Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2008-05-20
2008-05-20
Saeed, Kamal A. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S207000
Reexamination Certificate
active
10492065
ABSTRACT:
There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them.In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III):whereina, b and c are each an integer of 0-6;Z is CH2or NH;W is O or S;T is O or N—R15wherein R15is H, a C1-C6 alkyl group,a benzyl group or a phenethyl group; andR1is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like.The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
REFERENCES:
patent: 4560684 (1985-12-01), Sugasawa et al.
patent: 4791112 (1988-12-01), Bagley et al.
patent: 4912109 (1990-03-01), Bagley et al.
patent: 0 160 422 (1985-11-01), None
patent: 0 277 794 (1988-08-01), None
patent: 63-264460 (1988-11-01), None
patent: WO 94/27967 (1994-12-01), None
Martin et al. “The Effects of Morphine- and Nalorphine- Like Drugs in the Nondependent and Morphine-Dependent Chronic Spinal Dog.” The Journal of Pharmacology and Experimental Therapeutics. vol. 197, No. 3, pp. 517-532, 1976.
Konturek et al. “Influence of methionine-enkephalin and morphine on myoelectric activity of small bowel.” Am. J. Physiol. 238: G-384-389, 1980.
Orwoll et al. “β-Endorphin and Adrenocorticotropin in Extrapituitary Sites: Gastrointestinal Tract.” Endocrinology, vol. 107, No. 2, 438-442, 1980.
“Enkephalins and Endorphins Stress and the Immune System.” Ed. by Plotnikoff et al., Plenum Press, New York, pp. 35-45, 1986.
Simonin et al. “The Human δ-Opioid Receptor: Genomic Organization, cDNA Cloning, Functional Expression, and distribution in Human Brain.” Molecular Pharmacology. 46:1015-1021, 1994.
Wang et al. “Human μ opiate receptor cDNA and genomic clones, pharmacologic characterization and chromosomal assignment.” FEBS Letters 338, pp. 217-222, 1994.
Simonin et al. “k-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.” Proc. Natl. Acad. Sci. USA, 92: 7006-7010, 1995.
Yamaguchi et al. “Itch-Associated Response and Antinociception Induced by Intracisternal Endomorphins in Mice.” Jpn. J. Pharmacol. 78: 337-343, 1998.
Fukutomi Ryuuta
Hagihara Kouichirou
Inoue Hitoshi
Kawamura Koji
Kishimoto Takuya
Havlin Robert
Kyorin Pharmaceutical Co. Ltd.
Nisshin Pharma Inc.
Ohlandt Greeley Ruggiero & Perle L.L.P.
Saeed Kamal A.
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