http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-096473-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-0048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-724 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-186 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-724 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-10 |
| filingDate | 2014-06-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2015-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-096473-A1 |
| titleOfInvention | Topical aqueous ophthalmic compositions containing a derivative of 1H-INDOL-1-CARBOXAMIDE AND USE OF THESE FOR THE TREATMENT OF AN OPHTHALMIC DISEASE |
| abstract | Topical multi-dose ophthalmic composition containing a 1H-indole-1-carboxamide and use of it for the treatment of ophthalmic disease. More specifically, this refers to a multi-dose aqueous ophthalmic composition (for example, a solution, a suspension, an emulsion or the like) containing a 1H-indole-1-carboxamide (eg, N- (1-methyl -5- (trifluoromethyl) -1H-pyrazol-3-yl) -5 - ((6 - ((methylamino) methyl) pyrimidin-4-yl) oxy) -1H-indole-1-carboxamide) and use this for the treatment of an ophthalmic disease in the back of the eye, such as age-related macular degeneration (AMD). Claim 1: An aqueous multi-dose ophthalmic composition, comprising: an effective concentration of a 1H-indole-1-carboxamide suitable for treating a condition in the back of the eye, wherein 1H-indole-1-carboxamide is a compound of the formula (1), or a pharmaceutically acceptable salt thereof, wherein: R¹ is hydrogen or C₁₋₆ alkyl; R³ is hydrogen or C₁₋₆ alkyl; R⁵ is hydrogen or halogen; R⁷ is hydrogen or C₁₋₆ alkyl; X is O or S; R⁸ is selected from the group consisting of hydrogen and C₁₋₄ alkyl; R⁹ is selected from the group consisting of (CR¹¹R¹²) ₙNR¹³R¹⁴, (CR¹¹R¹²) ₙ-heterocycle, (CR¹¹R¹²) ₙOR¹⁵, (CR¹¹R¹²) ₙC (O) ER¹³ and (CR¹¹R¹²) ₙS (O) ₘR¹⁷; or R⁸ and R⁹, taken together with the atoms to which they are attached form a saturated 4-7 membered heterocyclic ring having 1 or 2 ring heteroatoms that are selected from N, O or S, whose heterocyclic ring is substituted by 0 , 1 or 2 groups that are independently selected from the group consisting of C₁₋₆ alkyl, C₁₋₆ haloalkyl, halogen, C₁₋₆ hydroxyalkyl, C₁₋₆ aminoalkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, C₁₋₄ heterocycloalkyl , C₁₋₆ alkanoyl, mono- and di-C₁₋₆-aminocarbonyl alkyl, C₁₋₆carbonyl alkoxy and C₁₋₆sulfonyl alkyl; Ar² is phenyl, naphthyl, 5 or 6 membered monocyclic heteroaryl, where each heteroaryl has 1, 2 or 3 ring heteroatoms that are selected from N, O or S and where the phenyl, naphthyl or heteroaryl group is substituted or unsubstituted with 1, 2 or 3 groups that are independently selected from the group consisting of C₁₋₆ alkyl, C₁₋₆ haloalkyl, halo, hydroxyl, CO₂-C₁₋₆ alkyl, phenyl and C₃₋₇ cycloalkyl; m is 0, 1, or 2; n is 1, 2 or 3; E is O or NR¹⁸; R¹¹, R¹² and R¹⁸ are the same or different and are independently selected at each occurrence from the group consisting of hydrogen and C₁₋₄ alkyl; and R¹³, R¹⁴, R¹⁵, R¹⁶ and R¹⁷ are independently selected at each occurrence from the group consisting of hydrogen, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, phenyl and heterocycle, each of which is substituted with 0, 1 or 2 groups that are independently selected from hydroxyl, amino and mono- and di-Cmino alkylamino; an ophthalmic vehicle composed of at least 80% w / v of water and two or more ingredients that are selected from the group consisting of a surfactant, a buffer, a polyol, a suspending agent, an osmolality agent and a preservative; where the composition has a pH in the range of 4 to 9 and an osmolality of 200 to 450 mOsm / kg. Claim 2: An ophthalmic composition as in claim 1, wherein the composition includes the buffer and the polyol, and the buffer is borate. Claim 3: An ophthalmic composition as in claim 1 or 2, wherein the polyol includes mannitol and / or sorbitol and / or the polyol includes propylene glycol and / or glycerol. Claim 4: An ophthalmic composition as in claim 3 wherein the mannitol and / or sorbitol is in the composition at a concentration that is greater than about 0.15% w / v but less than about 0.5% w / v , propylene glycol and / or glycerol is in the composition at a concentration that is greater than about 0.5% w / v but less than about 1.8% w / v and the borate is in the composition at a concentration that is greater than about 0.1% w / v but less than about 0.4% w / v. Claim 5: An ophthalmic composition as in any one of claims 1-4, wherein the preservative is present in the composition and is selected from the group consisting of benzalkonium chloride and a polymeric quaternary ammonium compound. |
| priorityDate | 2013-06-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 82.