Optical isomers of an Iloperidone metabolite

Details Optical isomers of an Iloperidone metabolite Optical isomers of an Iloperidone metabolite

2011-07-12

2011-07-12

Chang, Celia (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S198000

Reexamination Certificate

active

07977356

ABSTRACT:
The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.

REFERENCES:
patent: 4804663 (1989-02-01), Kennis et al.
patent: 5158952 (1992-10-01), Janssen et al.
patent: 5364866 (1994-11-01), Strupczewski et al.
patent: 2004/0204401 (2004-10-01), Migaly
patent: 402644 (1995-08-01), None
patent: H03-63263 (1991-03-01), None
patent: H09-511215 (1997-11-01), None
Caccia “Biotransformation of post . . . ” Clin. Pharmacokinet. v. 38(6) p. 393-414 (2000).
Corbett et al. “Iloperidone: preclinical profile . . . ” Drug Rev. v.3(2) p. 120-147 (1997).
Subramanian et al. “Receptor profile of P88 . . . ” Prog. Neuro-Psychophram. Biol. Psy. v.26 p. 553-560 (2002).
Imamura et al. “Interactions . . . ” CA 102:214444(1985).
Ookawa et al. “Antitumor complexes . . . ” CA 120:62270 (1994).
Garattini “Active drug metabolites . . . ” Clin. Pharmacokinet. v.10, p. 216-227 (1985).
Strupczewski, J.T. et al. 3-(Arylozy) Alkylpiperidinyl-1,2-Benziosoxazoles as D2/5-HT2 Antagonists with Potential Atypical Antipsychotic Activity: Antipsychotic Profile of Iloperidone (HP 873), Journal of Medicinal Chemistry, vol. 38, No. 7, pp. 1119-1131, 1995.
Subramanian, N. et al., “Receptor profile of P88-8991 and P95-12113, metabolites of the novel antipsychotic iloperidone,” Progress in Neuro-Psychopharmacology & Biological Psychiatry, 26:553-560, 2002.
64 USPQ2d 1032 Decided Aug. 2002.
Corey E. J. et al., “A Stable and Easily Prepared Catalyst for the Enantioselective Reduction of Ketones. Applications to Multistep Syntheses”, Journal of the American Chemical Society, vol. 109, No. 25, pp. 7925-7926, 1987.
Mutlib, A.E. et al., “Application of Liquid Chromatography/Mass Spectrometry in Accelerating the Identification of Human Liver Cytochrome P450 Isoforms Involved in the Metabolism of Iloperidone”, The Journal of Pharmacology and Experimental Theraputics, vol. 286, No. 3 pp. 1285-1293.
Mutlib, A.E. et al., “Picogram determination of iloperidone in human plasma by solid-phase extraction and by high-performance liquid chromatography-selected-ion monitoring electrospray mass spectrometry”, Journal of Chromatography B. 669, 1995, pp. 237-246.
Meltzer, H., “The Role of Serotonin an Antipsychotic Drug Action”, Neuropsyhopharmacology, vol. 21, No. 2S, 1999.
Williams et al., “Importance of Drug Enantiomers in Clinical Pharmacology”, Department of Clinical Pharmacology, St. Vincent's Hospital, Darlinghurst, Sydney, Drugs 30, 1985, pp. 333-354.
Kuntzelmann, “Functional characterization of the enantiomers of P88-8991 at the human a2c adrenoceptor and the human dopamine D2A receptor”, Novartis Pharma AG report, Sep. 27, 2001, 8 pages.
Neumann, “The effect of the enantiomers of P88-8991 in ilperidone on spontaneous locomotion and amphetamine-induced locomotion in rats” Novartis Pharma AG report, Sep. 27, 2001, 10 pages.
Fura, Aberra, “Role of pharmacologically active metabolites in drug discovery and development”, Drug Discovery Today, Feb. 2006, 11(3/4): 133-142.
Clarke, Frank H., “Role of Drug Metabolism in Drug Research and Development: View of a Medicinal Chemist”, Journal of Pharmaceutical Sciences, 1678.
Blumer et al., “NVP-AES059-NX1 and NVP-AES060-NX-1; Enantiomers of the P88 8991 metabolite of Iloperidone: Receptor Affinity Profile (Short List)”, Novartis Pharma AG report, Jan. 28, 2001, 10 pages.
Grimler et al., U.S. Appl. No. 10/488,128, 4-32076A, Office Action Communication, Mar. 16, 2006, 8 pages.
Grimler et al., U.S. Appl. No. 10/488,128, 4-32076A, Office Action Communication, Sep. 25, 2006, 7 pages.
Grimler et al., U.S. Appl. No. 10/488,128, 4-32076A, Office Action Communication, Jun. 14, 2007, 8 pages.
Grimler et al., U.S. Appl. No. 10/488,128, 4-32076A, Office Action Communication, Mar. 6, 2008, 9 pages.
Grimler et al., U.S. Appl. No. 10/488,128, 4-32076A, Office Action Communication, Oct. 17, 2008, 13 pages.
Grimler et al, U.S. Appl. No. 60/316,390, PV Application, Aug. 31, 2001.
Nozulak et al., U.S. Appl. No. 10/575,040, filed Dec. 6, 2006, Office Communication dated May 5, 2010, 7 pages.
Waller et al., Prodrugs, 1989, pp. 497-507, Br. J. Clin. Pharmac, vol. 28.
Bundgaard, “Design of Prodrugs”, 1985, pp. 1-3, Elsevier Science Publishers B.V.

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