EP 1957515 A2 20080820 - PRODRUG ERbeta-SELECTIVE SUBSTANCES, METHODS FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS
Title (en)
PRODRUG ERbeta-SELECTIVE SUBSTANCES, METHODS FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS
Title (de)
PRODRUGS ERbeta-SELEKTIVER SUBSTANZEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN
Title (fr)
PROMEDICAMENTS DE SUBSTANCES ERbeta-SELECTIVES, PROCEDES DE REALISATION ASSOCIES ET COMPOSITIONS PHARMACEUTIQUES CONTENANT CES COMPOSES
Publication
Application
Priority
- EP 2006011729 W 20061127
- DE 102005057224 A 20051129
Abstract (en)
[origin: DE102005057224A1] Sulfamoyl compounds (I) of 9alpha -substituted estratrienes and their pharmaceutically acceptable salts are new. Sulfamoyl compounds, of formula STEROID-Z (I), of 9alpha -substituted estratrienes and their pharmaceutically acceptable salts are new. Z : group of formula (a); n : 0-4; one of R 1>, R 2>, R 3>-SO 2NH 2 or -NHSO 2NH 2; others of R 1>, R 2>, R 3>, X, X 1>H, halo, cyano, nitro, 1-6C alkyl, C pF 2p+1, OCOR 20>, COOR 20>, OR 20>, CONHR 20> or OCONHR 21>; p : 1-3; R 20>, R 21>1-5C alkyl, 3-8C cycloalkyl, aryl, 1-4C alkylene-(aryl or 3-8C cycloalkyl) or 3-6C cycloalkylene(1-4C)alkyl, and R 20> may also be H; STEROID : group of formula (b); R 3>Z; R 16>hydroxy, tri(1-4C alkyl)silyloxy or OCOR 20>; alternatively, R 16>Z and then R 3> = hydroxy, methoxy, tri(1-4C alkyl)silyloxy or OCOR 20>; R 7>H, F, methyl or ethyl; R 9>linear or branched, optionally partly or entirely halogenated, alkyl, alkenyl or alkynyl of up to 3 C; and R 17>H or halo, and R 7>, R 16> and R 17> may be in alpha or beta positions. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antiinfertility; Osteopathic; Cardiant; Vasotropic; Antiinflammatory; Antiarthritic; Antirheumatic; Immunosuppressive; Cytostatic; Gynecological. MECHANISM OF ACTION : Carboanhydrase (CA) inhibitor. 3-Hydroxy-9alpha -vinylestra-1,3,5(10)-trien-16alpha -yl-3-sulfamoylbenzoate showed IC50 against CAI and CAII of 3400 and 490 nM, respectively.
IPC 8 full level
C07J 41/00 (2006.01); A61K 31/565 (2006.01); A61P 5/28 (2006.01); A61P 5/32 (2006.01); A61P 15/00 (2006.01); A61P 19/10 (2006.01)
CPC (source: EP KR)
A61K 31/565 (2013.01 - KR); A61P 1/04 (2017.12 - EP); A61P 5/24 (2017.12 - EP); A61P 5/28 (2017.12 - EP); A61P 5/30 (2017.12 - EP); A61P 5/32 (2017.12 - EP); A61P 5/34 (2017.12 - EP); A61P 5/36 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 9/02 (2017.12 - EP); A61P 13/08 (2017.12 - EP); A61P 15/00 (2017.12 - EP); A61P 15/08 (2017.12 - EP); A61P 17/00 (2017.12 - EP); A61P 17/14 (2017.12 - EP); A61P 19/00 (2017.12 - EP); A61P 19/08 (2017.12 - EP); A61P 19/10 (2017.12 - EP); A61P 25/00 (2017.12 - EP); A61P 29/00 (2017.12 - EP); A61P 37/00 (2017.12 - EP); A61P 37/02 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07J 41/00 (2013.01 - KR); C07J 41/0033 (2013.01 - EP)
Citation (search report)
See references of WO 2007062877A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA HR MK RS
DOCDB simple family (publication)
DE 102005057224 A1 20070531; AU 2006319383 A1 20070607; BR PI0619065 A2 20110920; CA 2629587 A1 20070607; CN 101316857 A 20081203; CR 9981 A 20080922; EA 200801352 A1 20081030; EC SP088481 A 20080630; EP 1957515 A2 20080820; EP 2039702 A2 20090325; JP 2009517427 A 20090430; KR 20080070839 A 20080731; NO 20082913 L 20080729; WO 2007062877 A2 20070607; WO 2007062877 A3 20071108; ZA 200805656 B 20091125
DOCDB simple family (application)
DE 102005057224 A 20051129; AU 2006319383 A 20061127; BR PI0619065 A 20061127; CA 2629587 A 20061127; CN 200680044862 A 20061127; CR 9981 A 20080516; EA 200801352 A 20061127; EC SP088481 A 20080529; EP 06829357 A 20061127; EP 08161982 A 20061127; EP 2006011729 W 20061127; JP 2008542681 A 20061127; KR 20087012803 A 20080528; NO 20082913 A 20080627; ZA 200805656 A 20080627