JP2011518828A5 - - Google Patents
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- JP2011518828A5 JP2011518828A5 JP2011506352A JP2011506352A JP2011518828A5 JP 2011518828 A5 JP2011518828 A5 JP 2011518828A5 JP 2011506352 A JP2011506352 A JP 2011506352A JP 2011506352 A JP2011506352 A JP 2011506352A JP 2011518828 A5 JP2011518828 A5 JP 2011518828A5
- Authority
- JP
- Japan
- Prior art keywords
- pai
- medicament
- compound
- combinations
- group
- 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
- 239000003814 drug Substances 0.000 claims description 37
- -1 SK-116 Chemical compound 0.000 claims description 32
- 102000012335 Plasminogen Activator Inhibitor 1 Human genes 0.000 claims description 29
- 108010022233 Plasminogen Activator Inhibitor 1 Proteins 0.000 claims description 29
- 229940079593 drug Drugs 0.000 claims description 15
- ASGMFNBUXDJWJJ-JLCFBVMHSA-N (1R,3R)-3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethylcyclopentane-1-carboxamide Chemical compound BrC1=NN(C2=NC(=NC=C21)N[C@H]1C[C@@](CC1)(C(=O)NC)C)C1=CC=C(C=C1)C=1SC(=NN=1)C ASGMFNBUXDJWJJ-JLCFBVMHSA-N 0.000 claims description 12
- DQYBRTASHMYDJG-UHFFFAOYSA-N Bisindolylmaleimide Chemical compound C1=CC=C2C(C=3C(=O)NC(C=3C=3C4=CC=CC=C4NC=3)=O)=CNC2=C1 DQYBRTASHMYDJG-UHFFFAOYSA-N 0.000 claims description 12
- 229940127007 Compound 39 Drugs 0.000 claims description 12
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 102000003978 Tissue Plasminogen Activator Human genes 0.000 claims description 10
- 108090000373 Tissue Plasminogen Activator Proteins 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 10
- 229960000187 tissue plasminogen activator Drugs 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 9
- 230000005764 inhibitory process Effects 0.000 claims description 9
- 101100256985 Arabidopsis thaliana SIS3 gene Proteins 0.000 claims description 8
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims description 8
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims description 8
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims description 8
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims description 8
- QHKYPYXTTXKZST-UHFFFAOYSA-N SB-202190 Chemical compound C1=CC(O)=CC=C1C1=NC(C=2C=CC(F)=CC=2)=C(C=2C=CN=CC=2)N1 QHKYPYXTTXKZST-UHFFFAOYSA-N 0.000 claims description 8
- CDKIEBFIMCSCBB-CALJPSDSSA-N SIS3 Chemical compound Cl.C1C=2C=C(OC)C(OC)=CC=2CCN1C(=O)\C=C\C(C1=CC=CN=C1N1C)=C1C1=CC=CC=C1 CDKIEBFIMCSCBB-CALJPSDSSA-N 0.000 claims description 8
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims description 8
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 8
- DVEXZJFMOKTQEZ-JYFOCSDGSA-N U0126 Chemical compound C=1C=CC=C(N)C=1SC(\N)=C(/C#N)\C(\C#N)=C(/N)SC1=CC=CC=C1N DVEXZJFMOKTQEZ-JYFOCSDGSA-N 0.000 claims description 8
- ACPOUJIDANTYHO-UHFFFAOYSA-N anthra[1,9-cd]pyrazol-6(2H)-one Chemical compound C1=CC(C(=O)C=2C3=CC=CC=2)=C2C3=NNC2=C1 ACPOUJIDANTYHO-UHFFFAOYSA-N 0.000 claims description 8
- 229960005370 atorvastatin Drugs 0.000 claims description 8
- 229960004844 lovastatin Drugs 0.000 claims description 8
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims description 8
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims description 8
- 229960002965 pravastatin Drugs 0.000 claims description 8
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims description 8
- 229940121649 protein inhibitor Drugs 0.000 claims description 8
- 239000012268 protein inhibitor Substances 0.000 claims description 8
- 229960002855 simvastatin Drugs 0.000 claims description 8
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims description 8
- 208000010412 Glaucoma Diseases 0.000 claims description 5
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 claims description 5
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 claims description 5
- FJLGEFLZQAZZCD-MCBHFWOFSA-N (3R,5S)-fluvastatin Chemical compound C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 FJLGEFLZQAZZCD-MCBHFWOFSA-N 0.000 claims description 4
- 208000022873 Ocular disease Diseases 0.000 claims description 4
- 239000000556 agonist Substances 0.000 claims description 4
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims description 4
- 239000002585 base Substances 0.000 claims description 4
- 239000002876 beta blocker Substances 0.000 claims description 4
- 229940097320 beta blocking agent Drugs 0.000 claims description 4
- 239000000872 buffer Substances 0.000 claims description 4
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 claims description 4
- 239000003623 enhancer Substances 0.000 claims description 4
- 229960003765 fluvastatin Drugs 0.000 claims description 4
- 239000003349 gelling agent Substances 0.000 claims description 4
- 230000002209 hydrophobic effect Effects 0.000 claims description 4
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 4
- 230000003547 miosis Effects 0.000 claims description 4
- 239000003604 miotic agent Substances 0.000 claims description 4
- 239000004090 neuroprotective agent Substances 0.000 claims description 4
- 230000035515 penetration Effects 0.000 claims description 4
- 239000003755 preservative agent Substances 0.000 claims description 4
- 150000003180 prostaglandins Chemical class 0.000 claims description 4
- 239000003590 rho kinase inhibitor Substances 0.000 claims description 4
- 239000011780 sodium chloride Substances 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 4
- 239000002562 thickening agent Substances 0.000 claims description 4
- 239000003981 vehicle Substances 0.000 claims description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 206010030043 Ocular hypertension Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 102000001938 Plasminogen Activators Human genes 0.000 description 1
- 108010001014 Plasminogen Activators Proteins 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 229940127126 plasminogen activator Drugs 0.000 description 1
- 229960005356 urokinase Drugs 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4817608P | 2008-04-26 | 2008-04-26 | |
| US61/048,176 | 2008-04-26 | ||
| US12/421,456 US20090202524A1 (en) | 2007-10-31 | 2009-04-09 | Pai-1 expression and activity inhibitors for the treatment of ocular disorders |
| US12/421,456 | 2009-04-09 | ||
| PCT/US2009/040149 WO2009131850A2 (en) | 2008-04-26 | 2009-04-10 | Pai-1 expression and activity inhibitors for the treatment of ocular disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011518828A JP2011518828A (ja) | 2011-06-30 |
| JP2011518828A5 true JP2011518828A5 (enExample) | 2013-03-14 |
Family
ID=40810596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011506352A Pending JP2011518828A (ja) | 2008-04-26 | 2009-04-10 | 眼球障害の処置のためのｐａｉ−１の発現および活性インヒビター |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20090202524A1 (enExample) |
| EP (1) | EP2296647A2 (enExample) |
| JP (1) | JP2011518828A (enExample) |
| KR (1) | KR20100135953A (enExample) |
| CN (1) | CN102046168A (enExample) |
| AR (1) | AR071393A1 (enExample) |
| CL (1) | CL2009000986A1 (enExample) |
| TW (1) | TW200946113A (enExample) |
| UY (1) | UY31786A1 (enExample) |
| WO (1) | WO2009131850A2 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005237543B2 (en) * | 2004-04-26 | 2011-02-10 | Alcon, Inc. | Statins for the treatment of ocular hypertension and glaucoma |
| US10946076B2 (en) | 2013-02-13 | 2021-03-16 | The Research Foundation For The State University Of New York | Glaucoma treatment |
| US9845363B2 (en) | 2013-08-13 | 2017-12-19 | Sanofi | Antibodies to plasminogen activator inhibitor-1 (PAI-1) and uses thereof |
| JP6730701B2 (ja) * | 2013-11-14 | 2020-07-29 | 学校法人同志社 | 細胞増殖促進または細胞障害抑制による角膜内皮治療薬 |
| EP3381472A4 (en) | 2015-12-24 | 2019-07-31 | The Doshisha | MEDICINAL PRODUCTS FOR THE TREATMENT OR PREVENTION OF DISTURBANCES CAUSED BY TGF SIGNALS AND USE THEREOF |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4214215A1 (de) * | 1992-04-30 | 1993-11-04 | Behringwerke Ag | Verwendung von inhibitoren von plasminogenaktivatoren zur behandlung von entzuendungen |
| CA2358400C (en) * | 1999-01-05 | 2012-05-15 | Nancy A. Noble | Methods for treating conditions associated with the accumulation of excess extracellular matrix |
| DE60221391T2 (de) * | 2001-06-20 | 2008-04-17 | Wyeth | Substituierte indolsäurederivate als inhibitoren von plasminogen-aktivator-inhibitor-1 (pai-1) |
| KR20040104566A (ko) * | 2002-04-30 | 2004-12-10 | 알콘, 인코퍼레이티드 | 안압 저하 및 녹내장성 망막병증/시신경병증 치료를 위한특유의 수단으로서의 결합 조직 성장 인자 (ｃｔｇｆ)의활성 및/또는 발현 조절, 저해, 또는 변조제 |
| WO2005053683A1 (en) * | 2003-11-26 | 2005-06-16 | Duke University | A method of preventing or treating glaucoma |
| AU2005237543B2 (en) * | 2004-04-26 | 2011-02-10 | Alcon, Inc. | Statins for the treatment of ocular hypertension and glaucoma |
| WO2006040839A1 (ja) * | 2004-10-15 | 2006-04-20 | Advanced Medicine Research Institute | 眼疾患処置用点眼剤及びキット |
| US7803824B2 (en) * | 2004-10-29 | 2010-09-28 | Alcon, Inc. | Use of inhibitors of Jun N-terminal kinases to treat glaucoma |
| US20060094753A1 (en) * | 2004-10-29 | 2006-05-04 | Alcon, Inc. | Use of inhibitors of Jun N-terminal kinases for the treatment of glaucomatous retinopathy and ocular diseases |
| US8969295B2 (en) * | 2006-04-14 | 2015-03-03 | Massachusetts Institute Of Technology | Identifying and modulating molecular pathways that mediate nervous system plasticity |
| AU2007313684A1 (en) * | 2006-10-31 | 2008-05-08 | Alcon Research, Ltd. | PAI-1 binding modulators for the treatment of ocular disorders |
-
2009
- 2009-04-09 US US12/421,456 patent/US20090202524A1/en not_active Abandoned
- 2009-04-10 KR KR1020107026494A patent/KR20100135953A/ko not_active Withdrawn
- 2009-04-10 CN CN2009801185568A patent/CN102046168A/zh active Pending
- 2009-04-10 JP JP2011506352A patent/JP2011518828A/ja active Pending
- 2009-04-10 WO PCT/US2009/040149 patent/WO2009131850A2/en not_active Ceased
- 2009-04-10 EP EP09735222A patent/EP2296647A2/en not_active Withdrawn
- 2009-04-21 TW TW098113153A patent/TW200946113A/zh unknown
- 2009-04-22 AR ARP090101418A patent/AR071393A1/es not_active Application Discontinuation
- 2009-04-24 UY UY31786A patent/UY31786A1/es not_active Application Discontinuation
- 2009-04-24 CL CL2009000986A patent/CL2009000986A1/es unknown
-
2011
- 2011-01-14 US US13/006,984 patent/US20110105574A1/en not_active Abandoned
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