Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-10-18
2011-11-08
Anderson, Rebecca (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S254080, C544S364000, C544S369000, C544S372000
Reexamination Certificate
active
08053436
ABSTRACT:
The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular efficient inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.
REFERENCES:
patent: 4379160 (1983-04-01), Harfenist et al.
patent: 5958919 (1999-09-01), Olney et al.
patent: 1 167 510 (1958-11-01), None
patent: 3-251564 (1991-11-01), None
patent: 6-228095 (1994-08-01), None
patent: 787352 (1978-11-01), None
patent: 1 584 341 (1995-03-01), None
patent: 96 06863 (1996-03-01), None
patent: 97 01635 (1997-01-01), None
patent: 97/14865 (1997-04-01), None
patent: 97 26881 (1997-07-01), None
Hromatka et al., Mh. Chem., 92, 1242 (1961).
Michael D. Jacobson: “Apoptosis: Bcl-2-related proteins get connected” Current Biology, 7:R277-R281 1997.
Guido Kroemer: “The proto-oncogene Bcl-2 and its role in regulating apoptosis” Nature Medicine, vol. 3, No. 6, pp. 614-620 Jun. 1997.
John C. Reed: “Double identity for proteins of the Bcl-2 family” Nature, vol. 387, pp. 773-776 Jun. 19, 1997.
Ameeta Kelekar et al.: “Bcl-2-family proteins: the role of the BH3 domain in apoptosis” Trends in Cell Biology, vol. 8, pp. 324-330 Aug. 1998.
Isabelle Martinou et al.: “Viral proteins E1B19K and p35 protect sympathetic neurons from cell death induced by NGF deprivation” The Journal of Cell Biology, vol. 128, No. 1-2, pp. 201-208 Jan. 1995.
Thomas L. Deckwerth, et al.: “BAX is required for nuronal death after trophic factor deprivation and during development” Neuron, vol. 17, pp. 401-411 Sep. 1996.
Gloria I. Perez et al.: “Prolongation of ovarian lifespan into advanced chronological age by Bax-deficiency” Nature Genetics, vol. 21, pp. 200-103 Feb. 1999.
N.A. Komissarenko et al.: “Synthesis of 1-lw-(benzhydrypiperazin-1-yl)alkyl[indoles, 9-[3-(4-benzhydrylpiperazin-1-yl)propyl)carbazole and its derivatives and their antiallergic activity” Khim. Farm. Zh., vol. 24, No. 10, pp. 54-56 1990.
Tetsuto Tsunoda et al.: “Mitsunobu-type alkylation with active methine compounds” Tetrahedron Letters, vol. 37, No. 14, pp. 2459-2462 1996.
Domenico Albanese et al.: “Chemoselective N-alkylation of 2-hydroxycarbazole as a model for the synthesis of N-substituted pyrrole derivatives containing acidic functions” Tetrahedron Letters, vol. 51, No. 19, pp. 5681-5688 1995.
Keith Smith et al.: “A new method for bromination of carbazoles, B-carbolines and iminodibenzyls by use of N-bromosuccinimide and silica gel” Tetrahedron Letters, vol. 48, No. 36, pp. 7479-7488 1992.
T. Ross Kelly et al: “Structure revision of the APHEs through synthesis” Tetrahedron Letters, vol. 40, pp. 1857-1860 1999.
D.A. Patrick et al.: “Anti-pneumocystis carinii pneumonia activity of dicationic carbazoles” Eur. J. Med. Chem, vol. 32, pp. 781-793 1997.
Koert Gerzon et al.: “Structure-activity relationship of some diamine, bis-epoxIdes in mouse leukaemia” Journal of Medicinal and Pharmaceutical Chemistry, vol. 1, No. 3, pp. 223-243, 1959.
Solange Desagher et al.: “Bid-induced conformational change of Bas is responsible for miotchondrial cytochrome c release during apoptosis” The Journal of Cell Biology, vol. 144, No. 5, pp. 891-901 Mar. 8, 1999.
Robert E. King, phD., Pharmaceutical Preparations and Their Manufacture, Remington's Pharmaceutical Sciences 17thEdition, Part 8, pp. 1409-1677.
Antonsson Bruno
Bombrun Agnes
Church Dennis
Gerber Patrick
Halazy Serge
Anderson Rebecca
Merck Serono SA
Oblon, Spivak McClelland, Maier & Neustadt, L.L.P.
LandOfFree
9-(piperazinylalkyl) carbazoles as bax-modulators does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 9-(piperazinylalkyl) carbazoles as bax-modulators, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 9-(piperazinylalkyl) carbazoles as bax-modulators will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4305779