JPH11507355A - タンパク質チロシンキナーゼher−2の自己リン酸化能を選択的に阻害するアリール及びヘテロアリールキナゾリン化合物 - Google Patents
タンパク質チロシンキナーゼher−2の自己リン酸化能を選択的に阻害するアリール及びヘテロアリールキナゾリン化合物Info
- Publication number
- JPH11507355A JPH11507355A JP9501889A JP50188997A JPH11507355A JP H11507355 A JPH11507355 A JP H11507355A JP 9501889 A JP9501889 A JP 9501889A JP 50188997 A JP50188997 A JP 50188997A JP H11507355 A JPH11507355 A JP H11507355A
- Authority
- JP
- Japan
- Prior art keywords
- dimethoxyquinazoline
- pharmaceutically acceptable
- substituted
- hydrogen
- unsubstituted
- 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.)
- Ceased
Links
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- C07C43/205—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring the aromatic ring being a non-condensed ring
- C07C43/2055—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring the aromatic ring being a non-condensed ring containing more than one ether bond
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.ヒト上皮増殖因子受容体2型(HER2)の活性によって特徴付けられる細 胞の増殖及び分化の選択的治療法であって、 以下に示す式: (式中、Aは、炭素数が約5〜約12の、置換又は未置換の、単環式又は二環 式、アリール、ヘテロアリール、シクロアルキル又はヘテロシクロアルキル環系 であり、置換基はRによって表わされ、環系のあらゆる適当な部位に存在してい てもよく、Xは結合、O、S、SO、SO2、OCH2、CR4=CR4、C≡C、 NR4又はNR4CH2であり、Rは独立して、水素、アルキル、フェニル、ハロ フェニル、アラルキル、ヒドロキシ、アルコキシ、アリールオキシ、アシルオキ シ、ハロ、ハロアルキル、アミノ、モノ−及びジ−アルキルアミノ、アシルアミ ノ、カルボキシ、アミド、モノ−及びジ−アルキルアミド、アルキルチオ、アル キルスルフィニル並びにアルキルスルホニルであり、R4は水素、アルキル又は アラルキルであり、R5、R6、R7及びR8は独立して水素、アルコキシ又はアラ ルコキシである)、 で示される化合物又はその薬学的に許容しうる塩の、HER2受容体阻害に効 果的な量を、該治療の必要のある患者に投与することを特徴とする方法。 2.Aが、フェニル、ピロリル、チエニル、フリル、チアゾリル、イミダゾリル 、ピラゾリル、ピリジル、ピラジニル、ピリミジニル、ピリダジニル、イソチア ゾリル、イソオキサゾリル及びオキサゾリルから選ばれる、置換又は未置換の、 単環式アリール環又はヘテロアリール環である、請求の範囲第1項記載の方法。 3.Aが、ナフチル、テトラリニル、1,2,3,4−テトラヒドロキノリニル 、 ベンゾフリル、ベンゾチエニル、インダニル、インドリル、インドリニル、1, 3−ベンゾジオキソリル、ベンゾジオキサニル、キノリニル、テトラヒドロキノ リニル、イソキノリニル、キナゾリニル及びキノキサリニルから選ばれる、置換 又は未置換の、二環式アリール又はヘテロアリール環である、請求の範囲第1項 記載の方法。 4.Aが、シクロペンチル、シクロヘキシル、シクロヘプチル、デカリニル、ピ ペリジニル、ピペラジニル、モルホリニル又はデカヒドロキノリルから選ばれる 、置換又は未置換の、単環式のシクロアルキル又はヘテロシクロアルキル環であ る、請求の範囲第1項記載の方法。 5.Aが、デカリニル又はデカヒドロキノリニルから選ばれる、置換又は未置換 の、二環式のシクロアルキル又はヘテロシクロアルキル環である、請求の範囲第 1項記載の方法。 6.Aが、置換又は未置換の、フェニル、ピリジル、チエニル、フリル、ピラゾ リル、ナフチル、テトラリニル、1,2,3,4−テトラヒドロキノリニル、イ ンダニル、インドリル、インドリニル、キノリニル、テトラヒドロキノリニル、 シクロヘキシル、ピペリジニル又はピペラジニルであり、Xが、結合、O、S又 はNR4であり、Rが、水素、アルキル、アルコキシ、ハロ、ハロアルキル、ア ルキルチオ、アルキルスルフィニル、アルキルスルホニル、フェニル及びアラル キルであり、R4が、水素、アルキル又はアラルキルであり、R5、R6、R7及び R8が独立して水素又はアルコキシである、請求の範囲代1項記載の方法。 7.Aが、置換又は未置換のフェニル、ナフチル又はインドリルであり、Xが結 合であり、Rが水素、メトキシ、エトキシ、クロロ、トリフルオロメチル、メチ ルスルホニル、フェニル及びベンジルであり、R4が水素、メチル又はベンジル であり、R5、R6、R7及びR8が独立して水素又はメトキシである、請求の範囲 第6項記載の方法。 8.投与される化合物が、4−(2−フェニルエチレニル)−6,7−ジメトキ シキナゾリン又はその薬学的に許容しうる塩である、請求の範囲第2項記載の方 法。 9.投与される化合物が、6,7−ジメトキシ−4−ナフタレン−1−イル−エ チニルキナゾリン又はその薬学的に許容しうる塩である、請求の範囲第3項記載 の方法。 10.投与される化合物が、4−(2−メトキシピリジン−5−イル)−6,7− ジメトキシキナゾリン、4−(4−フェニルピペリジン−1−イル)−6,7− ジメトキシキナゾリン、4−[4−(3−クロロフェニル)ピペラジン−1−イ ル]−6,7−ジメトキシキナゾリン及び4−(1,2,3,4−テトラヒドロ キノリン−1−イル)−6,7−ジメトキシキナゾリン並びにその薬学的に許容 しうる塩から選ばれる請求の範囲第6項記載の方法。 11.投与される化合物が、6,7−ジメトキシ−4−(β−ナフチルアミノ)キ ナゾリン、4−[N−(5−インダニル)アミノ]−6,7−ジメトキシキナゾ リン、N−ベンジル−N−(6,7−ジメトキシキナゾリン−4−イル)−N− フェニルアミン、6,7−ジメトキシ−4−(N−メチルアニリノ)キナゾリン 、N−(3−クロロフェニル)−N−(6,7−ジメトキシキナゾリン−4−イ ル)−N−メチルアミン、4−(3−アミノピラゾリル)−6,7−ジメトキシ キナゾリン及び4−(シクロヘキシルアニリノ)−6,7−ジメトキシキナゾリ ン並びにその薬学的に許容しうる塩から選ばれる、請求の範囲第6項記載の方法 。 12.投与される化合物が、6,7−ジメトキシ−4−(α−ナフチルアミノ)キ ナゾリン又はその薬学的に許容しうる塩である、請求範囲第6項記載の方法。 13.投与される化合物が、4−(ナフタレン−1−イル)−6,7−ジメトキシ キナゾリン、4−(ナフタレン−2−イル)−6,7−ジメトキシキナゾリン、 4−(3−フェニルフェニル)−6,7−ジメトキシキナゾリン、4−(インド ール−3−イル)−6,7−ジメトキシキナゾリン及び4−(1−メチルインド ール−3−イル)−6,7−ジメトキシキナゾリン並びにその薬学的に許容しう る塩から選ばれる、請求の範囲第7項記載の方法。 14.投与される化合物が、4−(1−ベンジルインドール−3−イル)−6,7 −ジメトキシキナゾリン又は薬学的に許容しうる塩である、請求の範囲第7項記 載の方法。 15.ヒト上皮増殖因子受容体2型(HER2)の活性により特徴付けられる細胞 の増殖及び分化を選択的に処理する医薬組成物であって、以下に示す式: (式中、Aは、炭素数が約5〜約12の、置換又は未置換の、単環式又は二環 式、アリール、ヘテロアリール、シクロアルキル又はヘテロシクロアルキル環系 であり、置換基はRによって表わされ、環系のあらゆる適当な部位に存在してい てもよく、Xは結合、O、S、SO、SO2、OCH2、CR4=CR4、C≡C、 NR4又はNR4CH2であり、Rは独立して、水素、アルキル、フェニル、ハロ フェニル、アラルキル、ヒドロキシ、アルコキシ、アリールオキシ、アシルオキ シ、ハロ、ハロアルキル、アミノ、モノ−及びジ−アルキルアミノ、アシルアミ ノ、カルボキシ、アミド、モノ−及びジ−アルキルアミド、アルキルチオ、アル キルスルフィニル並びにアルキルスルホニルであり、R4は水素、アルキル又は アラルキルであり、R5、R6、R7及びR8は独立して水素、アルコキシ又はアラ ルコキシである)、 で示される化合物又はその薬学的に許容しうる塩と、薬学的に許容しうる担体 との混合物を含む医薬組成物。 16.Aが、置換又は未置換の、フェニル、ピリジル、チエニル、フリル、ピラゾ リル、ナフチル、テトラリニル、1,2,3,4−テトラヒドロキノリニル、イ ンダニル、インドリル、インドリニル、キノリニル、テトラヒドロキノリニル、 シクロヘキシル、ピペリジニル又はピペラジニルであり、Xが結合、O、S又は NR4であり、Rが水素、アルキル、アルコキシ、ハロ、ハロアルキル、アルキ ルチオ、アルキルスルフィニル、アルキルスルホニル、フェニル及びアラルキル であり、R4が水素、アルキル又はアラルキルであり、R5、R6、 R7及びR8が、独立して水素又はアルコキシである請求の範囲第15項記載の組 成物。 17.化合物が、6,7−ジメトキシ−4−(α−ナフチルアミノ)キナゾリン又 はその薬学的に許容しうる塩である、請求の範囲第16項記載の組成物。 18.化合物が、4−(1−ベンジルインドール−3−イル)−6,7−ジメトキ シキナゾリン又はその薬学的に許容しうる塩である、請求の範囲第16項記載の 組成物。 19.6,7−ジメトキシ−4−(α−ナフチルアミノ)キナゾリン又はその薬学 的に許容しうる塩。 20.4−(1−ベンジルインドール−3−イル)−6,7−ジメトキシキナゾリ ン又はその薬学的に許容しうる塩。
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US08/469,147 US5721237A (en) | 1991-05-10 | 1995-06-06 | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
US08/469,147 | 1995-06-06 | ||
PCT/US1996/009606 WO1996039145A1 (en) | 1995-06-06 | 1996-06-06 | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of her-2 autophosphorylation properties |
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JP9501889A Ceased JPH11507355A (ja) | 1995-06-06 | 1996-06-06 | タンパク質チロシンキナーゼher−2の自己リン酸化能を選択的に阻害するアリール及びヘテロアリールキナゾリン化合物 |
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EP (1) | EP0831831A4 (ja) |
JP (1) | JPH11507355A (ja) |
KR (1) | KR19990022533A (ja) |
CN (1) | CN1100540C (ja) |
AU (1) | AU696456B2 (ja) |
BR (1) | BR9608638A (ja) |
CA (1) | CA2223016C (ja) |
CZ (1) | CZ289338B6 (ja) |
EA (1) | EA000840B1 (ja) |
HU (1) | HUP9802702A3 (ja) |
SI (1) | SI9620092A (ja) |
SK (1) | SK284475B6 (ja) |
WO (1) | WO1996039145A1 (ja) |
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JP2016507537A (ja) * | 2013-02-07 | 2016-03-10 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 置換アセチレン誘導体およびmGluR4の正のアロステリックモジュレーターとしてのそれらの使用 |
JP2016537396A (ja) * | 2013-11-20 | 2016-12-01 | シグナルケム・ライフサイエンシーズ・コーポレイションSignalchem Lifesciences Corporation | Tamファミリーキナーゼ阻害剤としてのキナゾリン誘導体 |
JP2017505288A (ja) * | 2013-12-09 | 2017-02-16 | ユーシービー バイオファルマ エスピーアールエル | Tnf活性のモジュレーターとしての縮合二環式ヘテロ芳香族誘導体 |
Also Published As
Publication number | Publication date |
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SK284475B6 (sk) | 2005-04-01 |
EA199800020A1 (ru) | 1998-06-25 |
EP0831831A4 (en) | 1998-05-27 |
MX9709430A (es) | 1998-10-31 |
AU6104496A (en) | 1996-12-24 |
CA2223016C (en) | 2003-05-20 |
EA000840B1 (ru) | 2000-04-24 |
KR19990022533A (ko) | 1999-03-25 |
AU696456B2 (en) | 1998-09-10 |
HUP9802702A3 (en) | 2001-11-28 |
EP0831831A1 (en) | 1998-04-01 |
BR9608638A (pt) | 1999-06-29 |
CA2223016A1 (en) | 1996-12-12 |
CN1100540C (zh) | 2003-02-05 |
CN1187129A (zh) | 1998-07-08 |
SK166397A3 (en) | 1998-06-03 |
CZ289338B6 (cs) | 2002-01-16 |
CZ350397A3 (cs) | 1998-03-18 |
SI9620092A (sl) | 1998-08-31 |
WO1996039145A1 (en) | 1996-12-12 |
HUP9802702A2 (hu) | 1999-03-29 |
US5721237A (en) | 1998-02-24 |
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