Organic compounds -- part of the class 532-570 series – Organic compounds – 9,10-seco-cyclopentanohydrophenanthrene ring system or...
Patent
1999-02-22
2000-02-22
Dees, Jose' G.
Organic compounds -- part of the class 532-570 series
Organic compounds
9,10-seco-cyclopentanohydrophenanthrene ring system or...
552653, 514178, 514167, C07C40100, A61K 3159
Patent
active
060282088
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to vitamin D.sub.3 derivatives useful as pharmaceutical products or pharmaceutically permissible solvates thereof, treating agents using same, pharmaceutical compositions containing same, and a method for manufacturing same. More particularly, the invention relates to 1 .alpha.-hydroxyvitamin D.sub.3 derivatives having neutrophilic infiltration-suppressing activity, the growth suppression and differentiation induction of malignant tumor cells, etc., or pharmaceutically permissible solvates thereof, treating agents for inflammatory respiratory diseases, malignant tumors, etc., containing same as active ingredients, pharmaceutical compositions containing same and a method for manufacturing same.
BACKGROUND ART
An active vitamin D.sub.3 derivative has calcium absorption-stimulating activity in the small intestine, and activity such as the control of bone resorption and osteogenesis in the bones, and it is used as a treating agent for diseases caused by various kinds of calcium metabolism disorders. In recent years, immunoregulatory activity, cell proliferation inhibitory activity and cell differentiation inducting activity have been found besides these activities. For example, applications to a treating agent for rheumatoid arthritis (Japanese Unexamined Patent Publication No. 56-26820), an antiallergic agent (Japanese Un-examined Patent Publication No. 63-107928, English Patent Publica-tion No. 2260904(GB 2260904-A)), a treating agent for psoriasis (Japanese Unexamined Patent Publication No. 3-68009), a treating agent for diseases attributable to thromboxane A.sub.2 production (Japanese Unexamined Patent Publication No. 5-294834), a treating agent for eczema and dermatitis (Japanese Unexamined Patent Publication No. 7-291868), etc., are being studied.
On the other hand, respiratory tract infection is a disease which is established when pathogens invade getting over infection preventing mechanisms of the respiratory tract, and the treatment is mainly based on the improvement of respiratory tract clearance by using a bronchodilator, an expectorant, etc. But, in the case of acute exacerbation with infection, the main treatment is a strong antibacterial treatment against phlogogenic bacteria. However, most underlying diseases constantly becomes worse when acute exacerbation is repeated. Further, present treatments, which depends on antibacterial agents in the extreme, are under reconsideration owing to the emergence of resistant bacteria such as MRSA.
Recently, the usefulness of a low-dose long administration of erythromycin for a chronic lower airway infectious disease has been reported, and it is attracting attention. A chronic lower airway infectious disease is a generic name for bacterial infections observed in chronic bronchitis, diffuse panbronchiolitis, bronchiectasis, etc., (sometimes, it includes bronchial asthma, chronic pulmonary emphysema, pulmonary tuberculosis sequela, etc., accompanied by infection). Although these are different in the name of disease, it is known that all of the diseases take common morbid states such as purulent sputum in large amount, fatigue dyspnea and hypoxemia. Regarding the working mechanism of erythromycin, it is understood that erythromycin's function does not depend simply on its antibacterial activity, namely, erythromycin acts not on bacteria themselves but rather on inflammatory cells which accumulate on the airway accompanied by the bacteria, especially acts on neutrophils. That is, neutrophils infiltrate into tissues by the various kinds of stimulation caused by the infection to release protease as well as active oxygen, and these substances cause epithelium damage, the trouble of ciliary movement and mucosa hypersecretion to exert a bad influence upon respiratory physiological effect, and erythromycin acts on these processes. Based on such consideration, a medicine, which suppresses the pulmonary tissue infiltration of neutrophils or suppresses the activity of neutrophils, can be useful as a treating agent for infl
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patent: 4851401 (1989-07-01), DeLuca et al.
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patent: 5478955 (1995-12-01), DeLuca et al.
patent: 5585368 (1996-12-01), Steinmeyer et al.
Chokki Manabu
Furuya Minoru
Gao Qingzhi
Hazato Atsuo
Ishizuka Seiichi
Dees Jos,e G.
Qazi Sabiha N.
Teijin Limited
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