JP5119919B2 - 多発性硬化症に伴う痒みに対する止痒剤 - Google Patents
多発性硬化症に伴う痒みに対する止痒剤 Download PDFInfo
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- JP5119919B2 JP5119919B2 JP2007507193A JP2007507193A JP5119919B2 JP 5119919 B2 JP5119919 B2 JP 5119919B2 JP 2007507193 A JP2007507193 A JP 2007507193A JP 2007507193 A JP2007507193 A JP 2007507193A JP 5119919 B2 JP5119919 B2 JP 5119919B2
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- 0 C[C@@]1(*(B*)C1C(C1)[C@]1C12*)C11c3c(*)c(*)ccc3*C2N(*)CC1 Chemical compound C[C@@]1(*(B*)C1C(C1)[C@]1C12*)C11c3c(*)c(*)ccc3*C2N(*)CC1 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
R1 は炭素数4から7のシクロアルキルアルキルを表し、
R2はヒドロキシを表し、
R3はヒドロキシを表し、
Aは−XC(=Y)−(ここでXはNR4を表し、YはOを表し、R4は炭素数1から5の直鎖又は分岐アルキルを表す)を表し、
Bは−C=C−を表し、
R5 は、
R6とR7は一緒になって−O−を表し、
R8は水素を表し、
R12及びR13は共に水素を表す。また、一般式(I)は(+)体、(−)体、(±)体を包含する。]
で表される化合物又はその薬理学的に許容される酸付加塩を有効成分とする多発性硬化症に伴う痒みに対する止痒剤を提供する。
MRL/lpr系マウスにおける引っ掻き行動回数および血清中イムノグロブリン抗体価の週齢変化
SPF環境において飼育中の雌性および雄性MRL/lpr系マウスを観察用ケージ(1区分:10×14×30cm)の1区分に1匹ずつ個別に入れ、以後1時間の行動を無人環境下で上方よりビデオ撮影することにより、加齢による自然誘発性の引っ掻き行動回数の変化について検討した。撮影は、8週齢から20週齢まで2週間に1回の頻度で同じマウスを用いて実施した。ビデオテープの再生により引っ掻き行動を観察し、60分間に発生した後肢による引っ掻き行動回数を目視により計測した。なお、引っ掻き行動は、マウスが後肢を引っ掻き開始のために上げてから降ろすまでの一連の動作を1回として計測した。この結果を表1に示す。雌性マウスでは、10週齢以上の週齢で、1時間の平均の引っ掻き行動回数が40回以上を示すことが判明した。表中**は対照群(8週齢時)との差が統計学的に有意である(p<0.01)ことを示す(1群の時点間の多重比較検定)。また雄性マウスに比べ、雌性MRL/lpr系マウスでは、10週齢から顕著な引っ掻き行動が認められ、20週齢における平均の引っ掻き行動回数は300回を越えたことから、評価には雌性マウスを用いることが望ましいことが示された。
MRL/lpr系マウスにおける自然誘発性引っ掻き行動に対する(-)-17-シクロプロピルメチル-4,5α-エポキシ-3,14β-ジヒドロキシ-6β-(N-メチル-トランス-3-(3-フリル)アクリルアミド)モルヒナン塩酸塩(化合物1)の効果
自然誘発性の引っ掻き行動が認められる20週齢の雌性MRL/lpr系マウスを用いて、そう痒に対するオピオイドκ受容体作動性化合物である化合物1
Claims (4)
- 一般式(I)において、R1がシクロプロピルメチルである化合物又はその薬理学的に許容される酸付加塩を有効成分とする請求項1記載の多発性硬化症に伴う痒みに対する止痒剤。
- 一般式(I)において、Aが−XC(=Y)−(ここでXはNR4を表し、YはOを表し、R4はメチルを表す)である化合物又はその薬理学的に許容される酸付加塩を有効成分とする請求項1記載の多発性硬化症に伴う痒みに対する止痒剤。
- 一般式(I)で表される化合物が、(−)−17−(シクロプロピルメチル)−4,5α−エポキシ−3,14β−ジヒドロキシ−6β−[N-メチル-トランス−3−(3−フリル)アクリルアミド]モルヒナンである請求項1記載の多発性硬化症に伴う痒みに対する止痒剤。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2007507193A JP5119919B2 (ja) | 2005-03-10 | 2006-03-09 | 多発性硬化症に伴う痒みに対する止痒剤 |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005066666 | 2005-03-10 | ||
JP2005066666 | 2005-03-10 | ||
PCT/JP2006/304655 WO2006095836A1 (ja) | 2005-03-10 | 2006-03-09 | 多発性硬化症に伴う痒みに対する止痒剤 |
JP2007507193A JP5119919B2 (ja) | 2005-03-10 | 2006-03-09 | 多発性硬化症に伴う痒みに対する止痒剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2006095836A1 JPWO2006095836A1 (ja) | 2008-08-21 |
JP5119919B2 true JP5119919B2 (ja) | 2013-01-16 |
Family
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Family Applications (1)
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JP2007507193A Expired - Fee Related JP5119919B2 (ja) | 2005-03-10 | 2006-03-09 | 多発性硬化症に伴う痒みに対する止痒剤 |
Country Status (11)
Country | Link |
---|---|
US (1) | US9051335B2 (ja) |
EP (1) | EP1870413B1 (ja) |
JP (1) | JP5119919B2 (ja) |
KR (1) | KR101324539B1 (ja) |
CN (1) | CN101137658B (ja) |
AU (1) | AU2006221314B2 (ja) |
CA (1) | CA2604071C (ja) |
ES (1) | ES2423004T3 (ja) |
PL (1) | PL1870413T3 (ja) |
PT (1) | PT1870413E (ja) |
WO (1) | WO2006095836A1 (ja) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2685126C (en) | 2007-04-24 | 2015-04-14 | Toray Industries, Inc. | Therapeutic or prophylactic agent for dyskinesia |
AU2008268202B2 (en) | 2007-06-22 | 2012-12-20 | Toray Industries, Inc. | Remedy or preventive for integration dysfunction syndrome |
BRPI0817804A8 (pt) | 2007-10-05 | 2017-04-18 | Toray Industries | Agente terapêutico para melhorar as propriedades da pele compreendendo um derivado de morfinano ou qualquer um de seus sais de adição de ácido farmacologicamente permissíveis como um ingrediente ativo |
AU2011211223B2 (en) | 2010-01-29 | 2014-10-23 | Toray Industries, Inc. | Therapeutic or prophylactic agent for biliary diseases |
MX2013008749A (es) | 2011-01-31 | 2013-10-17 | Toray Industries | Agente terapeutico o profilactico para caquexia. |
CN102266317A (zh) * | 2011-06-24 | 2011-12-07 | 中国人民解放军第三军医大学 | 丙戊酸及其衍生物的应用 |
CN102526732A (zh) * | 2011-12-20 | 2012-07-04 | 同济大学 | 靶向调节组蛋白乙酰化水平的药物在制备用于预防或治疗自身免疫性疾病的药物中的用途 |
JPWO2016152953A1 (ja) * | 2015-03-24 | 2018-01-11 | 東レ株式会社 | モルヒナン誘導体及びその医薬用途 |
EP3761982A4 (en) | 2018-03-08 | 2021-12-15 | Victoria Link Ltd | TREATMENT OF DEMYELINIZATION DISEASES |
US11135197B2 (en) | 2020-02-07 | 2021-10-05 | Argentum Pharmaceuticals Llc | Dosage regimen of an S1P receptor modulator |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001014383A1 (fr) * | 1999-08-24 | 2001-03-01 | Toray Industries, Inc. | Remedes contre les douleurs neuropathiques et modeles animaux de douleurs neuropathiques |
Family Cites Families (6)
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JPH0578243A (ja) * | 1990-12-11 | 1993-03-30 | Shiseido Co Ltd | 鎮痒剤及び鎮痒組成物 |
EP1327444B1 (en) * | 1996-11-25 | 2005-03-23 | Toray Industries, Inc. | Antipruritic agent |
WO2001041705A2 (en) | 1999-11-29 | 2001-06-14 | Adolor Corporation | Novel methods for the treatment and prevention of dizziness and pruritus |
JP2001163784A (ja) | 1999-12-06 | 2001-06-19 | Toray Ind Inc | 角膜または結膜用止痒剤 |
JP2002308769A (ja) * | 2001-04-12 | 2002-10-23 | Toray Ind Inc | 止痒剤 |
WO2005048926A2 (en) * | 2003-11-13 | 2005-06-02 | The General Hospital Corporation | Methods for treating pain |
-
2006
- 2006-03-09 WO PCT/JP2006/304655 patent/WO2006095836A1/ja active Application Filing
- 2006-03-09 KR KR1020077020357A patent/KR101324539B1/ko active IP Right Grant
- 2006-03-09 AU AU2006221314A patent/AU2006221314B2/en not_active Ceased
- 2006-03-09 CN CN2006800078067A patent/CN101137658B/zh not_active Expired - Fee Related
- 2006-03-09 JP JP2007507193A patent/JP5119919B2/ja not_active Expired - Fee Related
- 2006-03-09 ES ES06715476T patent/ES2423004T3/es active Active
- 2006-03-09 US US11/885,946 patent/US9051335B2/en not_active Expired - Fee Related
- 2006-03-09 CA CA2604071A patent/CA2604071C/en not_active Expired - Fee Related
- 2006-03-09 PL PL06715476T patent/PL1870413T3/pl unknown
- 2006-03-09 PT PT67154765T patent/PT1870413E/pt unknown
- 2006-03-09 EP EP06715476.5A patent/EP1870413B1/en not_active Not-in-force
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001014383A1 (fr) * | 1999-08-24 | 2001-03-01 | Toray Industries, Inc. | Remedes contre les douleurs neuropathiques et modeles animaux de douleurs neuropathiques |
Also Published As
Publication number | Publication date |
---|---|
CN101137658B (zh) | 2011-06-08 |
CA2604071C (en) | 2013-10-08 |
US20090170888A1 (en) | 2009-07-02 |
KR101324539B1 (ko) | 2013-11-01 |
WO2006095836A1 (ja) | 2006-09-14 |
AU2006221314B2 (en) | 2012-09-06 |
US9051335B2 (en) | 2015-06-09 |
JPWO2006095836A1 (ja) | 2008-08-21 |
KR20070117574A (ko) | 2007-12-12 |
CA2604071A1 (en) | 2006-09-14 |
PT1870413E (pt) | 2013-10-01 |
CN101137658A (zh) | 2008-03-05 |
PL1870413T3 (pl) | 2013-12-31 |
EP1870413B1 (en) | 2013-07-10 |
AU2006221314A1 (en) | 2006-09-14 |
EP1870413A1 (en) | 2007-12-26 |
EP1870413A4 (en) | 2009-12-23 |
ES2423004T3 (es) | 2013-09-17 |
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