Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2006-08-07
2011-12-13
Fetterolf, Brandon (Department: 1628)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S232800, C514S290000, C514S538000, C514S411000, C514S339000, C548S427000, C546S276700, C546S015000, C546S111000, C544S142000, C560S102000
Reexamination Certificate
active
08076348
ABSTRACT:
[Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2Breceptor and 5-HT7receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine.[Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2Breceptor and 5-HT7receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2Breceptor and 5-HT7receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
REFERENCES:
patent: 5288758 (1994-02-01), Vidaluc et al.
patent: 5629317 (1997-05-01), Audia et al.
patent: 5643916 (1997-07-01), Audia et al.
patent: 5663178 (1997-09-01), Audia et al.
patent: 5688807 (1997-11-01), Audia et al.
patent: 5705519 (1998-01-01), Audia et al.
patent: 5736544 (1998-04-01), Audia et al.
patent: 5861408 (1999-01-01), Audia et al.
patent: 5861409 (1999-01-01), Audia et al.
patent: 5861410 (1999-01-01), Audia et al.
patent: 5869691 (1999-02-01), Audia et al.
patent: 5886004 (1999-03-01), Audia et al.
patent: 6440988 (2002-08-01), Craig
patent: 6444477 (2002-09-01), Borman et al.
patent: 6482822 (2002-11-01), Bigg et al.
patent: 6514968 (2003-02-01), TenBrink
patent: 6534535 (2003-03-01), Zhu et al.
patent: 7098233 (2006-08-01), Di Cesare et al.
patent: 7402680 (2008-07-01), Carruthers et al.
patent: 2003/0027128 (2003-02-01), Borman et al.
patent: 2004/0235899 (2004-11-01), Maria Assunta et al.
patent: 2004/0266775 (2004-12-01), Kleemann et al.
patent: 2005/0119295 (2005-06-01), Carruthers et al.
patent: 2005/0148632 (2005-07-01), Tokumasu et al.
patent: 2008/0161419 (2008-07-01), Akuzawa
patent: 2008/0171788 (2008-07-01), Akuwaza et al.
patent: 2008/0200551 (2008-08-01), Yamada
patent: 2009/0036421 (2009-02-01), Seo et al.
patent: 2009/0062363 (2009-03-01), Kaku et al.
patent: 2 537 079 (2005-09-01), None
patent: 0 309 422 (1989-03-01), None
patent: 0 622 356 (1994-11-01), None
patent: 0 639 573 (1995-02-01), None
patent: 1 264 820 (2002-12-01), None
patent: 1 541 172 (2005-06-01), None
patent: 1 716 867 (2006-11-01), None
patent: 1 852 129 (2007-11-01), None
patent: 5-194359 (1993-08-01), None
patent: 9-510216 (1997-10-01), None
patent: 11-506468 (1999-06-01), None
patent: 2004-534816 (2004-11-01), None
patent: 2005-162657 (2005-06-01), None
patent: 2008-048671 (2008-03-01), None
patent: WO 96/39382 (1996-12-01), None
patent: WO 98/55115 (1998-06-01), None
patent: WO 99/20599 (1999-04-01), None
patent: WO 00/17191 (2000-03-01), None
patent: WO 01/68585 (2001-09-01), None
patent: WO 02/056010 (2002-07-01), None
patent: WO 2004/014428 (2004-02-01), None
patent: WO 03/000252 (2004-11-01), None
patent: WO 2005/040169 (2005-05-01), None
patent: WO 2005/079845 (2005-09-01), None
patent: WO 2005/080322 (2005-09-01), None
patent: WO 2006/085510 (2006-08-01), None
Patani et al “Bioisosterim: A rational approach in drug design”, Chem., Rev., 1996, vol. 98, No. 8, pp. 3147-3176.
D. Hoyer et al., “International Union of Pharmacology Classification of Receptors for 5-Hydroxytryptamine (Serotonin),”Pharmacological Reviews, vol. 46, No. 2, pp. 157-203 (1994).
C. P. Bearcroft et al., “Postprandial Plasma 5-Hydroxytryptamine in Diarrhoea Predominant Irritable Bowel Syndrome: A Pilot Study,”Gut, vol. 42, pp. 42-46 (1998).
D.-Y. Kim, “Serotonin: A Mediator of the Brain-Gut Connection,”The American Journal of Gastroenterology, vol. 95, No. 10, pp. 2698-2709 (2000).
N. J. Talley, “Pharmacologic Therapy for the Irritable Bowel Syndrome,”The American Journal of Gastroenterology, vol. 98, No. 4, pp. 750-758 (2003).
F. De Ponti et al., “Irritable Bowel Syndrome (New Agents Targeting Serotonin Receptor Subtypes),”Drugs, vol. 61, No. 3, pp. 317-332 (2001).
R. A. Borman et al., “Functional Evidence for a 5-HT2BReceptor Mediating Contraction of Longitudinal Muscle in Human Small Intestine,”British Journal of Pharmacology, vol. 114, pp. 1525-1527 (1995).
R. A. Borman et al., “5-HT2BReceptors Play a Key Role in Mediating the Excitatory Effects of 5-HT in Human Colon in vitro,”British Journal of Pharmacology, vol. 135, pp. 1144-1151 (2002).
D. Carter et al., “Characterization of a Postjunctional 5-HT Receptor Mediating Relaxation of Guinea-pig Isolated Ileum,”European Journal of Pharmacology, vol. 280, pp. 243-250 (1995).
H. Liu et al., “Expression Patterns of 5-HT7Receptor Isoforms in the Rat Digestive Tract,”Life Sciences, vol. 69, pp. 2467-2475 (2001).
B. Tuladhar et al., “5-HT7Receptors Mediate the Inhibitory Effect of 5-HT on Peristalsis in the Isolated Guinea-pig Ileum,”British Journal of Pharmacology, vol. 138, pp. 1210-1214 (2003).
E. J. Mylecharane, “5-HT2Receptor Antagonists and Migraine Therapy,”Journal of Neurology, vol. 238, pp. S45-S52 (1991).
K. W. Johnson et al., “Neurogenic Dural Protein Extravasation Induced by Meta-Chlorophenylpiperazine (mCPP) Involves Nitric Oxide and 5-HT2BReceptor Activation,”Cephalalgia, vol. 23, pp. 117-123 (2003).
P. Manivet et al., “PDZ-dependent Activation of Nitric-oxide Synthases by the Serotonin 2B Receptor,”The Journal of Biological Chemistry, vol. 275, No. 13, pp. 9324-9331 (2000).
E. P. Wei et al., “Calcitonin Gene-Related Peptide Mediates Nitroglycerin and Sodium Nitroprusside-Induced Vasodilation in Feline Cerebral Arterioles,”Circulation Research, vol. 70, No. 6, pp. 1313-1319 (1992).
D. W. Bonhaus et al., “RS-127445, A Selective 5-HT2BReceptor Antagonist, Blocks mCPP-Evoked Plasma Protein Extravasation in dura mater and Capsaicin-Evokedc-fosExpression in Trigeminal Nucleus Caudalis of Rat,”Cluster Headache&Related Conditions, J. Olesen et al., eds., Oxford University Press, pp. 278-286 (1999).
J. Terrón et al., 5-HT7Receptor mRNA Expression in Human Trigeminal Ganglia,Neuroscience Letters, Vo. 302, pp. 9-12 (2001).
J. Terrón, “Is the 5-HT7Receptor Involved in the Pathogenesis and Prophylactic Treatment of Migraine?”European Journal of Pharmacology, vol. 439, pp. 1-11 (2002).
P. Pierce et al., “Dual Effect of the Serotonin Agonist, Sumatriptan, on Peripheral Neurogenic Inflammation,”Regional Anesthesia, vol. 21, No. 3, pp. 219-225 (1996).
European Search Report dated Sep. 9, 2009.
Office Action dated Nov. 6, 2009 from a corresponding Mexican application.
Office Action dated Jun. 7, 2010, from corresponding European application No. 06782418.5.
Non-final Office Action mailed Nov. 8, 2010, for U.S. Appl. No. 10/589,892.
Extended European Search Report dated Jun. 17, 2009, for related European Application No. 06 713 158.1, related to co-pending U.S. Appl. No. 11/883,651.
English language Abstract of JP 9-510216.
Bonhaus, Douglas W.; Flippin, Lee A.; Greenhouse, Robert J.; Jaime, Saul; Rocha, Cindy; Dawson, Mark; Van Natta, Kristine; Chang, L.K.; Pulido-Rios, Tess; Webber, Andrea; Leung, Edward; Eglen, Richard M.; and Martin, Graeme R., “RS-127445: a selective, high affinity, orally bioavailable 5-HT2Breceptor antagonist”, British Journal of Pharmacology, 1999, 127, pp. 1075-1082.
D. W. Bonhaus, et al., “RS-127445, a selective 5-HT2Breceptor antagonist, blocks mCPP-evoked plasma protein extravasation in dura mater and capsaicin-evoked c-fos expression in trigeminal nucleus caudalis of rat,” vol. 9, (United Kingdom), Oxford University Press, 1999, pp. 278-286.
Lovell, Peter J.; Bromidge, Steven M.; Dabbs, Steven; Duckworth, D. Malcolm; Forbes, Ian T.; Jennings, Andrew J.; King, Frank D.; Middlemiss, Derek N.; Rahman, Shirle
Akuzawa Shinobu
Harada Koichiro
Itahana Hirotsune
Matsuzawa Takaho
Moritomo Ayako
Astellas Pharma Inc.
Cornet Jean
Fetterolf Brandon
Finnegan Henderson Farabow Garrett & Dunner LLP
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