Global Patent Index - EP 1173213 A1

EP 1173213 A1 20020123 - COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS

Title (en)

COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS

Title (de)

ZUSAMMENSETZUNGEN DIE BENZIMIDAZOLONEN UND PROGESTAGENE ENTHALTEN

Title (fr)

COMPOSITIONS A BASE DE BENZIMIDAZOLONES ET DE PROGESTERONES

Publication

EP 1173213 A1 20020123 (EN)

Application

EP 00932006 A 20000501

Priority

  • US 0011845 W 20000501
  • US 55235500 A 20000419

Abstract (en)

[origin: WO0066168A1] This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (1) wherein: A is O, S, or NR<4>; B is a bond between A and C=Q, or the moiety CR<5>R<6>; R<4>, R<5>, R<6> are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R<4> and R<5> to form a 5 to 7 membered ring; R<1> is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alkynyl, -COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 to C3 aminoalkyl) groups; R<2> is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R<3> is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate. These combinations may also be used in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.

IPC 1-7

A61K 45/06; A61K 31/57; A61P 15/18

IPC 8 full level

A61K 31/415 (2006.01); A61K 31/535 (2006.01); A61K 31/54 (2006.01); A61K 31/56 (2006.01); A61K 31/57 (2006.01); A61K 45/06 (2006.01); A61P 15/18 (2006.01)

CPC (source: EP)

A61K 31/415 (2013.01); A61K 31/535 (2013.01); A61K 31/54 (2013.01); A61K 31/56 (2013.01); A61K 31/57 (2013.01); A61K 45/06 (2013.01); A61P 15/18 (2017.12)

Citation (search report)

See references of WO 0066168A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

DOCDB simple family (publication)

WO 0066168 A1 20001109; AU 4980100 A 20001117; EP 1173213 A1 20020123

DOCDB simple family (application)

US 0011845 W 20000501; AU 4980100 A 20000501; EP 00932006 A 20000501