Gastrin releasing peptide compounds

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound

Reexamination Certificate

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C424S001110, C424S001650, C424S001210, C514S002600

Reexamination Certificate

active

07850947

ABSTRACT:
New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure:wherein R1-R5 and FG are define herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

REFERENCES:
patent: 4885363 (1989-12-01), Tweedle
patent: 4988496 (1991-01-01), Srinivasan et al.
patent: 5068222 (1991-11-01), Camble et al.
patent: 5084555 (1992-01-01), Coy et al.
patent: 5217955 (1993-06-01), Bogden et al.
patent: 5244883 (1993-09-01), Cai et al.
patent: 5369094 (1994-11-01), Schally et al.
patent: 5410018 (1995-04-01), Spindel et al.
patent: 5428018 (1995-06-01), Edwards et al.
patent: 5428019 (1995-06-01), Edwards et al.
patent: 5474756 (1995-12-01), Tweedle et al.
patent: 5534497 (1996-07-01), Verbruggen
patent: 5620955 (1997-04-01), Knight et al.
patent: 5620959 (1997-04-01), Leban et al.
patent: 5649537 (1997-07-01), Anelli et al.
patent: 5686410 (1997-11-01), Albert et al.
patent: 5723578 (1998-03-01), Coy et al.
patent: 5833985 (1998-11-01), Ball et al.
patent: 5834433 (1998-11-01), Krstenansky
patent: 5965695 (1999-10-01), Simon et al.
patent: 5981504 (1999-11-01), Buchsbaum et al.
patent: 6075121 (2000-06-01), Simon et al.
patent: 6191290 (2001-02-01), Safavy
patent: 6200546 (2001-03-01), Hoffman et al.
patent: 6307017 (2001-10-01), Coy et al.
patent: 6461588 (2002-10-01), Anelli et al.
patent: 6866837 (2005-03-01), Reubi et al.
patent: 6921526 (2005-07-01), Hoffman et al.
patent: 7226577 (2007-06-01), Cappelletti et al.
patent: 7611692 (2009-11-01), Cappelletti et al.
patent: 2002/0054855 (2002-05-01), Hoffman et al.
patent: 2002/0164287 (2002-11-01), Rajagopalan
patent: 2002/0176819 (2002-11-01), Hoffman et al.
patent: 2003/0050436 (2003-03-01), Coy et al.
patent: 2003/0171561 (2003-09-01), Pillai et al.
patent: 2003/0224998 (2003-12-01), Reubi et al.
patent: 2004/0136906 (2004-07-01), Cappelletti et al.
patent: 2005/0163710 (2005-07-01), Hoffman et al.
patent: 2005/0171014 (2005-08-01), Tarasova et al.
patent: 2006/0067886 (2006-03-01), Hoffman et al.
patent: 2007/0161047 (2007-07-01), Zhong et al.
patent: 2007/0270575 (2007-11-01), Jakobovits et al.
patent: 2008/0008649 (2008-01-01), Cappelletti et al.
patent: 0309297 (1989-03-01), None
patent: 0436005 (1995-03-01), None
patent: 0489089 (1996-06-01), None
patent: 0438519 (1998-05-01), None
patent: 1181936 (2002-02-01), None
patent: 0749325 (2002-06-01), None
patent: 1001977 (2005-10-01), None
patent: 89/02897 (1989-04-01), None
patent: 90/03980 (1990-04-01), None
patent: WO91/01144 (1991-02-01), None
patent: 91/02746 (1991-03-01), None
patent: 95/24220 (1995-09-01), None
patent: 9532741 (1995-12-01), None
patent: WO96/03427 (1996-02-01), None
patent: 98/47524 (1998-10-01), None
patent: 9847524 (1998-10-01), None
patent: 99/62563 (1999-12-01), None
patent: 0038738 (2000-07-01), None
patent: 00/50059 (2000-08-01), None
patent: 01/52900 (2001-07-01), None
patent: 0152900 (2001-07-01), None
patent: 0162777 (2001-08-01), None
patent: 02087631 (2002-11-01), None
patent: 02087631 (2002-11-01), None
patent: 03/72754 (2003-09-01), None
patent: 2004062574 (2004-07-01), None
patent: 2004065407 (2004-08-01), None
Eckelman et al (1993), The Design of Site-Directed Radiopharmaceuticals for use in Drug Discovery, Nuclear Imaging in Drug Discovery, Development, and Approval (eds) H.D. Burns et al, Birkauser Publ. Inc., Boston, MA, pp. 113-134.
Hoffman et al (Jun. 1997), Synthesis and Characterizationof Rh-105 Labeled Bombesin Analogues: Enhancement of GRP Receptor Binding Affinity Utiliing Aliphatic Carbon Chain Linkers, 12thInternational Symposium on Radiopharmaceutical Chemistry, pp. 490-492.
International Search Report, PCT/US09/44447.Oct. 6, 2009, 3 pages.
Giblin et al. (1998), Proc. Natl. Aca. Sci., USA, vol. 95, pp. 12814-12818.
Walsh et al., Western Journal of Medicine, vol. 155, pp. 152-163, 1991.
Heppeler et al., Receptor Targeting for Tumor Localization and Therapy with Radiopeptides. Current Medicinal Chemistry 2000, 7:971-994.
Sethi et al., Growth of small cell lung cancer cells: stimulation by multiple neuropeptides and inhibition by broad spectrum antagonists in vitro and in vivo, Cancer Res. May 1, 1992;52(9 Suppl):2737s-2742s.
Halmos, T., Wittliff, J.L., and Schally, A.V., Characterization of bombesin/gastrin releasing peptide receptors on human breast cancer and their Relationship to steroid receptor expression, Cancer Research 55:280-287, 1995.
Kelly, K., Kane, M.A., and Bunn, P.A., “Growth factors in lung cancer: Possible etiologic role and clinical target”, Medical and Pediatric Oncology 19:449-458, 1991.
Jensen, R.T., Mrozinski, J.E., and Coy, D.H., “Bombesin receptor antagonists: Different classes and cellular basis of action”, Recent Results in Cancer Research 129:87-113.
Reile, H., Armatis, P.E., and Schally, A.V., Characterization of high-affinity receptors for bombesin/gastrin releasing peptide on the human prostate cancer cell lines PC-3 and DU-145: internalization of receptor bound 125I-(Tyr4) bombesin by tumor cells, Prostate, Jul. 1994;25(1):29-38.
Schutte, J., and Seeber, S., “Bombesin antagonists: Experimental and clinical results”, Recent Results in Cancer Research 129:115-129, 1993.
Walsh, J.H., Karnes, W.E., Cuttitta, F., and Walker, A., “Autocrine growth factors and solid tumor malignancy”, Western Journal of Medicine 155: 152-163, 1991.
Leban, et al., Potent gastrin-releasing peptide (GRP) antagonists derived from GRP (19-27) with a C-terminal DPro psi [CH2NH]Phe-NH2 and N-terminal aromatic residues, J Med Chem. Feb. 18, 1994;37(4):439-45.
Li, et al.; In-Vivo and In-Vitro Characterization of a Rh-105-Tetrathiamacrocycle Conjugate of a Bombesin Analogue, Proceedings of the 43rd Annual Meeting, vol. 37, No. 5, May 1996 Supplement, p. 61.
Zhu, et al.; Binding, internalization, and processing of bombesin by rat pancreatic acini, Bombesin Binding and Internalization, 1991, pp. G57-G64.
Moody, et al.; BW1023U90: A new GRP Receptor Antagonist for Small-Cell Lung Cancer Cells, Peptides vol. 17, No. 8, pp. 1337-1343, 1996.
Moody, et al.; A GRP Receptor Antagonist Which Inhibits Small-Cell Lung Cancer Growth; Life Sciences, vol. 56, No. 7, pp. 521-529, 1995.
Seifert, et al.; No. Carrier Added Preparations of ‘3+1’ Mixed-ligand 99mTc Complexes, Appl. Radiat. Isot. vol. 49, Nos. 1-2, pp. 5-11, 1998.
Smith, et al.; In Vivo and in Vitro Characterization of Novel Water-Soluble Dithio-Bisphosphine 99mTc Complexes, Nuclear Medicine & Biology, vol. 24, pp. 685-691, 1977.
Coy et al, “Short Chain Pseudopeptide bombesin receptor antagonists with enhanced binding affinities for pancreatic Acinar and swiss 3T3 cells display strong Antimitotic activity” J. Biol. Chem., vol. 264, No. 25, pp. 14691-14697, 1989.
Thomas et al., Antitumoral Activity of Bombesin Analogues on Small Cell Lung Cancer Xenografts: Relationship with Bombesin Receptor Expression, Cancer Res. Sep. 15, 1992;52(18):4872-7.
Radulovic et al., Inhibitory effects of antagonists of bombesin/gastrin releasing peptide (GRP) and somatostatin analog (RC-160) on growth of HT-29 human colon cancers in nude mice, Acta Oncol. 1994;33(6):693-701.
Qin, et al., Inhibitory effect of bombesin receptor antagonist RC-3095 on the growth of human pancreatic cancer cells in vivo and in vitro, Cancer Res. Feb. 15, 1994;54(4):1035-41.
Qin, et al., Antagonists of bombesin/gastrin-releasing peptide inh

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