JP2009298808A - Rhoキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 - Google Patents
Rhoキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 Download PDFInfo
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- 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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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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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
Abstract
【解決手段】
Rhoキナーゼ阻害剤(ただし(R)−(+)−N−(1H−ピロロ[2,3−b]ピリジン−4−イル)−4−(1−アミノエチル)ベンズアミドを除く)とプロスタグランジン類(ただしラタノプロストを除く)とを組み合わせることで、眼圧下降作用をお互いに補完および/または増強する。投与の形態としては、併用投与しても、合剤として投与してもよい。
【選択図】なし
Description
本発明におけるRhoキナーゼ阻害剤((R)−(+)−N−(1H−ピロロ[2,3−b]ピリジン−4−イル)−4−(1−アミノエチル)ベンズアミド二塩酸塩)とプロスタグランジン類(イソプロピルウノプロストン)とを配合した点眼剤の一般的な製剤例を以下に示す。
(R)−(+)−N−(1H−ピロロ[2,3−b]ピリジン−4−イル)−4−(1−アミノエチル)ベンズアミド二塩酸塩 0.3g
イソプロピルウノプロストン 0.06g
ホウ酸 0.2g
濃グリセリン 0.25g
塩化ベンザルコニウム 0.005g
希塩酸 適量
水酸化ナトリウム 適量
精製水 適量
上記処方において、Rhoキナーゼ阻害剤およびプロスタグランジン類の種類および量を変えて、また、添加剤の量を適宜変化させることで、所望の組み合わせおよび所望の濃度の点眼液を調製することができる。
Rhoキナーゼ阻害剤とプロスタグランジン類との組み合わせによる有用性を調べるため、日本白色ウサギ(系統:JW,性別:雄性)またはカニクイザル(性別:雄性)にRhoキナーゼ阻害剤とプロスタグランジン類を併用投与した時の眼圧下降効果を検討した。Rhoキナーゼ阻害剤としては(R)−(+)−N−(1H−ピロロ[2,3−b]ピリジン−4−イル)−4−(1−アミノエチル)ベンズアミド二塩酸塩[化合物A]または1−(5−イソキノリンスルホニル)ホモピペラジン二塩酸塩[化合物B]を、プロスタグランジン類としてはイソプロピルウノプロストンまたはラタノプロストを使用した。
1.Rhoキナーゼ阻害剤溶液の調製
Rhoキナーゼ阻害剤を生理食塩水に溶解した後、水酸化ナトリウムを加えて溶液を中和し(pH6.0〜7.0)、所望の濃度のRhoキナーゼ阻害剤溶液を調製した。
市販のイソプロピルウノプロストン点眼液(商品名:レスキュラ点眼液)またはラタノプロスト点眼液(商品名:キサラタン点眼液)をそのまま、または、生理食塩水で希釈して、所望の濃度のプロスタグランジン類溶液を調製した。
Rhoキナーゼ阻害剤とプロスタグランジン類とを併用投与した時の眼圧下降効果を検討した。比較対照として、Rhoキナーゼ阻害剤単独投与またはプロスタグランジン類単独投与した時の眼圧下降効果についても検討した。コントロールには基剤(生理食塩水)のみを投与した。また、実験動物として、日本白色ウサギ(系統:JW、性別:雄性)またはカニクイザル(性別:雄性)を使用した。
1.Rhoキナーゼ阻害剤とプロスタグランジン類との併用投与
1)0.4%塩酸オキシブプロカイン点眼液を実験動物の両眼に一滴点眼し局所麻酔をした。
プロスタグランジン類溶液を生理食塩水に代えて、他は上記併用投与試験と同じ方法で試験をした。
Rhoキナーゼ阻害剤溶液を生理食塩水に代えて、他は上記併用投与試験と同じ方法で試験をした。
Rhoキナーゼ阻害剤溶液およびプロスタグランジン類溶液を生理食塩水に代えて、他は上記併用投与試験と同じ方法で試験をした。
各試験において用いるRhoキナーゼ阻害剤溶液、プロスタグランジン類溶液および実験動物を表1に示す。なお、試験1、2および4は本発明に対応する実施例である。試験3は本発明に対応しない参考例である。上述した(試験方法)および(投与方法および測定方法)に従って、試験1〜4を実施した。
試験1の結果を図1に、試験2の結果を図2、試験3の結果を図3、試験4の結果を図4に示す。眼圧は初期眼圧からの変化値を示す。
Claims (4)
- Rhoキナーゼ阻害剤(ただし(R)−(+)−N−(1H−ピロロ[2,3−b]ピリジン−4−イル)−4−(1−アミノエチル)ベンズアミドを除く)とプロスタグランジン類(ただしラタノプロストを除く)との組み合わせからなる緑内障治療剤。
- Rhoキナーゼ阻害剤(ただし(R)−(+)−N−(1H−ピロロ[2,3−b]ピリジン−4−イル)−4−(1−アミノエチル)ベンズアミドを除く)とプロスタグランジン類(ただしラタノプロストを除く)との組み合わせからなり、お互いにその作用を補完および/または増強することを特徴とする緑内障治療剤。
- Rhoキナーゼ阻害剤が(R)−トランス−N−(ピリジン−4−イル)−4−(1−アミノエチル)シクロヘキサンカルボキサミド、1−(5−イソキノリンスルホニル)ホモピペラジン若しくは1−(5−イソキノリンスルホニル)−2−メチルピペラジンである請求項1または請求項2記載の緑内障治療剤。
- プロスタグランジン類がイソプロピルウノプロストン、トラボプロスト若しくはビマトプロストである請求項1または請求項2記載の緑内障治療剤。
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JP2009220230A JP5174777B2 (ja) | 2002-08-29 | 2009-09-25 | Rhoキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 |
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JP2002250223 | 2002-08-29 | ||
JP2002250223 | 2002-08-29 | ||
JP2009220230A JP5174777B2 (ja) | 2002-08-29 | 2009-09-25 | Rhoキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 |
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JP2003305583A Division JP4482726B2 (ja) | 2002-08-29 | 2003-08-29 | Rhoキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 |
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JP2009298808A true JP2009298808A (ja) | 2009-12-24 |
JP5174777B2 JP5174777B2 (ja) | 2013-04-03 |
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JP2009220230A Expired - Fee Related JP5174777B2 (ja) | 2002-08-29 | 2009-09-25 | Rhoキナーゼ阻害剤とプロスタグランジン類からなる緑内障治療剤 |
Country Status (11)
Country | Link |
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US (4) | US20050245509A1 (ja) |
EP (2) | EP1541151B1 (ja) |
JP (1) | JP5174777B2 (ja) |
KR (2) | KR101092048B1 (ja) |
CN (1) | CN100425241C (ja) |
AT (1) | ATE546143T1 (ja) |
AU (1) | AU2003257588A1 (ja) |
CA (1) | CA2496797C (ja) |
ES (1) | ES2382733T3 (ja) |
TW (2) | TWI350170B (ja) |
WO (1) | WO2004019951A1 (ja) |
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Cited By (1)
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EP3461484B1 (en) | 2013-03-15 | 2020-11-18 | Aerie Pharmaceuticals, Inc. | Dimesylate salts of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl, their combinations with prostaglandins and the use thereof in the treatment of ocular disorders |
Also Published As
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KR20110004920A (ko) | 2011-01-14 |
KR101092048B1 (ko) | 2011-12-12 |
US20100041671A1 (en) | 2010-02-18 |
US20120040994A1 (en) | 2012-02-16 |
EP1541151A4 (en) | 2007-07-18 |
CN100425241C (zh) | 2008-10-15 |
WO2004019951A1 (ja) | 2004-03-11 |
CA2496797C (en) | 2012-01-10 |
US20100063060A1 (en) | 2010-03-11 |
EP1541151A1 (en) | 2005-06-15 |
CA2496797A1 (en) | 2004-03-11 |
TWI337881B (en) | 2011-03-01 |
EP2314299A1 (en) | 2011-04-27 |
KR101160780B1 (ko) | 2012-06-27 |
JP5174777B2 (ja) | 2013-04-03 |
TW201032807A (en) | 2010-09-16 |
CN1684689A (zh) | 2005-10-19 |
US20050245509A1 (en) | 2005-11-03 |
ATE546143T1 (de) | 2012-03-15 |
TW200409654A (en) | 2004-06-16 |
TWI350170B (en) | 2011-10-11 |
ES2382733T3 (es) | 2012-06-13 |
KR20050057014A (ko) | 2005-06-16 |
EP1541151B1 (en) | 2012-02-22 |
AU2003257588A1 (en) | 2004-03-19 |
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