JP2003089643A - Apoptosis suppressing agent - Google Patents

Apoptosis suppressing agent

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Publication number
JP2003089643A
JP2003089643A JP2001285662A JP2001285662A JP2003089643A JP 2003089643 A JP2003089643 A JP 2003089643A JP 2001285662 A JP2001285662 A JP 2001285662A JP 2001285662 A JP2001285662 A JP 2001285662A JP 2003089643 A JP2003089643 A JP 2003089643A
Authority
JP
Japan
Prior art keywords
disease
apoptosis
diseases
propylaminopentane
benzofuran
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP2001285662A
Other languages
Japanese (ja)
Other versions
JP4953040B2 (en
Inventor
Fumio Yoneda
文郎 米田
Joseph Knoll
クノール ジョセフ
Seiichiro Shimazu
誠一郎 島津
Mayumi Watabe
真由美 渡部
Yoshiyasu Take
誉泰 岳
Masanao Nakatani
昌尚 中谷
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FUJIMOTO CORP KK
Original Assignee
FUJIMOTO CORP KK
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Priority to JP2001285662A priority Critical patent/JP4953040B2/en
Publication of JP2003089643A publication Critical patent/JP2003089643A/en
Application granted granted Critical
Publication of JP4953040B2 publication Critical patent/JP4953040B2/en
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PROBLEM TO BE SOLVED: To obtain an apoptosis suppressing agent containing (R)-1-(benzofuran-2-yl)-2-propylaminopentane or its pharmacologically permissible salt, hydrate or solvate as an active component. SOLUTION: (R)-1-(Benzofuran-2-yl)-2-propylaminopentane or its pharmacologically permissible salt, hydrate or solvate has excellent apoptosis suppressing action and is useful as an apoptosis suppressing agent for the treatment of neurological diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, retinitis pigmentosa, glaucoma and spinocerebellar degeneration, brain ischemic diseases such as cerebral apoplexy and peripheral nervous disorder induced by diabetes and further AIDS and toxic diseases.

Description

【発明の詳細な説明】Detailed Description of the Invention

【0001】[0001]

【発明の属する技術分野】この発明は、(R)−1−
(ベンゾフラン−2−イル)−2−プロピルアミノペン
タンおよびその薬理学的に許容される塩、またはそれら
の水和物もしくは溶媒和物を有効成分として含むアポト
ーシス抑制剤に関するものであって、特に、アルツハイ
マー病、パーキンソン病、ハンチントン病、筋萎縮性側
索硬化症、網膜色素変性症、緑内障、脊髄小脳変性症等
の神経疾患、脳卒中等の脳虚血性疾患、糖尿病で観察さ
れる末梢性神経障害等の神経変性疾患、エイズ、中毒性
疾患による神経変性疾患などのアポトーシスが亢進した
疾患の治療剤または予防剤に関するものである。
TECHNICAL FIELD The present invention relates to (R) -1-
(Benzofuran-2-yl) -2-propylaminopentane and a pharmacologically acceptable salt thereof, or an apoptosis inhibitor containing a hydrate or solvate thereof as an active ingredient, Neurological diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, retinitis pigmentosa, glaucoma, spinocerebellar degeneration, cerebral ischemic diseases such as stroke, and peripheral neuropathy observed in diabetes The present invention also relates to a therapeutic or prophylactic agent for neurodegenerative diseases such as, and diseases in which apoptosis is enhanced such as AIDS and neurodegenerative diseases due to addictive diseases.

【0002】[0002]

【従来の技術】アポトーシスは、細胞の遺伝子に制御さ
れた細胞自壊プログラムが発動することによって起こる
細胞死であり、例えば、器官の発達、変態、隆形成、表
皮細胞の細胞交代などにおいてみられる。アポトーシス
の亢進による細胞死の形態は、細胞質の濃縮、原形質膜
毛の消失、核の分節化、染色体ヌクレオソーム単位での
切断によって達成される。このような生理機能としての
アポトーシスは、通常の発生・分化、正常組織や細胞の
ターンオーバーなどの一部として機能している反面、そ
の機能亢進によって様々な疾患を発生させる可能性が指
摘されている(プロシーディングス・オブ・ザ・ナショ
ナル・アカデミー・オブ・サイエンシズ・オブ・ザ・ユ
ナイテッド・ステーツ・オブ・アメリカ(Proc. Natl. A
cad. Sci.USA)、1997年、94巻、12736−12737ペー
ジ)。例えば、ガン、自己免疫疾患、ウイルス感染、エ
イズ、中毒性疾患、神経変性疾患(アルツハイマー病、
パーキンソン病、ハンチントン病、筋萎縮性側索硬化
症、網膜色素変性症、緑内障、脊髄小脳変性症等)など
における細胞死はアポトーシスと密接な関係を有すると
いわれている(臨床医、「特集;アポトーシスの臨
床」、1995年、21巻、9号)。
2. Description of the Related Art Apoptosis is a cell death caused by activation of a cell self-destructing program controlled by a gene of a cell, and is observed in, for example, organ development, metamorphosis, ridge formation, and cell replacement of epidermal cells. The morphology of cell death due to increased apoptosis is achieved by cytoplasmic enrichment, loss of plasma membrane hairs, nuclear segmentation, and cleavage at chromosomal nucleosome units. Apoptosis as such a physiological function functions as a part of normal development / differentiation, turnover of normal tissues and cells, etc., but it has been pointed out that hyperactivity may cause various diseases. Proceedings of the National Academy of Sciences of the United States of America (Proc. Natl. A
cad. Sci. USA), 1997, 94, 12736-12737). For example, cancer, autoimmune disease, viral infection, AIDS, addictive disease, neurodegenerative disease (Alzheimer's disease,
Cell death in Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, retinitis pigmentosa, glaucoma, spinocerebellar degeneration, etc. is said to have a close relationship with apoptosis (Clinician, "Special feature; Clinic of Apoptosis ", 1995, Volume 21, No. 9).

【0003】アルツハイマー病、パーキンソン病、脳卒
中等の脳虚血性疾患等の神経変性疾患においては、従来
から、神経伝達物質の遊離促進により症状を改善すると
いうような、対症療法的な治療が行われているが(ニュ
ーロロジー(Neurology)、1998年51巻(サプルメント
1)、S30ページ、ランセット(Lancet)、1977年、1
巻、439−443ページ)、これらは対症療法的な治療であ
るがために、疾患の特徴である進行的な神経細胞死や変
性を抑制するものではなく、疾患の根本的な治療には結
びつくものではなかった。そのため、現在、このような
アポトーシスの亢進を抑制し、疾患自体を治療または予
防する薬剤が切望されている。
In neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and cerebral ischemic diseases such as stroke, conventionally, symptomatic treatment such as improving symptoms by promoting release of neurotransmitters is performed. (Neurology, 1998, Volume 51 (Supplement 1), S30 page, Lancet, 1977, 1
Vol., Pp. 439-443), these are symptomatic treatments, so they do not suppress the progressive neuronal cell death and degeneration that are characteristic of the disease, and lead to the fundamental treatment of the disease. It wasn't something. Therefore, currently, a drug that suppresses such promotion of apoptosis and treats or prevents the disease itself is desired.

【0004】一方、塩酸セレギリンは、モノアミンオキ
シダーゼB型(MAO−B)阻害活性を有するパーキン
ソン病治療薬であり、黒質線条体におけるドパミンニュ
ーロンに作用して、シナプス間隙のドパミン量の調整を
図り、神経刺激をコントロールすることを特徴としてい
る。また、塩酸セレギリンは、MAO−B阻害活性のほ
かアポトーシスの抑制作用を有することが報告され、こ
のアポトーシス抑制作用が、神経細胞死もしくはその変
性進行を抑制する細胞死抑制効果または細胞保護効果を
もたらしているといわれている。
On the other hand, selegiline hydrochloride is a therapeutic agent for Parkinson's disease having monoamine oxidase type B (MAO-B) inhibitory activity and acts on dopamine neurons in the nigrostriatum to regulate the amount of dopamine in the synaptic cleft. It is characterized by aiming and controlling nerve stimulation. In addition, selegiline hydrochloride has been reported to have an inhibitory effect on apoptosis in addition to a MAO-B inhibitory activity, and this inhibitory effect on apoptosis brings about a cell death inhibitory effect or a cell protective effect that suppresses neuronal cell death or its progression of degeneration. It is said that

【0005】他方、(R)−1−(ベンゾフラン−2−
イル)−2−プロピルアミノペンタンは、CAE/SA
E (Catecholaminergic and Serotoninergic Activity
Enhancer)効果を有する化合物であり、この効果によ
り、パーキンソン病治療において対症療法的に有効な作
用を示すことは知られている。尚、CAE/SAE効果
とは、ドパミン、ノルアドレナリン、セロトニン作動性
神経に作用し、神経発火活動に依存してこれらの神経伝
達物質の遊離を促進する機構をいう(国際公開番号WO 9
9/07667号)。
On the other hand, (R) -1- (benzofuran-2-
Yl) -2-propylaminopentane is CAE / SA
E (Catecholaminergic and Serotoninergic Activity
It is known that the compound has an enhancer effect, and that this effect shows a symptomatically effective action in treating Parkinson's disease. The CAE / SAE effect refers to a mechanism that acts on dopamine, noradrenaline, and serotonergic nerves to promote the release of these neurotransmitters depending on nerve firing activity (International Publication No. WO 9
No. 9/07667).

【0006】[0006]

【発明が解決しようとする課題】この発明における解決
すべき課題は、アルツハイマー病、パーキンソン病、ハ
ンチントン病、筋萎縮性側索硬化症、網膜色素変性症、
緑内障、脊髄小脳変性症等の神経疾患、脳卒中等の脳虚
血性疾患、ならびに、糖尿病で観察される末梢性神経障
害等の神経変性疾患、エイズ、中毒性疾患などの治療ま
たは予防に有用なアポトーシス抑制剤を提供することに
ある。
The problems to be solved by the present invention include Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, retinitis pigmentosa,
Apoptosis useful for the treatment or prevention of neurological diseases such as glaucoma and spinocerebellar degeneration, cerebral ischemic diseases such as stroke, and neurodegenerative diseases such as peripheral neuropathy observed in diabetes, AIDS, toxic diseases, etc. To provide an inhibitor.

【0007】[0007]

【課題を解決するための手段】本発明者らは、鋭意研究
を行った結果、本化合物である(R)−1−(ベンゾフ
ラン−2−イル)−2−プロピルアミノペンタンに、細
胞保護または細胞死抑制の優れた抗アポトーシス作用を
有することを見出し、この発明を完成した。
Means for Solving the Problems As a result of intensive studies, the present inventors have found that (R) -1- (benzofuran-2-yl) -2-propylaminopentane, which is the compound of the present invention, can be used for cell protection or The inventors have found that they have an excellent anti-apoptotic effect of suppressing cell death and completed the present invention.

【0008】この発明は、(R)−1−(ベンゾフラン
−2−イル)−2−プロピルアミノペンタン、または、
その薬理学的に許容される塩、水和物、溶媒和物を有効
成分として含むアポトーシス抑制剤に関するものであ
り、アポトーシスの亢進が起因する疾患の治療剤、また
は、予防剤に関するものを含む。ここで、アポトーシス
の亢進が起因する疾患としては、例えば、脳虚血性疾
患、糖尿病で観察される末梢性神経障害、エイズ、中毒
性疾患などや、アルツハイマー病、パーキンソン病、ハ
ンチントン病、筋萎縮性側索硬化症、網膜色素変性症、
脊髄小脳変性症などの神経変性疾患が挙げられる。
The present invention provides (R) -1- (benzofuran-2-yl) -2-propylaminopentane, or
The present invention relates to an apoptosis inhibitor containing a pharmacologically acceptable salt, hydrate or solvate thereof as an active ingredient, and includes a therapeutic agent or a preventive agent for a disease caused by promotion of apoptosis. Here, as a disease caused by the promotion of apoptosis, for example, cerebral ischemic disease, peripheral neuropathy observed in diabetes, AIDS, addictive disease and the like, Alzheimer's disease, Parkinson's disease, Huntington's disease, muscle atrophy Lateral sclerosis, retinitis pigmentosa,
Neurodegenerative diseases such as spinocerebellar degeneration are mentioned.

【0009】上記において、薬理学的に許容される塩と
は、例えば、塩酸、臭化水素酸、ヨウ化水素酸、硫酸、
硝酸、リン酸等の無機酸との塩や、ぎ酸、酢酸、プロピ
オン酸、シュウ酸、マロン酸、こはく酸、フマル酸、マ
レイン酸、乳酸、リンゴ酸、クエン酸、酒石酸、ピクリ
ン酸、メタンスルホン酸、グルタミン酸等の有機酸との
塩が挙げられるが、薬理学的に許容されるものであれば
特には限定されない。
In the above, pharmacologically acceptable salts include, for example, hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid,
Salts with inorganic acids such as nitric acid and phosphoric acid, formic acid, acetic acid, propionic acid, oxalic acid, malonic acid, succinic acid, fumaric acid, maleic acid, lactic acid, malic acid, citric acid, tartaric acid, picric acid, methane Examples thereof include salts with organic acids such as sulfonic acid and glutamic acid, but are not particularly limited as long as they are pharmacologically acceptable.

【0010】この発明の対象化合物である(R)−1−
(ベンゾフラン−2−イル)−2−プロピルアミノペン
タンおよびその薬理学的に許容される塩、またはそれら
の水和物もしくは溶媒和物は、日本国特許出願番号2000
-109622号に記載した方法によって製造することができ
る。
(R) -1-, which is the object compound of the present invention
(Benzofuran-2-yl) -2-propylaminopentane and pharmacologically acceptable salts thereof, or hydrates or solvates thereof are described in Japanese Patent Application No. 2000.
-109622 can be manufactured by the method described in it.

【0011】この発明の対象化合物である(R)−1−
(ベンゾフラン−2−イル)−2−プロピルアミノペン
タンおよびその薬理学的に許容される塩、またはそれら
の水和物もしくは溶媒和物は、細胞死抑制効果もしくは
細胞保護効果を示し、上述の通り、アポトーシスの亢進
に起因する疾患を治療または予防するためのアポトーシ
ス抑制剤として使用することができる。ヒトまたは動物
に投与する医薬組成物としては、通常の製剤化技法を用
い、必要に応じて、担体、賦形剤、その他の薬理学的に
許容される添加剤とともに調製される。このとき、担
体、賦形剤としては、固体、液体のいずれでもよく、投
与に際しては、錠剤、丸剤、カプセル剤、顆粒剤、散
剤、液剤、注射剤、軟膏剤、点眼剤、懸濁剤、乳剤、シ
ロップ剤、ローション剤、坐剤、ハップ剤などの形態と
して、治療または予防に有効な量を投与することができ
る。
(R) -1-, which is the object compound of the present invention
(Benzofuran-2-yl) -2-propylaminopentane and a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof exhibit a cell death inhibitory effect or a cell protective effect, and are as described above. , And can be used as an apoptosis inhibitor for treating or preventing a disease caused by promotion of apoptosis. A pharmaceutical composition to be administered to humans or animals is prepared by using a usual formulation technique and, if necessary, a carrier, an excipient, and other pharmacologically acceptable additives. At this time, the carrier or excipient may be solid or liquid, and upon administration, tablets, pills, capsules, granules, powders, solutions, injections, ointments, eye drops, suspensions , An emulsion, a syrup, a lotion, a suppository, a suppository and the like, which can be administered in an amount effective for treatment or prevention.

【0012】以下、実施例を示してこの発明をより詳し
く説明するが、ここに示す実施例は単に例示するのみで
あり、これらによってこの発明が限定されることはな
い。
Hereinafter, the present invention will be described in more detail with reference to examples, but the examples shown here are merely illustrative and the present invention is not limited thereto.

【0013】[0013]

【実施例】培地中の血清除去によるPC12細胞死に対
する本発明化合物の細胞死抑制効果を検討した。PC1
2細胞をポリエチレンイミンでコーティングした24穴
マルチウェルプレートに播種し[10%牛胎児血清(F
BS),5%馬血清(HS)含有 ダルベッコ改変イー
グル培地(DMEM),1X105cells/1mL/well]2日間
培養した。その後、NGF(nerve growth factor)を
50ng/mL添加した分化誘導用培地(2%FBS,1%
HS含有DMEM)にて5日間培養後、培地交換と同時
に血清(−)・NGF(+)群(NGF群), 血清
(−)・NGF(−)群(コントロール群), 血清
(−)・NGF(−)・薬物(+)群(薬物群)を設け
た。24時間培養後トリパンブルーで染色し、倒立顕微
鏡下で視野あたりの生・死細胞数を計数した。示す値
は、NGF群,薬物群の各細胞生存率の平均値からコン
トロール群の平均値を差し引き、NGF群の細胞死抑制
効果を100として計算した。
[Examples] The cell death inhibitory effect of the compound of the present invention on PC12 cell death due to removal of serum from the medium was examined. PC1
2 cells were seeded in a 24-well multiwell plate coated with polyethyleneimine [10% fetal bovine serum (F
BS), Dulbecco's modified Eagle medium (DMEM) containing 5% horse serum (HS), 1 × 10 5 cells / 1 mL / well] and cultured for 2 days. Then, a differentiation inducing medium (2% FBS, 1%) supplemented with 50 ng / mL of NGF (nerve growth factor)
After culturing in HS-containing DMEM) for 5 days, the medium was replaced, and at the same time, the serum (-) / NGF (+) group (NGF group), the serum (-) / NGF (-) group (control group), the serum (-). An NGF (-) / drug (+) group (drug group) was provided. After culturing for 24 hours, the cells were stained with trypan blue, and the number of live and dead cells per visual field was counted under an inverted microscope. The value shown was calculated by deducting the average value of the control group from the average value of the cell survival rates of the NGF group and the drug group, and setting the cell death inhibitory effect of the NGF group as 100.

【0014】その結果、表1に示されるように、この発
明化合物は、一般的に抗アポトーシス作用があるとされ
る塩酸セレギリンより細胞死抑制効果(もしくは細胞保
護効果)において優れており、その高いアポトーシス抑
制作用が確認された。
As a result, as shown in Table 1, the compound of the present invention is superior to selegiline hydrochloride, which is generally considered to have an anti-apoptotic action, in the cell death inhibitory effect (or cytoprotective effect) and its high level. An apoptosis inhibitory action was confirmed.

【0015】[0015]

【表1】 [Table 1]

【0016】[0016]

【発明の効果】この発明の完成により、アポトーシス亢
進に起因するアルツハイマー病、パーキンソン病、ハン
チントン病、筋萎縮性側索硬化症、網膜色素変性症、緑
内障、脊髄小脳変性症等の神経疾患、脳卒中等の脳虚血
性疾患、糖尿病で観察される末梢性神経障害等の神経変
性疾患、エイズ、中毒性疾患の治療および予防に有用な
アポトーシス抑制剤が提供される。
EFFECTS OF THE INVENTION With the completion of the present invention, neurological diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, retinitis pigmentosa, glaucoma, spinocerebellar degeneration caused by hyperapoptosis, stroke And a neurodegenerative disease such as peripheral neuropathy observed in diabetes, AIDS, and an addictive disease, which are useful in the treatment and prevention of apoptosis.

【0017】この発明の対象化合物は、すでに国際公開
番号WO 00/26204号に開示されているように、CAE/
SAE効果を有し、ドパミン、ノルアドレナリン、セロ
トニン作動性神経に作用して、神経発火活動に依存して
これらの神経伝達物質の遊離を促進することにより、ア
ルツハイマー病、パーキンソン病などの対症的治療効果
も有することが知られている。すなわち、この発明の対
象化合物である(R)−1−(ベンゾフラン−2−イ
ル)−2−プロピルアミノペンタンおよびその薬理学的
に許容される塩、またはそれらの水和物もしくは溶媒和
物は、アポトーシス抑制作用による細胞死抑制効果また
は神経等の細胞保護効果により疾患の進行を抑制すると
ともに、対症的治療効果も有しており、アルツハイマー
病、パーキンソン病、ハンチントン病、筋萎縮性側索硬
化症、網膜色素変性症、緑内障、脊髄小脳変性症等の神
経疾患、脳卒中等の脳虚血性疾患、糖尿病で観察される
末梢性神経障害等の神経変性疾患、エイズ、中毒性疾患
の治療剤および予防剤として、有益な効果をもたらすも
のである。
The compounds of the present invention are CAE / compounds, as already disclosed in WO 00/26204.
It has a SAE effect, acts on dopamine, noradrenaline, and serotonergic nerves, and promotes the release of these neurotransmitters depending on nerve firing activity, thereby providing symptomatic therapeutic effects such as Alzheimer's disease and Parkinson's disease. Is also known to have. That is, (R) -1- (benzofuran-2-yl) -2-propylaminopentane and its pharmacologically acceptable salts, which are the target compounds of this invention, or their hydrates or solvates are It suppresses the progression of disease by suppressing cell death by suppressing apoptosis or protecting cells such as nerves, and also has symptomatic therapeutic effects. Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis , Retinitis pigmentosa, glaucoma, neurological diseases such as spinocerebellar degeneration, cerebral ischemic diseases such as stroke, neurodegenerative diseases such as peripheral neuropathy observed in diabetes, AIDS, therapeutic agents for addictive diseases and It has a beneficial effect as a preventive agent.

───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 FI テーマコート゛(参考) A61P 25/14 A61P 25/14 25/16 25/16 25/28 25/28 27/02 27/02 27/06 27/06 31/18 31/18 39/02 39/02 43/00 105 43/00 105 C07D 307/81 C07D 307/81 (72)発明者 渡部 真由美 大阪府松原市西大塚1丁目4番10号 株式 会社藤本創薬研究所内 (72)発明者 岳 誉泰 大阪府松原市西大塚1丁目4番10号 株式 会社藤本創薬研究所内 (72)発明者 中谷 昌尚 大阪府松原市西大塚1丁目4番10号 株式 会社藤本創薬研究所内 Fターム(参考) 4C037 PA09 4C086 AA01 AA02 BA06 MA01 MA04 NA14 ZA01 ZA02 ZA15 ZA16 ZA20 ZA33 ZA94 ZB21 ZC37 ZC55 ─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. 7 Identification code FI theme code (reference) A61P 25/14 A61P 25/14 25/16 25/16 25/28 25/28 27/02 27/02 27 / 06 27/06 31/18 31/18 39/02 39/02 43/00 105 43/00 105 C07D 307/81 C07D 307/81 (72) Inventor Mayumi Watanabe 1-4-10 Nishi-Otsuka, Matsubara-shi, Osaka No. 1 in Fujimoto Discovery Research Institute, Inc. (72) Inventor Takayasu Gaku, 1-4-10 Nishiotsuka, Matsubara-shi, Osaka Prefecture Incorporated Fujimoto Discovery Research Institute, Inc. (72) Masahisa Nakatani 1-4-4 Nishiotsuka, Matsubara-shi, Osaka No. 10 Fujimoto Pharmaceutical Research Institute F-term (reference) 4C037 PA09 4C086 AA01 AA02 BA06 MA01 MA04 NA14 ZA01 ZA02 ZA15 ZA16 ZA20 ZA33 ZA94 ZB21 ZC37 ZC55

Claims (4)

【特許請求の範囲】[Claims] 【請求項1】(R)−1−(ベンゾフラン−2−イル)
−2−プロピルアミノペンタンおよびその薬理学的に許
容される塩、またはそれらの水和物もしくは溶媒和物の
いずれかを有効成分として含むアポトーシス抑制剤。
1. (R) -1- (Benzofuran-2-yl)
An apoptosis inhibitor containing, as an active ingredient, 2-propylaminopentane, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.
【請求項2】(R)−1−(ベンゾフラン−2−イル)
−2−プロピルアミノペンタンおよびその薬理学的に許
容される塩、またはそれらの水和物もしくは溶媒和物の
いずれかを有効成分として含むアポトーシスの亢進に起
因する疾患の治療剤。
2. (R) -1- (benzofuran-2-yl)
-2-Propylaminopentane, a therapeutic agent for a disease caused by enhancement of apoptosis, which comprises, as an active ingredient, either a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof.
【請求項3】神経変性疾患、脳虚血性疾患、糖尿病で観
察される末梢性神経障害、エイズまたは中毒性疾患のい
ずれかに用いられることを特徴とする請求項1記載のア
ポトーシス抑制剤。
3. The apoptosis inhibitor according to claim 1, which is used for any of neurodegenerative diseases, cerebral ischemic diseases, peripheral neuropathy observed in diabetes, AIDS and toxic diseases.
【請求項4】神経変性疾患が、アルツハイマー病、パー
キンソン病、ハンチントン病、筋萎縮性側索硬化症、網
膜色素変性症、緑内障または脊髄小脳変性症のいずれか
である請求項3記載のアポトーシス抑制剤。
4. The suppression of apoptosis according to claim 3, wherein the neurodegenerative disease is Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, retinitis pigmentosa, glaucoma or spinocerebellar degeneration. Agent.
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008156160A1 (en) 2007-06-21 2008-12-24 Fujimoto Co., Ltd. Composition for transdermal or transmucosal administration
US8318799B2 (en) * 2004-11-25 2012-11-27 National University Corporation Kyushu University Therapeutic agent for substance dependence
WO2015098591A1 (en) 2013-12-25 2015-07-02 株式会社フジモト・コーポレーション Prophylactic and therapeutic agent for attention-deficit/hyperactivity disorder
WO2017121766A1 (en) 2016-01-12 2017-07-20 Kaleyde Pharmaceuticals Ag Pharmaceutical formulations and their use for the treatment of retinitis pigmentosa

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2714893C2 (en) 2014-12-05 2020-02-20 Земмельвайс Юнивёрсити Arylalkylamine compounds for use in preventing or treating cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000026204A1 (en) * 1998-10-29 2000-05-11 Fujimoto Brothers Co., Ltd. Novel optically active aminopentane derivative

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000026204A1 (en) * 1998-10-29 2000-05-11 Fujimoto Brothers Co., Ltd. Novel optically active aminopentane derivative

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8318799B2 (en) * 2004-11-25 2012-11-27 National University Corporation Kyushu University Therapeutic agent for substance dependence
WO2008156160A1 (en) 2007-06-21 2008-12-24 Fujimoto Co., Ltd. Composition for transdermal or transmucosal administration
WO2015098591A1 (en) 2013-12-25 2015-07-02 株式会社フジモト・コーポレーション Prophylactic and therapeutic agent for attention-deficit/hyperactivity disorder
KR20160096184A (en) 2013-12-25 2016-08-12 가부시키가이샤 후지모토 코포레이션 Prophylactic and therapeutic agent for attention-deficit/hyperactivity disorder
WO2017121766A1 (en) 2016-01-12 2017-07-20 Kaleyde Pharmaceuticals Ag Pharmaceutical formulations and their use for the treatment of retinitis pigmentosa

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