Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-01-28
1999-01-05
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 81, 546 86, 546 87, 546 88, C07D47106, C07D47104, A61K 31435, A61K 3144
Patent
active
058563342
DESCRIPTION:
BRIEF SUMMARY
This application has been filed under 35 USC 371 as a national stage application of PCT/JP94/01900 filed Nov. 10, 1994.
TECHNICAL FIELD
This invention relates to novel imidazoquinoline derivatives, processes for producing them, and agents, that contain at least one of said imidazoquinoline derivatives as an active ingredient, for preventing and/or treating diseases manifesting the increase of eosinophils.
BACKGROUND ART
Phenomena characterized by the increase of eosinophils in blood or tissues, namely, their differentiation, induction and infiltration, are recognized in many diseases. For clinical purposes, it is important to distinguish between two groups of diseases, those in which the increase of eosinophils is often observed but is not assumed to participate directly in their pathophysiology and those in which eosinophils are believed to participate in their pathophysiology as the primary immunocytes. Diseases of the first group include Addison's disease, ulcerative colitis and the like. Diseases of the second group include verminations, hypereosinophilic syndrome (HES), eosinophilic pneumonia, eosinophilic enterogastritis and the like, as well as bronchial asthma. Eosinophils are closely involved in the pathophysiology of bronchial asthma and the pathophysiological concept, "eosinophilic bronchitis" is becoming established in these days. In particular, the actions of eosinophils participating in the diseases under consideration share several features, that may be summarized as the following three points: 1) accelerated eosinophil production and differentiation by interleukin-5 (IL-5) and other eosinophil growth lymphokines; 2) migration and accumulation of eosinophils in involved organs due to the eosinophil chemotactic activity; and 3) the activation of eosinophils in foci and the extension of their life survival. In the diseases under consideration, these three factors and events are believed to cause eosinophils to exhibit their cytotoxic and inflammation inducing actions, thereby participating in the pathophysiology of the diseases although their lesions, the severity of their clinical symptoms and other Kosankyu no Rinshoshindanjo no Igi (Significance of Eosinophils in Clinical Diagnosis), in "Kosankyo (Eosinophils)", Sohei Makino and Takashi Ishikawa (eds.), pp. 165 -173, Kokusai Igaku Shuppan, 1991!.
Therefore, compounds that can inhibit the increase or activation of eosinophils in blood or tissues have the potential of application to diseases in which eosinophils are believed to participate as primary immunocytes in their pathophysiology, namely, virminations, hypereosinophilic syndrome (HES), eosinophilic pneumonia, eosinophilic enterogastritis, bronchial asthma, etc.
The sole therapeutic approach currently taken against diseases that manifest the increase of eosinophils is symptomatic treatments involving the administration of steroids and no treatment methods are available that target against eosinophils. Steroids cause frequent occurrence of characteristic side effects such as the lowering of resistance to bacterial infections, hyperglycemia, glycosuria, gastric ulcer, hypercalcemia, osteoporosis and obesity. In addition, the method of using steroids is strictly regulated as exemplified by prohibition of sudden discontinuation of administration and, hence, the use of steroids is extremely difficult from a practical viewpoint. Conventional drugs for curing asthma have primarily been based on their ability to inhibit histamine release, however, it has become increasingly clear that eosinophils are also involved closely in the pathophysiology of asthma and targeting against eosinophils is believed to have the potential of application to asthma which cannot be completely cured by existing methods. Under these circumstances, compounds that are safe and which yet have great potency in controlling eosinophils will provide a radical therapy for various diseases in which the increase of eosinophils is involved and, hence, the development of such compounds useful for pharmaceutical composition
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Peet et al., "Synthesis and Antiallergic Activity of Some Quinolinones and Immidazoquinolinones", J. Med. Chem., vol. 28, pp. 298-302, 1985.
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Kato Kazuo
Mizuguchi Kiyoshi
Mochizuki Hidenori
Yamamoto Ichiro
Dees Jos,e G.
Mochida Pharmaceutical Co. Ltd.
Qazi Sabiha N.
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