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TANDOSPIRONE DERIVATIVE meetings

Foreign code F210010295
File No. (H30-S09)
Posted date Jan 28, 2021
Country WIPO
International application number 2020JP019911
International publication number WO 2020235587
Date of international filing May 20, 2020
Date of international publication Nov 26, 2020
Priority data
  • P2019-095359 (May 21, 2019) JP
Title TANDOSPIRONE DERIVATIVE meetings
Abstract A compound represented by formula (1) or a pharmaceutically acceptable salt thereof can be used as an active ingredient of a drug for central nervous system diseases or as a candidate compound for a precursor of said active ingredient. In formula (1), R1, R2, and R3 each independently represent a substance selected from the group consisting of a hydrogen atom, a hydroxy group, and an alkoxy group having 1-6 carbon atoms, and at least one of R1, R2, and R3 is a hydroxy group.
Outline of related art and contending technology BACKGROUND ART
Central nervous system diseases are known as psychiatric and neurological diseases. Schizophrenia, bipolar disorder, depression, autologous spectrumsis, anxiety disorder, adaptive disorder, Alzheimer's disease, dementia, epilepsy, Parkinson's disease are representative central nervous system diseases.
Schizophrenia is psychiatric dysfunction in which the) capability of consolidating psychiatric functions such as thinking, behavior, and feelings decreases over a long period of time, and various symptoms such as hallucinations, delusions, abnormal behavior, decreased motivation, cognitive dysfunction, and the like appear during the course of schizophrenia. The prevalence of schizophrenia is about 1%, which is a disease with a high incidence. It mainly develops in adolescents and progresses chronically.
Symptoms of schizophrenia are large and divided into positive symptoms, negative symptoms and cognitive impairment. Positive symptoms include hallucinations, delusions, disorders of consciousness that are perceived as being dominated by someone, disorders of thinking that conduct an unorganized conversation or behavior, abnormal behavior that severely excites or subtle behavior, and the like. Negative symptoms include symptoms such as flattening of feelings that lead to poor expression of comfort, diminishing of motivation, diminishing of thinking power, diminishing of involvement with a person, and hindering communication with a person that leads to self-closing. Cognitive impairment is an impairment in intellectual ability of memory, thinking, understanding, calculation, learning, language, judgment, and the like.
The negative symptoms of schizophrenia and the etiology of cognitive impairment are associated with a decrease in the volume of the frontal cortex of a patient, and one of the major factors of the volume decrease in frontal cortex is believed to be a decrease in palbumin positive GABA neurons. Parb albumin-positive GABA neurons are cells that express parb albumin in suppressive neurons (that release GABA (γ-aminobutyric acid) present in the cerebral neocortex (. Non-Patent Document 1 suggests that the reduction of parb albumin positive GABA neurons in a schizophrenia animal model is mediated by oxidative stress.
Also, according to the N-methyl-D-aspartate (NMDA) receptor decline hypothesis and oxidative stress / GABA agonistic origin hypothesis, which are the main hypotheses of schizophrenia, the decline of NMDA receptors on GABA-agonistic neurons causes oxidative stress; Non-Patent Documents 2 and 3) result in a decrease in parb albumin-positive GABA neurons resulting in impaired synchronous firing on a number of pyramid neurons innervated by the parb albumin-positive GABA neurons, resulting in cognitive impairment and a number of psychiatric symptoms.
Scope of claims (In Japanese)[請求項1]
 下記式(1)で示される化合物又はその薬剤学的に許容できる塩。
[化1]
(省略)
(式(1)中、R 1、R 2及びR 3は、それぞれ独立に、水素原子、ヒドロキシ基及び炭素数1~6のアルコキシ基からなる群から選択される基であり、R 1、R 2及びR 3のうちの少なくとも1つがヒドロキシ基である。)

[請求項2]
 式(1)中、R 1、R 2及びR 3が、それぞれ独立に、水素原子、ヒドロキシ基及びメトキシ基からなる群から選択される基であり、R 1、R 2及びR 3のうちの少なくとも1つがヒドロキシ基である、請求項1に記載の化合物又はその薬剤学的に許容できる塩。

[請求項3]
 式(1)中、R 1がメトキシ基であり、R 2がヒドロキシ基であり、R 3が水素原子である、請求項1又は2に記載の化合物又はその薬剤学的に許容できる塩。

[請求項4]
 式(1)中、R 1がヒドロキシ基であり、R 2がメトキシ基であり、R 3が水素原子である、請求項1又は2に記載の化合物又はその薬剤学的に許容できる塩。

[請求項5]
 式(1)中、R 1及びR 2がそれぞれヒドロキシ基であり、R 3が水素原子である、請求項1又は2に記載の化合物又はその薬剤学的に許容できる塩。

[請求項6]
 請求項1~5のいずれか一項に記載の化合物又はその薬剤学的に許容できる塩を有効成分として含有する医薬組成物。

[請求項7]
 神経保護薬である、請求項6に記載の医薬組成物。

[請求項8]
 中枢神経系疾患治療薬である、請求項6又は7に記載の医薬組成物。

[請求項9]
 統合失調症治療薬である、請求項6~8のいずれか一項に記載の医薬組成物。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • UNIVERSITY OF TOYAMA
  • KANAZAWA MEDICAL UNIVERSITY
  • Inventor
  • KONDO Takashi
  • ABE Hitoshi
  • KURACHI Masayoshi
  • SUZUKI Michio
  • UEHARA Takashi
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN WS ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL ST SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN TD TG
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