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1. (WO2007002214) ACYL GUANIDINES AS BETA-SECRETASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/002214 International Application No.: PCT/US2006/024172
Publication Date: 04.01.2007 International Filing Date: 20.06.2006
IPC:
C07D 261/18 (2006.01) ,C07D 275/02 (2006.01) ,C07D 231/14 (2006.01) ,C07D 413/12 (2006.01) ,A61K 31/4155 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
261
Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02
not condensed with other rings
06
having two or more double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
18
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
275
Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings
02
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
4155
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants:
BRISTOL-MYERS SQUIBB COMPANY [US/US]; Route 206 and Province Line Road Princeton, New Jersey 08543-4000, US (AllExceptUS)
GERRITZ, Samuel [US/US]; US (UsOnly)
ZHAI, Weixu [US/US]; US (UsOnly)
SHI, Shuhao [US/US]; US (UsOnly)
ZHU, Shirong [CN/US]; US (UsOnly)
GOOD, Andrew C. [GB/US]; US (UsOnly)
THOMPSON, Lorin, A., III [US/US]; US (UsOnly)
Inventors:
GERRITZ, Samuel; US
ZHAI, Weixu; US
SHI, Shuhao; US
ZHU, Shirong; US
GOOD, Andrew C.; US
THOMPSON, Lorin, A., III; US
Agent:
ALGIERI, Aldo A., Ph. D. ; Bristol-Myers Squibb Company P.O. Box 4000 Princeton, New Jersey 08543-4000, US
Priority Data:
60/692,60021.06.2005US
60/788,74803.04.2006US
Title (EN) ACYL GUANIDINES AS BETA-SECRETASE INHIBITORS
(FR) ACYLGUANIDINES EN TANT QU'INHIBITEUR DE BETA-SECRETASE
Abstract:
(EN) There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2. R3, R4 and R5 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by Beta-secretase and, more specifically, inhibit the production of ABeta-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to Beta-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
(FR) L'invention concerne une série de guanidines à substitution acyle représentées par la formule (I) ou un de leurs stéréoisomères ou un de leurs sels acceptables sur le plan pharmaceutique, dans laquelle R1, R2. R3, R4 et R5 correspondent à leur définition dans le descriptif, leurs compositions pharmaceutiques et méthodes d'utilisation. Ces composés inhibent l'effet exercé sur la protéine précurseur d'amyloïde (APP) par béta-sécrétase et, de façon plus spécifique, inhibent la production du Abéta-peptide. L'invention concerne des composés utiles pour le traitement de troubles neurologiques relatifs à la production des béta-amyloïdes, tels que la maladie d'Alzheimer ou d'autres états associés à l'activité anti-amyloïde.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)