[(1H-indazol-3-yl)methyl]phenols and...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S403000, C514S023000, C548S361100, C536S017400

Reexamination Certificate

active

07598286

ABSTRACT:
This invention provides anti-inflammatory agents of formula I, having the structurewherein A and R1-R10are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.

REFERENCES:
patent: 5691362 (1997-11-01), McCormick et al.
patent: 0 358 903 (1990-03-01), None
patent: 0 538 000 (1993-04-01), None
patent: 0 562 832 (1993-09-01), None
patent: 0 671 390 (1995-09-01), None
patent: 93/13099 (1993-07-01), None
patent: 95/15758 (1995-06-01), None
patent: 98/09961 (1998-03-01), None
patent: 98/43969 (1998-10-01), None
patent: 2004/031159 (2004-04-01), None
Adams, M. R. et al., “Inhibition of Coronary Artery Atherosclerosis by 17-beta Estradiol in Ovariectomized Monkeys,”Arterio., 1990, 10(6), 1051-1057.
Alexander et. al., “Initiation of Hormone Replacement Therapy After Acute Myocardial Infarction Is Associated With More Cardiac Events During Follow-Up,”J. Am. Coll. Cardio., 2001, 38, 1-7.
Bauer M. A., Herrmann F., “Interleukin-6 in clinical medicine,”Ann. Hematol., 1991, 62, 203-210.
Boulton, B. E. et al., “Kinetics, Stoichiometry and Mechanism in the Bromination of Aromatic Heterocycles. III Aqueous Bromination of Indazole,”Aust. J. Chem., 1974, 27, 2343-2347.
Cefalu, W., “The Use of Hormone Replacement Therapy in Postmenopausal Women with Type 2 Diabetes,”J Womens Health&Gender-based Med., 2001, 10(3), 241-255.
Cercek, B. et al., “Nuclear factor-κB Activity and arterial response to balloon injury,”Atherosclerosis131, 59-66 (1997).
Chandrasekar, B. et al. “Ischemia-Reperfusion of Rat Myocardium Activates Nuclear Factor-κB and Induces Neutrophil Infiltration Via Lipopolysaccharide-Induced CXC Chemokine,”Circulation, 2001 103, 2296-2302.
Collot, V. et al., “Heck cross-coupling reaction of 3-iodoindazoles with methyl acrylate: a mild and flexible strategy to design 2-azatryptamines,”Tetrahedron Letters, 2000, 41, 4363.
Collot, V. et al., “Suzuki-Type Cross-Coupling Reaction of 3-Iodoindazoles with Aryl Boronic Acids: a General and Flexible Route to 3-Arylindazoles,”Tetrahedron, 1999, 55, 6917.
Collot, V. et al., “First combined selective N- and C-arylations with boronic acids: application to the synthesis of 1,3-diarylindazoles,”Tetrahedron Letters, 2000, 41, 9053-9057.
Cuzzocrea, S. et al., “17β-Estradiol Antiinflammatory Activity in Carrageenan-Induced Pleurisy,”Endocrinology, 2000, 141, 1455-1463.
Delyani, J. A. et al., “Protection from Myocardial Reperfusion Injury by Acute Administration of 17 β-Estradiol,”J. Molec. Cell. Cardiol., 1996, 28, 1001-1008.
Dietrich, H. et al., “Mouse Model of Transplant Arteriosclerosis,”Arterioscler. Thromb. Vasc. Biol., 2000, 20, 343-352.
Dubal, D. B. et al., “Estradiol Modulates bcl-2 in Cerebral Ischemia: A Potential Role for Estrogen Receptors,”J. Neurosci., 1999, 19, 6385-6393.
Dubal, D. B. et al., “Estrogen receptor α, not β, is a critical link in estradiol-mediated protection against brain injury,”PNAS, USA, 2001, 98, 1952-1957.
Felson, D. T. et al., “The effects of estrogen on osteoarthritis,”Curr Opinion Rheum, 1998, 10, 269-272.
Fludzinski, P. et. al., “Indazoles as indole bioisosteres: synthesis and evaluation of the tropanyl ester and amide of indazole-3-carboxylate as antagonists at the serotonin 5HT3 receptor,”J. Med. Chem, 1987, 30(9), 1535-1537.
Grodstein F. et. al., “Postmenopausal Hormone Use and Secondary Prevention of Coronary Events in the Nurses' Health Study,”Ann. Int. Med, 2001, 135, 1-8.
Grodstein, F. et. al., “A Prospective, Observational Study of Postmenopausal Hormone Therapy and Primary Prevention of Cardiovascular Disease,”Ann. Int. Med., 2000, 133, 933-41.
Harada, H. et al., “Development of potent serotonin-3 (5-HT3) receptor antagonists. II. Structrue-activity relationships of N-(1-benzyl-4-methylhexahydro-1H-1,4-diazepin-6-yl)carboxamides,”Chem. Pharm. Bull., 1995, 43(11), 1912-1930.
Hulley, S. et. al., “Randomized Trial of Estrogen Plus Progestin for Secondary Prevention of Coronary Heart Disease in Postmenopausal Women,”J. Am. Med. Assoc., 1998, 280, 605-13.
Ishiyama, H. et al., “Palladium-Catalyzed Carbonylative Cross-Coupling Reaction of Arylboronic Acids with Aryl Electrophiles: Synthesis of Biaryl Ketones,”J. Org. Chem., 1998, 63, 4726-4731.
Izumi, T. et al., “Blockade of the natriuretic peptide receptor guanylyl cyclase-A inhibits NF-κB activation and alleviates myocardial ischemia/reperfusion injury,”J. Clin. Invest., 2001, 108, 203-213.
Kadokami, T. et al., “Anti-Tumor Necrosis Factor-α Antibody Limits Heart Failure in a Transgenic Model,”Circulation, 2001, 104, 1094-1097.
Karas, R. H. et al., “Effects of Estrogen on the Vascular Injury Response in Estrogen Receptor α,β (Double) Knockout Mice,”Circ. Res., 2001, 89, 534-539.
Kurebayashi S. et. al., “Characterization of Mechanisms of Interleukin-6 Gene Repression by Estrogen Receptor,”J. Steroid Biochem. Molec. Biol., 1997, 60, 11-17.
Lin, C. C. et.al., “Pulmonary function changes and increased Th-2 cytokine expression and nuclear factor kB activation in the lung after sensitization and allergen challenge in brown Norway rats,”Immunol. Lett., 2000, 73, 57-64.
Lou, H. et al., “Inhibition of Transplant Coronary Arteriosclerosis in Rabbits by Chronic Estradiol Treatment Is Associated With Abolition of MHC Class II Antigen Expression,”Circulation, 1996, 94, 3355-3361.
Lundeen, S. G. et al., “Rat uterine complement C3 expression as a model for progesterone receptor modulators: characterization of the new progestin trimegestone,”J. Steroid Biochem Biol., 2001, 78, 137-143.
Mankin, H. J. et al., “Biochemical and Metabolic Abnormalities in Articular Cartilage from Osteo-Arthritic Human Hips,”Journal of Bone&Joint Surgery—American vol. 53, 523-537 (1971).
Merchenthaler, I. et al., “The effect of estrogens and antiestrogens in a rat model for hot flush,”Maturitas, 1998, 30, 307-316.
Nahm, S. et al., “N-Methoxy-N-Methylamides as Effective Acylating Agents,”Tetrahedron Lett.1981, 22(39), 3815-3818.
Nathan, L. et. al., “Estradiol Inhibits Leukocyte Adhesion and Transendothelial Migration in Rabbits In Vivo,”Circ. Res., 1999, 85, 377-385.
Pelletier et al., “Osteoarthritis, an Inflammatory Disease,”Arthr.&Rheum., 2001, 44, 1237-1247.
Poole, A. R et al., “Rheumatoid-Like Joint Lesions in Rabbits Injected Intravenously with Bovine Serum,”International Archives of Allergy&Applied Inmunology, 1977, 54, 97-113.
Prokai, L. et al., “Synthesis and Biological Evaluation of 17β-Alkoxyestra-1,3,5(10)-trienes as Potential Neuroprotectants Against Oxidative Stress,”J. Med. Chem., 2001, 44, 110-114.
Reis et. al., “Estrogen Is Associated With Improved Survival in Aging Women With Congestive Heart Failure: Analysis of the Vesnarinone Studies,”J. Am. Coll. Cardio., 2000, 36, 529-33.
Robertson, D. W. et al., “Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors,”J. Med. Chem., 1990, 23, 3176-3181.
Roth, A. et. al., “Phytoestrogen Kaempferol (3,4′,5,7-Tetrahydroxylflavone) Protects PC12 and T47D Cells From β-Amyloid-Induced Toxicity,”J. Neurosci. Res., 1999, 57, 399-404.
Schonknecht, P. et. al., “Reduced cerebrospinal fluid estradiol levels are associated with increased β-amyloid levels in female patients with Alzheimer's disease,”Neurosci. Lett., 2001, 307, 122-124.
Shughrue, P. J. et al., “Regulation of Progesterone Receptor Messenger Ribonucle

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