Compounds, isomer thereof, or pharmaceutically acceptable...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S253010, C514S318000, C514S343000, C514S351000, C514S352000, C514S357000, C544S131000, C544S360000, C546S194000, C546S278400, C546S300000, C546S309000, C546S337000

Reexamination Certificate

active

07858621

ABSTRACT:
This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same.The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.

REFERENCES:
patent: 02/16318 (2002-02-01), None
patent: 03/049702 (2003-06-01), None
patent: 2005/003084 (2005-01-01), None
patent: 2006/051378 (2006-05-01), None
patent: 2006-095263 (2006-09-01), None
patent: 2006-097817 (2006-09-01), None
patent: 2006-098554 (2006-09-01), None
patent: 2006-101318 (2006-09-01), None
patent: 2006-101321 (2006-09-01), None
Mezey et al., “Distribution of mRNA for vanilloid receptor subtype 1 (VR1), and VR1-like immunoreactivity, in the central nervous system of the rat and human”, PNAS, Mar. 28, 2000, vol. 97(7), 3655-3660.
Cortright et al., “The Tissue Distribution and Functional Characterization of Human VR1”, Biochemical and Biophysical Research Communications, vol. 281(5), 2001, 1183-1189.
Nagy et al., “The role of the vanilloid (capsaicin) receptor (TRPV1) in physiology and pathology”, European Journal of Pharmacology 500 (2004), 351-369.
Petersen et al., “Capsaicin evoked pain and allodynia in post-herpetic neuralgia”, Pain 88 (2000) 125-133.
Walker et al., “The VR1 Antagonist Capsazepine Reverses Mechanical Hyperalgesia in Models of Inflammatory and Neuropathic Pain”, The Journal of Pharmacology and Experimental Therapeutics, vol. 304(1), 2003, 56-62.
Akerman et al., “Anandamide acts as a vasodilator of dural blood vessels in vivo by activating TRPV1 receptors”, British Journal of Pharmacology (2004) 142(8), 1354-1360.
Kim et al., “Transient Receptor Potential Vanilloid Subtype 1 Mediates Cell Death of Mesencephalic Dopaminergic Neurons In Vivo and In Vitro”, The Journal of Neuroscience, Jan. 19, 2005, vol. 25(3), 662-671.
Kamei et al., “Role of vanilloid VR1 receptor in thermal allodynia and hyperalgesia in diabetic mice”, European Journal of Pharmacology 422 (2001), 83-86.
Chan et al., “Sensory fibres expressing capsaicin receptor TRPV1 in patients with rectal hypersensitivity and faecal urgency”, The Lancet, vol. 361, Feb. 1, 2003, 385-391.
Yiangou et al., “Vanilloid receptor 1 immunoreactivity in inflamed human bowel”, The Lancet, vol. 357, Apr. 28, 2001, 1338-1339.
Holzer, Peter, “TRPV1 and the gut: from a tasty receptor for a painful vanilloid to a key player in hyperalgesia”, European Journal of Pharmacology 500 (2004) 231-241.
Hwang et al., “Hot channels in airways: pharmacology of the vanilloid receptor”, Current Opinion in Pharmacology 2002, vol. 2, 235-242.
Geppetti et al., “The transient receptor potential vanilloid 1: Role in airway inflammation and disease”, European Journal of Pharmacology 533 (2006) 207-214.
Birder et al., “Altered urinary bladder function in mice lacking the vanilloid receptor TRPV1”, Nature Neuroscience, vol. 5(9), Sep. 2002, 856-860.
Birder et al., “Vanilloid receptor expression suggests a sensory role for urinary bladder epithelial cells”, PNAS, Nov. 6, 2001, vol. 98(23), 13396-13401.
Southall et al., “Activation of Epidermal Vanilloid Receptor-1 Induces Release of Proinflammatory Mediators in Human Keratinocytes”, The Journal of Pharmacology and Experimental Therapeutics, vol. 304(1), 217-222, 2003.
Tominaga et al., “The Cloned Capsaicin Receptor Integrates Multiple Pain-Producing Stimuli”, Neuron, vol. 21, Sep. 1998, 531-543.
Balaban et al., “Type 1 vanilloid receptor expression by mammalian inner ear ganglion cells”, Hearing Research 175 (2003), 165-170.
Scotland et al., “Vanilloid Receptor TRPV1, Sensory C-Fibers, and Vascular Autoregulation”, Circulation Research, Nov. 12, 2004, vol. 95, 1027-1034.
Bodo et al., “A Hot New Twist to Hair Biology, Involvement of Vanilloid Receptor-1 (VR1/TRPV1) Signaling in Human Hair Growth Control”, American Journal of Pathology, vol. 166(4), Apr. 2005, 985-998.
Biro et al., “Hair Cycle Control by Vanilloid Receptor-1 (TRPV1): Evidence from TRPV1 Knockout Mice”, Journal of Investigative Dermatology (2006), vol. 126, 1909-1912.
Dinis et al., “Anandamide-Evoked Activation of Vanilloid Receptor 1 Contributes to the Development of Bladder Hyperreflexia and Nociceptive Transmission to Spinal Dorsal Horn Neurons in Cystitis”, The Journal of Neuroscience, Dec. 15, 2004, vol. 24(50), 11253-11263.
Sculptoreanu et al., “Protein kinase C contributes to abnormal capsaicin responses in DRG neurons from cats with feline interstitial cystitis”, Neuroscience Letters 381 (2005), 42-46.

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