claim
20 words
A pharmaceutical composition comprising a diagnostically or therapeutically effective amount of conjugate of claim 6 and a pharmaceutically acceptable carrier.
Claim 24
Dependent Claim
20 words
A pharmaceutical composition comprising a diagnostically or therapeutically effective amount of conjugate of claim 8 and a pharmaceutically acceptable carrier.
Claim 25
Dependent Claim
20 words
A pharmaceutical composition comprising a diagnostically or therapeutically effective amount of conjugate of claim 9 and a pharmaceutically acceptable carrier.
Claim 26
Dependent Claim
31 words
A method of targeting a pharmaceutical agent to a desired site in a patient or sample comprising administering to the patient or contacting the sample with a conjugate of claim 1.
Claim 27
Dependent Claim
31 words
A method of targeting a pharmaceutical agent to a desired site in a patient or sample comprising administering to the patient or contacting the sample with a conjugate of claim 6.
Claim 28
Dependent Claim
31 words
A method of targeting a pharmaceutical agent to a desired site in a patient or sample comprising administering to the patient or contacting the sample with a conjugate of claim 4.
Claim 29
Dependent Claim
31 words
A method of targeting a pharmaceutical agent to a desired site in a patient or sample comprising administering to the patient or contacting the sample with a conjugate of claim 8.
Claim 30
Dependent Claim
31 words
A method of targeting a pharmaceutical agent to a desired site in a patient or sample comprising administering to the patient or contacting the sample with a conjugate of claim 9.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-03-10 | 1995-09-09 | 1996-03-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-03-10 | 1999-09-09 | 2000-03-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-03-10 | 2003-09-09 | 2004-03-10 | $7700.00 | Window Closed / Lapsed |