Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Reexamination Certificate
2002-04-02
2003-09-23
Raymond, Richard L. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
C514S562000, C514S604000, C514S618000, C514S619000, C560S138000, C560S142000
Reexamination Certificate
active
06624193
ABSTRACT:
This application is a 371 of PCT/JP00/06014 filed Sep. 5, 2000.
TECHNICAL FIELD
The present invention relates to a prophylactic and therapeutic medicament for ophthalmic diseases having a leukocyte (neutrophil)-derived elastase inhibitory activity.
BACKGROUND OF THE INVENTION
JP-B 5-81586 and JP-A 5-194366 (corresponding to EP-A 539223) disclose a compound represented by the formula (I):
(hereinafter referred to as a compound of Formula (I)) and a salt or hydrate thereof, which has a human neutrophil-derived elastase inhibitory activity and is effective for preventing and treating diseases such as pulmonary emphysema, atherosclerosis and rheumatoid arthritis.
On the other hand, the ophthalmologic field also involves various diseases relating to leukocytes and their elastases. For example, ophthalmic infections, corneal traumas, corneal ulcers and uveitis may be mentioned in an ophthalmic infection, the cellular infiltration of leukocytes results in an intraocular abscess [Invest. Ophthalmol. Vis. Sci., 40, 385-391 (1999)]. An alkaline trauma (erosion) which is one of corneal traumas allows leukocytes to, be infiltrated into corneal stromal cells at an early stage of the alkaline erosion, two to three weeks after which the elevation of leukocyte elastase activity is observed [Ophthalmic. Res., 29, 154-160 (1997)]. Also in a case of corneal ulcers, a corneal wound or detachment results in the infiltration of leukocytes into a corneal stroma, which leads to the release or secretion of a protease such as an elastase or collagen [Klin. Monatsbl. Augenheilkd, 188, 593-595 (1986)]. An uveitis, especially Behcet's disease, was reported to undergo an increase in a plasma leukocyte elastase [Clin. Chim. Acta 236:129-134 (1995), Acta, Ophthalmol. Scand. 75:287-289 (1997), J.Reumatol. 25: 326-328 (1998)]. While leukocytes or their elastases were reported to be involved in the ophthalmic diseases mentioned above, no actual effect of the administration of an elastase inhibitor was reported.
While in JP-A 5-221872 (corresponding to EP-A 519354) and JP-A 6-509232 (corresponding to EP-A 596118), a microbe-derived substance having human leukocyte elastase inhibitory activity is described generally to be useful as a prophylactic and therapeutic medicament against a corneal scar tissue formation or a fibroblast proliferation [eye solidification (burn, mechanical or chemical damage, keratoconjunctivitis) and the like], it was not administered actually to verify its effect, and is different totally from a compound of Formula (I).
OBJECTS OF THE INVENTION
An objective of the present invention is to develop a prophylactic and therapeutic medicament for ophthalmic diseases containing as an active ingredient a compound of Formula (I).
REFERENCES:
patent: 347168 (1989-12-01), None
patent: 0 519 354 (1992-12-01), None
patent: 539223 (1993-04-01), None
patent: 0 596 118 (1994-05-01), None
patent: 90/04409 (1990-05-01), None
J. Cejkova et al., “Histochemical changes in the rabbit cornea and plasmin activity in the tear fluid during contact lens wear. Favourable influence of protease inhiitors (aprotinin, PC5, elastatinal)” Histochemistry, vol. 97, No. 1, 1992, pp. 69-76.
A. Spierer et al., “The effect of 2-mercaptoacetyl-L-phenylalanyl-L-leucine, a specific inhibitor of Pseudomonas aeruginos a elastase, on experimental Pseudomonas keratitis in rabbit eyes,” Curr. Eye Res., vol. 3, No. 4, 1984, pp. 645-650.
Principles of Ambulatory Medicine, Fourth Edition. Barker et al, editors, pp. 943-952 and 1428-1431. Williams & Wilkins (1995).*
Webster's II New Riverside University Dictionary, p. 933, Houghton Mifflin Co. (1984).*
Gregory D. Sloop, et al., “Acute Inflammation of the Eyelid and Cornea inStaphylococcusKeratitis in the Rabbit,” Invest. Ophthalmol. Vis. Sci., Feb. 1999, vol. 40, No. 2, pp. 385-391.
Jitka {haeck over (C)}ejková, “Histochemical Study of Leukocyte Elastase Activity in Alkali-Burned Rabbit Cornea,” Opthalmic Research, 1997; 29, pp. 154-160.
O. Schmut, et al., “PMN-Elastase-Bestimmung in der Tränenflüssigkeit bei Ulcus corneae,” Klin. Mbl. Augenheilk. 188, 1986, pp. 593-595.
Orhan De{haeck over (g)}er al., “Polymorphonuclear leukocyte elastase levels in patients with Behçet's disease,” Clinica Chimica Acta, 236, 1995, pp. 129-134.
Nurettin Akyol, et al., “The importance of plasma polymorphonuclear (PMN) elastase determination in patients with uveitis,” Acta Ophthalmol. Scandinavica, 1997, pp. 287-289.
Kiyohiro Tsutsui, et al., “Increased Plasma Granulocyte Elastase Levels in Behçet's Disease, ” Journal of Rheumatology, 1998; 25:2, pp. 326-328.
J.P. Barletta et al., “Inhibition of Pseudomonal Ulceration in Rabbit Corneas by a Synthetic Matrix Metalloproteinase Inhibitor,” Invest. Ophthalmol. Vis. Sci., 1996, vol. 37, No. 1, pp. 20-28.
Kawabata Kazuhito
Naka Hiroaki
Tokushige Hideki
Ono Pharmaceutical Co. Ltd.
Raymond Richard L.
Tucker Zachary C.
Wenderoth , Lind & Ponack, L.L.P.
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