Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2001-04-20
2003-01-21
Huang, Evelyn Mei (Department: 1625)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C514S314000
Reexamination Certificate
active
06509468
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline (hereinafter referred to as FR173657) and a pharmaceutical composition comprising it.
BACKGROUND ART
FR173657 is a compound of the following formula [I], and is disclosed in Japanese Patent Laid-Open No. 2780/1995 or in Journal of Medicinal Chemistry, 1998, Vol. 41, No. 21, 4062-4079.
This possesses activity as a bradykinin antagonist, and is useful as an agent for the prevention and/or the treatment of, for example, allergy, inflammation, autoimmune disease, shock, pain, or the like.
FR173657 possesses an excellent activity as a bradykinin antagonist. However, FR173657 described in the laid-open specification mentioned above is in amorphous form as obtained through solidification in a solvent. This amorphous form has a melting point broadly ranging between 133 and 139° C., and its solid stability is poor. Therefore, this is problematic in that products of quality sufficiently stable to be acceptable as medicines are difficult to produce and supply.
FR173657 involves crystallographic polymorphism, of which crystal hydrates having high purity and good solid stability and easy to handle for formulation into medicines, more preferably three types of crystals referred to as crystal type A, crystal type B and crystal type C, have been found (Japanese Patent Laid-Open No. 316677/1998). However, though having good solid stability and releasability, the crystal type A is problematic in that it is often contaminated with the crystal type C, making impossible production with stable quality. The crystal type B is the most stable and there is no problem in producing it, but is problematic in that its releasability is much inferior to that of the crystal type A. The crystal type C is also problematicin that its solid stability is inferior to that of the crystal type B and its releasability is inferior to that of the crystal type A. Therefore, further studies for finding out another form of FR173657 more suitable to medicines are needed.
Given that situation, we, the present inventors have assiduously studied FR173657, and, as a result, have found a vitreous form of FR173657 having high purity, good solid stability, good solubility and good releasability and capable of production with stable quality, and have completed the present invention.
REFERENCES:
patent: 5958455 (1999-09-01), Roser
patent: 0 622 361 (1994-11-01), None
patent: 10-316677 (1998-12-01), None
Aoki Osamu
Ishikuro Hiroshi
Ohike Atsuo
Ohnishi Norio
Okimoto Kazuto
Fujisawa Pharmaceutical Co. Ltd.
Huang Evelyn Mei
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
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