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Machine translation
1. (WO2000058277) ARYL SULFONIC ACIDS AND DERIVATIVES AS FSH ANTAGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2000/058277    International Application No.:    PCT/US2000/008365
Publication Date: 05.10.2000 International Filing Date: 29.03.2000
Chapter 2 Demand Filed:    17.10.2000    
IPC:
C07C 309/51 (2006.01), C07C 309/76 (2006.01), C07C 311/29 (2006.01), C07C 317/44 (2006.01), C07C 317/48 (2006.01), C07D 295/13 (2006.01), C07D 295/26 (2006.01)
Applicants: AMERICAN HOME PRODUCTS CORPORATION [US/US]; Five Giralda Farms, Madison, NJ 07940-0874 (US)
Inventors: WROBEL, Jay, Edward; (US).
ROGERS, John, Francis; (US).
GREEN, Daniel, Michael; (US).
KAO, Wenling; (US).
JETTER, James, Winfield; (US)
Agent: MILOWSKY, Arnold, S.; American Home Products Corporation, Patent Law Department - 2B, One Campus Drive, Parsippany, NJ 07054 (US).
WILEMAN, David Francis; c/o Wyeth Laboratories, Huntercombe Lane South, Taplow, Maidenhead, Berkshire SL6 0PH (GB)
Priority Data:
09/282,823 31.03.1999 US
Title (EN) ARYL SULFONIC ACIDS AND DERIVATIVES AS FSH ANTAGONISTS
(FR) ACIDES SULFONIQUES ARYLES ET DERIVES TELS QUE LES ANTAGONISTES FSH
Abstract: front page image
(EN)This invention provides compounds of formula (I) having the structure wherein Q is hydrogen or -SO¿2?R?1¿; X is a bond, O, S(O)¿n?, -CH=CH-, -CH¿2?CH¿2?-, -C$m(Z)C-, or -CH¿2?S(O)¿n?CH¿2?-; R?1¿ is OH, NH¿2?, C¿1? to C¿6? alkoxy, C¿1? to C¿3? perfluoroalkoxy; Ar is (a) or (b); Ar' is (c) or (d); R?2¿ and R?4¿ are each, independently, hydrogen, OR?6¿, -S(O)¿m?R?6¿, -NHR?6¿, -N(R?6¿)¿2?, or -CH¿2?SO¿2?CH¿3?; R?3¿ and R?5¿ are each, independently, hydrogen, -NO¿2?, -NH¿2?, -SO¿2?R?9¿, or -CH¿2?R?9¿; R?6¿ is hydrogen, C¿1? to C¿6? alkyl, C¿3? to C¿6? alkenyl, -CH¿2?CH¿2?Z, -CH¿2?COR?7¿, -CH¿2?CH=CHCOR?7¿, (e), (f) or (g); Y¿1? and Y?3¿ are each, independently, N, or CH; Y?2¿ and Y?4¿ are each independently, O, S, or NR?13¿; R?7¿ is -OR?8¿, -NHR?8¿, -N(R?8¿)¿2?, or -NHCH¿2?CH¿2?OR?8¿; Z is -OR¿8?, -OCH¿2?CH¿2?OR?8¿, -N(R?8¿)¿2?, or (h); R¿8? is hydrogen or C¿1? to C¿3? alkyl; R?9¿ is C¿1? to C¿6? alkyl, C¿3? to C¿6? alkenyl, OH, NHR?10¿, N(R?10¿)¿2?, CH¿2?COR?11¿, -CH¿2?CH=CHCOR?11¿, or (i); R?10¿ is C¿1? to C¿3? alkyl, C¿3? to C¿4? alkenyl, phenyl, -CH¿2?CH¿2?OCH¿3?, or -(j); R?11¿ is -OR?12¿, -NHR?12¿, -N(R?12¿)¿2?, or -NHCH¿2?CH¿2?OR?12¿; R?12¿ is hydrogen, or C¿1? to C¿3? alkyl; R?13¿ is hydrogen, or C¿1? to C¿3? alkyl; W is a bond, CH¿2?, CH¿2?CH¿2?, O, S(O)¿q?, NCHO, NCOCH¿3?, or NR?12¿; m is 0 - 2; n is 0 - 2; q is 0 - 2, with the proviso that R?2¿ and R?3¿ are not both hydrogen; or pharmaceutically acceptable salt thereof, which are useful as contraceptive agents.
(FR)La présente invention concerne des composés de formule (I) de structure (I). Dans cette formule Q est hydrogène ou -SO¿2?R?1¿; X est une liaison, O, S(O)¿n?, -CH=CH-, -CH¿2?CH¿2?-, -C$m(Z)C-, ou -CH¿2?S(O)¿n?CH¿2?-; R?1¿ est OH, NH¿2?, C¿1? à C¿6? alcoxy, C¿1? à C¿3? perfluoroalcoxy; Ar est (a) ou (b); Ar' est (c) ou (d); R?2¿ et R?4¿ sont chacun indépendamment, hydrogène, OR?6¿, -S(O)¿m?R?6¿, -NHR?6¿, -N(R?6¿)¿2?, ou -CH¿2?SO¿2?CH¿3?; R?3¿ et R?4¿ sont chacun indépendamment, hydrogène, -NO¿2?, -NH¿2?, -SO¿2?R?9¿, ou -CH¿2?R?9¿; R?6¿ est hydrogène, C¿1? à C¿6? alkyle, C¿3? à C¿6? alcényle, -CH¿2?CH¿2?Z, -CH¿2?COR?7¿, -CH¿2?CH=CHCOR?7¿, (e), (f) ou (g); Y¿1? et Y?3¿ sont chacun indépendamment, N, ou CH; Y?2¿ et Y?4¿ sont chacun indépendamment, O, S, ou NR?13¿; R?7¿ est -OR?8¿, -NHR?8¿, -N(R?8¿)¿2?, ou -NHCH¿2?CH¿2?OR?8¿; Z est -OR¿8?, -OCH¿2?CH¿2?OR?8¿, -N(R?8¿)¿2?, ou (h); R¿8? est hydrogène ou C¿1? à C¿3? alkyle R?9¿ est C¿1? à C¿6? alkyle, C¿3? à C¿6? alcényle, OH, NHR?10¿, N(R?10¿)¿2?, CH¿2?COR?11¿, -CH¿2?CH=CHCOR?11¿, ou (i); R?10¿ est C¿1? à C¿3? alkyle, C¿3? à C¿4? alcényle, phényle, -CH¿2?CH¿2?OCH¿3?, ou -(j); R?11¿ est -OR?12¿, -NHR?12¿, -R(R?12¿)¿2?, ou -NHCH¿2?CH¿2?OR?12¿; R?12¿ est hydrogène, ou C¿1? à C¿3? alkyle; R?13¿ est hydrogène, ou C¿1? à C¿3? alkyle; W est une liaison, CH¿2?, CH¿2?CH¿2?, O, S(O)¿q?, NCHO, NCOCH¿3?, OR NR?12¿; m est 0 - 2; n est 0 - 2; q est 0 - 2, à condition que R?2¿ et R?3¿ ne soient pas tous les deux hydrogène; ou cette formule contient des sels pharmaceutiquement acceptables de ces composés, qui conviennent comme agents contraceptifs.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, UZ, VN, YU, ZA, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)