JP2000514402A - Vegfに関連する目の病気に関する治療処置 - Google Patents
Vegfに関連する目の病気に関する治療処置Info
- Publication number
- JP2000514402A JP2000514402A JP09539298A JP53929897A JP2000514402A JP 2000514402 A JP2000514402 A JP 2000514402A JP 09539298 A JP09539298 A JP 09539298A JP 53929897 A JP53929897 A JP 53929897A JP 2000514402 A JP2000514402 A JP 2000514402A
- Authority
- JP
- Japan
- Prior art keywords
- vegf
- inhibitor
- retinal
- protein kinase
- isozyme
- 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
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 目の血管障害を治療する方法であって、そのような治療を必要とす る哺乳動物に、治療上有効な量のプロテインキナーゼCのβアイソザイムの阻害 剤を投与することを含む、前記の治療方法。 2. プロテインキナーゼCのβアイソザイムの阻害剤が、ビス−インド リルマレイミドまたは大環状のビス−インドリルマレイミドである、請求項1記 載の方法。 3. 阻害剤がアイソザイム選択的であり、そのアイソザイム選択性が、 β−1およびβ−2アイソザイムからなる群より選択される、請求項1記載の方 法。 4. プロテインキナーゼC阻害剤が、以下の式 (式中、 Wは、−O−、−S−、−SO−、−SO2−、−CO−、C2−C6アルキレ ン、置換アルキレン、C2−C6アルケニレン、−アリール−、−アリール(CH2 )mO−、−複素環−、−複素環−(CH2)mO−、−縮合二環式−、−縮合二 環式−(CH2)mO−、−NR3−、−NOR3−、−CONH−、または−NH CO−であり; XおよびYは、独立的に、C1−C4アルキレン、置換アルキレンであるか、ま たは、X、YおよびWは、共に合わさって、−(CH2)n−AA−を形成し; R1は、水素であるか、またはハロ、C1−C4アルキル、ヒドロキシ、C1−C4 アルコキシ、ハロアルキル、ニトロ、NR4R5あるいはNHCO(C1−C4ア ル キル)から独立的に選択された最大で4種類の所望の置換基であり; R2は、水素、CH3CO−、NH2またはヒドロキシであり; R3は、水素、(CH2)mアリール、C1−C4アルキル、−COO(C1−C4 アルキル)、−CONR4R5、−(C=NH)NH2、−SO(C1−C4アルキ ル)、−SO2(NR4R5)、または−SO2(C1−C4)アルキルであり; R4およびR5は、独立的に、水素、C1−C4アルキル、フェニル、ベンジルで あるか、または窒素と結合して飽和または不飽和の5または6員環を形成し; AAは、アミノ酸残基であり、 mは、独立的に、0、1、2または3であり;そして、 nは、独立的に、2、3、4または5である) を持つ、または、その薬剤的に許容しうる塩、プロドラッグあるいはエステルで ある、請求項3記載の方法。 5. プロテインキナーゼC阻害剤が、以下の式 (式中、Zは、−(CH2)p−または−(CH3)p−O−(CH2)p−であり; R4は、ヒドロキシ、−SH、C1−C4アルキル、(CH2)mアリール、−N H(アリール)、−N(CH3)(CF3)、−NH(CF3)または−NR5R6 であり;R5は、水素またはC1−C4アルキルであり;R6は、水素、C1−C4ア ルキルまたはベンジルであり;pは、0、1または2であり;そして、nは、独 立的に2または3である) を持つ、または、その薬剤的に許容しうる塩、プロドラッグあるいはエステルで ある、請求項4記載の方法。 6. プロテインキナーゼC阻害剤が、以下の式 (式中、Zは−(CH2)p−であり;R4は、−NR5R6、−NH(CF3)また は−N(CH3)(CF3)であり;R5およびR6は独立的にHまたはC1−C4ア ルキルであり;pは、0、1または2であり;そして、mは、独立的に2または 3である) を持つ、またはその薬剤的に許容しうる塩、プロドラッグあるいはエステルであ る、請求項4記載の方法。 7, プロテインキナーゼC阻害剤が、(S)−3,4−[N,N’−1 ,1’−{(2”−エトキシ)−3'''(O)−4'''−(N,N−ジメチルアミ ノ)−ブタン}−ビス−(3,3’−インドリル)]−1(H)−ピロール−2 ,5−ジオンまたはその薬剤的に許容しうる酸塩を含む、請求項4記載の方法。 8. 目の血管障害が、黄斑変性、黄斑浮腫、血管網膜障害、虹彩の新生 血管形成、網膜静脈閉塞、ヒストプラスマ症および虚血性網膜疾病からなる群よ り選択される、請求項1記載の方法。 9. 目の血管障害が、黄斑変性、黄斑浮腫および網膜静脈閉塞からなる 群より選択される、請求項1記載の方法。 10. 該血管網膜障害が未熟による網膜障害である、請求項8記載の方法 。 11. VEGFによって刺激される内皮細胞の増殖を阻害する方法であっ て、そのような治療を必要とする哺乳動物に、治療上有効な量のプロテインキナ ーゼCのβアイソザイムの阻害剤を投与することを含む、前記の阻害方法。 12. 浮腫と関連する毛細血管透過性を刺激するVEGFを阻害する方法 であって、そのような治療を必要とする哺乳動物に、治療上有効な量のプロテイ ンキナーゼCのβアイソザイムの阻害剤を投与することを含む、上記の阻害方法 。
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Application Number | Priority Date | Filing Date | Title |
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US1665896P | 1996-05-01 | 1996-05-01 | |
US60/016,658 | 1996-05-01 | ||
US08/841,739 | 1997-04-30 | ||
US08/841,739 US6114320A (en) | 1996-05-01 | 1997-04-30 | Therapeutic treatment for VEGF related ocular diseases |
PCT/US1997/007800 WO1997040831A1 (en) | 1996-05-01 | 1997-05-01 | Therapeutic treatment for vegf related occular diseases |
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JP2000514402A true JP2000514402A (ja) | 2000-10-31 |
JP2000514402A5 JP2000514402A5 (ja) | 2006-03-23 |
JP4122060B2 JP4122060B2 (ja) | 2008-07-23 |
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JP53929897A Expired - Fee Related JP4122060B2 (ja) | 1996-05-01 | 1997-05-01 | Vegfに関連する目の病気に関する治療処置 |
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US (1) | US6114320A (ja) |
EP (1) | EP0918519B1 (ja) |
JP (1) | JP4122060B2 (ja) |
KR (1) | KR100364487B1 (ja) |
CN (1) | CN1158073C (ja) |
AT (1) | ATE270548T1 (ja) |
AU (1) | AU724923B2 (ja) |
BR (1) | BR9710705A (ja) |
CA (1) | CA2253613C (ja) |
CZ (1) | CZ296711B6 (ja) |
DE (1) | DE69729798T2 (ja) |
EA (1) | EA001752B1 (ja) |
ES (1) | ES2224249T3 (ja) |
HK (1) | HK1020017A1 (ja) |
HU (1) | HU226378B1 (ja) |
IL (1) | IL126836A (ja) |
NO (1) | NO322209B1 (ja) |
NZ (2) | NZ538109A (ja) |
PL (1) | PL189020B1 (ja) |
PT (1) | PT918519E (ja) |
UA (1) | UA54427C2 (ja) |
WO (1) | WO1997040831A1 (ja) |
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US5723456A (en) * | 1993-12-07 | 1998-03-03 | Eli Lilly & Company | Therapeutic treatment for cardiovascular diseases |
US6093740A (en) * | 1997-04-30 | 2000-07-25 | Eli Lilly And Company | Therapeutic treatment for skin disorders |
WO2000009098A2 (en) * | 1998-08-13 | 2000-02-24 | Novartis Ag | Method for treating ocular neovascular diseases |
JP2002530342A (ja) * | 1998-11-23 | 2002-09-17 | ノバルティス アクチエンゲゼルシャフト | 眼血管新生疾患の処置のためのスタウロスポリン誘導体の使用 |
US6214819B1 (en) | 1998-11-23 | 2001-04-10 | Novartis Ag | Method for treating ocular neovascular diseases |
JP4731016B2 (ja) | 1998-12-22 | 2011-07-20 | ジェネンテック, インコーポレイテッド | 血管内皮細胞増殖因子アンタゴニストとその用途 |
US6271233B1 (en) | 1999-08-10 | 2001-08-07 | Ciba Vision Corporation | Method for treating ocular neovascular diseases |
US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
AU2001236698A1 (en) | 2000-02-07 | 2001-08-14 | Abbott Gesellschaft Mit Beschrankter Haftung & Company Kommanditgesellschaft | 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors |
MXPA03008560A (es) | 2001-03-22 | 2004-06-30 | Abbot Gmbh & Co Kg | Pirazolopirimidinas como agentes terapeuticos. |
US20020165158A1 (en) * | 2001-03-27 | 2002-11-07 | King George L. | Methods of modulating angiogenesis |
US20030119812A1 (en) * | 2001-11-08 | 2003-06-26 | Brazzell Romulus Kimbro | Method for decreasing capillary permeability in the retina |
US20030236246A1 (en) * | 2002-04-30 | 2003-12-25 | Brazzell Romulus Kimbro | Method for decreasing capillary permeability in the retina |
JP2005536516A (ja) * | 2002-07-23 | 2005-12-02 | ノバルティス アクチエンゲゼルシャフト | 薬剤、軟膏基剤および可溶化剤/分散剤を含む、眼科用軟膏組成物 |
US20040258769A1 (en) * | 2003-06-20 | 2004-12-23 | Barker Ronnie C. | Use of ocular vitamins in conjunction with other treatment methods for AMD |
AU2005221283C1 (en) * | 2004-03-17 | 2011-02-03 | Lars Michael Larsen | Prevention of retinopathy by inhibition of the visual cycle |
SG163576A1 (en) | 2004-04-02 | 2010-08-30 | Osi Pharm Inc | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
AR053090A1 (es) | 2004-07-20 | 2007-04-25 | Osi Pharm Inc | Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos |
AR057960A1 (es) | 2005-12-02 | 2007-12-26 | Osi Pharm Inc | Inhibidores de proteina quinasa biciclicos |
US7455447B2 (en) * | 2006-05-19 | 2008-11-25 | Mediatek Inc. | Method and apparatus for a portable device |
WO2008024734A2 (en) * | 2006-08-23 | 2008-02-28 | Novartis Ag | Use of pkc inhibitors in particular indolylmaleimide derivatives in ocular diseases |
WO2008042399A2 (en) * | 2006-10-03 | 2008-04-10 | The Trustees Of The University Of Pennsylvania | Method for treatment of macular degeneration |
WO2016153877A1 (en) | 2015-03-26 | 2016-09-29 | Eyekor, Llc | Image analysis |
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SK278989B6 (sk) * | 1988-02-10 | 1998-05-06 | F. Hoffmann-La Roche Ag | Substituované pyroly, ich použitie na výrobu lieči |
US5624949A (en) * | 1993-12-07 | 1997-04-29 | Eli Lilly And Company | Protein kinase C inhibitors |
HU219709B (hu) * | 1993-12-07 | 2001-06-28 | Eli Lilly And Co. | Proteinkináz C gátló hatású kondenzált indolszármazékok, eljárás előállításukra, és az ezeket tartalmazó gyógyászati készítmények |
DK0657411T3 (da) * | 1993-12-07 | 1999-11-15 | Lilly Co Eli | Forbedret syntese af bisindolylmaleimider |
US5545636A (en) * | 1993-12-23 | 1996-08-13 | Eli Lilly And Company | Protein kinase C inhibitors |
US5491242A (en) * | 1994-06-22 | 1996-02-13 | Eli Lilly And Company | Protein kinase C inhibitors |
US5481003A (en) * | 1994-06-22 | 1996-01-02 | Eli Lilly And Company | Protein kinase C inhibitors |
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