http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035260-A1

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filingDate 2002-08-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2004-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-035260-A1
titleOfInvention DERIVATIVES OF REPLACED AMINO PIPERIDINE, PHARMACEUTICAL COMPOSITIONS AND THE USE OF SUCH DERIVATIVES FOR THE PREPARATION OF MEDICINES AS INHIBITORS OF THE SECRETASE RANGE, AND FOR THE TREATMENT OF ALZHEIMER'S DISEASE
abstract Substituted amino piperidine derivatives, which comprise a compound of the formula (1) or pharmaceutically acceptable salts or solvates thereof, in which: Ar1 and Ar2 are independently selected from aryl and heteroaryl; Y is a bond, or Y represents a group - (C (R3) 2) 1-3-; Each R1 is independently selected from: (C1-6) alkyl; aryl; aryl substituted with one or more substituents independently selected from halogen, CF3, (C1-6) alkyl, (C1-6) alkoxy, OCF3, NH2 or CN; heteroaryl; heteroaryl substituted with one or more substituents independently selected from halogen, CF3, (C1-6) alkyl, (C1-6) alkoxy, OCF3, NH2 or CN; halogen; -CF3; -OCF3; -CN; -NO2; -NH2; -C (O) NH (C1-6) alkyl; -C (O) N ((C1-6) alkyl) 2, where each (C1-6) alkyl group is the same or different from the others; -C (O) N ((C1-6) alkyl) 2, where each (C1-6) alkyl group is the same or different from the others and said (C1-6) alkyl groups taken together with the nitrogen to which they are attached they form a ring; -NHC (O) (C1-6) alkyl, -NHC (O) Oalkyl (C1-6), -NHC (O) NHalkyl (C1-6), -NHSO2alkyl (C1-6); -OH; -OC (O) (C1-6) alkyl; -Alkyl (C1-6); -Oarilo; or -Oaralkyl (C1-6); Each R2 is independently selected from: (C1-6) alkyl; halogen; -CF3; -OCF3; -CN; -NO2; -NH2; -C (O) C 1-6 alkyl; -C (O) NH (C1-6) alkyl, -N ((C1-6) alkyl) 2- where each (C1-6) alkyl substituent is the same or different from the others; -N ((C1-6) alkyl) 2, where each (C1-6) alkyl substituent is the same or different from the others and (C1-6) alkyl substituents, together with the nitrogen atom to which they are attached form a ring; -NHC (O) (C1-6) alkyl; -NHC (O) Oalkyl (C1-6); -NHC (O) NHalkyl (C1-6); -NHSO2 (C1-6) alkyl; -OH; -OC (O) (C1-6) alkyl; -Alkyl (C1-6); -Oarilo; Oar-C1-6 alkyl; aryl; aryl substituted with one or more substituents independently selected from: halogen, CF3, (C1-6) alkyl, (C1-6) alkoxy, OCF3, NH2 or CN; heteroaryl; heteroaryl substituted with one or more substituents independently selected from halogen, CF3, (C1-6) alkyl, (C1-6) alkoxy OCF3, NH2 or CN; -C (O) N ((C1-6) alkyl) 2 where each alkyl group is independently selected; -C (O) N ((C 1-6) alkyl) 2 where each alkyl group is independently selected and where the alkyl groups, taken together with the nitrogen atom, form a heterocycloalkyl ring; or a group selected from the residues of formulas (2) to (6); Each R3 is independently selected from H and (C1-3) alkyl; Each R4 is independently selected from: (C1-3) alkyl; -OH; or -C 1-3 alkyl; R5 is selected from: hydrogen; (C1-6) alkyl; aryl; heteroaryl; -alkyl (C1-3) -Oalkyl (C1-3); -alkyl (C1-6) -S (O) 0-2 (C1-3) alkyl; -alkyl (C1-8) -S (O) 0-2NH (C1-3) alkyl; -C (O) (C1-6) alkyl; C (O) aryl; -C (O) aralkyl (C1-3), -C (O) heteroaryl; -C (O) heteroaralkyl (C1-3); -C (O) C 1-6 alkyl; -C (O) NH (C1-6) alkyl; -C (O) N ((C1-6) alkyl) 2, where each C1-6 alkyl group is the same or different from the others; -C (O) N ((C1-6) alkyl) 2, where each C1-6 alkyl group is the same or different from the others and where C1-6 alkyl groups, taken together with the nitrogen to which they are attached, form a heterocycloalkyl ring; -C (O) alkylene (C1-3) -NHalkyl (C1-3); -C (O) alkylene (C1-3) -N (alkyl (C1-3)) 2; where each alkyl group is independently selected; -SO2 (C1-6) alkyl; -SO2NH (C1-6) alkyl; -SO2N ((C1-6) alkyl) 2; where each C1-6 alkyl group is the same or different from the others; -SO2N ((C1-6) alkyl) 2, where each C1-6 alkyl group is the same or different from the others and where the C1-6 alkyl groups, taken together with the nitrogen to which they are attached, form a heterocycloalkyl ring or a group of the formula (7), (8), (9) or (10); R6 is -H or (C1-6) alkyl; X is selected from CH2, O, S, SO, SO2 or N-R7; R7 is selected from (C1-6) alkyl, cycloalkyl (C3-6), alkylene (C1-3) -cycloalkyl (C3-6); aryl, aralkyl (C1-3), heteroaryl, heteroaralkyl (C1-3), -C (O) (C1-6) alkyl, -C (O) aryl; -C (O) aralkyl (C1-3), -C (O) heteroaryl; -C (O) heteroaralkyl (C1-3), -C (O) Oalkyl (C1-6), -C (O) NHalkyl (C1-6), -C (O) N (alkyl (C1-6)) 2, where each C1-6 group is the same or different from the others; -C (O) N ((C1-6) alkyl) 2, where each C1-6 alkyl group is the same or different from the others and where C1-6 alkyl groups, taken together with the nitrogen to which they are attached, form a heterocycloalkyl ring; -C (O) alkylene (C1-3) -NHalkyl (C1-3), -C (O) alkylene (C1-3) -N (alkyl (C1-3)) 2, where C1-3 alkyl groups are same or different; or -C1-3 alkyl-O3C3 alkyl; n and p are independently selected from 0 to 3 to form a 4 to 7 member ring; r represents from 0 to 3; q represents from 0 to 3 and t represents from 0 to 3. Pharmaceutical compositions and the use of said compounds for the preparation of medicaments to inhibit the secretase range and for the treatment of Alzheimer's disease are also described.
priorityDate 2001-08-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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