WO1998043612B1 - Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma - Google Patents
Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucomaInfo
- Publication number
- WO1998043612B1 WO1998043612B1 PCT/US1998/005941 US9805941W WO9843612B1 WO 1998043612 B1 WO1998043612 B1 WO 1998043612B1 US 9805941 W US9805941 W US 9805941W WO 9843612 B1 WO9843612 B1 WO 9843612B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- sodium
- retinal ganglion
- composition
- blocker
- manufacture
- Prior art date
Links
- 208000010412 Glaucoma Diseases 0.000 title claims abstract 5
- 238000004519 manufacturing process Methods 0.000 title claims 5
- 239000003814 drug Substances 0.000 title claims 4
- 210000001328 Optic Nerve Anatomy 0.000 title abstract 3
- 230000004380 optic nerve Effects 0.000 title abstract 3
- 206010056677 Nerve degeneration Diseases 0.000 title 1
- 239000003195 sodium channel blocking agent Substances 0.000 title 1
- 210000003994 Retinal Ganglion Cells Anatomy 0.000 claims abstract 11
- 102000018674 Sodium Channels Human genes 0.000 claims abstract 9
- 108010052164 Sodium Channels Proteins 0.000 claims abstract 9
- 230000000903 blocking Effects 0.000 claims abstract 9
- 239000000203 mixture Substances 0.000 claims abstract 8
- 150000001875 compounds Chemical class 0.000 claims abstract 7
- 230000000415 inactivating Effects 0.000 claims abstract 6
- 241000124008 Mammalia Species 0.000 claims abstract 4
- 230000030833 cell death Effects 0.000 claims abstract 4
- 210000004027 cells Anatomy 0.000 claims abstract 2
- 239000011734 sodium Substances 0.000 claims 8
- 229910052708 sodium Inorganic materials 0.000 claims 8
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 7
- HTDFEXRUDGWNHA-UHFFFAOYSA-N 1-benzhydryl-4-[[5-methyl-2-(4-methylphenyl)-1H-imidazol-4-yl]methyl]piperazine Chemical compound CC=1NC(C=2C=CC(C)=CC=2)=NC=1CN(CC1)CCN1C(C=1C=CC=CC=1)C1=CC=CC=C1 HTDFEXRUDGWNHA-UHFFFAOYSA-N 0.000 claims 3
- 229950003413 Lifarizine Drugs 0.000 claims 3
- FTALBRSUTCGOEG-UHFFFAOYSA-N Riluzole Chemical compound C1=C(OC(F)(F)F)C=C2SC(N)=NC2=C1 FTALBRSUTCGOEG-UHFFFAOYSA-N 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229960004181 riluzole Drugs 0.000 claims 3
- 208000003098 Ganglion Cysts Diseases 0.000 claims 2
- 229940054534 Ophthalmic Solution Drugs 0.000 claims 2
- 208000005400 Synovial Cyst Diseases 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000002997 ophthalmic solution Substances 0.000 claims 2
- 206010002660 Anoxia Diseases 0.000 claims 1
- 241000976983 Anoxia Species 0.000 claims 1
- 102000003922 Calcium Channels Human genes 0.000 claims 1
- 108090000312 Calcium Channels Proteins 0.000 claims 1
- 239000003416 antiarrhythmic agent Substances 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000003834 intracellular Effects 0.000 claims 1
- 210000002569 neurons Anatomy 0.000 claims 1
- 230000000324 neuroprotective Effects 0.000 claims 1
- 230000002207 retinal Effects 0.000 claims 1
- 235000020945 retinal Nutrition 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- FKNQFGJONOIPTF-UHFFFAOYSA-N sodium cation Chemical compound [Na+] FKNQFGJONOIPTF-UHFFFAOYSA-N 0.000 abstract 5
- 229910001415 sodium ion Inorganic materials 0.000 abstract 5
- 231100000518 lethal Toxicity 0.000 abstract 2
- 230000001665 lethal Effects 0.000 abstract 2
- 230000004941 influx Effects 0.000 abstract 1
- 230000028161 membrane depolarization Effects 0.000 abstract 1
- 230000001575 pathological Effects 0.000 abstract 1
- 230000002441 reversible Effects 0.000 abstract 1
Abstract
A method and composition for altering a plausible sequence of pathological events in retinal ganglion cells associated with glaucoma, the sequence including membrane depolarization, influx of millimolar amounts of Na+ via non-inactivating Na+ channels, and the lethal elevation of cell Ca2+ due to reversal of the Na+ exchanger. The method includes blocking, by administration of a selected composition, of associated, non-inactivating Na+ channels in retinal ganglion cells in order to limit Na+/Ca2+ exchange in the retinal ganglion cells and prevent buildup of the Ca2+ level in the retinal ganglion cells to a lethal level. The results in a method of preventing retinal ganglion cell death, associated with glaucoma, by administering to the optic nerve of a mammal, a compound which blocks the non-inactivating sodium ion channels of the optic nerve. Alternately, said invention relates to a method of preventing optic retinal ganglion cell death in a human by administering to the retinal ganglion cells of said human a compound which blocks the non-inactivating sodium ion channel of the retinal ganglion cells.
Claims
1. The use of a sodium blocker in the manufacture of a medicament for maintaining normal intracellular Na and Ca in ganglion cells following a period of anoxia, the sodium blocker comprising a composition for blocking of noninactivating calcium channel activity in the retinal ganglion neuronal cells.
2. The use according to claim 1 wherein the composition for blocking non-inactivating sodium channels is selected from the group comprising of benzothialzole riluzole, lubelezole, phenyl benzothiozole and lifarizine.
3. The use according to claim 2 wherein the composition having noninactivating sodium channel blocking activity comprises an antiarrhythmic agent.
4. The use according to claim 1 wherein the composition comprises an ophthalmic solution adapted for administration to the eye of a mammal in the form of intracameral injection.
5. The use of a sodium blocker in the manufacture of a pharmaceutical composition useful for preventing retinal ganglion cell death, associated with glaucoma, in the eye of a mammal, the composition comprising as its active ingredient one or more compounds having noninactivating sodium channel blocking activity.
6. The use according to claim 5 wherein the compound having noninactivating sodium channel blocking activity is selected from the group consisting of benzothialzole riluzole, lubelezole, phenyl benzothiozole and lifarizine.
7. The use according to claim 5 where the composition is an ophthalmic solution, adapted for administration to
18
the eye of a mammal in the form of an intracameral injection.
8. The use of a sodium blocker in the manufacture of a medicament for preventing retinal ganglion cell death, associated with glaucoma, in an animal of the mammalian species, including humans, the sodium blocker pharmaceutical composition which comprises as its active ingredient one or more compounds having noninactivating sodium channel blocking activity.
9. The use of a sodium blocker in the manufacture of a medicament for providing neuroprotective effect to retinal ganglion cells in the eye of a human, the sodium blocker comprising a pharmaceutical composition which comprises as its active ingredient one or more compounds having noninactivating sodium channel blocking activity.
10. The use according to claim 9 wherein the compound having non-inactivating sodium channel blocking activity is selected from the group consisting of benzothialzole riluzole, lubelezole, phenyl benzothiozole and lifarizine.
Priority Applications (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BR9807895-0A BR9807895A (en) | 1997-03-27 | 1998-03-26 | Use of the sodium channel blocker in the manufacture of a medication for the prevention of optic nerve degeneration associated with glaucoma. |
| KR1019997008435A KR100610997B1 (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
| JP54179498A JP2001521500A (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blockers in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
| AU67762/98A AU734432B2 (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
| NZ337604A NZ337604A (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker for preventing optic nerve degeneration associated with glaucoma |
| EP98913141A EP0973500A1 (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
| IL13200198A IL132001A (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
| CA002284940A CA2284940A1 (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
| NO994674A NO994674L (en) | 1997-03-27 | 1999-09-24 | Use of sodium channel blocker for the manufacture of a medicament for the prevention of optic nerve degeneration associated with glaucoma |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/827,194 US5922746A (en) | 1997-03-27 | 1997-03-27 | Inhibition of noninactivating Na channels of mammalian optic nerve as a means of preventing optic nerve degeneration associated with glaucoma |
| US08/827,194 | 1997-03-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO1998043612A1 WO1998043612A1 (en) | 1998-10-08 |
| WO1998043612B1 true WO1998043612B1 (en) | 1998-11-12 |
Family
ID=25248552
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1998/005941 WO1998043612A1 (en) | 1997-03-27 | 1998-03-26 | Use of sodium channel blocker in the manufacture of a medicament for preventing optic nerve degeneration associated with glaucoma |
Country Status (13)
| Country | Link |
|---|---|
| US (6) | US5922746A (en) |
| EP (1) | EP0973500A1 (en) |
| JP (1) | JP2001521500A (en) |
| KR (1) | KR100610997B1 (en) |
| CN (1) | CN1251520A (en) |
| AU (1) | AU734432B2 (en) |
| BR (1) | BR9807895A (en) |
| CA (1) | CA2284940A1 (en) |
| HU (1) | HUP0001268A2 (en) |
| IL (1) | IL132001A (en) |
| NO (1) | NO994674L (en) |
| NZ (1) | NZ337604A (en) |
| WO (1) | WO1998043612A1 (en) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001041756A2 (en) * | 1999-12-02 | 2001-06-14 | University Of South Florida | Method and composition for treatment of ischemic neuronal reperfusion injury |
| GB0002666D0 (en) | 2000-02-04 | 2000-03-29 | Univ London | Blockade of voltage dependent sodium channels |
| US20060013814A1 (en) * | 2000-08-29 | 2006-01-19 | Davies Collison Cave | Methods for preventing pressure-induced apoptotic neural-cell death |
| WO2002042842A2 (en) * | 2000-11-22 | 2002-05-30 | Allergan, Inc. | A high-throughput screen for identifying channel blockers that selectively distinguish transient from persistent sodium channels |
| US6479458B1 (en) * | 2001-11-08 | 2002-11-12 | Allergan, Inc. | Targeting the reverse mode of the Na+/Ca2+ exchanger for the treatment of optic neuropathy associated with glaucoma and ischemic optic neuropathy |
| US7361478B2 (en) * | 2001-11-20 | 2008-04-22 | Allergan, Inc. | High-throughput screen for identifying selective persistent sodium channels channel blockers |
| US20040058313A1 (en) * | 2002-04-24 | 2004-03-25 | Abreu Marcio Marc | Compositions, targets, methods and devices for the therapy of ocular and periocular disorders |
| WO2004093814A2 (en) * | 2003-04-22 | 2004-11-04 | Pharmacia Corporation | Compositions of a cyclooxygenase-2 selective inhibitor and a sodium channel blocker |
| US7125908B2 (en) * | 2003-08-29 | 2006-10-24 | Allergan, Inc. | Treating pain using selective antagonists of persistent sodium current |
| BRPI0413920A (en) * | 2003-08-29 | 2006-10-24 | Allergan Inc | selective persistent sodium current antagonists to treat neurological disorders and pain |
| US7060723B2 (en) | 2003-08-29 | 2006-06-13 | Allergan, Inc. | Treating neurological disorders using selective antagonists of persistent sodium current |
| CA2661448A1 (en) | 2005-08-25 | 2007-03-01 | Steven Michael Weiss | Reducing myocardial damage and the incidence of arrhythmia arising from loss, reduction or interruption in coronary blood flow |
| WO2016100209A1 (en) * | 2014-12-15 | 2016-06-23 | The Children's Medical Center Corporation | Non-toxic topical anesthetic ophthalmic compositions |
| US10791651B2 (en) | 2016-05-31 | 2020-09-29 | Carbice Corporation | Carbon nanotube-based thermal interface materials and methods of making and using thereof |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06172176A (en) * | 1992-12-03 | 1994-06-21 | Rohto Pharmaceut Co Ltd | Intraocular tension depressant with azimarin as essential ingredient |
| FR2702148B1 (en) * | 1993-03-05 | 1995-04-07 | Rhone Poulenc Rorer Sa | Application of anti-convulsants in the treatment of neuro-AIDS. |
| GB9326010D0 (en) * | 1993-12-21 | 1994-02-23 | Sandoz Ltd | Improvements in or relating to organic compounds |
| FR2714828B1 (en) * | 1994-01-12 | 1996-02-02 | Rhone Poulenc Rorer Sa | Application of riluzole in the treatment of mitochondrial diseases. |
| JPH09510961A (en) * | 1994-01-14 | 1997-11-04 | ジュニア シャヒニアン，リー | Methods of persistent and long-term corneal analgesia |
-
1997
- 1997-03-27 US US08/827,194 patent/US5922746A/en not_active Expired - Fee Related
-
1998
- 1998-03-26 HU HU0001268A patent/HUP0001268A2/en unknown
- 1998-03-26 KR KR1019997008435A patent/KR100610997B1/en not_active IP Right Cessation
- 1998-03-26 EP EP98913141A patent/EP0973500A1/en not_active Withdrawn
- 1998-03-26 AU AU67762/98A patent/AU734432B2/en not_active Ceased
- 1998-03-26 BR BR9807895-0A patent/BR9807895A/en not_active Application Discontinuation
- 1998-03-26 WO PCT/US1998/005941 patent/WO1998043612A1/en active IP Right Grant
- 1998-03-26 IL IL13200198A patent/IL132001A/en active IP Right Grant
- 1998-03-26 NZ NZ337604A patent/NZ337604A/en unknown
- 1998-03-26 JP JP54179498A patent/JP2001521500A/en not_active Ceased
- 1998-03-26 CN CN98803734A patent/CN1251520A/en active Pending
- 1998-03-26 CA CA002284940A patent/CA2284940A1/en not_active Abandoned
-
1999
- 1999-03-22 US US09/273,832 patent/US6326389B1/en not_active Expired - Fee Related
- 1999-09-24 NO NO994674A patent/NO994674L/en not_active Application Discontinuation
-
2001
- 2001-08-21 US US09/935,554 patent/US6420402B2/en not_active Expired - Fee Related
- 2001-09-14 US US09/952,733 patent/US6426358B1/en not_active Expired - Fee Related
- 2001-12-12 US US10/017,660 patent/US20020137777A1/en not_active Abandoned
-
2002
- 2002-04-03 US US10/116,492 patent/US20020183368A1/en not_active Abandoned
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