JP2007536243A5 - - Google Patents
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- JP2007536243A5 JP2007536243A5 JP2007511494A JP2007511494A JP2007536243A5 JP 2007536243 A5 JP2007536243 A5 JP 2007536243A5 JP 2007511494 A JP2007511494 A JP 2007511494A JP 2007511494 A JP2007511494 A JP 2007511494A JP 2007536243 A5 JP2007536243 A5 JP 2007536243A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- phospholipase
- membered ring
- groups
- inhibitors
- 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
- 102000015439 Phospholipases Human genes 0.000 claims 38
- 108010064785 Phospholipases Proteins 0.000 claims 38
- ZIIUUSVHCHPIQD-UHFFFAOYSA-N 2,4,6-trimethyl-N-[3-(trifluoromethyl)phenyl]benzenesulfonamide Chemical compound CC1=CC(C)=CC(C)=C1S(=O)(=O)NC1=CC=CC(C(F)(F)F)=C1 ZIIUUSVHCHPIQD-UHFFFAOYSA-N 0.000 claims 32
- 239000003112 inhibitor Substances 0.000 claims 22
- 125000001424 substituent group Chemical group 0.000 claims 21
- 235000013305 food Nutrition 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000002837 carbocyclic group Chemical group 0.000 claims 16
- 230000000694 effects Effects 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 16
- 239000002253 acid Chemical group 0.000 claims 14
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 14
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 14
- 239000001301 oxygen Substances 0.000 claims 14
- 125000003342 alkenyl group Chemical group 0.000 claims 12
- 125000003277 amino group Chemical group 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 12
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 10
- 125000004442 acylamino group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 239000011593 sulfur Substances 0.000 claims 10
- 230000001419 dependent effect Effects 0.000 claims 9
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 230000002496 gastric effect Effects 0.000 claims 6
- 239000003428 phospholipase inhibitor Substances 0.000 claims 6
- 229910052698 phosphorus Inorganic materials 0.000 claims 6
- 239000011574 phosphorus Substances 0.000 claims 6
- 239000000126 substance Substances 0.000 claims 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 5
- 206010022489 Insulin Resistance Diseases 0.000 claims 4
- 208000008589 Obesity Diseases 0.000 claims 4
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 4
- -1 indole compound Chemical class 0.000 claims 4
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 4
- 235000020824 obesity Nutrition 0.000 claims 4
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims 4
- 239000003358 phospholipase A2 inhibitor Substances 0.000 claims 4
- 230000028327 secretion Effects 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 2
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 239000004367 Lipase Substances 0.000 claims 2
- 102000004882 Lipase Human genes 0.000 claims 2
- 108090001060 Lipase Proteins 0.000 claims 2
- 102000011720 Lysophospholipase Human genes 0.000 claims 2
- 108020002496 Lysophospholipase Proteins 0.000 claims 2
- 239000011575 calcium Substances 0.000 claims 2
- 229910052791 calcium Inorganic materials 0.000 claims 2
- 230000001925 catabolic effect Effects 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 230000037406 food intake Effects 0.000 claims 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 235000019421 lipase Nutrition 0.000 claims 2
- 210000004877 mucosa Anatomy 0.000 claims 2
- 150000002894 organic compounds Chemical class 0.000 claims 2
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims 2
- 150000008104 phosphatidylethanolamines Chemical class 0.000 claims 2
- 150000003904 phospholipids Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 210000002966 serum Anatomy 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 235000005911 diet Nutrition 0.000 claims 1
- 230000037213 diet Effects 0.000 claims 1
- 235000021069 high fat-high sugar diet Nutrition 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- 0 *C1C(*)C2C(*)C(*)C(*)C(*)C2C1* Chemical compound *C1C(*)C2C(*)C(*)C(*)C(*)C2C1* 0.000 description 6
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/838,879 US20050244367A1 (en) | 2004-05-03 | 2004-05-03 | Phospholipase inhibitors localized in the gastrointestinal lumen |
| PCT/US2005/015281 WO2005112953A2 (en) | 2004-05-03 | 2005-05-03 | Treatment of hypercholesterolemia, hypertriglyceridemia and cardiovascular-related conditions using phosphalipase-a2 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007536243A JP2007536243A (ja) | 2007-12-13 |
| JP2007536243A5 true JP2007536243A5 (enExample) | 2008-06-19 |
Family
ID=35187321
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007511494A Pending JP2007536243A (ja) | 2004-05-03 | 2005-05-03 | ホスホリパーゼ−ａ２阻害薬を用いた、高コレステロール血症、高トリグリセリド血症、心臓血管疾患の治療 |
| JP2007511528A Pending JP2007536249A (ja) | 2004-05-03 | 2005-05-03 | 消化器官管腔集中性ホスホリパーゼ阻害薬 |
| JP2007511527A Pending JP2007538009A (ja) | 2004-05-03 | 2005-05-03 | インドールおよび関連化合物から成るホスホリパーゼ−ａ２阻害薬を用いた、食事関連疾患の治療 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007511528A Pending JP2007536249A (ja) | 2004-05-03 | 2005-05-03 | 消化器官管腔集中性ホスホリパーゼ阻害薬 |
| JP2007511527A Pending JP2007538009A (ja) | 2004-05-03 | 2005-05-03 | インドールおよび関連化合物から成るホスホリパーゼ−ａ２阻害薬を用いた、食事関連疾患の治療 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US20050244367A1 (enExample) |
| EP (3) | EP1750730A4 (enExample) |
| JP (3) | JP2007536243A (enExample) |
| CA (3) | CA2565448A1 (enExample) |
| WO (3) | WO2005112646A2 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7666898B2 (en) | 2005-11-03 | 2010-02-23 | Ilypsa, Inc. | Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors |
| AU2006311765A1 (en) * | 2005-11-03 | 2007-05-18 | Ilypsa, Inc. | Phospholipase inhibitors, including multi-valent phospholipase inhibitors, and use thereof, including as lumen-localized phospholipase inhibitors |
| BRPI0717943A2 (pt) * | 2006-10-31 | 2013-10-29 | Wyeth Corp | Composição farmacêutica; forma de dosagem farmacêutica; processo para a preparação de uma composição farmacêutica; e produto preparado pelo processo |
| WO2008055148A2 (en) * | 2006-10-31 | 2008-05-08 | Wyeth | Semi-solid formulations of phospholipase enzyme inhibitors |
| WO2009082491A1 (en) * | 2007-12-26 | 2009-07-02 | Alp Life Sciences, Llc | Nanovesontm: treatment, biomarkers and diagnostic tests for liver diseases and comorbid diseases |
| US20090197955A1 (en) * | 2008-01-31 | 2009-08-06 | Monsanto Company | Methods of improving dha deposition and related function and/or development |
| EP3578177A1 (en) | 2008-09-02 | 2019-12-11 | Amarin Pharmaceuticals Ireland Limited | Pharmaceutical composition comprising eicosapentaenoic acid and nicotinic acid and methods of using same |
| WO2018129556A1 (en) | 2017-01-09 | 2018-07-12 | Ardelyx, Inc. | Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders |
| JP5502106B2 (ja) | 2008-12-31 | 2014-05-28 | アーデリクス，インコーポレーテッド | 体液貯留または塩分過負荷と関連する障害および消化管障害の治療におけるｎｈｅ媒介性アンチポートを阻害するための組成物および方法 |
| MX2011011517A (es) | 2009-04-29 | 2012-06-19 | Amarin Corp Plc | Composiciones farmaceuticas que comprenden epa y un agente cardiovascular y metodos para utilizar el mismo. |
| CN102458109B (zh) | 2009-04-29 | 2015-02-11 | 阿马里纳制药公司 | 稳定的药物组合物和使用其的方法 |
| LT2443246T (lt) | 2009-06-15 | 2018-03-26 | Amarin Pharmaceuticals Ireland Limited | Kompozicijos ir būdai, skirti trigliceridų sumažinimui, nepakeliant ldl-c lygio subjekte, kartu taikant statino terapiją |
| US20110071176A1 (en) | 2009-09-23 | 2011-03-24 | Amarin Pharma, Inc. | Pharmaceutical composition comprising omega-3 fatty acid and hydroxy-derivative of a statin and methods of using same |
| US11712429B2 (en) | 2010-11-29 | 2023-08-01 | Amarin Pharmaceuticals Ireland Limited | Low eructation composition and methods for treating and/or preventing cardiovascular disease in a subject with fish allergy/hypersensitivity |
| AU2011336856A1 (en) | 2010-11-29 | 2013-07-04 | Amarin Pharmaceuticals Ireland Limited | Low eructation composition and methods for treating and/or preventing cardiovascular disease in a subject with fish allergy/hypersensitivity |
| US20130131170A1 (en) | 2011-11-07 | 2013-05-23 | Amarin Pharmaceuticals Ireland Limited | Methods of treating hypertriglyceridemia |
| US11291643B2 (en) | 2011-11-07 | 2022-04-05 | Amarin Pharmaceuticals Ireland Limited | Methods of treating hypertriglyceridemia |
| WO2013103958A1 (en) | 2012-01-06 | 2013-07-11 | Amarin Pharmaceuticals Ireland Limited | Compositions and methods for lowering levels of high-sensitivity (hs-crp) in a subject |
| BR112014032905B1 (pt) | 2012-06-29 | 2022-02-22 | Amarin Pharmaceuticals Ireland Limited | Uso de éster etílico do ácido eicosapentaenóico para redução do risco de morte cardiovascular, revascularização coronária e/ou angina instável em um indivíduo em terapia com estatina |
| US10376481B2 (en) | 2012-08-21 | 2019-08-13 | Ardelyx, Inc. | Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders |
| KR102138390B1 (ko) | 2012-08-21 | 2020-07-27 | 알데릭스, 인코포레이티드 | 체액 저류 또는 염 과부하와 연관된 장애 및 위장관 장애의 치료에서 ｎｈｅ-매개된 역수송 저해를 위한 화합물 및 방법 |
| US20150265566A1 (en) | 2012-11-06 | 2015-09-24 | Amarin Pharmaceuticals Ireland Limited | Compositions and Methods for Lowering Triglycerides without Raising LDL-C Levels in a Subject on Concomitant Statin Therapy |
| US20140187633A1 (en) | 2012-12-31 | 2014-07-03 | Amarin Pharmaceuticals Ireland Limited | Methods of treating or preventing nonalcoholic steatohepatitis and/or primary biliary cirrhosis |
| US9814733B2 (en) | 2012-12-31 | 2017-11-14 | A,arin Pharmaceuticals Ireland Limited | Compositions comprising EPA and obeticholic acid and methods of use thereof |
| US9452151B2 (en) | 2013-02-06 | 2016-09-27 | Amarin Pharmaceuticals Ireland Limited | Methods of reducing apolipoprotein C-III |
| US9624492B2 (en) | 2013-02-13 | 2017-04-18 | Amarin Pharmaceuticals Ireland Limited | Compositions comprising eicosapentaenoic acid and mipomersen and methods of use thereof |
| US9662307B2 (en) | 2013-02-19 | 2017-05-30 | The Regents Of The University Of Colorado | Compositions comprising eicosapentaenoic acid and a hydroxyl compound and methods of use thereof |
| US9283201B2 (en) | 2013-03-14 | 2016-03-15 | Amarin Pharmaceuticals Ireland Limited | Compositions and methods for treating or preventing obesity in a subject in need thereof |
| US20140271841A1 (en) | 2013-03-15 | 2014-09-18 | Amarin Pharmaceuticals Ireland Limited | Pharmaceutical composition comprising eicosapentaenoic acid and derivatives thereof and a statin |
| KR102287207B1 (ko) | 2013-04-12 | 2021-08-09 | 알데릭스, 인코포레이티드 | Nhe3-결합 화합물 및 포스페이트 수송을 저해하는 방법 |
| US10966968B2 (en) | 2013-06-06 | 2021-04-06 | Amarin Pharmaceuticals Ireland Limited | Co-administration of rosiglitazone and eicosapentaenoic acid or a derivative thereof |
| US20150065572A1 (en) | 2013-09-04 | 2015-03-05 | Amarin Pharmaceuticals Ireland Limited | Methods of treating or preventing prostate cancer |
| US9585859B2 (en) | 2013-10-10 | 2017-03-07 | Amarin Pharmaceuticals Ireland Limited | Compositions and methods for lowering triglycerides without raising LDL-C levels in a subject on concomitant statin therapy |
| US10561631B2 (en) | 2014-06-11 | 2020-02-18 | Amarin Pharmaceuticals Ireland Limited | Methods of reducing RLP-C |
| US10172818B2 (en) | 2014-06-16 | 2019-01-08 | Amarin Pharmaceuticals Ireland Limited | Methods of reducing or preventing oxidation of small dense LDL or membrane polyunsaturated fatty acids |
| US10406130B2 (en) | 2016-03-15 | 2019-09-10 | Amarin Pharmaceuticals Ireland Limited | Methods of reducing or preventing oxidation of small dense LDL or membrane polyunsaturated fatty acids |
| CN107684550B (zh) * | 2016-08-03 | 2020-04-10 | 徐天宏 | 糖尿病治疗产品及其制备与应用 |
| CA3049679A1 (en) | 2017-01-09 | 2018-07-12 | Ardelyx, Inc. | Inhibitors of nhe-mediated antiport |
| UA126283C2 (uk) | 2017-01-09 | 2022-09-14 | Арделікс, Інк. | Сполуки, придатні для лікування розладів шлунково-кишкового тракту |
| WO2018213663A1 (en) | 2017-05-19 | 2018-11-22 | Amarin Pharmaceuticals Ireland Limited | Compositions and methods for lowering triglycerides in a subject having reduced kidney function |
| MX2020001412A (es) | 2017-08-04 | 2020-08-03 | Ardelyx Inc | Compuestos y métodos para tratar la hiperpotasemia. |
| US11058661B2 (en) | 2018-03-02 | 2021-07-13 | Amarin Pharmaceuticals Ireland Limited | Compositions and methods for lowering triglycerides in a subject on concomitant statin therapy and having hsCRP levels of at least about 2 mg/L |
| MA51766A (fr) | 2018-09-24 | 2020-12-16 | Amarin Pharmaceuticals Ie Ltd | Procédés de réduction du risque d'événements cardiovasculaires chez un sujet |
| JP7735185B2 (ja) | 2019-02-07 | 2025-09-08 | アルデリックス， インコーポレイテッド | 高カリウム血症の治療で使用するためのグリチルレチン酸誘導体 |
| EP3972599B1 (en) | 2019-05-21 | 2025-10-22 | Ardelyx, Inc. | Combination for lowering serum phosphate in a patient |
| CN114980973A (zh) | 2019-11-12 | 2022-08-30 | 阿马里纳药物爱尔兰有限公司 | 降低心房纤颤和/或心房扑动受试者心血管事件风险的方法 |
| AU2022263358A1 (en) | 2021-04-21 | 2023-11-30 | Amarin Pharmaceuticals Ireland Limited | Methods of reducing the risk of heart failure |
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2004
- 2004-05-03 US US10/838,879 patent/US20050244367A1/en not_active Abandoned
-
2005
- 2005-05-03 EP EP05779968A patent/EP1750730A4/en not_active Withdrawn
- 2005-05-03 WO PCT/US2005/015416 patent/WO2005112646A2/en not_active Ceased
- 2005-05-03 CA CA002565448A patent/CA2565448A1/en not_active Abandoned
- 2005-05-03 EP EP05779544A patent/EP1750699A4/en not_active Withdrawn
- 2005-05-03 JP JP2007511494A patent/JP2007536243A/ja active Pending
- 2005-05-03 US US11/579,251 patent/US20070292385A1/en not_active Abandoned
- 2005-05-03 US US11/579,253 patent/US20080021049A1/en not_active Abandoned
- 2005-05-03 EP EP05741781A patent/EP1747003A4/en not_active Withdrawn
- 2005-05-03 WO PCT/US2005/015418 patent/WO2005107766A1/en not_active Ceased
- 2005-05-03 WO PCT/US2005/015281 patent/WO2005112953A2/en not_active Ceased
- 2005-05-03 CA CA002565416A patent/CA2565416A1/en not_active Abandoned
- 2005-05-03 JP JP2007511528A patent/JP2007536249A/ja active Pending
- 2005-05-03 CA CA002565384A patent/CA2565384A1/en not_active Abandoned
- 2005-05-03 JP JP2007511527A patent/JP2007538009A/ja active Pending
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