JP2010248224A - 治療又は予防薬 - Google Patents
治療又は予防薬 Download PDFInfo
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- JP2010248224A JP2010248224A JP2010144691A JP2010144691A JP2010248224A JP 2010248224 A JP2010248224 A JP 2010248224A JP 2010144691 A JP2010144691 A JP 2010144691A JP 2010144691 A JP2010144691 A JP 2010144691A JP 2010248224 A JP2010248224 A JP 2010248224A
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
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- 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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- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
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- Medicinal Chemistry (AREA)
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- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
前記一般式(1)で示されるピラゾロ[1,5−a]ピリジン誘導体は公知である。中でも一般名イブジラスト(Ibudilast、3−イソブチリル−2−イソプロピルピラゾロ[1,5−a]ピリジン)は脳循環改善剤、気管支喘息治療剤及びアレルギー性結膜炎治療剤として広く用いられている。
パーキンソン病は線状体へのドーパミン供給が減少することが原因で起こることが知られる。ドーパミンは線状体(被殻、尾状核)に存在するドーパミン・レセプターD1及びD2を介して、線状体のcAMP濃度の調節を行っていると考えられている。従って、これらの部位に特異的に存在するPDE10Aの阻害剤は新規なパーキンソン病治療薬として期待できる。
1)実験方法
各全長PDE、すなわちPDE1A3,PDE2A3,PDE3A,PDE3B,PDE4A4,PDE4B2,PDE4C2,PDE4D3,PDE5A1,PDE5A2,PDE5A3,PDE7A2,PDE8A1,PDE9A2,PDE10A1,PDE11A1のcDNAはヒト由来のRNAよりそれぞれRT−PCRを行い単離した。各単離したcDNA断片をGatewaysystem(Invitrogen社製)及びBac−to−Bac(登録商標)Baculovirus Expression system(Invitrogen社製)で昆虫細胞Sf9に導入し、目的の各PDEタンパクを発現させた。これら組み換えPDE1A3,PDE2A3,PDE3A,PDE4A4,PDE4B2,PDE4C2,PDE4D3,PDE5A1,PDE5A2,PDE5A3,PDE7A2,PDE8A1,PDE9A2,PDE10A1,PDE11A1はこれらPDEタンパクを高発現したSf9細胞の培養上清もしくは細胞抽出液からそれぞれイオン交換クロマトグラフィーで精製した。組み換えPDE3BはPDE3Bタンパクを高発現したSf9細胞をRIPAbuffer[150mM NaCl,10mM Tris−HCl(pH8.3),0.1%proteaseinhibitor cocktail(製品番号:P8849、Sigma社製)]で懸濁し、その全懸濁液を以下に示す実験に用いた。
表2に示すように、組み換えヒトPDEを用いたin vitroの実験でイブジラストはPDE10A1に対して特に強い阻害作用を示すことが明らかとなった。
Claims (6)
- 前記一般式(1)で示される化合物が3−イソブチリル−2−イソプロピルピラゾロ[1,5−a]ピリジンである請求項1に記載の統合失調症の治療又は予防薬。
- 前記一般式(1)で示される化合物が3−イソブチリル−2−イソプロピルピラゾロ[1,5−a]ピリジンである請求項3に記載のパーキンソン病の治療又は予防薬。
- 前記一般式(1)で示される化合物が3−イソブチリル−2−イソプロピルピラゾロ[1,5−a]ピリジンである請求項5に記載のハンチントン病の治療又は予防薬。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2010144691A JP5192517B2 (ja) | 2002-12-03 | 2010-06-25 | 治療又は予防薬 |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2002350804 | 2002-12-03 | ||
JP2002350804 | 2002-12-03 | ||
JP2010144691A JP5192517B2 (ja) | 2002-12-03 | 2010-06-25 | 治療又は予防薬 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004556869A Division JP4589122B2 (ja) | 2002-12-03 | 2003-12-01 | ホスホジエステラーゼ10a阻害剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2010248224A true JP2010248224A (ja) | 2010-11-04 |
JP5192517B2 JP5192517B2 (ja) | 2013-05-08 |
Family
ID=32463120
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004556869A Expired - Fee Related JP4589122B2 (ja) | 2002-12-03 | 2003-12-01 | ホスホジエステラーゼ10a阻害剤 |
JP2010144691A Expired - Fee Related JP5192517B2 (ja) | 2002-12-03 | 2010-06-25 | 治療又は予防薬 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004556869A Expired - Fee Related JP4589122B2 (ja) | 2002-12-03 | 2003-12-01 | ホスホジエステラーゼ10a阻害剤 |
Country Status (6)
Country | Link |
---|---|
US (3) | US20060106054A1 (ja) |
EP (1) | EP1570847B1 (ja) |
JP (2) | JP4589122B2 (ja) |
AU (1) | AU2003302588A1 (ja) |
CA (1) | CA2508194C (ja) |
WO (1) | WO2004050091A1 (ja) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6953774B2 (en) * | 2000-08-11 | 2005-10-11 | Applied Research Systems Ars Holding N.V. | Methods of inducing ovulation |
EP1570847B1 (en) * | 2002-12-03 | 2012-04-25 | Kyorin Pharmaceutical Co., Ltd. | Phosphodiesterase 10a inhibitors for use in the treatment of parkinson's disease, huntington's disease and schizophrenia |
US8338420B1 (en) | 2002-12-04 | 2012-12-25 | Mitsubishi Tanabe Pharma Corporation | Treatment of Parkinson's disease and enhancement of dopamine signal using PDE 10 inhibitor |
PL1928438T3 (pl) * | 2005-09-26 | 2013-08-30 | Avigen Inc | Zastosowanie ibudilastu do leczenia uzależnień od środków odurzających |
CA2653345A1 (en) * | 2006-05-31 | 2007-12-13 | Avigen, Inc. | Ibudilast for inhibiting macrophage migration inhibitory factor (mif) activity |
US20090028816A1 (en) * | 2007-07-27 | 2009-01-29 | Lance Sultzbaugh | Treatment of depression, psychosis, and anxiety |
WO2010005520A2 (en) * | 2008-06-30 | 2010-01-14 | Concert Pharmaceuticals, Inc. | 2-alkyl-3-acylpyrazolo[1,5-a]pyridine derivatives |
US8017604B2 (en) * | 2009-09-24 | 2011-09-13 | Hoffmann-La Roche Inc. | Imidazopyridines |
RU2013110517A (ru) * | 2010-08-12 | 2014-09-20 | Керин Фармасьютикал Ко., Лтд. | Средство для профилактики или лечения неалкогольного стеатогепатита |
US10039764B2 (en) | 2013-07-12 | 2018-08-07 | University Of South Alabama | Treatment and diagnosis of cancer and precancerous conditions using PDE10A inhibitors and methods to measure PDE10A expression |
US10433342B2 (en) | 2016-10-19 | 2019-10-01 | Qualcomm Incorporated | Enhanced random access channel (RACH) procedure |
US11770855B2 (en) | 2016-10-19 | 2023-09-26 | Qualcomm Incorporated | Random access channel (RACH) procedure design |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH02131424A (ja) * | 1988-11-11 | 1990-05-21 | Kyorin Pharmaceut Co Ltd | 記憶障害改善薬 |
WO2000009127A1 (fr) * | 1998-08-10 | 2000-02-24 | Kyorin Pharmaceutical Co., Ltd. | Traitements contre la sclerose en plaques |
WO2002066480A2 (en) * | 2001-02-20 | 2002-08-29 | Astrazeneca Ab | 2-arylamino-pyrimidines for the treatment of gsk3-related disorders |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1998014448A1 (fr) * | 1996-10-04 | 1998-04-09 | Kyorin Pharmaceutical Co., Ltd. | Derives de pyrazolopyridylpyridazinone et procede de preparation des ces derniers |
JP4293294B2 (ja) * | 1998-04-24 | 2009-07-08 | 藤原 道弘 | 痴呆改善薬 |
JP2000224992A (ja) * | 1998-11-30 | 2000-08-15 | Tanabe Seiyaku Co Ltd | 新規ホスホジエステラーゼ及びその遺伝子 |
AU7766300A (en) * | 1999-10-07 | 2001-05-10 | Novaneuron Inc. | Gene necessary for striatal function, uses thereof, and compounds for modulatingsame |
CA2392993A1 (en) * | 1999-11-30 | 2001-06-07 | Hiroshi Nagase | Agent for improving learning and/or memory |
EP1570847B1 (en) * | 2002-12-03 | 2012-04-25 | Kyorin Pharmaceutical Co., Ltd. | Phosphodiesterase 10a inhibitors for use in the treatment of parkinson's disease, huntington's disease and schizophrenia |
-
2003
- 2003-12-01 EP EP03812356A patent/EP1570847B1/en not_active Expired - Fee Related
- 2003-12-01 US US10/537,313 patent/US20060106054A1/en not_active Abandoned
- 2003-12-01 AU AU2003302588A patent/AU2003302588A1/en not_active Abandoned
- 2003-12-01 JP JP2004556869A patent/JP4589122B2/ja not_active Expired - Fee Related
- 2003-12-01 WO PCT/JP2003/015315 patent/WO2004050091A1/ja active Application Filing
- 2003-12-01 CA CA2508194A patent/CA2508194C/en not_active Expired - Fee Related
-
2007
- 2007-10-31 US US11/980,526 patent/US7846942B2/en not_active Expired - Fee Related
-
2010
- 2010-06-25 JP JP2010144691A patent/JP5192517B2/ja not_active Expired - Fee Related
- 2010-10-27 US US12/913,094 patent/US8404710B2/en not_active Expired - Fee Related
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH02131424A (ja) * | 1988-11-11 | 1990-05-21 | Kyorin Pharmaceut Co Ltd | 記憶障害改善薬 |
WO2000009127A1 (fr) * | 1998-08-10 | 2000-02-24 | Kyorin Pharmaceutical Co., Ltd. | Traitements contre la sclerose en plaques |
WO2002066480A2 (en) * | 2001-02-20 | 2002-08-29 | Astrazeneca Ab | 2-arylamino-pyrimidines for the treatment of gsk3-related disorders |
Non-Patent Citations (1)
Title |
---|
JPN5005011621; 笠原 洋勇: '脳循環・代謝改善薬とその使い方' クリニカ Vol.17, No.5, 1990, p.256-62 * |
Also Published As
Publication number | Publication date |
---|---|
JP4589122B2 (ja) | 2010-12-01 |
US20110039882A1 (en) | 2011-02-17 |
EP1570847A4 (en) | 2008-10-08 |
US7846942B2 (en) | 2010-12-07 |
EP1570847A1 (en) | 2005-09-07 |
JPWO2004050091A1 (ja) | 2006-03-30 |
WO2004050091A1 (ja) | 2004-06-17 |
CA2508194C (en) | 2011-05-24 |
US20060106054A1 (en) | 2006-05-18 |
US20080108650A1 (en) | 2008-05-08 |
US8404710B2 (en) | 2013-03-26 |
JP5192517B2 (ja) | 2013-05-08 |
CA2508194A1 (en) | 2004-06-17 |
AU2003302588A1 (en) | 2004-06-23 |
EP1570847B1 (en) | 2012-04-25 |
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