http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-073046-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_985e586742507c77adffd57be9bc530e |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-107 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-20 |
| filingDate | 2009-08-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2010-10-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-073046-A1 |
| titleOfInvention | ESPIRO BETA INHIBITING COMPOUNDS - SECRETASA |
| abstract | A compound of the formula (1). A pharmaceutical composition comprising a compound represented by the structural formula (1) and a method of using this compound to inhibit the activity of BACE in a subject in need of such treatment are also described. Claim 1: A compound represented by structural formula (1) or a pharmaceutically acceptable salt thereof, wherein R 1 is H, C 1-6 alkyl, C 1-6 arylalkyl, or C 1-6 heteroarylalkyl; each R2 is independently selected from a) -H, -F, -CI, -Br and -CN, and b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, aryl, heteroaryl, phenoxy or benzyloxy, each optionally substituted with 1 to 3 substituents selected from the group consisting of -F, -CI, -Br, -CN, -OR5, -NR6R7, S (O) iR5, NR11S (= O) iR5, -C (= O) OR5, -C (= O) NR12R13, -NR11C (= O) R5, -C (= S) NR12R13, -C (= O) R5, C1-6 alkyl, C3-6 cycloalkyl, C2-6 alkenyl, C1-6 haloalkyl, C1-3 alkyl-sulfonylaminoalkyl, C1-6 hydroxyalkyl, C1-6 cyanoalkyl, C1-3 alkyl C1 -6 carbonylaminoalkyl C1-3 alkoxy, C1-3 haloalkoxy, C1-6 alkoxy -C1-3 alkyl, aryl and heteroaryl; each R3 and R4 is independently -H, -halogen, -CN, -NO2, -OR5, -NR6R7, -S (O) iR5, -C (= O) OR5, -C (= O) NR12R13, -C ( = O) R 5, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-8 cycloalkyl, aryl or heteroaryl, where each C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-8 cycloalkyl , aryl or heteroaryl is optionally substituted with 1 to 3 substituents independently selected from the group consisting of -F, Cl, Br, -CN, -OR5, -NR6R7, -S (O) iR5, -NR11S (= O) R5 , -C (= O) OR5, -C (= O) NR12R13, -NR1C (= O) R5, -C (= S) NR12R13, -C (= O) R5, C1-6 alkyl, C2-6 alkenyl , C1-6 haloalkyl, C1-3 alkyl-sulfonylaminoalkyl, C1-6 hydroxyalkyl, C1-6 cyanoalkyl, C1-3 alkylcarbonylaminoalkyl C1-6, C1-3 alkoxy, C1-3 haloalkoxy, C1-6 alkoxy-C1 alkyl -3, an aryl group and a heteroaryl group; X is -O-, -S-, -SO-, -SO2-, -CH2O- or -OCH2-; each Y is independently -C (R8R9) -; W is -N (R14) -, -S-, -O-; Z is -C (= O) -, -C (= S) -, -C (= NR15) -, -O-, -C (= O) C (R15R17) -, -C (= S) C ( R16R17) -, -C (= NR15) C (R16R17) -, -N (R18) -, - (CR16R17) m- or -O- (CR16R17) -; R 5 is -H, C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-3 alkoxy-C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, C3-7 cycloheteroalkyl, aryl, heteroaryl or benzyl, each of which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of -F, -Cl, -Br, -CN, C1-6 alkyl, haloalkyl C1-6 and C1-3 alkoxy-C1-6 alkyl; each R6 and R7 are independently selected from -H, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, C3-8 cycloalkyl and C3-8 cycloalkyl-C1-6 alkyl, each optionally substituted with 1 to 3 substituents independently selected from the group consisting of -F, -CI, -Br, -CN, C1-6 alkyl, C1-6 haloalkyl and C1-3 alkoxy-C1-6 alkyl; each R8 and R9 are independently selected from H, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-14 cycloalkyl, C3-13 cycloheteroalkyl, aryl or heteroaryl, each one optionally substituted with 1 to 4 substituents independently selected from the group consisting of -F, -CI, -Br, -CN, -OR5, -NR6R7, -S (O) iR5, -NR11S (= O) iR5, - C (O) OR5, -C (= O) NR12R13, -NR11C (= O) R5, -C (= S) NR12R13, -C (= O) R5, C1-6 alkyl, C2-6 alkenyl, C1 haloalkyl -6, C1-3 alkyl-sulfonylaminoalkyl, C1-6 hydroxyalkyl, C1-6 cyanoalkyl, C1-3 alkyl-C1-6 carbonylaminoalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C1-6 alkoxy-C1-3 alkyl, aryl, heteroaryl, C3-8 cycloalkyl and C3-7 cycloheteroalkyl, or R8 and R9, together with the carbon to which they are attached, form ring A, which is a 3-14 membered monocyclic ring, 9-14 membered bicyclic or 9-14 member polycyclic, where ring A is optionally substituted with 1 to 4 substituents selects two independently between the group consisting of -F, -CI, -Br, -CN, -OR5, -NR6R7, -S (= O) iR5, -NR11S (= O) iR5, -C (= O) OR5, -C (= O) NR12R13, -NR11C (= O) R5, -C (= S) NR12R13, -C (= O) R5, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, C1- alkyl 3-sulfonylaminoalkyl, hydroxy C1-6 alkyl, cyanoalkyl C1-6, alkyl C1-3-carbonylaminoalkyl C1-6, alkoxy C1-3, haloalkoxy C1-3, alkoxy C1-6-alkyl C1-3, aryl and heteroaryl; R 11 is -H, C 1-6 alkyl or C 1-6 haloalkyl; each R12 and R13 is independently -H, C1-6 alkyl, C1-3 alkoxy-C1-6 alkyl, hydroxy C1-6 alkyl, C1-6 cyanoalkyl, C1-6 aminoalkyl, C1-3 alkylamino-C1-6 alkyl or dialkylamino C1-3-C1-6 alkyl; or R12 and R13, together with the nitrogen to which they are attached, form a 3-8-membered ring optionally substituted with 1 to 3 substituents independently selected from the group consisting of -F, -CI, -Br, -CN, - OR5, -NR6R7, -S (= O) iR5, -NR11S (= O) iR5, -C (= O) OR5, -C (= O) NR12R13, -NR11C (= O) R5, -C (= S ) NR12R13, -C (= O) R5, C 1-6 alkyl, C 2-6 alkenyl, C 1-6 haloalkyl, C 1-3 alkyl sulfonylaminoalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl, C 1-3 alkylcarbonylaminoC1 alkyl -6, C1-3 alkoxy, C1-3 haloalkoxy and C1-6 alkoxy-C1-3 alkyl, wherein the 3-8 membered ring optionally contains 1 to 3 additional heteroatoms, which are independently selected from O, N and S , where, when the additional heteroatom is nitrogen, the nitrogen is substituted with -H, C1-3 alkyl or C1-3 haloalkyl, and when the additional heteroatom is sulfur, the sulfur is optionally mono or di-oxygenated; R 14 is -H, C 1-6 alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, C 1-3 cycloheteroalkylalkyl, C 3-8 cycloalkyl-C 1-3 alkyl, C 1-6 arylalkyl, C 1-6 heteroarylalkyl, each optionally substituted with 1 to 3 substituents independently selected from the group consisting of -F, -CI, -Br, -CN, C1-6 alkyl, C1-6 haloalkyl and C1-3 alkoxy; R15 is -H or C1-6 alkyl; each of R16 and R17 is independently -H or C1-3 alkyl; R18 is -H or C1-3 alkyl; i is 0, 1 or 2; p is 1 or 2; m is 1 or 2; and n is 1 or 2. |
| priorityDate | 2008-08-19-04:00^^<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: 30.