JP2005513020A5 - - Google Patents
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- Publication number
- JP2005513020A5 JP2005513020A5 JP2003544054A JP2003544054A JP2005513020A5 JP 2005513020 A5 JP2005513020 A5 JP 2005513020A5 JP 2003544054 A JP2003544054 A JP 2003544054A JP 2003544054 A JP2003544054 A JP 2003544054A JP 2005513020 A5 JP2005513020 A5 JP 2005513020A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cor
- halogen
- alkoxy
- hydroxy
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 7
- -1 2- (diethylamino) ethyl Chemical group 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000005157 alkyl carboxy group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 C*(C**)C(C*(C(***)=*1)C(*I)=C(*)C1=O)=O Chemical compound C*(C**)C(C*(C(***)=*1)C(*I)=C(*)C1=O)=O 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0127140.2A GB0127140D0 (en) | 2001-11-10 | 2001-11-10 | Novel compounds |
| PCT/EP2002/012506 WO2003042218A1 (en) | 2001-11-10 | 2002-11-08 | Novel compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005513020A JP2005513020A (ja) | 2005-05-12 |
| JP2005513020A5 true JP2005513020A5 (enExample) | 2006-01-05 |
Family
ID=9925626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003544054A Pending JP2005513020A (ja) | 2001-11-10 | 2002-11-08 | 新規化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20050033052A1 (enExample) |
| EP (1) | EP1442043A1 (enExample) |
| JP (1) | JP2005513020A (enExample) |
| GB (1) | GB0127140D0 (enExample) |
| WO (1) | WO2003042218A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2014200542B2 (en) * | 2007-05-11 | 2016-08-25 | Rowan University | Methods of treatment and prevention of neurodegenerative diseases and disorders |
| US8962633B2 (en) * | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| US9029383B2 (en) | 2007-05-11 | 2015-05-12 | The Trustees Of The University Of Pennsylvania | Methods of treatment of skin ulcers |
| BRPI0721697A2 (pt) | 2007-05-11 | 2014-08-05 | Univ Jefferson | " métodos para tratar e/ou prevenir uma doença ou distúrbio neurodegenerativo em um indivíduo, para tratar e/ou prevenir um indivíduo com ou em risco de demência vascular, para tratar e/ou prevenir uma doença ou distúrbio associado com uma barreira hematoencefálica anormal em um indivíduo, para diminuir o acúmulo beta amilóide no cérebro de um indivíduo, para tratar e/ou prevenir mal de alzheimer em um indivíduo e para prevenir ou reduzir o risco de desenvolver mal de alzhheimer, e, uso de um agente que inibe a expressão e/ou atividade da proteína lp-pla2." |
| EA025527B1 (ru) * | 2007-05-11 | 2017-01-30 | Томас Джефферсон Юниверсити | Способы лечения и предупреждения нейродегенеративных заболеваний и нарушений |
| AU2011268127B2 (en) | 2010-06-18 | 2016-01-14 | Whitehead Institute For Biomedical Research | PLA2G16 as a target for antiviral compounds |
| US8637536B2 (en) | 2010-12-06 | 2014-01-28 | Glaxo Group Limited | Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by Lp-PLA2 |
| EP2651403B1 (en) | 2010-12-17 | 2020-12-02 | Glaxo Group Limited | Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases |
| US9273054B2 (en) | 2011-07-27 | 2016-03-01 | Glaxo Group Limited | Substituted pyrimido[1,6-a]pyrimidines as Lp-PLA2 inhibitors |
| EP2739627A4 (en) | 2011-07-27 | 2015-01-21 | Glaxo Group Ltd | 2,3-DIHYDROIMIDAZO- [1,2-C-] PYRIMIDIN-5 (1H) -ONE COMPOUNDS AS LP-PLA² INHIBITORS |
| JP2016505053A (ja) | 2013-01-25 | 2016-02-18 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｌｐ‐ＰＬＡ２の阻害剤としての二環式ピリミドン化合物 |
| WO2014114694A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors |
| CA2899124A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| WO2016012917A1 (en) | 2014-07-22 | 2016-01-28 | Glaxosmithkline Intellectual Property Development Limited | 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2 |
| WO2016012916A1 (en) | 2014-07-22 | 2016-01-28 | Glaxosmithkline Intellectual Property Development Limited | 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2 |
| CN111825695B (zh) * | 2019-04-15 | 2022-04-12 | 中国科学院上海药物研究所 | 噁唑烷酮类化合物、其制备方法、用途及其药物组合物 |
| CN114805389B (zh) | 2019-11-09 | 2023-08-29 | 上海赛默罗生物科技有限公司 | 三环二氢咪唑并嘧啶酮衍生物、其制备方法、药物组合物和用途 |
| CN115304620A (zh) | 2021-05-07 | 2022-11-08 | 上海赛默罗生物科技有限公司 | 嘧啶酮衍生物、其制备方法、药物组合物和用途 |
| JP2026516205A (ja) | 2023-04-18 | 2026-05-20 | サイニューロ セラピューティクス インコーポレイテッド | Ｌｐ－ｐｌａ２阻害剤と第２の薬剤の併用治療 |
| CN118221687B (zh) | 2023-07-17 | 2024-12-31 | 上海枢境生物科技有限公司 | 双环[5,6]咪唑嘧啶酮类衍生物、其制备方法和应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60139429D1 (de) * | 2000-02-16 | 2009-09-10 | Smithkline Beecham Plc | Pyrimidin-5-Onderivate als LDL-PLA2 Inhibitoren |
| GB0024807D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| GB0024808D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
-
2001
- 2001-11-10 GB GBGB0127140.2A patent/GB0127140D0/en not_active Ceased
-
2002
- 2002-11-08 EP EP02787608A patent/EP1442043A1/en not_active Withdrawn
- 2002-11-08 JP JP2003544054A patent/JP2005513020A/ja active Pending
- 2002-11-08 WO PCT/EP2002/012506 patent/WO2003042218A1/en not_active Ceased
- 2002-11-08 US US10/495,025 patent/US20050033052A1/en not_active Abandoned
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