JP2010265321A - p53阻害剤およびその治療用途 - Google Patents
p53阻害剤およびその治療用途 Download PDFInfo
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Abstract
【解決手段】 p53活性の阻害が有効な疾患を患った個体に対して、治療上有効な量のp53阻害剤を投与する。
【選択図】 なし
Description
a)UV(紫外線)照射、細胞変異、化学療法および放射線療法による損傷などといった、DNA損傷;
b)高熱症;ならびに
c)いくつかの化学療法剤によって惹起される(例えば、タキソールまたはビンカアルカロイド類を用いた処置)微小管の調節解除などでである。
(ii)治療用途で、充分に低い毒性を有するものであって、p53活性を阻害するのに充分な濃度で望ましくない副作用を起こすこともないこと;
(iii)長期のp53不活性化は、癌の危険性を有意に高め得るので、可逆的なp53阻害を呈すること;
(iv)一時的なp53阻害の際に、細胞は付されたストレスから回復すべきであり、そしてp53を活性化するシグナルは排除または低減されるべきである、さもなければ、p53活性化シグナルが活性化されている間のp53活性の復旧が、細胞損傷を惹起する可能性がある;
(v)p53抑制療法は、癌発生の頻度の劇的な増大に関わるものでなく、すなわち、治療的阻害剤は、ストレスに対する細胞性応答の、p53によって媒介される制御を標的としているが、p53によって媒介される発癌遺伝子の形質転換の制御に影響を及ぼすものではない。
mは0または1であり、
nは1〜4であり、
R1およびR2は独立して、水素、アルキル、アルケニル、アルキニル、アリール、アラルキル、アルカリール、複素環、ヘテロアリール、ヘテロアラルキル、ハロアルキル、ハロアリール、アルコキシ、アリールオキシ、アルコキシアルキル、アリールオキシアルキル、アラルコキシアルキル、ハロ、(アルキルチオ)アルキル、(アリールチオ)アルキル、および(アラルキルチオ)アルキルよりなる群から選択され、
または、R1およびR2は共に、脂肪族または芳香族の5乃至8員環で、炭素環または複素環のいずれかを形成し、
R3は、水素、アルキル、ハロアルキル、アルケニル、アルキニル、アリール、アラルキル、ハロアリール、ヘテロアラルキル、複素環、アルコキシ、アリールオキシ、ハロ、NR4R5、NHSO2R4R5、NHSO2R4、およびSO2NR4R5よりなる群から選択され、そして
R4およびR5は独立して、水素、アルキル、アリール、ヘテロアリール、および複素環よりなる群から選択され、
または、R4およびR5は共に、脂肪族または芳香族の5乃至8員環で、炭素環または複素環のいずれかを形成するものである]を有する化合物、ならびに医薬上容認され得るこれらの塩および水和物である。
(a)化学療法剤;および
(b)一時的なp53阻害剤
を含む組成物を提供することにある。
(a)該疾患を処置することができる薬物;および
(b)一時的なp53阻害剤
を含む組成物を提供することにある。
(a)一時的なp53阻害剤、および
(b)担体
を含む組成物を提供することにある。
mは0または1であり、
nは1〜4であり、
R1およびR2は独立して、水素、アルキル、アルケニル、アルキニル、アリール、アラルキル、アルカリール、複素環、ヘテロアリール、ヘテロアラルキル、ハロアルキル、ハロアリール、アルコキシ、アリールオキシ、アルコキシアルキル、アリールオキシアルキル、アラルコキシアルキル、ハロ、(アルキルチオ)アルキル、(アリールチオ)アルキル、および(アラルキルチオ)アルキルよりなる群から選択され、
または、R1およびR2は共に、脂肪族または芳香族の5乃至8員環で、炭素環または複素環のいずれかを形成し、
R3は、水素、アルキル、ハロアルキル、アルケニル、アルキニル、アリール、アルカリール、アラルキル、ハロアリール、ヘテロアラルキル、複素環、アルコキシ、アリールオキシ、ハロ、NR4R5、NHSO2R4R5、NHSO2R4、およびSO2NR4R5よりなる群から選択され、そして
R4およびR5は独立して、水素、アルキル、アリール、ヘテロアリール、および複素環よりなる群から選択され、
または、R4およびR5は共に、脂肪族または芳香族の5乃至8員環で、炭素環または複素環のいずれかを形成するものである]を有するもの、ならびに医薬上容認され得るこれらの塩および水和物が含まれる。
(V)−−2−[2−イミノ−4,5,6,7−テトラヒドロ−1,3−ベンゾチアゾール−3(2H)−イル]−1−(4−メチルフェニル)−1−エタノン;
(VI)−−2−(4−メチルフェニル)−5,6,7,8−テトラヒドロベンゾ[d]イミダゾ[2,1−b]チアゾール;
(VII)−−2−[2−イミノ−4,5,6,7−テトラヒドロ−1,3−ベンゾチアゾール−3(2H)−イル]−1−(4−ヨードフェニル)−1−エタノン;
(VIII)−−2−[2−イミノ−4,5,6,7−テトラヒドロ−1,3−ベンゾチアゾール−3(2H)−イル]−1−(ビフェニル)−1−エタノン;
(IX)−−2−フェニル−5,6,7,8−テトラヒドロベンゾ[d]イミダゾ[2,1−b]チアゾール;
(X)−−3−メチル−6−フェニルイミダゾ[2,1−b]−チアゾール;および
(XI)−−2,3−ジメチル−6−フェニルイミダゾ[2,1−b]チアゾールと命名される。 構造式(V)の化合物は、ピフィスリン−アルファおよびPFT−αの慣用名でも知られている。 構造式(VI)の化合物は、ピフィスリン−ベータおよびPFT−βの慣用名でも知られている。 構造式(VII)の化合物は、化合物86B10としても知られている。
(b)p53経路分析およびモジュレーションを研究するためのツールとしての、構造式(I)から(IV)までの化合物、例えば構造式(V)または(VI)の化合物などといった一時的なp53阻害剤の適用;
(c)種々のストレスの後の死亡から細胞を救出するための薬物としての、構造式(I)から(IV)までの化合物などの一時的なp53阻害剤の投与;
(d)抗癌治療に対してp53欠損細胞を高感度にするための薬物としての、構造式(I)から(IV)までの化合物などの一時的なp53阻害剤の投与;
(e)組織加齢を抑制するための潜在的抗老化薬物としての、構造式(I)から(IV)までの化合物などの一時的なp53阻害剤の投与;
(f)p53経路分析およびモジュレーションのためのツールとしてp53依存性のトランス活性化を抑制するための、構造式(I)から(IV)までの化合物などの一時的なp53阻害剤の適用;
(g)インビボでの放射線保護剤としての、構造式(I)から(IV)までの化合物などの一時的なp53阻害剤の投与;
(h)抗癌治療の副作用、急性炎症、傷害(例えば、熱傷および中枢神経系外傷)、細胞加齢、高熱症、発作、移植前の移植組織および臓器、骨髄移植のための宿主の準備、ならびに低酸素症(例えば、虚血および卒中)を含めた、異なる病理学的環境にて種々のストレスから細胞を保護するための、インビボでの、構造式(I)から(IV)までの化合物などの一時的なp53阻害剤の投与。
Claims (1)
- p53活性の阻害が利点をもたらす疾患または状態を処置する方法であって、当該疾患または状態に見舞われている個体に、一時的なp53阻害剤の治療上有効な量を投与する工程を含む方法。
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US11788199P | 1999-01-29 | 1999-01-29 |
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JP2000595668A Division JP2002535357A (ja) | 1999-01-29 | 2000-01-28 | p53阻害剤およびその治療用途 |
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JP2010265321A true JP2010265321A (ja) | 2010-11-25 |
JP2010265321A5 JP2010265321A5 (ja) | 2012-03-22 |
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JP2000595668A Pending JP2002535357A (ja) | 1999-01-29 | 2000-01-28 | p53阻害剤およびその治療用途 |
JP2010185868A Pending JP2010265321A (ja) | 1999-01-29 | 2010-08-23 | p53阻害剤およびその治療用途 |
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US (7) | US6593353B1 (ja) |
EP (1) | EP1143943B1 (ja) |
JP (2) | JP2002535357A (ja) |
AT (1) | ATE380548T1 (ja) |
AU (1) | AU3584200A (ja) |
CA (1) | CA2360671A1 (ja) |
DE (1) | DE60037394T2 (ja) |
IL (3) | IL144294A0 (ja) |
NZ (1) | NZ513487A (ja) |
WO (1) | WO2000044364A2 (ja) |
ZA (1) | ZA200105823B (ja) |
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ513487A (en) * | 1999-01-29 | 2003-02-28 | Univ Illinois | The use of a P53 inhibitor for the treatment of cancer, hyperthermia, hypoxia, a burn, trauma to the central nervous system, a seizure, acute inflammation, tissue ageing, preservation of organs for transplant and preparation of a host for bone marrow transplant |
EP1303502A2 (en) * | 2000-07-06 | 2003-04-23 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Tetrahydrobenzothiazole analogues as neuroprotective agents |
AU2001294515A1 (en) * | 2000-08-11 | 2002-02-25 | The Regents Of The University Of California | Use of stat-6 inhibitors as therapeutic agents |
US6696441B1 (en) | 2000-08-11 | 2004-02-24 | The Regents Of The University Of California | Inhibition of p53-induced stress response |
US6861431B2 (en) | 2001-03-23 | 2005-03-01 | The Board Of Trustees Of The University Of Illinois | Compounds capable of modulating the activity of multidrug transporters and therapeutic use of the same |
US7601846B2 (en) | 2001-06-26 | 2009-10-13 | The Regents Of The University Of California | Compounds having activity as inhibitors of apoptosis |
WO2004089345A1 (en) * | 2003-04-03 | 2004-10-21 | Semafore Pharmaceuticals Inc. | Bone targeting of biodegradable drug-containing nanoparticles |
US20040198783A1 (en) * | 2003-04-03 | 2004-10-07 | Semafore Pharmaceuticals Inc. | Targeted bone marrow protection agents |
US7657893B2 (en) * | 2003-04-23 | 2010-02-02 | International Business Machines Corporation | Accounting method and logic for determining per-thread processor resource utilization in a simultaneous multi-threaded (SMT) processor |
US7132421B2 (en) * | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
CA2536112A1 (en) * | 2003-08-20 | 2005-03-03 | Northern Sydney And Central Coast Area Health Service | Methods for enhancing embryo viability |
JP4991544B2 (ja) | 2004-08-23 | 2012-08-01 | イエダ リサーチ アンド デベロップメント カンパニー リミテッド | ストレス応答を媒介するためのペプチド阻害剤 |
DK1799269T3 (en) * | 2004-09-28 | 2016-10-03 | Quark Pharmaceuticals Inc | Oligoribonucleotides and methods of use thereof for treating alopecia, acute renal failure, and other diseases |
GB2423928B (en) * | 2004-11-16 | 2008-04-09 | Efflux Technology Inc | Methods and compositions for treating pain |
US20070087977A1 (en) * | 2004-11-16 | 2007-04-19 | Wendye Robbins | Methods and compositions for treating pain |
KR100877824B1 (ko) * | 2005-11-11 | 2009-01-12 | 한국생명공학연구원 | E2epf ucp-vhl 상호작용 및 그 용도 |
US9066976B2 (en) | 2005-11-11 | 2015-06-30 | Korea Research Institute Of Bioscience And Biotechnology | Method for therapeutic angiogenesis |
US20070110756A1 (en) * | 2005-11-14 | 2007-05-17 | Reinberg Danny F | Method for modulating P53 activity via methylation |
US7825099B2 (en) * | 2006-01-20 | 2010-11-02 | Quark Pharmaceuticals, Inc. | Treatment or prevention of oto-pathologies by inhibition of pro-apoptotic genes |
US7910566B2 (en) * | 2006-03-09 | 2011-03-22 | Quark Pharmaceuticals Inc. | Prevention and treatment of acute renal failure and other kidney diseases by inhibition of p53 by siRNA |
EP2103619A4 (en) * | 2006-12-14 | 2011-11-23 | Daiichi Sankyo Co Ltd | IMIDAZOTHIAZOLDERIVATE |
FR2910895B1 (fr) * | 2006-12-29 | 2010-08-27 | Biopharmed | "derives d'imino-tetrahydrobenzotriazoles ayant des proprietes anti-migratoires de metastases met dependantes" |
CA2939778C (en) * | 2007-01-31 | 2019-01-29 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
KR101525754B1 (ko) | 2007-03-28 | 2015-06-09 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 스티칭된 폴리펩티드 |
SI2170403T1 (sl) * | 2007-06-27 | 2014-07-31 | Quark Pharmaceuticals, Inc. | Sestavki in postopki za inhibicijo ekspresije pro-apoptotskih genov |
US8530238B2 (en) * | 2008-06-27 | 2013-09-10 | Kyoto University | Method of efficiently establishing induced pluripotent stem cells |
JP2012504645A (ja) * | 2008-10-01 | 2012-02-23 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 健康な細胞に対する電離放射線の影響を低下させる又は防止するための医薬組成物 |
WO2010039997A2 (en) * | 2008-10-01 | 2010-04-08 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors |
US20110288155A1 (en) | 2008-12-18 | 2011-11-24 | Elena Feinstein | Sirna compounds and methods of use thereof |
CA2761896A1 (en) | 2009-05-13 | 2010-11-18 | The University Of North Carolina At Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
AU2010279913B2 (en) | 2009-08-07 | 2016-04-28 | Kyoto University | Method of efficiently establishing induced pluripotent stem cells |
SI2603600T1 (sl) | 2010-08-13 | 2019-04-30 | Aileron Therapeutics, Inc. | Peptidomimetični makrocikli |
US20130230580A1 (en) * | 2010-09-14 | 2013-09-05 | Paul S. Frenette | Administration of SNS Neuroprotective Agents to Promote Hematopoietic Regeneration |
EP2640394A4 (en) | 2010-11-17 | 2015-02-25 | Univ North Carolina | PROTECTION OF RENAL TISSUES AGAINST ISCHEMIA THROUGH INHIBITION OF CDK4 AND CDK6 PROLIFERATIVE KINASES |
EP2715350B1 (en) | 2011-05-23 | 2017-09-27 | Yeda Research and Development Co. Ltd. | Use of akt phosphorylation as a biomarker for prognosing neurodegenerative diseases and treating same |
JP2014525399A (ja) * | 2011-08-09 | 2014-09-29 | ベス・イスラエル・ディーコネス・メディカル・センター,インコーポレイテッド | Dna損傷を処置する方法 |
KR20140100937A (ko) | 2011-10-18 | 2014-08-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
WO2013123267A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
CN104159595A (zh) | 2012-02-15 | 2014-11-19 | 爱勒让治疗公司 | 拟肽大环化合物 |
EP2895608B1 (en) | 2012-09-12 | 2018-12-05 | Quark Pharmaceuticals, Inc. | Double-stranded oligonucleotide molecules to p53 and methods of use thereof |
BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
EP2967050A4 (en) | 2013-03-15 | 2016-09-28 | G1 Therapeutics Inc | HIGH-ACTIVE ANTINEOPLASTIC AND ANTIPROLIFERATIVE AGENTS |
EP2968291A4 (en) | 2013-03-15 | 2016-09-28 | G1 Therapeutics Inc | HSPC-PROOF TREATMENTS FOR RB-POSITIVE ABNORMAL CELLULAR PROLIFERATION |
US10314826B2 (en) | 2014-02-07 | 2019-06-11 | University Of Maryland, Baltimore | Methods of treatment of ischemia-induced angiogenesis and arteriogenesis |
WO2015161288A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use as anti-neoplastic and anti-proliferative agents |
MX2016015635A (es) | 2014-05-29 | 2017-04-25 | Quark Pharmaceuticals Inc | Metodos y composiciones para evitar la lesion por isquemia-reperfusion en organos. |
WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
WO2016049355A1 (en) | 2014-09-24 | 2016-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and formulations thereof |
KR20170058424A (ko) | 2014-09-24 | 2017-05-26 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방 거대고리 및 이의 용도 |
AU2016235424A1 (en) | 2015-03-20 | 2017-10-05 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
EP3347372A4 (en) | 2015-09-10 | 2019-09-04 | Aileron Therapeutics, Inc. | PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF MCL-1 |
WO2017125429A1 (en) | 2016-01-18 | 2017-07-27 | Institut National De La Santé Et De La Recherche Médicale (Inserm) | The use of a temporary inhibitor of p53 for preventing or reducing cancer relapse |
US20180245065A1 (en) | 2016-11-01 | 2018-08-30 | Novartis Ag | Methods and compositions for enhancing gene editing |
WO2020023502A1 (en) | 2018-07-23 | 2020-01-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
WO2020206046A1 (en) | 2019-04-01 | 2020-10-08 | The Broad Institute, Inc. | Methods and compositions for cell therapy |
WO2020247336A1 (en) * | 2019-06-03 | 2020-12-10 | The Regents Of The University Of California | Pifithrin analogues and methods of treating rett syndrome |
JP7429035B2 (ja) | 2019-08-01 | 2024-02-07 | 東京都公立大学法人 | 機能不全ミトコンドリアを消去するための複合体、および細胞老化を抑制するための複合体 |
US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
WO2024052434A1 (en) | 2022-09-06 | 2024-03-14 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Engineering sox/oct heterodimerization to induce high-grade developmental reset |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2463774A1 (fr) * | 1979-08-21 | 1981-02-27 | Yamanouchi Pharma Co Ltd | Derives du 2-phenylimidazo(2,1-b)benzothiazole |
US5324731A (en) * | 1989-02-14 | 1994-06-28 | Amira, Inc. | Method of inhibiting transformation of cells in which purine metabolic enzyme activity is elevated |
CA2028756A1 (en) | 1989-11-24 | 1991-05-25 | Alfons H. M. Raeymaekers | Immunostimulating 6-aryl-5,6-dihydro-imidazo[2,1-b]thiazole derivatives |
US6372249B1 (en) * | 1991-12-16 | 2002-04-16 | Baylor College Of Medicine | Senscent cell-derived inhibitors of DNA synthesis |
JPH07291976A (ja) | 1994-04-27 | 1995-11-07 | Otsuka Pharmaceut Factory Inc | イミダゾ〔2,1−b〕チアゾール誘導体 |
JP3178843B2 (ja) | 1995-03-13 | 2001-06-25 | 日研化学株式会社 | イミダゾチアゾール化合物 |
JP3847366B2 (ja) * | 1996-02-22 | 2006-11-22 | アンジェスMg株式会社 | アンチセンスオリゴヌクレオチドを用いた固定性分裂終了細胞増殖剤 |
US5919808A (en) | 1996-10-23 | 1999-07-06 | Zymogenetics, Inc. | Compositions and methods for treating bone deficit conditions |
AU4988997A (en) | 1996-10-23 | 1998-05-15 | Osteoscreen, Inc. | Compositions and methods for treating bone deficit conditions |
JPH1129475A (ja) | 1997-07-07 | 1999-02-02 | Sumitomo Pharmaceut Co Ltd | Stat6活性化阻害剤 |
JPH11103640A (ja) | 1997-09-29 | 1999-04-20 | Mitsubishi Agricult Mach Co Ltd | ノッタの結節装置 |
JPH11106340A (ja) | 1997-10-02 | 1999-04-20 | Sumitomo Pharmaceut Co Ltd | Stat6活性化阻害剤 |
NZ513487A (en) * | 1999-01-29 | 2003-02-28 | Univ Illinois | The use of a P53 inhibitor for the treatment of cancer, hyperthermia, hypoxia, a burn, trauma to the central nervous system, a seizure, acute inflammation, tissue ageing, preservation of organs for transplant and preparation of a host for bone marrow transplant |
-
2000
- 2000-01-28 NZ NZ513487A patent/NZ513487A/xx unknown
- 2000-01-28 AT AT00914455T patent/ATE380548T1/de not_active IP Right Cessation
- 2000-01-28 IL IL14429400A patent/IL144294A0/xx unknown
- 2000-01-28 JP JP2000595668A patent/JP2002535357A/ja active Pending
- 2000-01-28 CA CA002360671A patent/CA2360671A1/en not_active Abandoned
- 2000-01-28 WO PCT/US2000/002104 patent/WO2000044364A2/en active Application Filing
- 2000-01-28 EP EP00914455A patent/EP1143943B1/en not_active Revoked
- 2000-01-28 AU AU35842/00A patent/AU3584200A/en not_active Abandoned
- 2000-01-28 DE DE60037394T patent/DE60037394T2/de not_active Expired - Lifetime
- 2000-01-28 US US09/493,527 patent/US6593353B1/en not_active Expired - Lifetime
-
2001
- 2001-06-13 US US09/880,417 patent/US7012087B2/en not_active Expired - Lifetime
- 2001-07-12 IL IL144294A patent/IL144294A/en not_active IP Right Cessation
- 2001-07-16 ZA ZA200105823A patent/ZA200105823B/en unknown
- 2001-09-06 US US09/947,757 patent/US20020019425A1/en not_active Abandoned
-
2003
- 2003-01-24 US US10/350,560 patent/US6982277B2/en not_active Expired - Lifetime
- 2003-01-28 US US10/352,597 patent/US7008956B2/en not_active Expired - Lifetime
-
2005
- 2005-05-24 US US11/136,231 patent/US20050222224A1/en not_active Abandoned
-
2008
- 2008-01-30 US US12/022,317 patent/US20080161426A1/en not_active Abandoned
- 2008-12-04 IL IL195723A patent/IL195723A/en not_active IP Right Cessation
-
2010
- 2010-08-23 JP JP2010185868A patent/JP2010265321A/ja active Pending
Non-Patent Citations (3)
Title |
---|
JPN6012068078; Brain Research Vol.797, No.2, 1998, p.295-304 * |
JPN6012068079; 医学のあゆみ 第183巻,第6号, 1997, p.401-405 * |
JPN6012068080; Journal of Cerebral Blood Flow & Metabolism Vol.14, No.6, 1994, p.887-891 * |
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US20020006941A1 (en) | 2002-01-17 |
US6593353B1 (en) | 2003-07-15 |
WO2000044364A2 (en) | 2000-08-03 |
DE60037394T2 (de) | 2009-01-02 |
EP1143943A2 (en) | 2001-10-17 |
JP2002535357A (ja) | 2002-10-22 |
US20050222224A1 (en) | 2005-10-06 |
US20030176318A1 (en) | 2003-09-18 |
ATE380548T1 (de) | 2007-12-15 |
US7012087B2 (en) | 2006-03-14 |
AU3584200A (en) | 2000-08-18 |
NZ513487A (en) | 2003-02-28 |
IL144294A (en) | 2010-04-15 |
US6982277B2 (en) | 2006-01-03 |
CA2360671A1 (en) | 2000-08-03 |
US20080161426A1 (en) | 2008-07-03 |
EP1143943B1 (en) | 2007-12-12 |
EP1143943A3 (en) | 2002-09-11 |
US7008956B2 (en) | 2006-03-07 |
WO2000044364A3 (en) | 2001-08-23 |
IL144294A0 (en) | 2002-05-23 |
US20030144331A1 (en) | 2003-07-31 |
IL195723A (en) | 2010-12-30 |
DE60037394D1 (de) | 2008-01-24 |
ZA200105823B (en) | 2002-05-07 |
US20020019425A1 (en) | 2002-02-14 |
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