http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2002013276-A1

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filingDate 2001-03-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_178811c0ba67f108dd7029c29cd3c159
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publicationDate 2002-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-2002013276-A1
titleOfInvention Investigational compounds
abstract The present invention provides a compound of formula I or a salt thereof: n n n wherein: n R 1 is benzoylphenyl or benzoylphenylC 1-6 alkyl wherein the benzoylphenyl moiety is optionally substituted by from one to nine bromine atoms and the alkyl moiety is optionally substituted by C 1-6 alkylsulfonylamino; or C 1-6 alkoxy; n R 2 and R 3 are independently chosen from C 1-10 alkyl, C 1-10 alkoxy, C 2-10 alkenyl, C 2-10 alkenyloxy, C 2-10 alkynyl or C 2-10 alkynyloxy; phenyl; naphthyl; a five-membered heteroaromatic ring containing 1, 2, 3 or 4 heteroatoms independently chosen from O, N and S, at most one of the heteroatoms being O or S; a six-membered heteroaromatic ring containing 1, 2 or 3 nitrogen atoms; and a group (CH 2 ) p Q 1 wherein Q 1 is phenyl, naphthyl, a five-membered heteroaromatic ring containing 1, 2, 3 or 4 heteroatoms independently chosen from O, N and S, at most one of the heteroatoms being O or S, and a six-membered heteroaromatic ring containing 1, 2 or 3 nitrogen atoms; and wherein each of R 2 and R 3 is independently optionally substituted by one to three groups independently chosen from: n (a) halogen, cyano and nitro, n (b) hydroxy, n (c) C 1-3 alkyl, C 2-3 alkenyl and C 2-3 alkynyl, n (d) C 1-3 alkoxy, n (e) NR 6 R 7 wherein R 6 and R 7 are independently chosen from hydrogen, C 1-5 alkyl and C 1-5 alkoxyC 1-5 alkyl, n (f) CO 2 R 8 wherein R 8 is hydrogen or C 1-4 alkyl, n (g) CONR 6 R 7 or OCONR 6 R 7 wherein R 6 and R 7 are independently as defined above, n (h) SO 2 NR 6 R 7 wherein R 6 and R 7 are independently as defined above, n (i) CH 2 NR 6 R 7 wherein R 6 and R 7 are independently as defined above, n (j) N(R 8 )COR 8 wherein R 8 is independently as defined above and R 8 is independently as defined for R 8 , n (k) NR 8 SO 2 R 8 where R 8 and R 8 are independently as defined above; n alternatively R 3 may be hydrogen; n R 4 and R 5 are independently chosen from hydrogen, C 1-6 alkyl optionally substituted by halogen, hydroxy, thiol, amino, C 1-4 alkoxy, C 1-4 alkylthio, carboxy, C 1-4 alkoxycarbonyl and (CH 2 ) q Q 2 wherein Q 2 is a five-membered unsaturated heterocycle containing 1, 2, 3 or 4 heteroatom optionally chosen from O, N, and S providing that not more than one heteroatom is O or S, a six-membered unsaturated heterocycle containing 1, 2 or 3 N atoms and phenyl and naphthyl, or a fused ring which is indolyl, each of the foregoing rings being optionally substituted with one to three groups independently chosen from hydroxy, C 1-4 alkyl, C 1-4 alkoxy, thiol, C 1-4 alkylthio, halogen, amino, carboxy, amido, CO 2 H and —NHC(NH 2 ) 2 and wherein each of the foregoing rings is optionally fused to a benzene ring; n alternatively R 5 may be benzoylbenzyl which is optionally substituted by from one to nine bromine atoms; n B is C═O or CHOH in the R configuration; n L is a bond or [(CH 2 ) m NHCO] n in which one of the methylene groups may be replaced by a disulphide group; n Z is (CH 2 ) k amino or biotin, or when L is a bond then Z is hydrogen or biotin providing that when Z is hydrogen then either R 1 is not C 1-3 alkoxy or R 5 is benzoxybenzyl; n k is an integer of from one to ten; n each m is independently an integer of from one to ten; n n is an integer of from one to ten; n p is zero, one, two or three; and n q is zero, one, two or three; n with the proviso that no carbon atom is substituted by more than one hydroxy group; processes for preparing them and their use in investigating APP processing.
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Total number of triples: 427.