Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters
Patent
1995-02-07
1999-08-24
Geist, Gary
Organic compounds -- part of the class 532-570 series
Organic compounds
Carboxylic acid esters
568326, 514680, C07C 6900, C07C 49215, A61K 3112
Patent
active
059426411
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a fluorenone derivative, a process for preparing the same and a central or peripheral nerve degeneration repair or protective agent.
BACKGROUND ART
At present, it is suggested that senile demantia represented by Alzheimer's disease causes serious change in central cholinergic nervous system, which H. "Biochemistry of Dementia", page 135 (1980), John Wiley & Sons.,!.
Accordingly, a compound having repair capacity (e.g. survival effect and neulite stretching effect) and protective action of nerve cells can be effectively used as a remedy or a preventive for senile demantia represented by Alzheimer's disease, Down's syndrome, Huntington's chorea, intellectual/learning disturbance (e.g. amnesia, memory disorder, etc.), and aftereffect and neuropathy caused by deterioration of acetylcholinergic nervous system function due to head injury, cerebral operation, drug intoxication, circulatory disorder, cerebral metabolic (1985)!.
Heretofore, NGF (nerve growth factor), GM1 (ganglioside) and the like have merely been known as the compound having repair capacity for nerve cells degeneration as described above. NGF is described, for example, in 214-216 (1986)! and the like. In addition, GM1 is described, for example, 375, 417-422 (1986)! and the like.
DISCLOSURE OF INVENTION
A fluorenone derivative of the present invention is represented by the following formulas (A) to (D). ##STR3## group;
R.sup.b and R.sup.c are the same or different and are a hydrogen atom, a lower alkenyl group, a lower alkyl group, a halogen atom, a lower alkoxy group, a lower alkylthio group, a lower alkenyloxy group, a group of the formula: ##STR4## (wherein R.sup.8 and R.sup.9 are the same or different and indicate a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl-substituted lower alkyl group, a pyrimidinyl group or pyrazinyl group, and R.sup.8 and R.sup.9 may bond together with the nitrogen atom to which they are attached to form a 5- or 6-membered saturated heterocycle through a nitrogen or oxygen atom or not (i.e., having a nitrogen or oxygen atom or not as other hetero atom), the heterocycle optionally containing a substituent selected from the group consisting of a lower alkyl group and a lower alkoxycarbonyl group; and A is a lower alkylene group), an imidazolyl-substituted lower alkyl group, a lower alkoxy-substituted lower alkyl group, a hydroxyl group-substituted lower alkoxy-lower alkoxy-substituted lower alkyl group or a lower trialkyl-substituted ammonium-substituted lower alkyl group; hydrogen atom, a lower alkenyl group, a lower alkyl group, a halogen atom, a lower alkoxy group, a lower alkenyloxy group, a group of the formula: ##STR5## (wherein R.sup.8 and R.sup.9 are as defined above), an imidazolyl-substituted lower alkyl group, a lower alkoxy-substituted lower alkyl group, a pyridylthio-substituted lower alkyl group, a phenylthio-substituted lower alkyl group optionally containing a lower alkoxy group as a substituent on a phenyl ring, a benzimidazolylthio-substituted lower alkyl group, an imidazolylthio-substituted lower alkyl group, a lower alkanoyl group, a cycloalkylthio-substituted lower alkyl group, a cyano-substituted lower alkyl group or a lower trialkyl-substituted ammonium-substituted lower alkyl group; R.sup.d, R.sup.e and R.sup.f are hydrogen atoms, R.sup.d, R.sup.e and R.sup.g are hydrogen atoms, R.sup.f are hydrogen atoms, and R.sup.a is a hydrogen atom or an acetyl group, R.sup.d, R.sup.d, R.sup.e and R.sup.g are hydrogen atoms, R.sup.f and R.sup.g are hydrogen atoms, and R.sup.a is a hydrogen atom or an acetyl group, or halogen atoms when R.sup.a is a hydrogen atom, R.sup.c, R.sup.d, R.sup.e, R.sup.f and R.sup.g are hydrogen atoms, R.sup.b, R.sup.c, R.sup.d, R.sup.e and R.sup.g are hydrogen atoms, and atom when R.sup.b and R.sup.c are hydrogen atoms and any one of R.sup.d, R.sup.e, R.sup.f and R.sup.g is a lower alkenyl group!; ##STR6## integer of 1 to 3; provided that, an acetyl group and R.sup.2a is a lower alkoxy group, atom and q is 1, and h
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Fujisawa Nobutaka
Hongoh Osamu
Nishi Takao
Sakurai Yohji
Tanaka Tatsuyoshi
Geist Gary
Keys Rosalynd
Otsuka Pharmaceutical Co. Ltd.
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