US 7,405,320 B2Granted

Therapeutic and diagnostic conjugates for use with multispecific antibodies

AssigneeImmunomedics, Inc.

InventorsWilliam J. McBride, David M. Goldenberg, Carl Noren, Hans J. Hansen

Life of this patent

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Abstract

Disclosed are compounds that include two or more haptens conjugated by a spacer or a carrier. The haptens may include diethylenetriaminepentaacetate (DTPA), histimine-succinyl-glutamine (HSG), or combinations of DTPA and HSG. The compound also includes an effector molecule which may be conjugated to one or more of the haptens, the spacer/carrier, or both. The effector molecule may be conjugated by a number of linkages including an ester linkage, an imino linkage, an amino linkage, a sulfide linkage, a thiosemicarbazone linkage, a semicarbazone linkage, an oxime linkage, an ether linkage, or combinations of these linkages. Also disclosed are methods of synthesizing the compounds and/or precursors of the compounds.

Claims15

Dependent claims

A method of preparing a polyalkylene polyamine substituted at one or more nitrogen positions with an alkyl carboxylate group, comprising:

reacting a polyalkylene polyamine having a formula NH2—R with a molecule having a formula Z-X1 to form a molecule (I) having a formula Z-NH—R, wherein R is a straight chain or branched alkyl group that has between 1 and 20 carbon atoms and includes one or more nitrogen atoms, Z is a protecting group, and X1 is a leaving group;
reacting molecule (I) with a molecule (II) having a formula:
wherein X2 is a leaving group and A1 and A2 are straight chain or branched alkyl groups having between 1 and 12 carbon atoms, to form a molecule (III) having a formula:
wherein one or more nitrogen atoms within R are optionally substituted with a molecule having the formula:
removing and replacing the protecting group Z;
wherein Z is removed and replaced by reacting molecule (III) with H2, palladium and glyoxylic acid monohydrate.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/776,470Filed 11 Feb 2004 · continuation in part
Priority: 22 Jun 1998
Published: US 2005/0002945 A16 Jan 2005
Granted: 29 Jul 2008
Term ends: Not estimatedThe source records don’t support an estimate.

Classification73 codes

A61K 51/0497
Organic compounds: conjugates with a carrier being an organic compounds
A61K 47/665
The modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells: the pre-targeting system, clearing…
A61K 51/04
Characterised by the carrier , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus: organic compounds
A61K 51/0455
Having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins: having six-membered rings with one nitrogen as the only ring hetero atom

Family

Application60/090,142Us provisional application · filed 22 Jun 1998
Application60/104,156Us provisional application · filed 14 Oct 1998
Application09/337,756Parent of this continuation-in-part · filed 22 Jun 1999
Application09/382,186Parent of this continuation-in-part · filed 23 Aug 1999
Application09/823,746Parent of this continuation-in-part · filed 3 Apr 2001
Application10/150,654Parent of this continuation-in-part · filed 17 May 2002
US 2005/0002945 A1Pre-grant publication · published 6 Jan 2005
US 7,138,103 B2Parent of this continuation-in-part
US 6,962,702 B2Parent of this continuation-in-part
US 7,052,872 B1Parent of this continuation-in-part
US 7,074,405 B1Parent of this continuation-in-part
US 2002/0006379 A1Published application
US 2003/0198595 A1Published application
US 7,405,320 B2This patent

From the US filing history. Foreign family members aren’t listed.