Haptens of paliperidone

Patent metadata

Field	Value
Publication number	US-9394354-B2
Application number	US-201313970660-A
Country	US
Kind code	B2
Filing date	Aug 20, 2013
Priority date	Aug 21, 2012
Publication date	Jul 19, 2016
Grant date	Jul 19, 2016

Abstract

The invention relates to compounds of Formula I, wherein L 1 , L 2 , and L 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from paliperidone. The invention also relates to conjugates of a paliperidone hapten and a protein.

First claim

We claim:

1. The compound of Formula I

wherein
L 1 is OC(O)(CH 2 ) n , or O(CH 2 ) n ;
wherein n is 1, 2, or 3;
L 2 is NHC(O),

or absent;
L 3 is (CH 2 ) m CO 2 H, or

wherein m is 0-3; provided that m may only be 0 if L 2 is absent, and further provided that when L 2 is absent L 3 is

2. The compound of claim 1 , wherein
L 1 is OC(O)(CH 2 ) n , or O(CH 2 ) n ;
wherein n is 1, 2, or 3;
L 2 is NHC(O),

or absent;
L 3 is (CH 2 ) m CO 2 H, or

wherein m is 0-2; provided that m may only be 0 if L 2 is absent, and further provided that when L 2 is absent L 3 is

3. The compound of claim 1 which is:

Assignees

• Janssen Pharmaceutica Nv
• Ortho Clinical Diagnostics Inc

Inventors

• Haspeslagh Pieter Rik
• Vliegen Maarten
• Hryhorenko Eric
• Decory Thomas R
• Sankaran Banumathi

Classifications

• A61K39/385 Primary

  Haptens or antigens, bound to carriers · CPC title

• A61K47/646

  the entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines · CPC title

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• A61K47/64

  Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65) · CPC title

• A61K2039/6081

  Albumin; Keyhole limpet haemocyanin [KLH] · CPC title