JP2010511628A - Ａ２ａアデノシン受容体アンタゴニスト - Google Patents
Ａ２ａアデノシン受容体アンタゴニスト Download PDFInfo
- Publication number
- JP2010511628A JP2010511628A JP2009539494A JP2009539494A JP2010511628A JP 2010511628 A JP2010511628 A JP 2010511628A JP 2009539494 A JP2009539494 A JP 2009539494A JP 2009539494 A JP2009539494 A JP 2009539494A JP 2010511628 A JP2010511628 A JP 2010511628A
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- JP
- Japan
- Prior art keywords
- pyrimidine
- methyl
- dione
- ethyl
- dihydrothiopheno
- 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.)
- Pending
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 26
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
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- WFAMKSGWIMBDLH-ZHACJKMWSA-N 1,5-dimethyl-6-[(e)-2-phenylethenyl]-3-prop-2-ynylthieno[2,3-d]pyrimidine-2,4-dione Chemical compound S1C=2N(C)C(=O)N(CC#C)C(=O)C=2C(C)=C1\C=C\C1=CC=CC=C1 WFAMKSGWIMBDLH-ZHACJKMWSA-N 0.000 claims description 3
- ZWQZMOOECQNJRH-ZHACJKMWSA-N 3-ethyl-1,5-dimethyl-6-[(e)-2-phenylethenyl]thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)N(C)C=2SC=1\C=C\C1=CC=CC=C1 ZWQZMOOECQNJRH-ZHACJKMWSA-N 0.000 claims description 3
- JPDDMSDKBBPCEK-CSKARUKUSA-N 6-[(e)-2-(3,4-dimethoxyphenyl)ethenyl]-3-ethyl-1,5-dimethylthieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)N(C)C=2SC=1\C=C\C1=CC=C(OC)C(OC)=C1 JPDDMSDKBBPCEK-CSKARUKUSA-N 0.000 claims description 3
- ZYRNLFPSWWUWDQ-WYMLVPIESA-N 6-[(e)-2-(3,4-dimethoxyphenyl)ethenyl]-3-ethyl-5-methyl-1-(phenylmethoxymethyl)thieno[2,3-d]pyrimidine-2,4-dione Chemical compound C1=2SC(\C=C\C=3C=C(OC)C(OC)=CC=3)=C(C)C=2C(=O)N(CC)C(=O)N1COCC1=CC=CC=C1 ZYRNLFPSWWUWDQ-WYMLVPIESA-N 0.000 claims description 3
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- VWRJRTRNYFJZAS-VAWYXSNFSA-N 1,3-diethyl-5-methyl-6-[(e)-2-phenylethenyl]thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)N(CC)C=2SC=1\C=C\C1=CC=CC=C1 VWRJRTRNYFJZAS-VAWYXSNFSA-N 0.000 claims description 2
- VVTDOAWVBUHYMP-MDZDMXLPSA-N 3-ethyl-1-(2-hydroxyethyl)-5-methyl-6-[(e)-2-phenylethenyl]thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)N(CCO)C=2SC=1\C=C\C1=CC=CC=C1 VVTDOAWVBUHYMP-MDZDMXLPSA-N 0.000 claims description 2
- VVTDOAWVBUHYMP-KTKRTIGZSA-N 3-ethyl-1-(2-hydroxyethyl)-5-methyl-6-[(z)-2-phenylethenyl]thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)N(CCO)C=2SC=1\C=C/C1=CC=CC=C1 VVTDOAWVBUHYMP-KTKRTIGZSA-N 0.000 claims description 2
- PGKMFTICSBOZHW-ZHACJKMWSA-N 3-ethyl-1-(3-hydroxypropyl)-5-methyl-6-[(e)-2-phenylethenyl]thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)N(CCCO)C=2SC=1\C=C\C1=CC=CC=C1 PGKMFTICSBOZHW-ZHACJKMWSA-N 0.000 claims description 2
- JRJYNEYIILYZEI-MDZDMXLPSA-N 3-ethyl-5-methyl-6-[(e)-2-(4-methylphenyl)ethenyl]-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=C(C)C=C1 JRJYNEYIILYZEI-MDZDMXLPSA-N 0.000 claims description 2
- QGLVDTJLFFMKDQ-SDNWHVSQSA-N 3-ethyl-5-methyl-6-[(e)-2-(4-phenylphenyl)ethenyl]-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C(C=C1)=CC=C1C1=CC=CC=C1 QGLVDTJLFFMKDQ-SDNWHVSQSA-N 0.000 claims description 2
- VPTDBYKUWMMYES-RMKNXTFCSA-N 3-ethyl-5-methyl-6-[(e)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=C(C(F)(F)F)C=C1 VPTDBYKUWMMYES-RMKNXTFCSA-N 0.000 claims description 2
- LHSOGOXUANFNEJ-VOTSOKGWSA-N 3-ethyl-5-methyl-6-[(e)-2-pyridin-3-ylethenyl]-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=CN=C1 LHSOGOXUANFNEJ-VOTSOKGWSA-N 0.000 claims description 2
- BLSAUMXBWNUVHN-CMDGGOBGSA-N 3-ethyl-6-[(e)-2-(2-fluorophenyl)ethenyl]-5-methyl-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=CC=C1F BLSAUMXBWNUVHN-CMDGGOBGSA-N 0.000 claims description 2
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- DNAWLGURDUWARK-BQYQJAHWSA-N 3-ethyl-6-[(e)-2-(3-fluorophenyl)ethenyl]-5-methyl-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=CC(F)=C1 DNAWLGURDUWARK-BQYQJAHWSA-N 0.000 claims description 2
- XDAYENCKGPZWCY-CMDGGOBGSA-N 3-ethyl-6-[(e)-2-(3-methoxyphenyl)ethenyl]-5-methyl-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=CC(OC)=C1 XDAYENCKGPZWCY-CMDGGOBGSA-N 0.000 claims description 2
- BMLNLXDZFDTYAY-RMKNXTFCSA-N 3-ethyl-6-[(e)-2-(4-fluorophenyl)ethenyl]-5-methyl-1h-thieno[2,3-d]pyrimidine-2,4-dione Chemical compound CC=1C=2C(=O)N(CC)C(=O)NC=2SC=1\C=C\C1=CC=C(F)C=C1 BMLNLXDZFDTYAY-RMKNXTFCSA-N 0.000 claims description 2
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Classifications
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- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
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- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87225406P | 2006-12-01 | 2006-12-01 | |
| PCT/US2007/085978 WO2008070529A2 (en) | 2006-12-01 | 2007-11-29 | A2a adenosine receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010511628A true JP2010511628A (ja) | 2010-04-15 |
| JP2010511628A5 JP2010511628A5 (https=) | 2012-01-05 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009539494A Pending JP2010511628A (ja) | 2006-12-01 | 2007-11-29 | Ａ２ａアデノシン受容体アンタゴニスト |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US7776868B2 (https=) |
| EP (1) | EP2121705A2 (https=) |
| JP (1) | JP2010511628A (https=) |
| CA (1) | CA2670788A1 (https=) |
| WO (1) | WO2008070529A2 (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016532721A (ja) * | 2013-10-07 | 2016-10-20 | バイエル ファーマ アクチエンゲゼルシャフト | 環状チエノウラシルカルボキサミドおよびその使用 |
| JP2017524016A (ja) * | 2014-08-11 | 2017-08-24 | ハイドラ バイオサイエンシズ インコーポレイテッドＨｙｄｒａ Ｂｉｏｓｃｉｅｎｃｅｓ，Ｉｎｃ． | ＴＲＰＣ５調節因子としての、精神神経障害の処置のためのチエノおよびフロ［２，３−ｄ］ピリミジン−２，４［１Ｈ，３Ｈ］−ジオン誘導体 |
| JP2018509443A (ja) * | 2015-03-26 | 2018-04-05 | バイエル ファーマ アクチエンゲゼルシャフト | アデノシン−Ａ２ｂ受容体の拮抗薬としての複素環メチル−チエノウラシル |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2644996A1 (en) * | 2006-03-02 | 2007-09-13 | Cv Therapeutics, Inc. | A2a adenosine receptor antagonists |
| TWI473614B (zh) | 2008-05-29 | 2015-02-21 | Kyowa Hakko Kirin Co Ltd | Anti-analgesic inhibitors |
| WO2011101861A1 (en) | 2010-01-29 | 2011-08-25 | Msn Laboratories Limited | Process for preparation of dpp-iv inhibitors |
| WO2018041771A1 (de) | 2016-09-02 | 2018-03-08 | Bayer Pharma Aktiengesellschaft | (1-methylcyclopropyl)methyl-substituierte thienouracile und ihre verwendung |
| WO2018054846A1 (de) | 2016-09-23 | 2018-03-29 | Bayer Aktiengesellschaft | N3-cyclisch substituierte thienouracile und ihre verwendung |
| KR101709307B1 (ko) * | 2016-10-31 | 2017-02-23 | 퓨쳐메디신 주식회사 | 아데노신 유도체를 포함하는 비알콜성 지방간염, 간섬유증 및 간경변증 예방 및 치료용 약학적 조성물 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002500666A (ja) * | 1997-05-28 | 2002-01-08 | アストラゼネカ・アクチエボラーグ | 新規な化合物 |
| JP2004518732A (ja) * | 2001-02-14 | 2004-06-24 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | マトリックスメタロプロテイナーゼ阻害剤としてのチエノ’２，３−ｄピリミジンジオン誘導体 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| DE69130869T2 (de) * | 1990-10-18 | 1999-06-10 | Kyowa Hakko Kogyo Co., Ltd., Tokio/Tokyo | Xanthinderivate |
| CA2644996A1 (en) | 2006-03-02 | 2007-09-13 | Cv Therapeutics, Inc. | A2a adenosine receptor antagonists |
-
2007
- 2007-11-29 EP EP07864929A patent/EP2121705A2/en not_active Withdrawn
- 2007-11-29 JP JP2009539494A patent/JP2010511628A/ja active Pending
- 2007-11-29 WO PCT/US2007/085978 patent/WO2008070529A2/en not_active Ceased
- 2007-11-29 US US11/947,690 patent/US7776868B2/en active Active
- 2007-11-29 CA CA002670788A patent/CA2670788A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002500666A (ja) * | 1997-05-28 | 2002-01-08 | アストラゼネカ・アクチエボラーグ | 新規な化合物 |
| JP2004518732A (ja) * | 2001-02-14 | 2004-06-24 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | マトリックスメタロプロテイナーゼ阻害剤としてのチエノ’２，３−ｄピリミジンジオン誘導体 |
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| JP2016532721A (ja) * | 2013-10-07 | 2016-10-20 | バイエル ファーマ アクチエンゲゼルシャフト | 環状チエノウラシルカルボキサミドおよびその使用 |
| JP2017524016A (ja) * | 2014-08-11 | 2017-08-24 | ハイドラ バイオサイエンシズ インコーポレイテッドＨｙｄｒａ Ｂｉｏｓｃｉｅｎｃｅｓ，Ｉｎｃ． | ＴＲＰＣ５調節因子としての、精神神経障害の処置のためのチエノおよびフロ［２，３−ｄ］ピリミジン−２，４［１Ｈ，３Ｈ］−ジオン誘導体 |
| JP2018509443A (ja) * | 2015-03-26 | 2018-04-05 | バイエル ファーマ アクチエンゲゼルシャフト | アデノシン−Ａ２ｂ受容体の拮抗薬としての複素環メチル−チエノウラシル |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008070529A2 (en) | 2008-06-12 |
| EP2121705A2 (en) | 2009-11-25 |
| US20080188495A1 (en) | 2008-08-07 |
| CA2670788A1 (en) | 2008-06-12 |
| WO2008070529A3 (en) | 2008-07-31 |
| US7776868B2 (en) | 2010-08-17 |
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