(19)
(11)EP 2 359 864 A3

(12)EUROPEAN PATENT APPLICATION

(88)Date of publication A3:
01.08.2012 Bulletin 2012/31

(43)Date of publication A2:
24.08.2011 Bulletin 2011/34

(21)Application number: 10190163.5

(22)Date of filing:  08.12.2006
(51)Int. Cl.: 
A61K 47/48  (2006.01)
A61K 49/22  (2006.01)
C07K 1/20  (2006.01)
C07K 1/00  (2006.01)
C07K 14/00  (2006.01)
C07K 1/18  (2006.01)
C12P 21/04  (2006.01)
A61K 38/16  (2006.01)
(84)Designated Contracting States:
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR

(30)Priority: 09.12.2005 US 749240 P
25.07.2006 US 833342 P

(62)Application number of the earlier application in accordance with Art. 76 EPC:
06840164.5 / 1966388

(71)Applicant: Bracco Suisse SA
6928 Manno (CH)

(72)Inventors:
  • Bussat, Philippe
    F-74160, Feigeres (FR)
  • Cherkaoui, Samir
    F-74160, Feigeres (FR)
  • Fan, Hong (Helen)
    Plainsboro, NJ 08536 (US)
  • Lamy, Bernard
    F-74160, Saint-Julien-en-Genevois (FR)
  • Nanjappan, Palaniappa
    Princeton, NJ 08540 (US)
  • Pillai, Radhakrishna, K.
    Cranbury, NJ 08512 (US)
  • Pochon, Sibylle
    CH-1256, Troinex (CH)
  • Song, Bo
    Princeton, NJ 08540 (US)
  • Swenson, Rolf, E.
    Princeton, NJ 08540 (US)

(74)Representative: Leonard, Thomas Charles 
Kilburn & Strode LLP 20 Red Lion Street
London WC1R 4PJ
London WC1R 4PJ (GB)

  


(54)Targeting Vector-Phospholipid Conjugates


(57) Peptide vectors having high KDR binding affinity and processes for making such vectors are provided. The peptide vectors may be conjugated to phospholipids and included in ultrasound contrast agent compositions. Such ultrasound contrast agents are particularly useful in therapeutic and diagnostic methods, such as in imaging KDR-containing tissue and in the evaluation and treatment of angiogenic processes associated with neoplastic conditions. The present invention also provides processes for the large scale production of highly pure dimeric and monomeric peptide phospholipid conjugates as well as precursor materials used to form the conjugates. The present invention further provides processes for the large scale production of highly pure peptide phospholipid conjugates which contain very low levels of TFA.