Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2005-02-24
2009-08-11
Desai, Rita J (Department: 1625)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C546S169000, C514S309000, C514S312000
Reexamination Certificate
active
07572913
ABSTRACT:
Substituted piperidine compounds represented by the structure I are provided,wherein each of R1a, R1b, R1c, R1d, R1e, R1f, R1g, R1h, R2, R2A, R3, R4, A, X, a, x and n is as defined in the specification. Substituted piperidine compounds of structure I may permeate or penetrate across a nerve cell membrane into the interior of a nerve cell, may inhibit intracellular Rho kinase enzyme found in nerve cells in mammals, and may find utility in repair of damaged nerves in the central and peripheral nervous system of such mammals. These compounds may induce the regeneration or growth of neurites in mammalian nerve cells and may thereby induce regeneration of damaged or diseased nerve tissue. These compounds also find additional utility as antagonists of the enzyme Rho kinase in treatment of disease states in which Rho kinase is implicated. Pharmaceutical compositions containing these substituted piperidine compounds may be useful to promote neurite growth and in the treatment of diseases in which Rho kinase inhibition is indicated.
REFERENCES:
patent: 3539573 (1970-11-01), Hunziker et al.
patent: 4584303 (1986-04-01), Huang et al.
patent: 4849521 (1989-07-01), Kudzma et al.
patent: 4857301 (1989-08-01), Czarniecki et al.
patent: 4866077 (1989-09-01), Bogeso et al.
patent: 4933353 (1990-06-01), Jensen et al.
patent: 4997834 (1991-03-01), Muro et al.
patent: 5478838 (1995-12-01), Arita et al.
patent: 5496846 (1996-03-01), Wilson et al.
patent: 5741792 (1998-04-01), Kimball et al.
patent: 5906819 (1999-05-01), Kaibuchi et al.
patent: 6020352 (2000-02-01), Kapin et al.
patent: 6140333 (2000-10-01), Tsuchiya et al.
patent: 6169097 (2001-01-01), Janssens et al.
patent: 6218410 (2001-04-01), Uehata et al.
patent: 6297228 (2001-10-01), Clark
patent: 6545022 (2003-04-01), Bryans et al.
patent: 7199147 (2007-04-01), Imazaki et al.
patent: 2304981 (1999-05-01), None
patent: 2342251 (2000-03-01), None
patent: 2325842 (2002-05-01), None
patent: 2443108 (2002-10-01), None
patent: WO 03/042174 (2003-05-01), None
U.S. Appl. No. 10/022,301, filed Aug. 29, 2002, McKerracher et al.
U.S. Appl. No. 09/903,738, filed Mar. 28, 2002, Steffan et al.
Ishizaki et al.; “The small GTP-binding protein Rho binds to . . . ”; EMBO; 1996; pp. 1885-1893; vol. 15; issue 8.
Sayas et al.; “Glycogen Synthase Kinase-3 . . . ”; J. Neuroscience; Aug. 15, 2002; pp. 6863-6875; vol. 2, issue 16.
Weggen et al.; “A subset of NSAIDs lower . . . ”; Nature; Nov. 8, 2001; pp. 212-216; vol. 414.
Ishizaki et al.; “Pharmacological Properties of Y-27632 . . . ”; Molecular Pharmacology; Jan. 12, 2000; pp. 976-983; vol. 57.
Leemhuis et al.; “The Protein Kinase A Inhibitor H89 . . . ”; J. Pharmacol. Exp. Ther.; Nov. 8, 2001; pp. 1000-1007; vol. 300; issue 3.
Ishizaki et al.; “p160ROCK, a Rho-associated coiled-coil forming protein kinase . . . ”; FEBBS Letters; Jan. 16, 1997; pp. 118-124; vol. 404; issue 2.
Wibberley et al.; “Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle”; British J. Pharmacology; 2003; pp. 757-766; vol. 138.
Jick et al.; “Statins and the risk of dementia”; Lancet; Nov. 11, 2000; pp. 1627-1631; vol. 356.
Kato et al.; “Statin blocks Rho/Rho-kinase signalling . . . ”; Biochimica et Biophysica Acta; May 31, 2004; pp. 267-272; vol. 1689.
DelPeso; “Rho proteins induce metastatic properties in vitro”; Oncogene; Aug. 13, 1997; pp. 3047-3057; vol. 15.
Alexopoulos et al.; “Design and Synthesis of Novel Biologically Active Thrombin Receptor . . . ”; J. Med. Chem.; 2004; pp. 3338-3352; vol. 47.
Lee et al.; “Neurodegenerative Tauopathies”; Annu. Rev. Neurosci.; 2001; pp. 1121-1159; vol. 24.
McGeer et al.; “Anti-inflammatory drugs and Alzheimer disease”; Lancet; 1990; p. 1037; vol. 335.
McKerracher et al.; “Identification of Myelin-Associated Glycoprotein . . . ”; Neuron; Oct. 1994; pp. 805-811; vol. 13.
Zhou et al.; “Nonsteroidal Anti-Inflammatory Drugs . . . ”; Science; Nov. 14, 2003; pp. 1215-1217; vol. 302.
Nakagawa et al.; “ROCK-I and ROCK-II, two isoforms of Rho-associated coiled-coil forming protein serine/threonine kinase in mice”; FEBBS Letters; 1996; pp. 189-193; vol. 392.
Registry No. 289476-26-2 CAPLUS; Jun. 26, 2003.
Registry No. 289476-24-0 CAPLUS; Jun. 26, 2003.
Gingras Karine
Lubell William
McKerracher Lisa
Snow Robert
Thouin Eryk
Bioaxone Therapeutique Inc.
Desai Rita J
K&L Gates LLP
Mabry John
LandOfFree
4-substituted piperidine derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 4-substituted piperidine derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 4-substituted piperidine derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4096985