Please download the dossier by clicking on the dossier button x
×

Process for production of crystals of 11ss-benzaldoxim-estra-4,9-diene derivatives, crystals obtained thereby and pharmaceutical preparations containing them

  • US 20030225050A1
  • Filed: 04/17/2003
  • Published: 12/04/2003
  • Est. Priority Date: 04/23/2002
  • Status: Active Grant
First Claim
Patent Images

1. A process for making crystals of a 11β

  • -benzaldoxim-estra-4,9-diene derivative, said crystals having an average particle size in a predetermined size range and a maximum particle size that does not exceed a predetermined maximum value, said process comprising subjecting a supersaturated solution containing said 11β

    -benzaldoxim-estra-4,9-diene derivative to a wet milling by a wet milling apparatus while crystallizing, in order to obtain a primary particle suspension;

    wherein said 11β

    -benzaldoxim-estra-4,9-diene derivative is a compound of formula (I), or a pharmacologically acceptable salt thereof;

    wherein R1 represents hydrogen or an alkyl group with 1 to 6 carbon atoms;

    R2 represents hydrogen, an alkyl group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms, an alkylaryl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a —

    CONHR4 group, R3 represents hydrogen, an alkyl group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms, an alkylaryl group with 1 to 10 carbon atoms, or a —

    (CH2)n

    CH2X, an —

    OR5 group, a —

    (CH2)o

    CH═

    CH(CH2)p

    R6 group or —

    (CH2)qC═

    CR7;

    wherein n is 0, 1 or 2, o is 0, 1, 2 or 3, p is 0, 1 or 2 and q is 0, 1 or 2;

    wherein X represents hydrogen, a fluoro group, a chloro group, a bromo group, an iodo group, a cyano group, an azido group, a rhodano group, an —

    OR5 group or an —

    SR5 group;

    wherein Z represents hydrogen, an alkyl group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms, an alkylaryl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms, a —

    CONHR4 group, a —

    COOR4 group, an alkali metal atom or an alkaline earth metal atom;

    wherein R4 represents an alkyl group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms or an alkylaryl group with 1 to 10 carbon atoms;

    wherein R5 represents hydrogen, an alkyl group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms, an alkylaryl group with 1 to 10 carbon atoms or an acyl group with 1 to 10 carbon atoms;

    wherein R6 represents a hydrogen, a hydroxy group, an alkyl group with 1 to 10 carbon atoms, an alkoxy group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms, an alkylaryl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or an acyloxy group with 1 to 10 carbon atoms; and

    wherein R7 represents a hydrogen, a fluoro group, a chloro group, a bromo group, an iodo group, an alkyl group with 1 to 10 carbon atoms, an aryl group with 1 to 10 carbon atoms, an aralkyl group with 1 to 10 carbon atoms, an alkylaryl group with 1 to 10 carbon atoms or an acyl group with 1 to 10 carbon atoms.

View all claims
  • 4 Assignments
Timeline View
Assignment View
    ×
    ×