http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2890226-T3
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cecb9a50e6c8193957701eca5ac224f0 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-007 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
filingDate | 2017-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2022-01-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b6d3c91835b03eda474a790312c54455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4e488082fa737e1de228535f2622e2e6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9b1b6bb1a15d8d68624b31c49b99e313 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_adb007b09b390e3fb1e19b0ff4ab96e8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fce16f265b07f85320b26ee950010042 |
publicationDate | 2022-01-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-2890226-T3 |
titleOfInvention | Benzodiazolium compounds as inhibitors of ENaC |
abstract | A compound of general formula (I) including all tautomeric forms, all enantiomers and isotopic variants and salts thereof: **(See formula)** wherein X- is an anion; R1 is: i. H or halo; or ii. -L1R10, where L1 is: -Z1-, -Q1-, -Z1Q1-, -Q1Z1-, -Z1Q1Z2-, -Q1Q2-, -Q1Q2Z1-, -Q1Q2Z1Q3Z2-, -Z1Q1OQ2OQ3-; -OZ1-, -OQ1-, -OZ1Q1-, -OQ1Z1-, -OZ1Q1Z2-, -OQ1Q2-, -OQ1Q2Z1-, -OQ1Q2Z1Q3Z2-, -OZ1Q1OQ2OQ3-; -Z1N(R7)Z2-, -Q1Z1N(R7)Z2-, -Z1N(R7)Z2Q1-, -Q1Z1N(R7)Z2Q2Z3-; -Z1O(CH2CH2O)nZ2-, -Z1O(CH2CH2O)nQ1-, -Z1O(CH2CH2O)nZ2Q1, -Z1O(CH2CH2O)nQ1Z2-, -Q1Z1O(CH2CH2O)nZ2-, -Q1Z1O(CH2CH2O)nQ1-, -Q1Z1O( CH2CH2O)nZ2Q1, -Z1O(CH2CH2O)nZ2Q1Z3-; -C(O)Z1Q1Z2-, -C(O)Q1Z1-, -C(O)Q1Q2-, -C(O)Q1Q2Z1-, -C(O)Z1-, -C(O)Q1-, -C (O)Z1Q1-, -C(O)Q1N(R7)C(O)Z1-, -C(O)Q1N(R7)C(O)Z1Q2-, -C(O)Q1N(R7)C(O )Z1Q2Q3-, -C(O)Q1N(R7)C(O)Z1Q2Z2-, -C(O)Z1Q1OQ2OQ3-; -C(O)N(R7)Z1-, -C(O)N(R7)Q1-, -C(O)N(R7)Z1Q1-, -C(O)N(R7)Z1Q1Z2-, -C (O)N(R7)Q1Z1-, -C(O)N(R7)Q1Q2-, -C(O)N(R7)Q1Q2Z1-, -C(O)N(R7)Z1Q1Q2Z2-, -C(O )N(R7)Z1O(CH2CH2O)nZ2-, -C(O)N(R7)Z1O(CH2O)nZ2-, -C(O)N(R7)Z1Q1Z2N(R8)Z3-, -C(O)N (R7)Z1N(R8)Z2-, -C(O)N(R7)Q1Z1N(R8)Z2-, -C(O)N(R7)Z1Q1OQ2OQ3-, -C(O)N(R7)Z1Q1OQ2OQ3Z2-; -Z1C(O)N(R7)Z2-, -Z1C(O)N(R7)Q1-, -Z1C(O)N(R7)Z2Q1-, -Z1C(O)N(R7)Q1Z2-, -Z1C (O)N(R7)Q1Q2-, -Z1C(O)Q1-, -Z1C(O)Q1Z2-, -Z1C(O)Q1Q2-, -Z1C(O)N(R7)Q1Q2Z2-; -C(O)OZ1-, -C(O)OQ1-, -C(O)OZ1Q1-, -C(O)OZ1Q1Z2-, -C(O)OQ1Z1-, -C(O)OQ1Q2-, -C (O)OQ1Q2Z1-; -Q1C(O)Q2-, Q1C(O)Z1-, -Q1C(O)Q2Z1-, Q1C(O)Q2Q3-, Q1C(O)Z1Q2-, Q1C(O)Q2Q3Z1-; -C(=NR9)N(R7)Z1-, -C(=NR9)N(R7)Q1-, -C(=NR9)N(R7)Z1Q1-, -C(=NR9)N(R7)Z1Q1Z2 -, - C(=NR9)N(R7)Q1Z1-, -C(=NR9)N(R7)Q1Q2- or C(=NR9)N(R7)Q1Q2Z1-; wherein each of Z1, Z2 and Z3 is independently C1-12 alkylene, C2-12 alkenylene, C2-12 alkynylene any of which is optionally substituted by one or more substituents selected from halo, OH, C(O)NR15R16, C(O)OR15 and NR15R16; each R15 and R16 is independently H or C1-6 alkyl or R15 and R16 together with the nitrogen atom to which it is attached may form a 5 or 6 membered heterocyclic ring optionally containing one or more additional heteroatoms selected from N, O and Yes; each of Q1, Q2 and Q3 is independently carbocyclyl, heterocyclyl, aryl or heteroaryl any of which is optionally substituted with one or more substituents selected from halo, OH, C1-4 alkyl, C1-4 haloalkyl, C(O)NR15R16 , C(O)OR15 and NR15R16, and, for cycloalkyl and heterocyclyl groups, oxo, where R15 and R16 are as defined earlier in this claim; n is 1 to 6; each R7 and R8 is independently selected from H and C1-12 alkyl optionally substituted with one or more halo or OH groups, or when one R7 and one R8 or two R8 groups are attached to a nitrogen atom may, together with the nitrogen combine to form a 5 or 6 membered heterocyclic ring optionally comprising one or more additional heteroatoms selected from N, O and S; 0 R9 is H or C1-6 alkyl; R10 is H, -N(R7)R8, -N(R7)C(=NR9)N(R8)2, -N(R7)-C(O)OR8, OR7 or -C(O)OR7; or a cationic group selected from -N(R7)-C(O)-(C1-3 alkylene)-N+(R8)3 and -N+(R8)3, in which case, an additional X- anion will be required; and R7, R8 and R9 are as defined earlier in this claim; or iii. -R12, -OR12 -SO2R12, -C(O)OR12, -C(O)NR12R13, -C(=NR9)NR12R13, -Q1R12-, -Q10R12 -Q1SO2R12, -Q1C(O)OR12, -Q1C(O )NR12R13, -Q1C(=NR7)NR12R13, -Q1Q2OR12, -Q1SO2R12, -Q1Q2C(O)OR12, -Q1Q2C(O)NR12R13 or -Q1Q2C(=NR9)NR12R13; where Q1 and Q2 are defined as above; and each R12 and R13 is independently H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, or C3-8 heterocyclyl, any of which is optionally substituted by one or more substituents selected from halo , OR7, C(O)OR7, -N(R7)R8 and C(O)N(R7)R8 and, in the case of cycloalkyl or heterocyclyl groups, oxo; wherein R7, R8 and R9 are as previously defined in this claim; each of R2 and R3 is independently C1-10 alkyl, wherein one or more -CH2- groups is optionally replaced by -O-, -S- or -NR7- provided that adjacent -CH2- groups are not replaced and which are optionally substituted with one or more substituents selected from halo, OH, SH, N(R7)R8, aryl, heteroaryl, cycloalkyl, heterocyclyl, -C(O)OR7, -C(O)N(R7)R8, OR7 and -N(R7)R8, where R7 and R8 are as defined above; R4 is H, halo, cyano, C1-6 alkyl, C(O)OR16, or C(O)N(R16)R17; wherein the alkyl groups are optionally substituted with one or more substituents selected from halo, -OR7 and -N(R7)R8, wherein R7 and R8 are as defined earlier in this claim; each R16 and R17 is independently H or C1-6 alkyl or R16 and R17 together with the nitrogen atom to which it is attached may form a 5 or 6 membered heterocyclic ring optionally containing one or more additional heteroatoms selected from O, N and yes; and R5 is H or methyl. |
priorityDate | 2016-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 90.