摘要:
A compound useful for central antioxidant having inhibitory activity of degeneration and necrocytosis of cerebral cells of the formula (I): ##STR1## wherein A and B are independently (1) a group of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are independently hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted heterocyclic group, or R.sub.1 together with R.sub.2 and the nitrogen atom to which they are bound may form a cyclic amino group, provided that both R.sub.1 and R.sub.2 are not hydrogen atom at the same time, or (2) a group of the formula: ##STR3## wherein D is O or S, R.sub.3 is hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group, m is 1, 2, or 3 and n is 0, 1, 2, 3 or 4;p is 1 or 2, provided that both A may be the same or different when p is 2; andR.sub.4, R.sub.5 and R.sub.6 are independently hydrogen atom, a lower alkyl or a lower alkoxy, or R.sub.5 and R.sub.6 may bond together to form --CH.dbd.CH--CH.dbd.CH--, or a salt thereof.
摘要:
The present invention provides an optically active isoindoline derivative represented by the formula: ##STR1## which is useful as an improving, therapeutic and preventive agent for anxiety-associated nervous symptoms, and an intermediate for synthesis thereof.
摘要:
The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.
摘要:
A compound of the formula: ##STR1## wherein m is an integer of 11 to 22; R.sub.1 is alkyl having 1 to 4 carbon atoms; R.sub.2 is hydrogen, alkyl having 1 to 4 carbon atoms or carboxylic acyl having 1 to 8 carbon atoms. Such compounds have pharmaceutical activities such as hypotensive, tissue metabolism stimulating, immuno-regulatory and lysosomal membrane stabilizing activity, and inhibit SRS-A production, and are useful as a heart failure remedy, cerebral circulation disturbance remedy, immuno-regulator, and antiallergic drug.
摘要:
A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
摘要:
An aminoketone compound of the formula ##STR1## wherein ring A' means a five through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O, S, N, as the ring-constituents; R.sup.1' means a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.2' means a hydrogen atom or a lower alkyl group; R.sup.3' means an aromatic group which may be substituted; R.sup.4' means a hydrogen atom, a lower alkyl group or aromatic group which may be substituted; n' means an integer of 2 to 7, or a salt thereof, is useful as an cholinesterase inhibitors and a cerebral function ameliorating agent.
摘要:
1. A cyclic amine compound of the formula ##STR1## wherein B means a saturated or unsaturated 5- to 7-membered aza-heterocyclic group which may be substituted; A means a bond or an alkylene or alkenylene group which may be substituted by hydrocarbon residues, oxo, hydroxyimino, and/or hydroxy, --means either a single bond or a double bond (provided that when A means a bond, --means a single bond); R.sub.2 and R.sub.3 independently mean a hydrogen atom or a hydrocarbon residue which may be substituted (provided that both of R.sub.2 and R.sub.3 are not hydrogen atoms) or jointly form a cyclic amino group together with the adjacent nitrogen atom, n is 0, 1 or 2 and p is 1 or 2 or a physiologically acceptable salt thereof.The compounds are useful for therapy of cerebral edema, acute symptoms in cerebral apoplexy and protection of brain and nerve cell, or useful as anticholinesterase or as brain function-improving agent.
摘要:
Azaspiro compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, a hydrocarbon residue which may have a substituent, or an acyl group which may have a substituent; R.sub.3 represents hydrogen or a hydrocarbon residue which may have a substituent; each of X.sub.1 and X.sub.2 is oxygen or sulfur; Y represents oxygen, sulfur or a group of the formula: --N(R.sub.4)--, wherein R.sub.4 represents hydrogen or a lower alkyl group; m represents 0 or 1; n represents 0 or 1, and its salt are novel compounds, possess excellent brain function-improving action, and are of use as drugs for the prevention and therapy of senile dementia of Alzheimer type, vascular-type dementia and dementia derived from Alzheimer's disease, Pick's disease, Huntington's disease, Creutzfeldt-Jakob's disease, Parkinson's disease and spinocerebellar degeneration.
摘要:
Novel steroid compounds are provided represented by the formula: ##SPC1##Wherein each of R.sup.1 and R.sup.2 represents hydrogen or methyl group or R.sup.1 and R.sup.2 may be combined with each other to represent methylene group, n is 2 or 3 and the dotted line means a double bond at 6-exo-position when n is 2 or between 6- and 7-position when n is 3.These novel compounds show a strong anti-androgenic activity, especially by oral administration, and can be used as a remedy for the prostatomegaly.
摘要:
A compound of the formula: wherein ring A is an optionally substituted benzene ring; ring B′ is an optionally substituted non-aromatic heterocyclic ring having, the same or different, two or more hetero atoms; R1 is a hydrogen atom or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; Y is an optionally substituted amino group or an optionally substituted N-containing saturated heterocyclic group; n denotes an integer of 1 to 10, provided that when the ring B′ is a 5- to 7-membered ring, the ring B′ contains at least one nitrogen atom as hetero atom and n denotes an integer of 2 to 10, or a salt thereof. The compounds and salts thereof have an excellent cholinesterase inhibitory activity and antidepressant activity, and are useful as therapeutic and/or prophylactic medicaments of senile dementia.