Global Patent Index - EP 1054676 A1

EP 1054676 A1 2000-11-29 - COMBINATION PREPARATION OF ESTROGEN AND ANTI-ESTROGEN

Title (en)

COMBINATION PREPARATION OF ESTROGEN AND ANTI-ESTROGEN

Title (de)

KOMBINATIONSPRÄPARAT AUS ÖSTROGEN UND ANTIÖSTROGEN

Title (fr)

PREPARATION COMBINEE D'OESTROGENE ET D'ANTI-OESTROGENE

Publication

EP 1054676 A1 (DE)

Application

EP 99908916 A

Priority

  • DE 19807791 A
  • EP 9901023 W

Abstract (en)

[origin: DE19807791A1] An estrogen/antiestrogen combination preparation comprises 17 beta -estradiol, 17 alpha -estradiol, estriol, estrone, estrone sulfate, estrogen sulfamate, 17 alpha -estradiol, mestranol, stilbestrol or a natural conjugated estrogen as the estrogen component and a 7 alpha -(xi-aminoalkyl)-estratriene (I) as the antiestrogen component. An estrogen/antiestrogen combination preparation comprises: a) 17 beta -estradiol, 17 alpha -estradiol, estriol, estrone, estrone sulfate, estrogen sulfamate, 17 alpha -estradiol, mestranol, stilbestrol or a natural conjugated estrogen as the estrogen component; and b) a 7 alpha -(xi-aminoalkyl)-estratriene (I) or one of its addition salts as the antiestrogen component. SK = -(CH2)m-N(A)-CH(B)-CH(D)-(CH2)n-SOx-(CH2)3-E; m = 4-6; n and x = 0-2; A = H or 1-5C alkyl and B and D = H; or A+B = -(CH2)p- and D = H; p = 2-5; E = ethyl optionally mono- to penta-substituted with F; or -(CH2)3-E is replaced with optionally substituted aryl or heteroaryl linked to SOx directly or via mono-, di- or trimethylene; R<3> = H; a hydrocarbyl group with up to 8C; or R<3>'-C(O)-; R<3>' = H; a hydrocarbyl group with up to 8C; or phenyl; R<11> = H; halo; or -O-NO2; R<14>, R<15>a, R15b, R16a and R16b = H; or R<14>+R15a = an additional bond or -CH2-; or R15b = methyl and R15a = H; or R15a and R15b = methyl; or R15b+R16b = -CH2-; or R16a or R16b = halo; or R16a+R16b = =CH2; and the rest of R<14>, R15a, R15b, R16a and R16b = H; R<17>' = H; 1-5C alkyl; 2-5C alkenyl; 2-5C alkynyl; or CF3; or alpha -position R<17>'+R<14> = an ethano bridge R<17>'' = H;or R<17>'''-C(O)-; R<17>''' = H or a hydrocarbyl group with up to 8C; compounds are excluded when R<11>, R<14>, R<15>a, R15b, R16a and R16b are each H and A+B is other than -(CH2)p or A+D is other than -(CH2)q-.

IPC 1-7 (main, further and additional classification)

A61K 31/565; A61K 31/10

IPC 8 full level (invention and additional information)

A61K 31/565 (2006.01); A61K 31/10 (2006.01); A61K 31/56 (2006.01); A61K 31/57 (2006.01); A61K 31/575 (2006.01); A61P 5/00 (2006.01); A61P 5/30 (2006.01); A61P 5/32 (2006.01)

CPC (invention and additional information)

A61K 31/57 (2013.01); A61K 31/567 (2013.01); A61K 31/575 (2013.01)

Combination set (CPC)

  1. A61K 31/575 + A61K 31/565
  2. A61K 31/57 + A61K 31/565
  3. A61K 31/57 + A61K 2300/00
  4. A61K 31/575 + A61K 2300/00

Citation (search report)

See references of WO 9942109A1

Designated contracting state (EPC)

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

Designated extension state (EPC)

AL LT LV MK RO SI

EPO simple patent family

DE 19807791 A1 19990826; AR 017982 A1 20011024; AU 2834799 A 19990906; BR 9908094 A 20001031; CA 2321427 A1 19990826; EP 1054676 A1 20001129; IL 137491 D0 20010724; JP 2002503695 A 20020205; PE 02612000 A1 20000522; US 6677324 B1 20040113; WO 9942109 A1 19990826; ZA 9901370 B 19991124

INPADOC legal status


2008-10-22 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20080429

2007-12-05 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: A61K 31/565 20060101AFI20071026BHEP

2007-12-05 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: A61K 31/10 20060101ALI20071026BHEP

2007-12-05 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: A61P 5/30 20060101ALI20071026BHEP

2007-12-05 [RIC1] CLASSIFICATION (CORRECTION)

- IPC: A61P 5/32 20060101ALI20071026BHEP

2007-05-09 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT

2007-05-02 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20020516

2007-05-02 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: BAYER SCHERING PHARMA AG

2002-07-03 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20020516

2000-11-29 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000719

2000-11-29 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

2000-11-29 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Free text: AL PAYMENT 20000719;LT PAYMENT 20000719;LV PAYMENT 20000719;MK PAYMENT 20000719;RO PAYMENT 20000719;SI PAYMENT 20000719