JPH11503449A - タキキニン受容体アンタゴニスト活性を有する新規な置換されたピペラジン誘導体 - Google Patents
タキキニン受容体アンタゴニスト活性を有する新規な置換されたピペラジン誘導体Info
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式 の化合物またはその立体異性体またはその医薬的に許容し得る塩。 上記式において、 G1は、-CH2-または-C(O)-であり; G2は、-CH2-または-C(O)-であり; G3は、-CH2-または-C(O)-であり; mは、0または1であり; Ar1は、群: (式中、Z1は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)から選択された基であり; Ar2は、群: (式中、Z2は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、 ヒドロキシ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択さ れた1〜3個の置換分である)から選択された基であり; Ar3は、群: (式中、Z3は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分でありそしてR6は水素、C1-C4アルキルまたは-CHOである)から選 択された基であり; R1は、水素、C1-C4アルキル、-(CH2)qAr4または-CH2C(O)Ar4〔式中、qは1 〜4の整数でありそしてAr4は、式 (式中、Z4は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)の基である〕であり;そして、 但し、G1が-C(O)-である場合は、G2は-C(O)-でなくそしてさらに、G3が-CH2 -である場合は、G1およびG2は-CH2-である。 2.R1が水素である請求項1記載の化合物。 3.G1が-CH2-でありそしてG2が-C(O)-である請求項2記載の化合物。 4.G3が-C(O)-である請求項3記載の化合物。 5.化合物が、(SまたはR)−2−〔(SまたはR)−3−(1H−イン ドール−3−イルメチル)−2−オキソ−ピペラジン−1−イル〕−1−〔N− メチル−N−ベンジル−3−(フェニル)−プロピオンアミド〕またはその混合 物である請求項1記載の化合物。 6.請求項1記載の化合物および医薬的に許容し得る担体からなる医薬組成物。 7.1種または2種以上の不活性担体と混合されたまたはさもなければ一緒にさ れた請求項1記載の化合物からなる医薬組成物。 8.医薬的に活性な化合物として使用するための請求項1記載の化合物。 9.タキキニン−仲介疾患および状態を治療するための請求項8記載の化合物。 10.喘息を治療するための請求項8記載の化合物。 11.咳を治療するための請求項8記載の化合物。 12.気管支炎を治療するための請求項8記載の化合物。 13.タキキニン−仲介疾患および状態を治療するための請求項6記載の医薬組成 物。 14.喘息を治療するための請求項6記載の医薬組成物。 15.咳を治療するための請求項6記載の医薬組成物。 16.気管支炎を治療するための請求項6記載の医薬組成物。 17.請求項1記載の化合物の治療的に有効な量を患者に投与することからなる治 療を必要とする患者のタキキニン−仲介疾患および状態を治療する方法。 18.請求項1記載の化合物の治療的に有効な量を患者に投与することからなる治 療を必要とする患者の喘息を治療する方法。 19.請求項1記載の化合物の治療的に有効な量を患者に投与することか らなる治療を必要とする患者の咳を治療する方法。 20.請求項1記載の化合物の治療的に有効な量を患者に投与することからなる治 療を必要とする患者の気管支炎を治療する方法。 21.カップリング試薬を使用して、式 (式中、m、G1、G2、Ar1、Ar2およびAr3は、後述する通りである)の化合物 を環化させ、そして場合によっては、アミンのアルキル化、インドール窒素に対 する付加反応またはアミデートの形成によって変性しそして場合によっては脱保 護しそして場合によってはさらに許容し得る酸または許容し得る塩基との反応に よって医薬的に許容し得る塩を製造することからなる式 {式中、 G1は、-CH2-または-C(O)-であり; G2は、-CH2-または-C(O)-であり; G3は、-C(O)-であり; mは、0または1であり; Ar1は、群: (式中、Z1は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)から選択された基であり; Ar2は、群: (式中、Z2は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)から選択された基であり; Ar3は、群: (式中、Z3は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分でありそしてR6は水素、C1-C4アルキルまたは-CHOである)から選 択された基であり; R1は、水素、C1-C4アルキル、-(CH2)qAr4または-CH2C(O)Ar4〔式中、qは1 〜4の整数でありそしてAr4は、式 (式中、Z4は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)の基である〕であり;そして、 但し、G1が-C(O)-である場合は、G2は-C(O)-でない} の化合物またはその立体異性体またはその医薬的に許容し得る塩の製法。 22.水素化アルミニウムリチウム、ジイソブチルアルミニウムヒドリドおよびボ ランジメチルスルフィド複合体からなる群から選択されたアミド還元剤を使用し て式 (式中、m、G1、G2、Ar1、Ar2およびAr3は後述する通りである)の化合物を 環元し、そして場合によっては、アミンのアルキル化、インドール窒素に対する 付加反応またはアミデートの形成によって変性しそして場合によっては脱保護し そして場合によっては、さらに許容し得る酸または許容し得る塩基との反応によ って医薬的に許容し得る塩を製造することからなる式 {式中、 G1は、-CH2-または-C(O)-であり; G2は、-CH2-または-C(O)-であり; G3は、-CH2-であり; mは、0または1であり; Ar1は、群: (式中、Z1は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)から選択された基であり; Ar2は、群: (式中、Z2は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)から選択された基であり; Ar3は、群: (式中、Z3は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分でありそしてR6は水素、C1-C4アルキルまたは-CHOである)から選 択された基であり; R1は、水素、C1-C4アルキル、-(CH2)qAr4または-CH2C(O)Ar4〔式中、qは1 〜4の整数でありそしてAr4は、式 (式中、Z4は、それぞれ独立して水素、ハロゲン、ベンジルオキシ、ヒドロキ シ、CF3、C1-C4アルキルおよびC1-C4アルコキシからなる群から選択された1〜 3個の置換分である)の基である〕であり;そして、 但し、G1が-C(O)-である場合は、G2は-C(O)-でない} の化合物またはその立体異性体またはその医薬的に許容し得る塩の製法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US42171995A | 1995-04-13 | 1995-04-13 | |
US08/421,719 | 1995-04-13 | ||
PCT/US1996/002568 WO1996032385A1 (en) | 1995-04-13 | 1996-03-11 | Novel substituted piperazine derivatives having tachykinin receptor antagonists activity |
Publications (2)
Publication Number | Publication Date |
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JPH11503449A true JPH11503449A (ja) | 1999-03-26 |
JP3950170B2 JP3950170B2 (ja) | 2007-07-25 |
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Application Number | Title | Priority Date | Filing Date |
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JP53099896A Expired - Fee Related JP3950170B2 (ja) | 1995-04-13 | 1996-03-11 | タキキニン受容体アンタゴニスト活性を有する新規な置換されたピペラジン誘導体 |
Country Status (19)
Country | Link |
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US (1) | US5672602A (ja) |
EP (1) | EP0830347B1 (ja) |
JP (1) | JP3950170B2 (ja) |
KR (1) | KR100414321B1 (ja) |
CN (1) | CN1098255C (ja) |
AR (1) | AR002986A1 (ja) |
AT (1) | ATE277021T1 (ja) |
AU (1) | AU700693B2 (ja) |
CA (1) | CA2217006C (ja) |
DE (1) | DE69633442T2 (ja) |
ES (1) | ES2224164T3 (ja) |
HU (1) | HUP9802036A3 (ja) |
IL (1) | IL117866A (ja) |
MX (1) | MX9707879A (ja) |
NO (1) | NO310357B1 (ja) |
NZ (1) | NZ306022A (ja) |
TW (1) | TW322476B (ja) |
WO (1) | WO1996032385A1 (ja) |
ZA (1) | ZA962817B (ja) |
Families Citing this family (55)
Publication number | Priority date | Publication date | Assignee | Title |
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ATE219064T1 (de) * | 1995-12-18 | 2002-06-15 | Fujisawa Pharmaceutical Co | Piperazinderivative als tachykinin antagonisten |
US6613801B2 (en) | 2000-05-30 | 2003-09-02 | Transtech Pharma, Inc. | Method for the synthesis of compounds of formula I and their uses thereof |
WO2002070473A2 (en) | 2001-03-05 | 2002-09-12 | Transtech Pharma, Inc. | Carboxamide derivatives as therapeutic agents |
WO2002069965A1 (en) | 2001-03-05 | 2002-09-12 | Transtech Pharma, Inc. | Benzimidazole derivatives as therapeutic agents |
US7718802B2 (en) | 2001-08-10 | 2010-05-18 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific piperazine compounds |
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DE69633442T2 (de) | 2006-01-05 |
NZ306022A (en) | 1998-09-24 |
EP0830347A1 (en) | 1998-03-25 |
AU700693B2 (en) | 1999-01-14 |
AU5417296A (en) | 1996-10-30 |
NO310357B1 (no) | 2001-06-25 |
DE69633442D1 (de) | 2004-10-28 |
HUP9802036A3 (en) | 1999-06-28 |
EP0830347B1 (en) | 2004-09-22 |
ATE277021T1 (de) | 2004-10-15 |
KR19980703846A (ko) | 1998-12-05 |
ES2224164T3 (es) | 2005-03-01 |
CN1098255C (zh) | 2003-01-08 |
CN1181753A (zh) | 1998-05-13 |
KR100414321B1 (ko) | 2004-02-18 |
NO974686D0 (no) | 1997-10-10 |
ZA962817B (en) | 1996-10-14 |
TW322476B (ja) | 1997-12-11 |
CA2217006A1 (en) | 1996-10-17 |
MX9707879A (es) | 1997-11-29 |
US5672602A (en) | 1997-09-30 |
AR002986A1 (es) | 1998-05-27 |
HUP9802036A2 (hu) | 1999-03-29 |
CA2217006C (en) | 2001-05-22 |
WO1996032385A1 (en) | 1996-10-17 |
NO974686L (no) | 1997-12-10 |
JP3950170B2 (ja) | 2007-07-25 |
IL117866A (en) | 2001-09-13 |
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