Title:
DIFUNCTIONAL LINKER
Document Type and Number:
Japanese Patent JPS62116592
Kind Code:
A
Abstract:
A selective bifunctional sequential linker has the formulaY=C=N-Q-A-C(O)-Zwherein Q is a homoaromatic or heteroaromatic ring system; A is a single bond or an unsubstituted or substituted divalent C1-30 bridging group; Y is O or S; and Z is Cl, Br, I, N₃, N-succinimidyloxy, imidazolyl, 1-benzotriazolyloxy, OAr where Ar is an electron-deficient activating aryl group, or OC(O)R where R is -A-Q-N=C=Y or C4-20 tertiary-alkyl. A method for activating an amine function towards reaction with a second amine involves reacting the amine with the foregoing linker. The resultant isocyanate or isothiocyanate derivative can then be reacted with a second amine to form a urea or thiourea conjugate.The linker is useful for producing conjugates of ligands with amine-containing polymers and/or proteins, especially for forming antibody conjugates with chelators, drugs, enzymes, detectable labels and the like.
Inventors:
SUNDORO BOBY M (US)
Application Number:
JP24728486A
Publication Date:
May 28, 1987
Filing Date:
October 16, 1986
Export Citation:
Assignee:
IMMUNOMEDICS INC (US)
International Classes:
C07H15/252; A61K38/00; A61K39/395; C07C265/12; C07C331/26; C07C331/28; C07D207/404; C07D249/18; C07D521/00; C07K17/00; G01N33/531; G01N33/532; G01N33/535; G01N33/543; G01N33/577; (IPC1-7): A61K37/02; A61K39/395; C07D207/404; C07D249/18; C07D521/00; C07H15/252
Domestic Patent References:
| JPS57183777A | 1982-11-12 | |||
| JPS57171949A | 1982-10-22 | |||
| JPS59186906A | 1984-10-23 |
Foreign References:
| GB1152978A | 1969-05-21 | |||
| GB1070043A | 1967-05-24 |
Attorney, Agent or Firm:
Akaoka Mio
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