Raloxifene acid addition salts and/or solvates thereof,...

Details Raloxifene acid addition salts and/or solvates thereof,... Raloxifene acid addition salts and/or solvates thereof,...

2011-06-21

2011-06-21

Chang, Celia (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C514S324000

Reexamination Certificate

active

07964734

ABSTRACT:
Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, compared with similar preparations based on raloxifene or raloxifene hydrochloride. The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The acid addition salts or solvates thereof are addition salts or solvates of raloxifene and a pharmaceutical acceptable acid selected among succinic acid, lactic acid, malonic acid or sulphuric acid. Further, crystalline forms of the raloxifene salts and solvates thereof are disclosed. The raloxifene acid addition salts and/or solvates thereof are useful for the preparation of pharmaceutical composition for oral administration capable of fast and reliable release of the active ingredients in the stomach of the patient, in particular for the treatment of cancer or osteoporosis, or for inhibiting cartilage degradation. A new method for preparation of raloxifene lactate is also disclosed.

REFERENCES:
patent: 4133814 (1979-01-01), Jones et al.
patent: 4418068 (1983-11-01), Jones
patent: 5852193 (1998-12-01), Chelius
patent: 0 062 503 (1982-10-01), None
patent: 0 062 504 (1982-10-01), None
patent: 0 062 505 (1982-10-01), None
patent: 0 584 952 (1994-03-01), None
patent: 0 652 002 (1995-05-01), None
patent: 0 670 162 (1995-09-01), None
patent: 0 674 903 (1995-10-01), None
patent: 0 675 121 (1995-10-01), None
patent: 0 693 488 (1996-01-01), None
patent: 0 699 672 (1996-03-01), None
patent: 0 699 673 (1996-03-01), None
patent: 0 781 555 (1997-07-01), None
patent: 0 826 682 (1998-03-01), None
patent: 0 875 511 (1998-11-01), None
patent: 2 293 382 (1996-03-01), None
patent: 2 293 602 (1996-04-01), None
patent: WO 95/34536 (1995-12-01), None
patent: WO 9609045 (1996-03-01), None
patent: WO 96/40676 (1996-12-01), None
patent: WO 96/40677 (1996-12-01), None
patent: WO 96/40678 (1996-12-01), None
patent: WO 96/40691 (1996-12-01), None
patent: WO 96/40693 (1996-12-01), None
patent: WO 97/30709 (1997-08-01), None
patent: WO 97/34888 (1997-09-01), None
patent: WO 97/35571 (1997-10-01), None
patent: WO 98/13369 (1998-04-01), None
patent: WO 98/08513 (1998-05-01), None
patent: WO 98/22456 (1998-05-01), None
patent: WO 98/48787 (1998-11-01), None
patent: WO 98/48792 (1998-11-01), None
patent: WO 98/48793 (1998-11-01), None
patent: WO 98/49156 (1998-11-01), None
patent: WO 00/04880 (2000-02-01), None
patent: WO 00/35485 (2000-06-01), None
patent: WO 0035485 (2000-06-01), None
patent: WO 00/50007 (2000-08-01), None
patent: WO 01/23369 (2001-04-01), None
patent: WO 02/42261 (2002-05-01), None
patent: WO 02/42289 (2002-05-01), None
patent: WO 2004/029046 (2004-04-01), None
patent: WO 2005/003116 (2005-01-01), None
Seddon “Pseudopolymorph . . . ” Crystal Growth and design p. 1087 (2004) (internet print out).
Braga et al. “Making crystals from . . . ” Chem. Commun. p. 3635-3645 92005).
Seddon “Pseudopolymorph . . . ” Cryst. growth and design 4(6) 1087 (2004) two page from internet.
Muzaffar et al. “Polymorphism and drug availability” J. Phar. 1(1) 59-66 (1979.
Jain et al. “Polymorphisom in pharmacey” Indian Drugs 23(g)315-329 (1986).
Doelker et al. “Crystalline modification . . . ” CA 138:209993 (2002).
Doelker et al. “Physicochemical behavior or active . . . ” CA 132:325872 (2000).
Otsuka et al. “Effect of polymorphic . . . ” Chem. Pharm. bull 47(6)852-856 (1999).
Lanz “Pharmaceutical powder tecnology . . . ” Basal (2006) p. 1-4.
CMU Pharmaceutical polymorphism, internet print out (2008) p. 1-3.
Yokoda et al. “Chiral separation . . . ”J. Chem. Eng. Japan v.37(10) p. 1284-1285 (2004).
Fasel et al. “Amplification of chirality . . . ” Nature v.439, January, p. 449-452 (2006).
Zhang et cl. “Racemic species of . . . ” J. pharm. Sci. v.92(7) p. 1356-1366 (2003).
Exhibit I, search result for C34H33NO7S/MF (2010).
Antiestrogens. 2.1. Structure-Activitiy Studies. in a Series of 3-Aroyl-2-arylbenzo [b] thien-3-y1[4-[2-(1-piperidinyl) ethosy]-phenyl]methanone Hydrochloride (LY156758), a Remarkably Effective Estrogen Antagonist with Only Minimal Intrinsic Estrogenicity, by C.D. Jones, et al. J. Med. Chem., vol. 27(8), 1057-1066.

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