CA2622975A1 - Adenosine a3 receptor agonists for the treatment of dry eye disorders - Google Patents
Adenosine a3 receptor agonists for the treatment of dry eye disorders Download PDFInfo
- Publication number
- CA2622975A1 CA2622975A1 CA002622975A CA2622975A CA2622975A1 CA 2622975 A1 CA2622975 A1 CA 2622975A1 CA 002622975 A CA002622975 A CA 002622975A CA 2622975 A CA2622975 A CA 2622975A CA 2622975 A1 CA2622975 A1 CA 2622975A1
- Authority
- CA
- Canada
- Prior art keywords
- dry eye
- agonist
- adenosine
- eye
- a3ar
- 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.)
- Granted
Links
- 208000003556 Dry Eye Syndromes Diseases 0.000 title claims abstract 10
- 206010013774 Dry eye Diseases 0.000 title claims abstract 10
- 239000002593 adenosine A3 receptor agonist Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 101150046889 ADORA3 gene Proteins 0.000 claims abstract 10
- 238000000034 method Methods 0.000 claims abstract 10
- 239000000556 agonist Substances 0.000 claims abstract 9
- 239000000203 mixture Substances 0.000 claims abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 238000011200 topical administration Methods 0.000 claims 4
- HUJXGQILHAUCCV-MOROJQBDSA-N 3-iodobenzyl-5'-N-methylcarboxamidoadenosine Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NC)O[C@H]1N1C2=NC=NC(NCC=3C=C(I)C=CC=3)=C2N=C1 HUJXGQILHAUCCV-MOROJQBDSA-N 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- IPSYPUKKXMNCNQ-PFHKOEEOSA-N (2s,3s,4r,5r)-5-[2-chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-n-methyloxolane-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NC)O[C@H]1N1C2=NC(Cl)=NC(NCC=3C=C(I)C=CC=3)=C2N=C1 IPSYPUKKXMNCNQ-PFHKOEEOSA-N 0.000 claims 2
- XTPOZVLRZZIEBW-SCFUHWHPSA-N (2r,3r,4s,5r)-2-[6-[2-(4-aminophenyl)ethylamino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol Chemical compound C1=CC(N)=CC=C1CCNC1=NC=NC2=C1N=CN2[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 XTPOZVLRZZIEBW-SCFUHWHPSA-N 0.000 claims 1
- LDYMCRRFCMRFKB-MOROJQBDSA-N (2s,3s,4r,5r)-5-[6-[(4-aminophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-n-methyloxolane-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NC)O[C@H]1N1C2=NC=NC(NCC=3C=CC(N)=CC=3)=C2N=C1 LDYMCRRFCMRFKB-MOROJQBDSA-N 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- 206010015958 Eye pain Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 206010047513 Vision blurred Diseases 0.000 claims 1
- 208000008784 apnea Diseases 0.000 claims 1
- MWEQTWJABOLLOS-UHFFFAOYSA-L disodium;[[[5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-oxidophosphoryl] hydrogen phosphate;trihydrate Chemical compound O.O.O.[Na+].[Na+].C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP([O-])(=O)OP(O)([O-])=O)C(O)C1O MWEQTWJABOLLOS-UHFFFAOYSA-L 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004356 excessive tearing Diseases 0.000 claims 1
- 230000007794 irritation Effects 0.000 claims 1
- 230000007803 itching Effects 0.000 claims 1
- 230000035807 sensation Effects 0.000 claims 1
- 208000032023 Signs and Symptoms Diseases 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Abstract
The present invention concerns methods and compositions for treating dry eye.
The method comprises providing an individual exhibiting ophthalmologic clinical symptoms and signs of dry eye with an A3 adenosine receptor (A3AR) agonist. The A3AR agonist is preferably administered to the subject either topically or orally.
The method comprises providing an individual exhibiting ophthalmologic clinical symptoms and signs of dry eye with an A3 adenosine receptor (A3AR) agonist. The A3AR agonist is preferably administered to the subject either topically or orally.
Claims (17)
1. A method for treating dry eye condition in an individual comprising administrating to said individual an amount of A3 adenosine receptor (A3AR) agonist, the amount being effective to ameliorate symptoms of dry eye in the individual.
2. The method of Claim 1, for treating dry eye syndrome.
3. The method of Claim 1, wherein said A3R agonist is orally administered.
4. The method of Claim 1, wherein said A3R agonist is topically administered to said individual.
5. The method of Claim 4, wherein said A3R agonist is administered to the eye.
6. The method of Claim 1, wherein said A3RAg is selected from N6-2- (4-aminophenyl)ethyladenosine (APNEA), N6-(4-amino-3-iodobenzyl) adenosine-5'-(N-methyluronamide) (AB-MECA), N6-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (IB-MECA) and 2-chloro-N6-(3-iodobenzyl)- adenosine-5'-N-methyluronamide (CI-IB-MECA).
7. The method of Claim 7, wherein said A3RAg is IB-MECA.
8. The method of Claim 1, wherein said ophthalmologic clinical symptoms is one selected from the group consisting of foreign body sensation, burning, itching, irritation, redness, eye pain, blurred vision, degraded vision and excessive tearing.
9. A pharmaceutical composition for treating a condition of dry eye, comprising an amount of an A3 adenosine receptor (A3AR) agonist and a pharmaceutically acceptable carrier, the amount of said A3AR agonist being effective to ameliorate symptoms of dry eye in the individual.
10. The composition of Claim 9, in a form suitable for oral administration.
11. The composition of Claim 9, in a form suitable for topical administration.
12. The composition of Claim 11, in a form suitable for topical administration to the eye.
13. Use of an A3 adenosine receptor (A3AR) agonist for the preparation of a pharmaceutical composition for treating dry eye condition.
14. The use of Claim 13, for treating dry eye syndrome.
15. The use of Claim 13, for the preparation of a pharmaceutical composition for oral administration.
16. The use of Claim 13, for the preparation of a pharmaceutical composition for topical administration.
17. The use of Claim 16, for the preparation of a pharmaceutical composition for topical administration to the eye.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US76250606P | 2006-01-27 | 2006-01-27 | |
| US60/762,506 | 2006-01-27 | ||
| PCT/IL2006/000130 WO2007086044A1 (en) | 2006-01-27 | 2006-02-01 | Adenosine a3 receptor agonists for the treatment of dry eye disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2622975A1 true CA2622975A1 (en) | 2007-08-02 |
| CA2622975C CA2622975C (en) | 2011-05-03 |
Family
ID=36794417
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2622975A Expired - Fee Related CA2622975C (en) | 2006-01-27 | 2006-02-01 | Adenosine a3 receptor agonists for the treatment of dry eye disorders |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1976494A1 (en) |
| JP (2) | JP5185139B2 (en) |
| KR (1) | KR101037095B1 (en) |
| CN (1) | CN101365430B (en) |
| AU (1) | AU2006336834B2 (en) |
| BR (1) | BRPI0621052A2 (en) |
| CA (1) | CA2622975C (en) |
| IL (1) | IL191271A (en) |
| WO (1) | WO2007086044A1 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008111082A1 (en) | 2007-03-14 | 2008-09-18 | Can-Fite Biopharma Ltd. | Process for the synthesis of ib-meca |
| IL184620A0 (en) * | 2007-07-15 | 2008-01-20 | Can Fite Biopharma Ltd | Composition for the treatment of inflammation |
| ES2531828T3 (en) | 2008-03-31 | 2015-03-20 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Purine derivatives as selective agonists of adenosine A3 receptors |
| US8916570B2 (en) | 2008-03-31 | 2014-12-23 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor agonists and antagonists |
| JP5431476B2 (en) | 2008-08-01 | 2014-03-05 | アメリカ合衆国 | A3 adenosine receptor antagonist and A3 adenosine receptor partial agonist |
| US9181253B2 (en) | 2008-08-01 | 2015-11-10 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Adenosine receptor agonists, partial agonists, and antagonists |
| CA2761499A1 (en) * | 2009-05-17 | 2010-11-25 | Can-Fite Biopharma Ltd. | A3 adenosine receptor agonists for the reduction of intraocular pressure |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5900407A (en) * | 1997-02-06 | 1999-05-04 | Inspire Pharmaceuticals, Inc. | Method of treating dry eye disease with uridine triphosphates and related compounds |
| JPH10158188A (en) * | 1996-11-29 | 1998-06-16 | Senju Pharmaceut Co Ltd | Composition for treating cornea |
| IL133680A0 (en) * | 1999-09-10 | 2001-04-30 | Can Fite Technologies Ltd | Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist |
| AU2003276988B2 (en) * | 2002-09-27 | 2009-11-05 | Bioenvision, Inc. | Methods and compositions for the treatment of autoimmune disorders using clofarabine |
| JPWO2005121320A1 (en) * | 2004-06-10 | 2008-04-10 | 協和醗酵工業株式会社 | Stem cell self-renewal promoter |
| DK1778239T3 (en) * | 2004-07-28 | 2013-12-02 | Can Fite Biopharma Ltd | ADENOSIN-A3 RECEPTOR AGONISTS FOR THE TREATMENT OF DISEASES CONNECTED WITH DRY EYES, INCLUDING SJÖGREN'S SYNDROME |
-
2006
- 2006-02-01 CN CN2006800475697A patent/CN101365430B/en not_active Expired - Fee Related
- 2006-02-01 BR BRPI0621052-0A patent/BRPI0621052A2/en not_active IP Right Cessation
- 2006-02-01 KR KR1020087020322A patent/KR101037095B1/en not_active IP Right Cessation
- 2006-02-01 JP JP2008551950A patent/JP5185139B2/en not_active Expired - Fee Related
- 2006-02-01 EP EP06701840A patent/EP1976494A1/en not_active Withdrawn
- 2006-02-01 WO PCT/IL2006/000130 patent/WO2007086044A1/en active Application Filing
- 2006-02-01 AU AU2006336834A patent/AU2006336834B2/en not_active Ceased
- 2006-02-01 CA CA2622975A patent/CA2622975C/en not_active Expired - Fee Related
-
2008
- 2008-05-06 IL IL191271A patent/IL191271A/en not_active IP Right Cessation
-
2012
- 2012-11-12 JP JP2012248668A patent/JP2013032396A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2009524647A (en) | 2009-07-02 |
| KR20080090517A (en) | 2008-10-08 |
| CN101365430B (en) | 2011-09-21 |
| EP1976494A1 (en) | 2008-10-08 |
| AU2006336834B2 (en) | 2009-12-10 |
| JP2013032396A (en) | 2013-02-14 |
| CN101365430A (en) | 2009-02-11 |
| JP5185139B2 (en) | 2013-04-17 |
| BRPI0621052A2 (en) | 2012-07-17 |
| IL191271A (en) | 2014-03-31 |
| IL191271A0 (en) | 2009-08-03 |
| WO2007086044A1 (en) | 2007-08-02 |
| CA2622975C (en) | 2011-05-03 |
| AU2006336834A1 (en) | 2007-08-02 |
| KR101037095B1 (en) | 2011-05-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2622975A1 (en) | Adenosine a3 receptor agonists for the treatment of dry eye disorders | |
| Partinen et al. | Efficacy and safety of pramipexole in idiopathic restless legs syndrome: a polysomnographic dose-finding study—the PRELUDE study | |
| JP5339916B2 (en) | Use of A3 adenosine receptor agonists in the treatment of osteoarthritis | |
| Hansen et al. | Orally administered N-acetylcysteine may improve general well-being in patients with mild chronic bronchitis | |
| US7825102B2 (en) | Treatment of dry eye conditions | |
| Steers et al. | Assessment of the efficacy and safety of Viagra®(sildenafil citrate) in men with erectile dysfunction during long-term treatment | |
| MX2010006326A (en) | Orally disintegrating tablets comprising diphenhydramine. | |
| WO2006011130A1 (en) | Adenosine a3 receptor agonists for the treatment of dry eye disorders including sjogren’s syndrome | |
| US20100190734A1 (en) | Method of treating dry eye disease with azithromycin | |
| Wilson et al. | Effects of 5 weeks of administration of fluoxetine and dothiepin in normal volunteers on sleep, daytime sedation, psychomotor performance and mood | |
| Sabbah et al. | Azelastine eye drops in the treatment of seasonal allergic conjunctivitis or rhinoconjunctivitis in young children | |
| Monti | Primary and secondary insomnia: prevalence, causes and current therapeutics | |
| Shinotoh et al. | Lamotrigine trial in idiopathic parkinsonism: a double‐blind, placebo‐controlled, crossover study | |
| Okubo et al. | Efficacy and safety of the emedastine patch, a novel transdermal drug delivery system for allergic rhinitis: phase III, multicenter, randomized, double-blinded, placebo-controlled, parallel-group comparative study in patients with seasonal allergic rhinitis | |
| Huang et al. | A double-blind, randomized, comparative study to evaluate the efficacy and safety of zaleplon versus zolpidem in shortening sleep latency in primary insomnia | |
| Cashman et al. | Assessment of a new hypnotic imidazo‐pyridine (zolpidem) as oral premedication. | |
| JP2008520672A (en) | Treatment of HIV infection by co-administration of tipranavir and darunavir | |
| ES2757856T3 (en) | Orodispersible tablets obtained by compression molding | |
| McCormack et al. | Daily oral grepafloxacin vs. twice daily oral doxycycline in the treatment of Chlamydia trachomatis endocervical infection | |
| RU2012138043A (en) | A3AR AGONISTS FOR TREATMENT OF UVEIT | |
| US20090054412A1 (en) | Treatment of Sleep Disorders | |
| JPH1045576A (en) | Orally administering agent for rhinitis | |
| RU2015105407A (en) | Adenosine A3 receptor ligands for use in the treatment of sexual dysfunction | |
| JP2015524465A5 (en) | ||
| Tamgadge et al. | Meth Mouth: A review on methamphetamine abuse, its oral manifestations and the role of a dentist. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20160201 |
|
| MKLA | Lapsed |
Effective date: 20160201 |