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US5087696A Expired / Lapsed US ⏱️ 0.0 years remaining

Conjugate compound

Assignee: Celltech R&D Ltd
•
Filing: 1987-02-13
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Granted: 1992-02-11
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Expires: 2007-02-13
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Abstract

Abstract A conjugate compound has the structure (I), wherein R 1 is --(CH 2 ) p --R 6 --(CH 2 ) q -- where p and q are the same or different and are 0, 1 or 2, and --R 6 -- is --(CH 2 ) n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R 1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R 6 is --CH 2 --; R 2 are --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R 3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R 4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R 7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R 4 is (III d), R 3 is not carboxyalkyl, R 5 is a linker, and Ab is an antibody. The conjugate compound provides for complexes of metals such as Tc, Co, Re, Cu, Au and Ag which are useful reagents for in vivo imaging and therapy.

Inventors

  • 👤 David Parker
  • 👤 Thomas A. Millican

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 13:46
CPC Classifications
C; C07; C07D; C07D273/00; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/10; A61K51/1093; C07D257/00; C07D257/02; C07D257/10; C07D401/00; C07D401/02; C07D401/12; C07D403/00; C07D403/02; C07D403/12; A61K2123/00

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 159 words
A compound having the structure: ##STR15## wherein R 1 is --(CH 2 )p--R 6 --(CH 2 )q-- where p and q are the same or different and are 0, 1 or 2, and --R 6 -- is --(CH 2 ) n --, where n is 0 or 1, --NH--, --O--, --S-- or ##STR16## R 1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R 6 is --CH 2 --, R 2 are --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted, R 4 is ##STR17## --CH 2 --CH 2 --CH-- or --CH 2 --CH--CH 2 -- optionally alkyl substituted, wherein R 7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R 4 is --CH 2 --CH--CH 2 --, R 3 is not carboxyalkyl, and R 8 comprises an exocylic amine having a pKa from 8 to 10 covalently attached to R 4 .
Claim 2
Dependent Claim 159 words
A compound having the structure: ##STR15## wherein R 1 is --(CH 2 )p--R 6 --(CH 2 )q-- where p and q are the same or different and are 0, 1 or 2, and --R 6 -- is --(CH 2 ) n --, where n is 0 or 1, --NH--, --O--, --S-- or ##STR16## R 1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R 6 is --CH 2 --, R 2 are --CH 2 CH 2 -- or --CH 2 CH 2 CH 2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted, R 4 is ##STR17## --CH 2 --CH 2 --CH-- or --CH 2 --CH--CH 2 -- optionally alkyl substituted, wherein R 7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R 4 is --CH 2 --CH--CH 2 --, R 3 is not carboxyalkyl, and R 8 comprises an exocylic amine having a pKa from 8 to 10 covalently attached to R 4 .
Claim 3
Dependent Claim 17 words
A compound according to claim 1 wherein R 8 is --CH 2 --Ar--CH 2 NH 2 .
Claim 4
Dependent Claim 27 words
The compound according to claim 1, wherein R 1 is --CH 2 CH 2 CH 2 -- or --CH 2 CH 2 OCH 2 CH 2 --.
Claim 5
Dependent Claim 19 words
The compound according to claim 1, wherein R 2 are the same and are --CH 2 CH 2 --.
Claim 6
Dependent Claim 15 words
The compound according to claim 1 wherein R 3 are the same and are --H.
Claim 7
Dependent Claim 11 words
The compound according to claim 1, including a complexed metal atom.
Claim 8
Dependent Claim 19 words
The compound according to claim 6 wherein the complexed metal atom is Tc, Re, Co, Cu, Au or Ag.
Claim 9
Dependent Claim 15 words
The compound according to claim 7, wherein the complexed metal atom is Tc or Cu.

References Cited (Backward Citations)

US4174428A Cited
US4678667A Cited
US4885363A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1995-02-10 1995-08-12 1996-02-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1999-02-10 1999-08-12 2000-02-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2003-02-10 2003-08-12 2004-02-11 $7700.00 Window Closed / Lapsed

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