Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-04-25
2004-08-17
Lambkin, Deborah (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S236000
Reexamination Certificate
active
06777435
ABSTRACT:
This application a 371 of PCT/JP00/07482 filed Oct. 26, 2000.
TECHNICAL FIELD
The present invention relates to crystals of an oxyiminoalkanoic acid derivative having an anti-diabetic action, to a pharmaceutical composition and a retinoid-related receptor function regulating agent, etc. comprising said crystals.
BACKGROUND ART
In many organic compounds, it has been known that the so-called polymorphism of crystals can occur where the crystal form is different even if the composition is same. With crystal polymorphism, there are cases where physical/chemical properties such as melting point, solubility and stability and biological properties such as pharmacokinetics (absorption, distribution, metabolism, excretion) and pharmacodynamics are different but it is impossible to predict them from the structure of the compound.
There has been a demand in the pharmaceutical industry for crystals having excellent properties as a medicine, such as stable crystals having good absorption.
DISCLOSURE OF INVENTION
As a result of intensive investigation, the present inventors have succeeded in preparing stable crystals of (E)-4-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino]-4-phenylbutyric acid (hereafter also abbreviated as compound A), and found for the first time that these crystals had excellent properties as a medicine (excellent properties as a final medicine and raw material medicine). Based on these findings, the present inventors have completed the present invention.
Namely, the present invention relates to:
(1) crystals of (E)-4-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino]-4-phenylbutyric acid (provided that crystals having a melting point of 126° C. to 127° C. are excluded);
(2) the crystals according to the above (1), which have a melting point of about 136° C. to about 139° C.;
(3) crystals of (E)-4-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino]-4-phenylbutyric acid showing diffraction patterns having characteristic peaks at the spacings (d values) of about 17.5 and about 6.0 Å by a powder x-ray crystal diffraction;
(4) a pharmaceutical composition comprising the crystals of the above (1) or (3);
(5) the pharmaceutical composition according to the above (4), which is an agent for preventing or treating diabetes mellitus;
(6) the pharmaceutical composition according to the above (4), which is an agent for preventing or treating hyperlipemia;
(7) the pharmaceutical composition according to the above (4), which is an agent for preventing or treating impaired glucose tolerance;
(8) the pharmaceutical composition according to the above (4), which is an agent for preventing or treating inflammatory diseases;
(9) the pharmaceutical composition according to the above (4), which is an agent for preventing or treating arteriosclerosis;
(10) a retinoid-related receptor function regulating agent comprising the crystals of the above (1) or (3);
(11) the agent according to the above (10), which is a ligand for peroxisome proliferator-activated receptors;
(12) the agent according to the above (10), which is a ligand for retinoid X receptors;
(13) the pharmaceutical composition according to the above (4), which is an insulin sensitivity enhancing agent;
(14) the pharmaceutical composition according to the above (4), which is an insulin resistance improving agent;
(15) a method for preventing or treating diabetes mellitus in a mammal in need thereof, which comprises administering to said mammal an effective amount of crystals as defined in the above (1) or (3); and
(16) use of crystals as defined in the above (1) or (3) for the manufacture of a pharmaceutical preparation for preventing or treating diabetes mellitus.
REFERENCES:
patent: 6518435 (2003-02-01), Yamane et al.
patent: 99/58510 (1999-11-01), None
Munzel, K. “Der Einfluss der Formgebung auf die Wirkung eines Arzneimittels”, Progres in Drug Research—Fortschritte Der Arzneimittelforschung—Progress Des Recherches Pharmaceutiques, CH, Birkhaeuser Verlag, Basel, vol. 10, 1966, pp. 227-230, XP-002078506, English translation enclosed.
Munzel, K. “Galenische Formgebung und Arznelmittelwirkung/Neue Erkenntnisse und Feststellungen”, Progress in Drug Research—Fortschritte Der Arzneimittelforschung—Progress Des Recherches Pharmaceutiques, CH, Birkhaeuser Verlag, Basel, vol. 14, 1970, pp. 309-321, XP-002078507, English translation enclosed.
T. Sohda et al., “Studies on Antidiabetic Agents, 11,' Novel Thiazolidinedione Derivatives as Potent Hypoglycemic and Hypolipidemic Agents”, J. Med. Chem., vol. 35, pp. 2617-2626, 1992.
Imoto Hiroshi
Momose Yu
Lambkin Deborah
Takeda Chemical Industries Ltd.
Wenderoth , Lind & Ponack, L.L.P.
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