JPH10508291A - 化合物、製剤用組成物及びこれらを含む診断装置とこれらの利用 - Google Patents
化合物、製剤用組成物及びこれらを含む診断装置とこれらの利用Info
- Publication number
- JPH10508291A JPH10508291A JP8507662A JP50766296A JPH10508291A JP H10508291 A JPH10508291 A JP H10508291A JP 8507662 A JP8507662 A JP 8507662A JP 50766296 A JP50766296 A JP 50766296A JP H10508291 A JPH10508291 A JP H10508291A
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- Prior art keywords
- leu
- ala
- dnr
- cells
- compound
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- Granted
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.細胞内活性部位(A.S.)を有し、末端基(W)と結合するアーム(Z )を含むリガンド(W−Z)と結合する成分(M)から成る化合物(W−Z−M )において、リガンド(W−Z)のアーム(Z)と成分(M)との間の結合が化 合物(W−Z−M)の細胞内進入を妨げ及び/またはマーカ(M)の発現を抑止 し、ターゲット細胞から分泌される因子によって前記結合を選択的に開裂するこ とにより、マーカ(M)の発現または前記ターゲット細胞への治療剤(M)の進 入を可能にすることができ、末端基(W)が血清及び循環血液中での化合物(W −Z−M)の安定性を可能にすることを特徴とする前記化合物(W−Z−M)。 2.末端基(W)を哺乳類には存在しないアミノ酸またはサクシニル基から成 るグループから選択したことを特徴とする請求の範囲第1項に記載の化合物。 3.末端基(W)が式: NH2−CH2−CH2−COOH で表わされるβ−アラニンであることを特徴とする請求の範囲第2項に記載の化 合物。 4.成分(M)とリカンド(W−Z)のアーム(Z)との間の結合がペプチド 結合であることを特徴とする請求の範囲第1項から第3項までのいずれか1項に 記載の化合物。 5.リガンド(W−Z)のアームが少なくとも2つの随意に置換されるアミノ 酸から成ることを特徴とする請求の範囲第1項から第4項までのいずれか1項に 記載の化合物。 6.リガンド(W−Z)のアーム(Z)を次のようなペプチド配列:L−ロイ シル−L−アラニル−L−ロイシル−,L− ロイシル−L−アラニル−,L−アラニル−L−ロイシル−L−フェニルアラニ ル−,L−アラニル−L−ロイシル−から成るグループから選択したことを特徴 とする請求の範囲第5項に記載の化合物。 7.治療剤が抗腫瘍性治療剤であり、ターゲット細胞が腫瘍細胞であることを 特徴とする請求の範囲第1項から第6項までのいずれか1項に記載の化合物。 8.治療剤が抗炎症薬であり、ターゲット細胞がマクロファージまたは単球で あることを特徴とする請求の範囲第1項から第6項までのいずれか1項に記載の 化合物。 9.治療剤(M)をアントラサイクリン,葉酸誘導体,ビンカアルカロイド, カリケアマイシン,ミトザントロン,シトシンアラビノシド(ARA−C)また はアデノシンアラビノシド(ARA−A),リン酸フルダラビン,メルファラン ,ブレオマイシン,ミトマイシン,L−カナバニン,トキソイド,カンプトテシ ン及びこれらの誘導体,特にTOPOTECAN(商品名,9−ジメチルアミノ メチル−10−ヒドロキシカンプトテシンヒドロクロリド),及びフルオロクロ ム誘導体,特にローダミン123,及び随意に置換または非置換アミノ酸と結合 しているそれらの誘導体から選択したことを特徴とする請求の範囲第1項から第 8項までのいずれか1項に記載の化合物。 10.治療剤(M)が随意に置換または非置換アミノ酸と結合しているドキソ ルビシンまたはダウノルビシンであることを特徴とする請求の範囲第9項に記載 の化合物。 11.治療剤が次の一般式に対応することを特徴とする請求の範囲第10項に 記載の化合物: 式の中で、 −R1は水素原子またはOH基、 −R2は水素原子または次式のラジカル: 式の中で、 −R3は水素原子または随意に置換されているアルキルラジカル、 −R4は水素原子またはR3と共に3または4個の炭素原子を有するアルキ レンラジカル、である。 12.R2が次式で表わされるラジカルまたはその同位体の1つであることを 特徴とする請求の範囲第11項に記載の化合物: 13.請求の範囲第1項から第12項までのいずれか1項に記載の化合物のほ かに製剤上許容できる補薬または賦形剤をも適宜含む製剤用組成物。 14.癌性腫瘍の治療薬の製造を目的とする請求の範囲第13項に記載の製剤 用組成物の利用。 15.請求の範囲第13項に記載の組成物を患者に投与することから成ること を特徴とする癌性腫瘍の治療方法。 16.炎症反応、好ましくはリウマチ疾患治療薬の製造を目的とする請求の範 囲第13項に記載の製剤用組成物の利用。 17.炎症反応、特にリウマチ疾患の治療方法において、請求の範囲第13項 に記載の組成物を患者に投与することから成ることを特徴とする前記治療方法。 18.マーカをクマリン、7−アミド−4−(トリフルオロメチル)クマリン 、パラ−ニトロアニリド、β−リフチルアミド及び4−メトキシ−β−ナフチル アミドから成るグループから選択したことを特徴とする請求の範囲第1項から第 6項までのいずれか1項に記載の化合物。 19.請求の範囲第1項から第6項までのいずれか1項また は請求の範囲第18項に記載の化合物を含む診断及び/または検査装置。
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BE9400751 | 1994-08-19 | ||
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BE9400751A BE1008580A3 (fr) | 1994-08-19 | 1994-08-19 | Prodrogues, composition pharmaceutiques les comprenant et leur utilisation. |
BE9400752A BE1008581A3 (fr) | 1994-08-19 | 1994-08-19 | Prodrogues, composition pharmaceutique les comprenant et leur utilisation. |
PCT/BE1995/000076 WO1996005863A1 (fr) | 1994-08-19 | 1995-08-21 | Composes, composition pharmaceutique et dispositif de diagnostic les comprenant et leur utilisation |
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JP2007301893A Pending JP2008069175A (ja) | 1994-08-19 | 2007-11-21 | 化合物、製剤用組成物及びこれらを含む診断装置とこれらの利用 |
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-
1995
- 1995-08-21 US US08/793,910 patent/US5962216A/en not_active Expired - Lifetime
- 1995-08-21 AU AU32486/95A patent/AU694546C/en not_active Expired
- 1995-08-21 WO PCT/BE1995/000076 patent/WO1996005863A1/fr active IP Right Grant
- 1995-08-21 DK DK95928905T patent/DK0769967T3/da active
- 1995-08-21 ES ES95928905T patent/ES2297832T3/es not_active Expired - Lifetime
- 1995-08-21 EP EP07119790A patent/EP1880737A1/fr not_active Withdrawn
- 1995-08-21 PT PT95928905T patent/PT769967E/pt unknown
- 1995-08-21 EP EP95928905A patent/EP0769967B1/fr not_active Expired - Lifetime
- 1995-08-21 CA CA2203622A patent/CA2203622C/en not_active Expired - Lifetime
- 1995-08-21 DE DE69535665T patent/DE69535665T2/de not_active Expired - Lifetime
- 1995-08-21 AT AT95928905T patent/ATE380559T1/de active
- 1995-08-21 NZ NZ291368A patent/NZ291368A/en not_active IP Right Cessation
- 1995-08-21 SI SI9530732T patent/SI0769967T1/sl unknown
- 1995-08-21 JP JP50766296A patent/JP4157600B2/ja not_active Expired - Lifetime
-
1997
- 1997-02-18 NO NO19970748A patent/NO324045B1/no not_active IP Right Cessation
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1999
- 1999-04-23 US US09/298,330 patent/US6342480B1/en not_active Expired - Lifetime
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2001
- 2001-11-09 US US10/012,576 patent/US7037898B2/en not_active Expired - Fee Related
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2006
- 2006-03-08 US US11/370,290 patent/US7390629B2/en not_active Expired - Fee Related
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2007
- 2007-11-21 JP JP2007301893A patent/JP2008069175A/ja active Pending
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2008
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2003518000A (ja) * | 1998-12-11 | 2003-06-03 | コールター ファーマシューティカル,インコーポレイティド | プロドラッグ化合物およびその調製方法 |
JP2010189419A (ja) * | 2000-11-14 | 2010-09-02 | Shire Llc | 硫酸アバカビルを含有する新規な薬剤化合物および同化合物の製造ならびに使用方法 |
JP2013532132A (ja) * | 2010-05-20 | 2013-08-15 | セントレ・ナショナル・デ・ラ・レシェルシェ・サイエンティフィーク | 新規な自己反応性アーム及び同物を含むプロドラッグ |
Also Published As
Publication number | Publication date |
---|---|
EP0769967B1 (fr) | 2007-12-12 |
EP0769967A1 (fr) | 1997-05-02 |
US20060148682A1 (en) | 2006-07-06 |
JP2008069175A (ja) | 2008-03-27 |
CA2203622C (en) | 2011-11-01 |
NO970748D0 (no) | 1997-02-18 |
JP4157600B2 (ja) | 2008-10-01 |
AU694546B2 (en) | 1998-07-23 |
NO324045B1 (no) | 2007-08-06 |
ATE380559T1 (de) | 2007-12-15 |
US6342480B1 (en) | 2002-01-29 |
US7037898B2 (en) | 2006-05-02 |
NZ291368A (en) | 1999-04-29 |
US20020160943A1 (en) | 2002-10-31 |
AU694546C (en) | 2001-09-06 |
MX9701283A (es) | 1997-09-30 |
PT769967E (pt) | 2008-02-18 |
DK0769967T3 (da) | 2008-03-31 |
ES2297832T3 (es) | 2008-05-01 |
US5962216A (en) | 1999-10-05 |
SI0769967T1 (sl) | 2008-06-30 |
DE69535665D1 (de) | 2008-01-24 |
US7951772B2 (en) | 2011-05-31 |
DE69535665T2 (de) | 2009-04-02 |
NO970748L (no) | 1997-04-10 |
US7390629B2 (en) | 2008-06-24 |
WO1996005863A1 (fr) | 1996-02-29 |
AU3248695A (en) | 1996-03-14 |
CA2203622A1 (en) | 1996-02-29 |
US20090137494A1 (en) | 2009-05-28 |
EP1880737A1 (fr) | 2008-01-23 |
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