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1. (WO2006086705) SUBSTITUTED BIS ARYL AND HETEROARYL COMPOUNDS AS SELECTIVE 5HT2A ANTAGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2006/086705 International Application No.: PCT/US2006/004879
Publication Date: 17.08.2006 International Filing Date: 10.02.2006
Chapter 2 Demand Filed: 08.11.2006
IPC:
C07D 209/08 (2006.01) ,C07D 277/68 (2006.01) ,C07D 263/58 (2006.01) ,C07D 239/96 (2006.01) ,C07D 235/26 (2006.01) ,C07D 231/56 (2006.01) ,C07D 265/34 (2006.01) ,C07D 249/18 (2006.01) ,C07D 401/14 (2006.01) ,C07D 413/14 (2006.01) ,C07D 471/04 (2006.01) ,C07D 405/04 (2006.01) ,C07D 413/12 (2006.01) ,C07D 409/14 (2006.01) ,C07D 409/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
08
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
60
condensed with carbocyclic rings or ring systems
62
Benzothiazoles
68
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 in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
52
condensed with carbocyclic rings or ring systems
54
Benzoxazoles; Hydrogenated benzoxazoles
58
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 in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
72
Quinazolines; Hydrogenated quinazolines
95
with hetero atoms directly attached in positions 2 and 4
96
Two oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
24
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 in position 2
26
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54
condensed with carbocyclic rings or ring systems
56
Benzopyrazoles; Hydrogenated benzopyrazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
34
condensed with carbocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
16
condensed with carbocyclic rings or ring systems
18
Benzotriazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants:
FINK, David Mark [US/US]; US (UsOnly)
SMITH, Helen Katherine [GB/GB]; GB (UsOnly)
TODD, Richard Simon [GB/GB]; GB (UsOnly)
EASTWOOD, Paul Robert [GB/ES]; ES (UsOnly)
HUNT, Hazel [GB/GB]; GB (UsOnly)
AVENTIS PHARMACEUTICALS INC. [US/US]; 300 Somerset Corporate Boulevard Bridgewater, New Jersey 08807-2854, US (AllExceptUS)
Inventors:
FINK, David Mark; US
SMITH, Helen Katherine; GB
TODD, Richard Simon; GB
EASTWOOD, Paul Robert; ES
HUNT, Hazel; GB
Agent:
GUPTA, Balaram ; Sanofi-Aventis Route 202-206 P. O. Box 6800 Bridgewater, NJ 08807-0800, US
Priority Data:
60/651,91110.02.2005US
Title (EN) SUBSTITUTED BIS ARYL AND HETEROARYL COMPOUNDS AS SELECTIVE 5HT2A ANTAGONISTS
(FR) COMPOSES BIS ARYLE ET HETEROARYLE SUBSTITUES, UTILES COMME ANTAGONISTES SELECTIFS DES RECEPTEURS 5HT2A
Abstract:
(EN) The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.
(FR) La présente invention concerne une série de composés bis aryle et hétéroaryle substitués, représentés par la formule générale (I). Dans cette formule, X, Y, Z, A, B, D, Ar, R1 et R2 désignent des éléments définis dans la partie descriptive de la présente demande. Les composés de la présente invention sont des antagonistes sélectifs des récepteurs 5HT2A et sont, par conséquent, utiles pour le traitement de diverses maladies, notamment, mais sans en exclure d'autres, un grand nombre de troubles du sommeil.
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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, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, 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, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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 Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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)