Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-09-30
2000-08-29
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514376, 514369, 514425, A61K 3144, A61K 3142, A61K 31425, A61K 3140
Patent
active
061109487
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a medicinal composition for the prophylaxis and treatment of cachexia which develops in chronic diseases such as malignant tumor, tuberculosis, diabetes, blood dyscrasia, endocrine disease, infectious disease, or acquired immunodeficiency syndrome.
BACKGROUND ART
Cachexia is a systemic syndrome with progressive loss of body weight, anemia, edema, and anorexia as cardinal symptoms which develops in chronic diseases such as malignant tumor, tuberculosis, diabetes, blood dyscrasia, endocrine disease, infectious disease, and acquired immunodeficiency syndrome [e.g. Kern et al., Cancer Cachexia, J. Parenteral and Enteral Nutrition, 12, 286-298 (1988) and American Journal of Medicine, 85, 289-291 (1988)].
In cachexia, therapeutic nutrition and endocrine therapy are generally administered but a satisfactory anticachectic modality remains to be established. Particularly where cachexia is caused by a malignant tumor, the available anticancer chemotherapy cannot be administered when cachexia is progressing, with the result that the treatment encounters a serious setback. Moreover, any therapeutic nutrition for relief of cachectic symptoms may rather exacerbate the malignant tumor and detract from the life expectancy of the patient. While cachexia is frequently caused by the malignant tumors, administration of an antitumor agent in such settings may result in control of the tumors but generally side effects of the drug develop in superimposition, the net result being no improvement in cachexia [Nelson et al., Journal of Clinical Oncology, 12, 213-225 (1994)].
In the above state of the art, there is a standing need for an anticachectic composition that should ameliorate or inhibit progression of cachectic symptoms such as loss of body weight.
DISCLOSURE OF INVENTION
The present invention relates to a medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: ##STR2## wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula --CO--, --CH(OH)--, or --NR.sup.3 -- (R.sup.3 represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bord or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R.sup.1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R.sup.1 ; L and M respectively represent hydrogen or may be combined with each other to form a bond; provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R.sup.1, L and M respectively represent hydrogen, and ring E does not have further substituents, R does not represent dihydrobenzopyranyl; or a salt thereof (hereinafter referred to simply as Compound (I)).
Referring to the hydrocarbon group that may be substituted for R, the hydrocarbon group includes aliphatic, alicyclic, alicyclic-aliphatic, aromatic-aliphatic, and aromatic hydrocarbon groups. The preferred number of carbon atoms constituting such hydrocarbon groups is 1 to 14.
The aliphatic hydrocarbon group is preferably a C.sub.1-8 aliphatic hydrocarbon group. The aliphatic hydrocarbon group includes saturated C.sub.1-8 aliphatic hydrocarbon groups (e.g. alkyl groups) such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, t-butyl, pentyl, isopentyl, neopentyl, t-pentyl, hexyl, isohexyl, heptyl, and octyl; and unsaturated C.sub.2-8 aliphatic hydrocarbon groups (e.g. alkenyl, alkadienyl, alkynyl, and alkadiynyl groups) such as ethenyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-1-propenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 3-methyl-2-butenyl, 1-hexenyl, 3-hexenyl, 2,4-hexadienyl, 5-hexenyl, 1-heptenyl, 1-octenyl, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-hexynyl, 3-hexynyl, 2,4-hexadiynyl
REFERENCES:
patent: 4775687 (1988-10-01), Meguro et al.
patent: 5478852 (1995-12-01), Olefsky et al.
patent: 5665748 (1997-09-01), Sohda et al.
Matsutani Etsuya
Momose Yu
Sohda Takashi
Goldberg Jerome D.
Takeda Chemical Industries Ltd.
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