http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010007382-A8
Outgoing Links
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| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D223-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D223-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 |
| filingDate | 2009-07-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ebdb70efefd3575e5c3f58811e3a123b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32b03f1ce27aacc83b13f2ef3a04998d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_720dc3700bd22b226dc7bf9ad5b32936 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_39325175b5e461de0dc347e71fd5e5b9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_570ad8203195a15b5b56dd3acc31a9a3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_53bb8263a4b724f444b73ac3af8a37e1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_39d4cd7cd237aa1bcea25339180c8982 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6f8a0815ee36e4c40af7cfdaffb6a644 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f68fc7a5ac41a2826f54c46a67db001c |
| publicationDate | 2010-03-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | WO-2010007382-A8 |
| titleOfInvention | Benzazepine derivatives and their use as hstamine h3 antagonists |
| abstract | A compound having the formula (1) wherein: R1 is a group selected from C 3-8 cycloalkyl, C 1-6 alkyl, C 1-6 alkylene-C 3-8 cycloalkyl, each of which groups may optionally be substituted with C 1-6 alkyl, halogen, haloC 1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C 1-6 alkyl, haloC 1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group -(CH 2 ) n - formed thereby being optionally substituted with a group selected from C 1-4 alkyl, C 3-8 cycloalkyl and arylsulfonyl; A is a group selected from -N(R2)CO-, -CON(R2)-, -OC(O)-, -C(O)O-, -CO-, -C(R2)(OR3)-, -C(=N-O-R3)-, - C(=CR2R3)-, -C 3-8 cycloalkylene-, -C(R2)(haloC 1-6 alkyl)-, C 1-4 alkylene and -C(OR3)(haloC 1-6 alkyl)-; R2 and R3 are each independently selected from H, C 1-6 alkyl, and C 3-8 cycloalkyl, or, when A is -N(R2)CO- and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C 1-4 alkylene or C 2-4 alkenylene, each of which may optionally be substituted with one or more C 1-4 alkyl groups, OR16, halogen or haloC 1-6 alkyl; Z is selected from aryl, heteroaryl, C 3-8 cycloalkyl, and heterocyclyl, each of which may optionally be substituted by a group selected from -Y-aryl, -Y-heteroaryl, -Y-C 3-8 cycloalkyl and -Y-heterocyclyl, or, when X is present, Z may be H, or, when X is absent and A is -C(R2)(OR3)- or -N(R2)CO-, Z may be H, or, when A is -N(R2)CO- and X is absent, Z may form, together with the adjacent nitrogen atom and R2, an N-containing heterocyclyl group which may optionally be substituted, wherein, when A is -CO-, Z is linked to X or A via a carbon atom and wherein, when A is -N(R2)CO- and Z is H, R1 is C 3-8 cycloalkyl; and Y represents a bond, C 1-6 alkylene, CO, NR14, COC 2-6 alkenylene, O, SO 2 or NHCOC 1-6 alkylene; wherein said cycloalkyl, aryl, heteroaryl and heterocyclyl groups Z may be optionally substituted by one or more substituents which may be the same or different, and which are selected from halogen, haloC 1-6 alkyl, hydroxy, cyano, nitro, =O, -R4, -CO 2 R4, -COR4, -NR5R6, -C 1-6 alkyl-NR5R6, -C 3-8 cycloalkyl-NR5R6, - CONR12R13, -NR12COR13, -NR5SO 2 R6, -OCONR5R6, -NR5CO 2 R6, -NR4CONR5R6 or -SO 2 NR5R6- SHR8, -alkyl-OR8, -SOR8, -OR9, -SO 2 R9, -OSO 2 R9, -alkyl-SO 2 R9, -alkyl-CONHR9, -alkyl-SONHR9, -alkyl-COR10, -CO-alkyl-R10, -O-alkyl-R11 (wherein R4, R5 and R6 independently represent hydrogen, C 1-6 alkyl, -C 3-8 cycloalkyl, -C 1-6 alkylene-C 3-8 cycloalkyl, aryl, heterocyclyl or heteroaryl, wherein R8 represents C 1-6 alkyl, wherein R9 represents C 1-6 alkyl or aryl, wherein R10 represents aryl, wherein R11 represents C 3-8 cycloalkyl or aryl, R12, R13, R14, R15 and R16 each independently represent H or C 1-6 alkyl, and wherein -NR5R6 and -NR12R13 may represent a nitrogen containing heterocyclyl group); wherein said R4, R5, R6 R8, R9, R11 and R11 groups may be optionally substituted by one or more substituents which may be the same or different, and which are selected from the group consisting of halogen, hydroxy, C 1-6 alkyl, C 1-6 alkoxy, cyano, amino, =O or trifluoromethyl; and wherein substituents of Z selected from -Y-aryl, -Y-heteroaryl, -Y-C 3-8 cycloalkyl and -Y-heterocyclyl may be optionally substituted by one or more substituents selected from =O, hydroxy, cyano, nitro, halogen, haloC 1-6 alkyl and C 1-6 alkyl; and wherein, when A is C 1-4 alkylene, said cycloalkyl, aryl, heteroaryl or heterocyclyl group Z (such as a heterocyclyl group Z) is substituted at least with hydroxy, CF 3 , or =0; and wherein, when A is CON(R2) n is 1; or a pharmaceutically acceptable salt or ester thereof, provided that: when A is -CO-, R1 is CH 3 , C 3-8 cycloalkyl-substituted C 1-6 alkylene or n-butyl, n is 0 and X is -CH 2 CH 2 -, Z is not N-benzyl substituted 4-piperidinyl, N-(3-fluorobenzyl)-substituted 4-piperidinyl or N-acetyl substituted 4-piperidinyl; when A is -OC(O)-, R1 is cyclobutyl, n is 0 and X is -CH 2 CH 2 -, Z is not H; when A is -OC(O)-, R1 is n-propyl, n is 0 and X is -CH 2 -, Z is not H; and when A is -CO-, R1 is CH 3 , n is 0 and X is CH 2 , Z is not H. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9108948-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8829041-B2 |
| priorityDate | 2008-07-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 73.