JP2004512328A5 - - Google Patents

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JP2004512328A5
JP2004512328A5 JP2002537718A JP2002537718A JP2004512328A5 JP 2004512328 A5 JP2004512328 A5 JP 2004512328A5 JP 2002537718 A JP2002537718 A JP 2002537718A JP 2002537718 A JP2002537718 A JP 2002537718A JP 2004512328 A5 JP2004512328 A5 JP 2004512328A5
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Japan
Prior art keywords
salt
methylpiperazin
ylamino
pyrimidin
ylmethyl
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JP2002537718A
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JP4386635B2 (ja
JP2004512328A (ja
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Priority claimed from PCT/EP2001/012442 external-priority patent/WO2002034727A2/en
Publication of JP2004512328A publication Critical patent/JP2004512328A/ja
Publication of JP2004512328A5 publication Critical patent/JP2004512328A5/ja
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【特許請求の範囲】
【請求項1】
消化管間質腫瘍の処置のための、活性成分として式I
【化1】
Figure 2004512328
で示される4−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドまたは薬学的に許容されるその塩を含む医薬。
【請求項2】
−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される塩が酸付加塩である、請求項1に記載の医薬。
【請求項3】
−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される酸付加塩がモノメタンスルホン酸塩である、請求項2に記載の医薬。
【請求項4】
4−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドのモノメタンスルホン酸塩がβ結晶形である、請求項3に記載の医薬。
【請求項5】
1日当たりの服用量が4−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミド遊離塩基の200〜600mgに相当する、請求項1〜4のいずれかに記載の医薬。
【請求項6】
服用が3ヶ月以上にわたる、請求項5に記載の医薬。
驚くべきことに、今回、GISTが「化合物I」または薬学的に許容されるその塩で成功裡に処置され得ることが証明された
「化合物I」のモノメタンスルホン酸付加塩(以後、「塩I」と呼ぶ。)およびその好ましい結晶形は、1999年1月28日に公開された国際公開第99/03854号に記載されている。

Claims (3)

  1. 消化管間質腫瘍の処置のための、活性成分として式I
    Figure 2004512328
    で示される4−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドまたは薬学的に許容されるその塩を含む医薬組成物。
  2. 式Iの4−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される塩が酸付加塩である、請求項1に記載の医薬組成物。
  3. 式Iの4−(4−メチルピペラジン−1−イルメチル)−N−[4−メチル−3−(4−ピリジン−3−イル)ピリミジン−2−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される酸付加塩がそのモノメタンスルホン酸塩である、請求項2に記載の医薬組成物。
JP2002537718A 2000-10-27 2001-10-26 消化管間質腫瘍の処置 Expired - Lifetime JP4386635B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24381000P 2000-10-27 2000-10-27
PCT/EP2001/012442 WO2002034727A2 (en) 2000-10-27 2001-10-26 Treatment of gastrointestinal stromal tumors

Publications (3)

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JP2004512328A JP2004512328A (ja) 2004-04-22
JP2004512328A5 true JP2004512328A5 (ja) 2009-02-19
JP4386635B2 JP4386635B2 (ja) 2009-12-16

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US (1) US6958335B2 (ja)
EP (1) EP1332137B1 (ja)
JP (1) JP4386635B2 (ja)
KR (1) KR100885129B1 (ja)
CN (1) CN1276754C (ja)
AT (1) ATE321556T1 (ja)
AU (2) AU1826202A (ja)
BR (1) BRPI0114870B8 (ja)
CA (1) CA2424470C (ja)
CY (1) CY1105055T1 (ja)
CZ (1) CZ303944B6 (ja)
DE (1) DE60118430T2 (ja)
DK (1) DK1332137T3 (ja)
ES (1) ES2260317T3 (ja)
HK (1) HK1058193A1 (ja)
HU (1) HU229106B1 (ja)
IL (2) IL155029A0 (ja)
MX (1) MXPA03003703A (ja)
NO (1) NO324948B1 (ja)
NZ (1) NZ525254A (ja)
PL (1) PL209733B1 (ja)
PT (1) PT1332137E (ja)
RU (1) RU2301066C2 (ja)
SK (1) SK287335B6 (ja)
WO (1) WO2002034727A2 (ja)
ZA (1) ZA200302155B (ja)

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