Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2000-10-10
2002-12-31
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
06500820
ABSTRACT:
This application is the National Stage of International Application No. PCT/JP99/02144, filed on Apr. 22, 1999.
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition for neurotrophic action having an excellent properties.
BACKGROUND ART
Proteins such as nerve growth factor (NGF), ciliary neurotrophic factor, insulin growth factor-I and brain-derived neurotrophic factor (BDNF) are known as neurotrophic factors (NTF). They are related to homeostasis of neurons in vivo and have (1) action of survival and retention of neurons, (2) action of synaptic proplasia, (3) action of protecting against cell death and (4) long term potentiation in the hippocampus. It is known that NGF, BDNF, etc. increase choline acetyltransferase (ChAT) activity and that compounds increasing ChAT activity have protective action on nerve cells and neurotrophic action [The Journal of Neuroscience, Vol.16, No.21, pages 6665-6675, (1996) and Neuroscience, Vol.55, No.3,pages 629-641, (1993)].
Therefore, through the above actions, medicines having neurotrophic like action are useful for preventing and/or treating (1) neurodegenerative diseases (e.g. senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, Creutzfelt-Jakob disease, amyotrophic lateral sclerosis, diabetic neuropathy, etc.), (2) neuropathy in cerebrovascular diseases (e.g. impairment of cerebral blood flow based on cerebral infarction, cerebral hemorrhage, cerebral sclerosis, etc.), brain trauma, spinal cord injury, cerebritis sequela and cerebral palsy, (3), dysmnesia (e.g. senile dementia, amnesia, etc.), (4) mental diseases (e.g. depression, panic disorder, schizophrenia, etc.), etc.
As cyclic amine derivatives activating ChAT, Japanese Patent Unexamined Publication No. 169569/1990(H2) describes a compound of the formula:
wherein J means
(a) a substituted or unsubstituted; {circle around (1)} phenyl, {circle around (2)} pyridyl, {circle around (3)} pyranyl, {circle around (4)} quinolyl, {circle around (5)} cyclohexyl, {circle around (6)} quinoxalyl or {circle around (7)} furyl,
(b) the following monovalent or divalent group which may be substituted with phenyl; {circle around (1)} indanyl, {circle around (2)} indanonyl, {circle around (3)} indenyl, {circle around (4)} indenonyl, {circle around (5)} indanedionyl, {circle around (6)} tetralonyl, {circle around (7)} benzosuberonyl, {circle around (8)} indanonyl and {circle around (9)} a group of the formula:
(c) monovalent group induced from cyclic amide compounds,
(d) a lower alkyl group, and
(e) a group of the formula R
1
—CH═CH— in which R
1
is a hydrogen atom or a lower alkoxycarbonyl group;
B means a group of the formula —CO—(C(R
2
)H)
n
—, etc, wherein n is 0 or an integer of 1 to 10 and
R
2
means an alkylene group of the formula —(C(R
2
)H)
n
— in which the groups do not have substituents, or means a hydrogen atom or methyl group which have one or more methyl;
T means a nitrogen atom or a carbon atom;
Q means a nitrogen atom, a carbon atom or a group of the formula >N→O;
K means a hydrogen atom, a substituted or unsubstituted
phenyl group, an arylalkyl group which may be substituted with phenyl, a cinnamyl group which may be substituted with phenyl, a lower alkyl group, a pyridylmethyl group, a cycloalkylalkyl group, an adamantanemethyl group, furylmethyl group, a cycloalkyl group, a lower alkoxycarbonyl group or an acyl group;
q means an integer of 1 to 3; and
means a single bond or a double bond;
or a pharmaceutically acceptable salt thereof.
As cyclic amine derivatives, Japanese Patent Unexamined Publication No. 140149/1993(H5) discloses a fused heterocyclic derivative of the formula:
wherein X represents R
1
—N< (R
1
represents a hydrogen atom, a hydrocarbon group which may be substituted or an acyl group which may be substituted), an oxygen atom or a sulfur atom; R
2
represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents a benzene ring which may be substituted; k represents an integer of 0 to 3; m represents an integer of 1 to 8; and n represents an integer of 1 to 6; or a salt thereof, which inhibits cholinesterase activity.
REFERENCES:
patent: 0487071 (1992-05-01), None
patent: 560235 (1993-09-01), None
patent: 2-169569 (1990-06-01), None
http://www.merck.com/pubs/mmanual/section14/chapter166/166a.htm*
Kato et al., Tak-147, an acetylcholinesterase inhibitor, increases choline acetyltransferase activity in cultured rat septal cholinergic neurons, Jan. 22, 1999, Neuroscience Letters, vol. 260, Issue 1, pp. 5-8.*
Yuji Ishihara et al., “Central Cholinergic Agents. 6. Synthesis and Evaluation of 3-[1-(Phenylmethyl)-4-piperidinyl]-1-(2,3,4,5,-tetrahydro-1H-1-benzazepin-8-yl)-1-propanones and Their Analogs as Central Selective Acetylcholinesterase Inhibitors”, Journal of Medicinal Chemistry, vol. 37, No.15, pp. 2292-2299 (1994).
J. Fournier et al., “Protective Effects of SR 57746A in Central and Peripheral Models of Neurodegenerative Disorders in Rodents and Primates”, Neuroscience vol. 55, No. 3, pp. 629-641 (1993).
Doris Nonner et al., “Neurotrophin Effects on Survival and Expression of Cholinergic Properties in Cultured Rat Septal Neurons under Normal and Stress Conditions”, The Journal of Neuroscience, vol. 16(21), pp. 6665-6675 (1996).
Ishihara Yuji
Kato Koki
Miyamoto Masaomi
Chao Mark
Jagoe Donna
Krass Frederick
Ramesh Elaine M.
Takeda Chemical Industries Ltd.
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