JP2007516211A5 - - Google Patents
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- Publication number
- JP2007516211A5 JP2007516211A5 JP2006520478A JP2006520478A JP2007516211A5 JP 2007516211 A5 JP2007516211 A5 JP 2007516211A5 JP 2006520478 A JP2006520478 A JP 2006520478A JP 2006520478 A JP2006520478 A JP 2006520478A JP 2007516211 A5 JP2007516211 A5 JP 2007516211A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- ethyl
- hydroxy
- methylsulfonyl
- phenylethyl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- XSRZJMIJNKWTJY-LJAQVGFWSA-N 2-(cyclohexylamino)-4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-N-methylsulfonylbenzamide Chemical compound CS(=O)(=O)NC(=O)C1=CC=C(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)C=C1NC1CCCCC1 XSRZJMIJNKWTJY-LJAQVGFWSA-N 0.000 claims 1
- WWFRXUDMACTFBI-NDEPHWFRSA-N 2-cyclohexyloxy-4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-N-methylsulfonylbenzamide Chemical compound CS(=O)(=O)NC(=O)C1=CC=C(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)C=C1OC1CCCCC1 WWFRXUDMACTFBI-NDEPHWFRSA-N 0.000 claims 1
- YLQMAAMFQNYJDU-MHZLTWQESA-N 2-cyclohexyloxy-4-[4-[2-[[(2R)-2-hydroxy-2-pyridin-3-ylethyl]amino]ethyl]phenyl]-N-methylsulfonylbenzamide Chemical compound CS(=O)(=O)NC(=O)C1=CC=C(C=2C=CC(CCNC[C@H](O)C=3C=NC=CC=3)=CC=2)C=C1OC1CCCCC1 YLQMAAMFQNYJDU-MHZLTWQESA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- SITWWMFSARAANL-KMRXNPHXSA-N 4-[4-[2-[[(1R,2S)-1-hydroxy-1-phenylpropan-2-yl]amino]ethyl]phenyl]-2-(2-methylpropyl)-N-methylsulfonylbenzamide Chemical compound C1=C(C(=O)NS(C)(=O)=O)C(CC(C)C)=CC(C=2C=CC(CCN[C@@H](C)[C@H](O)C=3C=CC=CC=3)=CC=2)=C1 SITWWMFSARAANL-KMRXNPHXSA-N 0.000 claims 1
- FKGYWDPSUXSSQK-MHZLTWQESA-N 4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-2-(2-methylpropyl)-N-methylsulfonylbenzamide Chemical compound C1=C(C(=O)NS(C)(=O)=O)C(CC(C)C)=CC(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)=C1 FKGYWDPSUXSSQK-MHZLTWQESA-N 0.000 claims 1
- IXBYTCUCLIPCPM-NDEPHWFRSA-N 4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-2-(3-methylbutyl)-N-methylsulfonylbenzamide Chemical compound C1=C(C(=O)NS(C)(=O)=O)C(CCC(C)C)=CC(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)=C1 IXBYTCUCLIPCPM-NDEPHWFRSA-N 0.000 claims 1
- FEQQLEGJQNYEQY-SANMLTNESA-N 4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-N-methylsulfonyl-2-(propan-2-ylamino)benzamide Chemical compound C1=C(C(=O)NS(C)(=O)=O)C(NC(C)C)=CC(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)=C1 FEQQLEGJQNYEQY-SANMLTNESA-N 0.000 claims 1
- HXFKZSVPCHUKBX-VWLOTQADSA-N 4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-N-methylsulfonyl-2-propan-2-ylsulfanylbenzamide Chemical compound C1=C(C(=O)NS(C)(=O)=O)C(SC(C)C)=CC(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)=C1 HXFKZSVPCHUKBX-VWLOTQADSA-N 0.000 claims 1
- HGOKKKSGWRCIHE-NDEPHWFRSA-N N-[2-cyclohexyloxy-4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]phenyl]sulfonylacetamide Chemical compound CC(=O)NS(=O)(=O)C1=CC=C(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)C=C1OC1CCCCC1 HGOKKKSGWRCIHE-NDEPHWFRSA-N 0.000 claims 1
- IWTORKZSDKQKNR-LJAQVGFWSA-N N-[2-cyclohexyloxy-4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]phenyl]sulfonylbutanamide Chemical compound CCCC(=O)NS(=O)(=O)C1=CC=C(C=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)C=C1OC1CCCCC1 IWTORKZSDKQKNR-LJAQVGFWSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000048 adrenergic agonist Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- -1 benzyloxy, nitro, amino Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
Claims (5)
- 式(I)
R1およびR12は、それぞれ水素、ハロゲン、低級アルキル、ヒドロキシ、低級アルコキシ、ベンジルオキシ、ニトロ、アミノまたは(低級アルキルスルホニル)アミノ、
R2は水素または任意に置換された低級アルキル、
R3は水素またはアミノ保護基、
R4、R5およびR6は、それぞれ水素または任意に置換された低級アルキル、
R7は−Z−R13
(式中、
Zは結合または−(CH 2 ) n −(式中、nは1)、
R 13 は(低級アルキルスルホニル)カルバモイルまたは低級アルカノイルスルファモイル、
をそれぞれ意味する。)
R8は−Y−R9
(式中、
Yは結合、−CH2−、−O−、−S−、−SO−、−SO2−、−NH−または
R9は水素、低級アルキル、シクロ(低級)アルキル、モノ(またはジまたはトリ)ハロ(低級)アルキル、低級アルカノイル、低級アルケニル、低級アルコキシ(低級)アルキル、ニトロ、アリールまたは複素環基、
をそれぞれ意味する。)、
R11は水素、低級アルキル、低級アルコキシ、アミノまたはモノ(またはジ)低級(アルキル)アミノをそれぞれ意味する]
で表される化合物またはその塩。 - Xが結合、
R1およびR12が、それぞれ水素またはハロゲン、
R3が水素、
R4が水素、
R8が−Y−R9
(式中、
Yは結合、−CH2−、−O−、−S−または−NH−、
R9は低級アルキルまたはシクロ(低級)アルキル、
をそれぞれ意味する。)、
R11が水素、
である請求項1に記載の化合物。 - (1) 4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−3−(3−メチルブチル)−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
(2) 4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−3−イソブチル−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
(3) 4’−[2−[[(1S,2R)−2−ヒドロキシ−1−メチル−2−フェニルエチル]アミノ]エチル]−3−イソブチル−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
(4) 4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−3−(イソプロピルチオ)−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
(5) 3−(シクロヘキシルオキシ)−4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
(6) 3−(シクロヘキシルオキシ)−4’−[2−[[(2R)−2−ヒドロキシ−2−(3−ピリジル)エチル]アミノ]エチル]−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
(7) 2−[3−(シクロヘキシルオキシ)−4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−4−ビフェニリル]−N−(メチルスルホニル)アセトアミド、
(8) 2−[3−(シクロヘキシルオキシ)−4’−[2−[[(2R)−2−ヒドロキシ−2−(3−ピリジル)エチル]アミノ]エチル]−4−ビフェニリル]−N−(メチルスルホニル)アセトアミド、
(9) N−[[3−(シクロヘキシルオキシ)−4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−4−ビフェニリル]スルホニル]アセトアミド、
(10) N−[[3−(シクロヘキシルオキシ)−4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−4−ビフェニリル]スルホニル]ブタンアミド、
(11) 3−(シクロヘキシルアミノ)−4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−N−(メチルスルホニル)−4−ビフェニルカルボキサミドおよび
(12) 4’−[2−[[(2R)−2−ヒドロキシ−2−フェニルエチル]アミノ]エチル]−3−(イソプロピルアミノ)−N−(メチルスルホニル)−4−ビフェニルカルボキサミド、
よりなる群から選択される請求項1に記載の化合物または医薬として許容されるその塩。 - 医薬として許容される担体または賦形剤と共に、請求項1に記載の化合物または医薬として許容されるその塩を有効成分として含有する医薬組成物。
- 用途が選択的β3アドレナリン性受容体作動薬である請求項4に記載の医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU2003907111A AU2003907111A0 (en) | 2003-12-23 | Aminoalcohol Derivatives | |
PCT/JP2004/019495 WO2005061433A2 (en) | 2003-12-23 | 2004-12-20 | Aminoalcohol derivatives |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2007516211A JP2007516211A (ja) | 2007-06-21 |
JP2007516211A5 true JP2007516211A5 (ja) | 2008-02-14 |
JP4618250B2 JP4618250B2 (ja) | 2011-01-26 |
Family
ID=34658494
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006520478A Expired - Fee Related JP4618250B2 (ja) | 2003-12-23 | 2004-12-20 | アミノアルコール誘導体 |
Country Status (10)
Country | Link |
---|---|
US (1) | US7417060B2 (ja) |
EP (1) | EP1697301A2 (ja) |
JP (1) | JP4618250B2 (ja) |
KR (1) | KR101071748B1 (ja) |
CN (1) | CN100582088C (ja) |
AR (1) | AR047351A1 (ja) |
CA (1) | CA2551167C (ja) |
MX (1) | MXPA06007173A (ja) |
TW (1) | TW200526551A (ja) |
WO (1) | WO2005061433A2 (ja) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ537206A (en) * | 2002-06-27 | 2007-06-29 | Astellas Pharma Inc | Aminoalcohol derivatives |
BRPI0407386A (pt) | 2003-02-14 | 2006-02-07 | Kissei Pharmaceutical | Derivados de álcool de amino, composições farmacêuticas contendo os mesmos e uso destes |
US7417169B2 (en) | 2003-10-24 | 2008-08-26 | Kissei Pharmaceutical Co., Ltd. | Amino alcohol derivatives, medicinal composition containing the same, and use of these |
CA2551167C (en) | 2003-12-23 | 2011-10-18 | Astellas Pharma Inc. | Aminoalcohol derivatives |
WO2006022237A1 (ja) * | 2004-08-24 | 2006-03-02 | Kissei Pharmaceutical Co., Ltd. | 脂肪肝の予防または治療剤 |
US7928264B2 (en) * | 2004-09-21 | 2011-04-19 | Astellas Pharma Inc. | Aminoalcohol derivatives |
CA2602609A1 (en) * | 2005-03-16 | 2006-09-21 | Junichi Yokotani | Novel anthranilic acid derivative or salt thereof |
KR100901664B1 (ko) | 2007-08-06 | 2009-06-09 | 주식회사 오스코텍 | β-아미노알콜 유도체, 이의 제조방법 및 이를유효성분으로 함유하는 TNF-α 매개성 질환의 예방 및치료용 약학적 조성물 |
PT3365321T (pt) | 2015-10-23 | 2024-01-12 | B3Ar Therapeutics Inc | Zwiterião de solabegron e suas utilizações |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3718638A1 (de) * | 1987-06-04 | 1988-12-22 | Thomae Gmbh Dr K | Neue phenylethanolamine, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
NO179246C (no) * | 1991-11-20 | 1996-09-04 | Sankyo Co | Aromatiske amino-alkoholderivater og mellomprodukter til fremstilling derav |
JPH11504649A (ja) * | 1995-05-10 | 1999-04-27 | ファイザー・インコーポレーテッド | β−アドレナリン作働性アゴニスト |
GB9812709D0 (en) * | 1998-06-13 | 1998-08-12 | Glaxo Group Ltd | Chemical compounds |
KR20030044013A (ko) * | 2000-10-20 | 2003-06-02 | 화이자 프로덕츠 인코포레이티드 | 알파-아릴 에탄올아민 및 이들의 베타-3 아드레날린성수용체 작용제로서의 용도 |
EP1448561B1 (en) * | 2001-11-20 | 2008-02-20 | Eli Lilly And Company | Beta 3 adrenergic agonists |
DOP2003000587A (es) * | 2002-02-27 | 2003-08-30 | Pfizer Prod Inc | AGONISTAS DEL RECEPTOR ß3-ADRENERGICO |
BR0307996A (pt) * | 2002-02-27 | 2004-12-07 | Pfizer Prod Inc | Processos e intermediários úteis na preparação de receptores de agonistas beta3-adrenérgicos |
MXPA04008918A (es) * | 2002-03-14 | 2004-11-26 | Fujisawa Pharmaceutical Co | Derivados de aminoalcohol como agonistas del receptor adrenergico beta-3. |
NZ537206A (en) * | 2002-06-27 | 2007-06-29 | Astellas Pharma Inc | Aminoalcohol derivatives |
AU2002952839A0 (en) | 2002-11-21 | 2002-12-05 | Fujisawa Pharmaceutical Co., Ltd. | Aminoalcohol derivatives |
BRPI0407386A (pt) * | 2003-02-14 | 2006-02-07 | Kissei Pharmaceutical | Derivados de álcool de amino, composições farmacêuticas contendo os mesmos e uso destes |
CA2551167C (en) | 2003-12-23 | 2011-10-18 | Astellas Pharma Inc. | Aminoalcohol derivatives |
-
2004
- 2004-12-20 CA CA2551167A patent/CA2551167C/en not_active Expired - Fee Related
- 2004-12-20 EP EP04807850A patent/EP1697301A2/en not_active Withdrawn
- 2004-12-20 KR KR1020067014417A patent/KR101071748B1/ko not_active IP Right Cessation
- 2004-12-20 CN CN200480041150A patent/CN100582088C/zh not_active Expired - Fee Related
- 2004-12-20 JP JP2006520478A patent/JP4618250B2/ja not_active Expired - Fee Related
- 2004-12-20 WO PCT/JP2004/019495 patent/WO2005061433A2/en active Application Filing
- 2004-12-20 MX MXPA06007173A patent/MXPA06007173A/es active IP Right Grant
- 2004-12-21 US US11/016,886 patent/US7417060B2/en not_active Expired - Fee Related
- 2004-12-22 TW TW093139942A patent/TW200526551A/zh unknown
- 2004-12-27 AR ARP040104909A patent/AR047351A1/es unknown
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