ES2557310T3 - 8-heteroaril xantinas substituidas - Google Patents
8-heteroaril xantinas substituidas Download PDFInfo
- Publication number
- ES2557310T3 ES2557310T3 ES10012271.2T ES10012271T ES2557310T3 ES 2557310 T3 ES2557310 T3 ES 2557310T3 ES 10012271 T ES10012271 T ES 10012271T ES 2557310 T3 ES2557310 T3 ES 2557310T3
- Authority
- ES
- Spain
- Prior art keywords
- compound
- ethyl
- propyl
- methyl
- cyclopropyl
- 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.)
- Expired - Lifetime
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- 229940065721 systemic for obstructive airway disease xanthines Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 39
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract description 13
- 150000003839 salts Chemical class 0.000 abstract description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract description 11
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract description 9
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 abstract description 7
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract description 7
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract description 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract description 6
- 239000001257 hydrogen Substances 0.000 abstract description 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract description 6
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 abstract description 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract description 4
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract description 4
- 125000001424 substituent group Chemical group 0.000 abstract description 4
- 125000001475 halogen functional group Chemical group 0.000 abstract description 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract description 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract description 2
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical compound O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 description 24
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- 238000000034 method Methods 0.000 description 6
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Classifications
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
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- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
- C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
Landscapes
- Health & Medical Sciences (AREA)
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- Ophthalmology & Optometry (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| US49787503P | 2003-08-25 | 2003-08-25 | |
| US497875P | 2003-08-25 |
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| ES04781752.3T Expired - Lifetime ES2440467T3 (es) | 2003-08-25 | 2004-08-20 | 8-heteroaril xantinas substituidas |
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| ES04781752.3T Expired - Lifetime ES2440467T3 (es) | 2003-08-25 | 2004-08-20 | 8-heteroaril xantinas substituidas |
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| WO (1) | WO2005021548A2 (OSRAM) |
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| JP4514452B2 (ja) * | 2001-10-01 | 2010-07-28 | ユニバーシティ オブ バージニア パテント ファウンデーション | Ａ２ａアゴニスト活性を有する２−プロピルアデノシン・アナログおよびその組成物 |
| US7317017B2 (en) * | 2002-11-08 | 2008-01-08 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US7205403B2 (en) * | 2002-02-01 | 2007-04-17 | King Pharmaceuticals Research And Development, Inc. | 8-Heteroaryl xanthine adenosine A2B receptor antagonists |
| CN101851238B (zh) * | 2003-08-25 | 2012-07-18 | 卓维斯医药品有限责任公司 | 取代的8-杂芳基黄嘌呤 |
| SG155182A1 (en) * | 2004-08-02 | 2009-09-30 | Univ Virginia | 2-propynyl adenosine analogs with modified 5æ-ribose groups having a2a agonist activity |
| TW200626153A (en) | 2004-09-20 | 2006-08-01 | Xenon Pharmaceuticals Inc | Heterocyclic derivatives and their use as therapeutic agents |
| MX2007003321A (es) | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
| MX2007003327A (es) | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa. |
| CN101084207A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途 |
| EP1804799B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| EP1807085B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| AR051094A1 (es) | 2004-09-20 | 2006-12-20 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| CN101083982A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 用于治疗硬脂酰CoA去饱和酶介导的疾病的杂环衍生物 |
| US7579348B2 (en) * | 2005-02-25 | 2009-08-25 | Pgxhealth, Llc | Derivatives of 8-substituted xanthines |
| WO2006091898A2 (en) * | 2005-02-25 | 2006-08-31 | Adenosine Therapeutics, Llc | Pyrazolyl substituted xanthines |
| WO2006091936A2 (en) * | 2005-02-25 | 2006-08-31 | Adenosine Therapeutics, Llc | Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines |
| GB0510141D0 (en) * | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B3 |
| BRPI0611187A2 (pt) | 2005-06-03 | 2010-08-24 | Xenon Pharmaceuticals Inc | derivados aminotiazàis como inibidores da estearoil-coa desaturase humana |
| JP5044823B2 (ja) * | 2005-06-16 | 2012-10-10 | ギリアード サイエンシーズ， インコーポレイテッド | Ａ２ｂアデノシンレセプターアンタゴニストのプロドラッグ |
| ES2270715B1 (es) | 2005-07-29 | 2008-04-01 | Laboratorios Almirall S.A. | Nuevos derivados de pirazina. |
| US7812025B2 (en) | 2005-08-12 | 2010-10-12 | Takeda Pharmaceutical Company Limited | Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder |
| US20070059740A1 (en) * | 2005-08-26 | 2007-03-15 | Linden Joel M | Method of targeting a2b adenosine receptor antagonist therapy |
| US7566401B2 (en) * | 2005-10-03 | 2009-07-28 | Kelm Mark A | Process for separating and isolating xanthines, individual polar protic monomers, and polar protic oligomers |
| ES2274712B1 (es) | 2005-10-06 | 2008-03-01 | Laboratorios Almirall S.A. | Nuevos derivados imidazopiridina. |
| US8178509B2 (en) * | 2006-02-10 | 2012-05-15 | University Of Virginia Patent Foundation | Method to treat sickle cell disease |
| GB0606774D0 (en) * | 2006-04-03 | 2006-05-10 | Novartis Ag | Organic compounds |
| CN101466382A (zh) | 2006-06-16 | 2009-06-24 | PGx健康有限责任公司 | 取代的8-[6-氨基-3-吡啶基]黄嘌呤 |
| US7884100B2 (en) * | 2006-06-16 | 2011-02-08 | Pgxhealth, Llc | Substituted 8-[6-amino-3-pyridyl]xanthines |
| US8188063B2 (en) * | 2006-06-19 | 2012-05-29 | University Of Virginia Patent Foundation | Use of adenosine A2A modulators to treat spinal cord injury |
| US8193200B2 (en) * | 2007-01-04 | 2012-06-05 | University Of Virginia Patent Foundation | Antagonists of A2B adenosine receptors for treatment of inflammatory bowel disease |
| RU2344137C1 (ru) * | 2007-07-18 | 2009-01-20 | Государственное образовательное учреждение высшего профессионального образования "БАШКИРСКИЙ ГОСУДАРСТВЕННЫЙ МЕДИЦИНСКИЙ УНИВЕРСИТЕТ Федерального Агентства по здравоохранению и социальному развитию" (ГОУ ВПО БГМУ РОСЗДРАВА) | Производные 8-амино-7-(2-гидроксипропил-1)-1,3-диметилксантина гидрохлорида, проявляющие гемореологическую активность |
| US7875608B2 (en) * | 2007-12-17 | 2011-01-25 | Thompson Robert D | Substituted 8-[6-amino-3pyridyl]xanthines |
| EP2268641B1 (en) | 2008-03-26 | 2014-09-03 | Advinus Therapeutics Pvt. Ltd. | Heterocyclic compounds as adenosine receptor antagonist |
| US20110118276A1 (en) * | 2008-07-16 | 2011-05-19 | Edward Leung | Methods of treating atherosclerosis |
| JP5765239B2 (ja) | 2009-03-13 | 2015-08-19 | アドヴィナス・セラピューティックス・リミテッド | 置換縮合ピリミジン化合物 |
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-
2004
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- 2004-08-20 CA CA2536553A patent/CA2536553C/en not_active Expired - Lifetime
- 2004-08-20 WO PCT/US2004/027133 patent/WO2005021548A2/en not_active Ceased
- 2004-08-20 NZ NZ545715A patent/NZ545715A/en not_active IP Right Cessation
- 2004-08-20 ES ES10012271.2T patent/ES2557310T3/es not_active Expired - Lifetime
- 2004-08-20 CN CN2004800314554A patent/CN1894250B/zh not_active Expired - Fee Related
- 2004-08-20 PT PT47817523T patent/PT1658291E/pt unknown
- 2004-08-20 AU AU2004268964A patent/AU2004268964B2/en not_active Ceased
- 2004-08-20 DK DK10012271.2T patent/DK2295434T3/en active
- 2004-08-20 BR BRPI0413922A patent/BRPI0413922B8/pt not_active IP Right Cessation
- 2004-08-20 RU RU2006109474/04A patent/RU2357969C2/ru active
- 2004-08-20 EP EP04781752.3A patent/EP1658291B1/en not_active Expired - Lifetime
- 2004-08-20 JP JP2006524755A patent/JP4769721B2/ja not_active Expired - Lifetime
- 2004-08-20 PL PL04781752T patent/PL1658291T3/pl unknown
- 2004-08-20 KR KR1020067003776A patent/KR101222364B1/ko not_active Expired - Fee Related
- 2004-08-20 EP EP10012271.2A patent/EP2295434B1/en not_active Expired - Lifetime
- 2004-08-20 US US10/923,592 patent/US7342006B2/en not_active Expired - Lifetime
- 2004-08-20 ES ES04781752.3T patent/ES2440467T3/es not_active Expired - Lifetime
- 2004-08-20 DK DK04781752.3T patent/DK1658291T3/da active
- 2004-08-25 AR ARP040103058A patent/AR045499A1/es not_active Application Discontinuation
- 2004-08-26 TW TW093125436A patent/TWI362390B/zh not_active IP Right Cessation
-
2006
- 2006-02-14 IL IL173723A patent/IL173723A/en active IP Right Grant
- 2006-03-22 ZA ZA200602333A patent/ZA200602333B/en unknown
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2007
- 2007-12-14 US US11/956,876 patent/US7732455B2/en not_active Expired - Lifetime
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2010
- 2010-04-19 US US12/762,711 patent/US20100273780A1/en not_active Abandoned
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