JPWO2012105475A1 - 悪液質の治療又は予防剤 - Google Patents
悪液質の治療又は予防剤 Download PDFInfo
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- JPWO2012105475A1 JPWO2012105475A1 JP2012507744A JP2012507744A JPWO2012105475A1 JP WO2012105475 A1 JPWO2012105475 A1 JP WO2012105475A1 JP 2012507744 A JP2012507744 A JP 2012507744A JP 2012507744 A JP2012507744 A JP 2012507744A JP WO2012105475 A1 JPWO2012105475 A1 JP WO2012105475A1
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
Abstract
Description
[1]
下記一般式(I)
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して含有する悪液質の治療又は予防剤。
[2]
一般式(I)において、R1が、シクロプロピルメチル、シクロブチルメチル、シクロペンチルメチル又はシクロヘキシルメチルであり、R2が、メチル、エチル又はプロピルである、[1]記載の悪液質の治療又は予防剤。
[3]
一般式(I)において、R1が、シクロプロピルメチルであり、R2が、メチルであり、Bが、トランス型の−CH=CH−である、[1]記載の悪液質の治療又は予防剤。
[4]
一般式(I)で表される化合物が、(−)−17−(シクロプロピルメチル)−3,14β−ジヒドロキシ−4,5α−エポキシ−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
[5]
悪液質が、がん悪液質である、[1]から[4]のいずれか一項記載の悪液質の治療又は予防剤。
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して含有する。
B16/F10 melanoma細胞の継代は、10%FCS含有RPMI1640培地を用いて行った。薬効評価には、4週齢の雄性C57BL/6マウス(日本エスエルシー)を購入し、3週間の馴化の後に使用した。悪液質モデル動物の作製は、以下のようにして行った。すなわち、B16/F10 melanoma細胞をマウスの足蹠に1匹あたり4×105個ずつ移植した。細胞移植から3週間後、腫瘍体積がある程度大きくなったことを確認し、悪液質モデル動物とした。また、腫瘍体積を測定して各群腫瘍体積の平均が均等になるよう群分けを行った。悪液質に対する治療効果の検討は、以下のようにして行った。
生理食塩水投与群の生存期間に対し、化合物1の投与は統計学的に有意な延長作用(p=0.0335:カプランマイヤー法ログランク検定)を示した。これに対し、CI−977及びモルヒネの投与は、生存期間の短縮傾向を示した。また、生理食塩水投与群の体重減少に対し、化合物1及びCI−977の投与は、統計学的に有意な抑制作用(化合物1 30μg/kg p=0.0365、化合物1 100μg/kg p=0.0007、CI−977 p=0.0009:経時型多重比較(Dunnett型比較))を示したが、モルヒネの投与はさらなる体重減少傾向を示した。
Claims (5)
- 一般式(I)において、R1が、シクロプロピルメチル、シクロブチルメチル、シクロペンチルメチル又はシクロヘキシルメチルであり、R2が、メチル、エチル又はプロピルである、請求項1記載の悪液質の治療又は予防剤。
- 一般式(I)において、R1が、シクロプロピルメチルであり、R2が、メチルであり、Bが、トランス型の−CH=CH−である、請求項1記載の悪液質の治療又は予防剤。
- 悪液質が、がん悪液質である、請求項1から4のいずれか一項記載の悪液質の治療又は予防剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2011018021 | 2011-01-31 | ||
JP2011018021 | 2011-01-31 | ||
PCT/JP2012/051937 WO2012105475A1 (ja) | 2011-01-31 | 2012-01-30 | 悪液質の治療又は予防剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2012105475A1 true JPWO2012105475A1 (ja) | 2014-07-03 |
JP5929753B2 JP5929753B2 (ja) | 2016-06-08 |
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Application Number | Title | Priority Date | Filing Date |
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JP2012507744A Active JP5929753B2 (ja) | 2011-01-31 | 2012-01-30 | 悪液質の治療又は予防剤 |
Country Status (8)
Country | Link |
---|---|
US (1) | US9006262B2 (ja) |
EP (1) | EP2671585B1 (ja) |
JP (1) | JP5929753B2 (ja) |
CN (1) | CN103327977B (ja) |
CA (1) | CA2825165C (ja) |
ES (1) | ES2586655T3 (ja) |
MX (1) | MX2013008749A (ja) |
WO (1) | WO2012105475A1 (ja) |
Families Citing this family (13)
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AU2011317183B2 (en) * | 2010-10-19 | 2016-10-20 | Memorial Sloan-Kettering Cancer Center | 6-amido derivatives of 4,5a-epoxymorphinans for treatment of pain |
WO2016152965A1 (ja) * | 2015-03-24 | 2016-09-29 | 東レ株式会社 | 低アルブミン血症の改善剤 |
EP4212532A3 (en) | 2015-04-30 | 2023-09-27 | Memorial Sloan Kettering Cancer Center | Mitragynine analogs and uses thereof |
WO2019171333A1 (en) | 2018-03-08 | 2019-09-12 | Victoria Link Ltd | Treatment of demyelinating diseases |
WO2020012248A1 (en) | 2018-07-13 | 2020-01-16 | Alkermes Pharma Ireland Limited | Novel naphthylenyl compounds for long-acting injectable compositions and related methods |
WO2020012245A1 (en) | 2018-07-13 | 2020-01-16 | Alkermes Pharma Ireland Limited | Thienothiophene-naltrexone prodrugs for long-acting injectable compositions |
WO2020094634A1 (en) | 2018-11-05 | 2020-05-14 | Alkermes Pharma Ireland Limited | Thiophene prodrugs of naltroxene for long-acting injectable compositions and related methods |
CN113614089A (zh) * | 2019-03-29 | 2021-11-05 | 人福医药美国公司 | 可用于治疗医学病症的新型吗啡喃 |
TW202128165A (zh) | 2019-10-24 | 2021-08-01 | 日商東麗股份有限公司 | 惡病質之治療劑或預防劑 |
US20230255955A1 (en) | 2020-06-30 | 2023-08-17 | Toray Industries, Inc. | Ameliorating agent or prophylactic agent for muscle weakness symptom in disease or syndrome associated with metabolic disorder |
EP4178666A1 (en) * | 2020-07-10 | 2023-05-17 | Duke University | Compositions and methods for treating cancer-associated cachexia |
JPWO2022225045A1 (ja) | 2021-04-23 | 2022-10-27 | ||
AU2022292554A1 (en) | 2021-06-14 | 2024-01-04 | Scorpion Therapeutics, Inc. | Urea derivatives which can be used to treat cancer |
Family Cites Families (25)
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JP2714731B2 (ja) | 1991-08-19 | 1998-02-16 | 株式会社大塚製薬工場 | 悪液質改善治療剤 |
ES2121988T3 (es) | 1992-01-23 | 1998-12-16 | Toray Industries | Derivado de morfinano y uso medicinal. |
AU683664B2 (en) | 1993-06-30 | 1997-11-20 | Toray Industries, Inc. | Antitussive |
WO1995003307A1 (fr) | 1993-07-19 | 1995-02-02 | Toray Industries, Inc. | Agent de protection de cellules cerebrales |
CN1291717C (zh) | 1996-11-25 | 2006-12-27 | 东丽株式会社 | 止痒药物 |
ATE361099T1 (de) | 1997-05-15 | 2007-05-15 | Chugai Pharmaceutical Co Ltd | Heilmittel für kachexie |
WO1999005146A1 (fr) | 1997-07-25 | 1999-02-04 | Toray Industries, Inc. | Remedes contre l'hyponatremie |
DE69830654T2 (de) | 1997-09-02 | 2006-05-04 | Toray Industries, Inc. | Heilmittel für die drogenabhängigkeit |
JP3214695B2 (ja) | 1998-07-21 | 2001-10-02 | 三共株式会社 | 悪液質の予防剤、又は治療剤 |
JP2000053572A (ja) | 1998-08-11 | 2000-02-22 | Toray Ind Inc | ORL1(opioid orphan)受容体拮抗薬 |
DE19939044A1 (de) * | 1999-08-18 | 2001-03-15 | Gruenenthal Gmbh | Verwendung von Morphinanderivaten als Arzneimittel |
EP1219624B1 (en) | 1999-08-24 | 2008-07-09 | Toray Industries, Inc. | Remedies for neuropathic pain and model animals of neuropathic pain |
JP2001163784A (ja) | 1999-12-06 | 2001-06-19 | Toray Ind Inc | 角膜または結膜用止痒剤 |
US7026484B2 (en) | 2001-02-23 | 2006-04-11 | Ligand Pharmaceuticals Incorporated | Tricyclic androgen receptor modulator compounds and methods |
ES2319265T3 (es) | 2001-03-30 | 2009-05-06 | Toray Industries, Inc. | Farmacos para el sindrome de piernas inquietas. |
CA2451133C (en) * | 2001-05-08 | 2012-09-18 | Toray Industries, Inc. | Therapeutic agent for sepsis |
EP1735055A1 (en) | 2004-03-30 | 2006-12-27 | Sapphire Therapeutics, Inc. | Method of reducing c-reactive protein using growth hormone secretagogues |
ES2423004T3 (es) | 2005-03-10 | 2013-09-17 | Toray Industries, Inc. | Agente antiprurítico para el prurito provocado por la esclerosis múltiple |
US8796301B2 (en) | 2007-04-24 | 2014-08-05 | Toray Industries, Inc. | Therapeutic or prophylactic agent for dyskinesia |
WO2009001764A1 (ja) | 2007-06-22 | 2008-12-31 | Toray Industries, Inc. | 統合失調症の治療または予防剤 |
WO2009044883A1 (ja) | 2007-10-05 | 2009-04-09 | Toray Industries, Inc. | モルヒナン誘導体また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皮膚性状改善治療薬 |
US8829020B2 (en) * | 2009-07-16 | 2014-09-09 | Mallinckrodt Llc | Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers |
CA2768236C (en) | 2009-07-16 | 2018-05-22 | Mallinckrodt Llc | (+)-morphinans as antagonists of toll-like receptor 9 and therapeutic uses thereof |
JP2011074018A (ja) | 2009-09-30 | 2011-04-14 | Toray Ind Inc | 線維筋痛症の治療剤又は予防剤 |
US10131672B2 (en) | 2010-01-29 | 2018-11-20 | Toray Industries, Inc. | Therapeutic or prophylactic agent for biliary diseases |
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2012
- 2012-01-30 CN CN201280007167.XA patent/CN103327977B/zh active Active
- 2012-01-30 US US13/982,578 patent/US9006262B2/en active Active
- 2012-01-30 EP EP12742214.5A patent/EP2671585B1/en active Active
- 2012-01-30 CA CA2825165A patent/CA2825165C/en active Active
- 2012-01-30 WO PCT/JP2012/051937 patent/WO2012105475A1/ja active Application Filing
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Publication number | Publication date |
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EP2671585B1 (en) | 2016-07-13 |
CN103327977B (zh) | 2016-05-04 |
US20130310414A1 (en) | 2013-11-21 |
ES2586655T3 (es) | 2016-10-18 |
EP2671585A1 (en) | 2013-12-11 |
CN103327977A (zh) | 2013-09-25 |
CA2825165C (en) | 2018-07-03 |
EP2671585A4 (en) | 2015-05-20 |
MX2013008749A (es) | 2013-10-17 |
JP5929753B2 (ja) | 2016-06-08 |
WO2012105475A1 (ja) | 2012-08-09 |
US9006262B2 (en) | 2015-04-14 |
CA2825165A1 (en) | 2012-08-09 |
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