Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2008-01-29
2008-01-29
Shiao, Rei-tsang (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S533000
Reexamination Certificate
active
10527062
ABSTRACT:
A proline ester represented by the following formula (I):wherein R1represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof.The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.
REFERENCES:
patent: 4374829 (1983-02-01), Harris et al.
patent: 2 207 129 (1989-01-01), None
patent: 196834 (1989-01-01), None
Green, et al., Protective Groups in Organic Chemistry, Chapter 5: Protection for the Carboxy Group, 3rd., p. 382, 388 and 390 (1999).
IP, Dominic P. et al. “Enalapril Maleate”, Analytical Profiles of Drug Substances, vol. 16, pp. 207-243 1987.
Shiromani, P.K. et al. “Effect of Moisture on the Physical and Chemical Stability of Granulations and Tablets of the Anglotensin Converting Enzyme Inhibitor, Enalapril Maleate”, Drug Development and Industrial Pharmacy, vol. 12, No. 14, pp. 2467-2480 1986.
Tocco, D.J. et al. “The Physiological Disposition and Metabolism of Enalapril Maleate in Laboratory Animals”, Drug Metabolism and Disposition, vol. 10, No. 1, pp. 15-19 1982.
Kunihiro Mimami et al., “Enalaprilat Yudotai no Keihi Kyushu-sei ni Kansuru Kento”, Dai 123 Kai The Pharmaceutical Society of Japan Nenkai Koen Yoshishu, No. 4, p. 106, Mar. 2003.
Li C. et al., The Study of Transdermal Administration of Ace Inhibitors and Improved Absorption of Their Prodrugs. Noven Pharmaceuticals, Inc., AAPS Annual Meeting and Exposiotion, 2000 & internet<URL:http://www.noven.com/NovenDoc3.pdf.>.
Fischer J. et al., Studies Relating to the Configuration and Conformation of 3, 5-Disubstituded Dihydro-2 (3H)-furanones. Liebigs Annalen der Chemie 1989, No. 11, pp. 1093 to 1097.
Furuishi Takayuki
Kimura Kunihiko
Komine Miho
Minami Kunihiro
Minowa Takayuki
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
Shiao Rei-tsang
Toaeiyo Ltd.
LandOfFree
Proline ester and preparation containing the same for... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Proline ester and preparation containing the same for..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Proline ester and preparation containing the same for... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3924740