http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-064414-A1
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a910d33c239980f3a705e312c5bad6a |
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| filingDate | 2007-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0b78c679f3bda302ac8a3b9941190a40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_daa1402e119a29c70ab55a100956f7c8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0cf2ec57a5aec30e7db44d6459fa4ba8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6864ca67a36d2c8600d30a52385ad24d |
| publicationDate | 2009-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-064414-A1 |
| titleOfInvention | DERIVATIVES OF 1-AZONIABICICLO [2, 2, 2] OCTANO AND 1-AZABICICLO [2, 2, 2] OCT-3-ILO, A PROCESS FOR THEIR PREPARATION, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM, PROCEDURE FOR OBTAINING THE SAME, ITS USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF COPD AND A PHARMACEUTICAL PRODUCT THAT |
| abstract | A process for its preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, its use in therapies and intermediates useful in its preparation. Claim 1: A compound, characterized in that it is of the formula (1), wherein R 1 represents C 1-6 alkyl; R2 represents phenyl or a 5- to 6-membered heteroaryl ring, each of which may be optionally substituted with one or more substituents independently selected from halogen, cyano, nitro, SH, S (O) 0-2R10, NR11R12, S (O) 2NR13R14, C (O) NR15R16, C (O) 2R17, NR18S (O) 2R19, NR20C (O) R21, NR22C (O) 2R23, NR24C (O) NR25R26, OR27 and C1-6 alkyl where I rent C1-6 may optionally be substituted with one or more substituents independently selected from halogen, hydroxyl, C1-6 alkoxy, NH2, NH (C1-6 alkyl) and N (C1-6 alkyl) 2; R3 and R4 together with the nitrogen atom to which both are attached form a 4 to 8-membered aliphatic heterocyclic ring which may optionally contain an additional heteroatom selected from oxygen, sulfur and nitrogen, and where the heterocyclic ring can be optionally substituted with one or more substituents independently selected from halogen, hydroxyl and C1-6 alkyl, where C1-6 alkyl may optionally be substituted with one or more substituents independently selected from halogen and hydroxyl; R5 represents a group of the formula (2) or (3) wherein Y is -CH2-, -CH2CH2- or -CH2CH2CH2- and the substitution on the group ring (2) can be in positions 3 or 4; a is 1 or 2; b is 1 or 2; Z is -CH2-; R6 represents a group of the formula (4), wherein w is 0 or 1; R7 represents C1-4 alkylene optionally substituted with one or more substituents independently selected from halogen, hydroxyl, C1-6 alkoxy, NH2, NH (C1-6 alkyl) and N (C1-6 alkyl) 2; when w is 0, and is 0; when w is 1, and is 0 or 1; Q represents O, C (O), S (O) 0-2, NR9, -CONR9-, -SO2NR9-, -NR9CO-, -NR9SO2, -OC (O) -, -C (O) O-, - HC = CH- or ethinylene; R 8 represents a cyclic group C 1 or a C 1-4 alkyl group where C 1-4 alkyl can be optionally substituted with one or more substituents independently selected from halogen, hydroxyl, C 1-4 alkoxy, NH 2, NH (C 1-4 alkyl) , N (C1-4 alkyl) 2, a cyclic group Cic2 and OCic2; and R8 may additionally represent hydrogen when Q represents O, NR9, CONR9-, -SO2NR9-, - C (O) O-, -HC = CH- or ethinylene; Cic1 and Cic2 each independently represent aryl, heteroaryl, a 3 to 8 membered aliphatic carbocyclic ring or a 4 to 8 membered aliphatic heterocyclic ring, each of which may optionally be substituted with one or more substituents selected in a form independent between halogen, cyano, nitro, SH, S (O) 0-2R10, NR11R12, S (O) 2NR13R14, C (O) NR15R16, C (O) 2R11, NR18S (O) 2R19, NR20C (O) R21, NR22C (O) 2R23, NR24C (O) NR25R26, OR27, phenyl, heteroaryl and C1-6 alkyl where phenyl, heteroaryl or C1-6 alkyl may optionally be substituted with one or more substituents independently selected from halogen, hydroxyl, cyano , C1-6 alkoxy, NH2, NH (C1-6 alkyl) and N (C1-6 alkyl) 2; R9 represents hydrogen or C1-6 alkyl; R10 and R19 each independently represent C1-6 alkyl, where C1-6 alkyl can optionally be substituted with one or more substituents independently selected from halogen, hydroxyl, C1-6 alkoxy, NH2, NH (C1-6 alkyl ) and N (C1-6 alkyl) 2; and R11, R12, R13, R14, R15, R16, R17, R18, R20, R21, R22, R23, R24, R25, R26 and R27 each independently represents hydrogen or C1-6 alkyl, where C1-6 alkyl it may optionally be substituted with one or more substituents independently selected from halogen, hydroxyl, C1-6 alkoxy, NH2, NH (C1-6 alkyl) and N (C1-6 alkyl) 2; or any of R11 and R12, R13 and R14, R15 and R16 or R25 and R26, together with the nitrogen atom to which both are attached, can form a 4- to 8-membered aliphatic heterocyclic ring, where the heterocyclic ring can be optionally substituted with one or more substituents independently selected from halogen, hydroxyl and C1-6 alkyl, where C1-6 alkyl may optionally be substituted with one or more substituents independently selected from halogen and hydroxyl; and X represents an anion acceptable for pharmaceutical use of a mono or polyvalent acid. Claim 10: A process for preparing a compound of the formula (1) as defined in clause 1, characterized in that it comprises reacting a compound of the formula (10) wherein R1, R2 and R3 have the values defined in the formula (1), or a C1-6 alkyl ester, acid anhydride or acid halide thereof, with a compound of the formula (11) or of the formula (12), wherein Y, Z, a and b are as defined in the formula (1) and the hydroxyl group in (11) are in position 3 or 4 to obtain a compound of the formula (5S) or (5b) wherein R1, R2 and R3 are as defined in clause 1 and subsequently reacting (5a) or (5b) with a compound R6-LG (13), wherein LG is a leaving group and R6 is as defined in formula (1): and optionally converting the compound into another compound of the formula (1); forming a salt acceptable for pharmaceutical use with an anion of a mono or polyvalent acid. |
| priorityDate | 2006-12-19-04:00^^<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: 85.