Global Patent Index - EP 0859761 A4

EP 0859761 A4 2000-01-26 - 4-AZASTEROIDS FOR TREATMENT OF HYPERANDROGENIC CONDITIONS

Title (en)

4-AZASTEROIDS FOR TREATMENT OF HYPERANDROGENIC CONDITIONS

Title (de)

4-AZASTEROIDE ZUR BEHANDLUNG VON HYPERANDROGENEN ZUSTÄNDEN

Title (fr)

4-AZASTEROIDES UTILISES POUR LE TRAITEMENT D'ETATS HYPERANDROGENIQUES

Publication

EP 0859761 A4 (EN)

Application

EP 96930822 A

Priority

  • GB 9603487 A
  • US 9614564 W
  • US 382695 P

Abstract (en)

[origin: WO9710217A1] Compounds of structural Formula (I), and pharmacologically acceptable salts and esters thereof possess 5 alpha -reductase inhibitory activity. These compounds inhibit 5 alpha -reductase type 1 and type 2. The compounds of structural Formula (I) are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent anti-androgens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

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

C07D 221/02; A61K 31/435; C07J 73/00

IPC 8 full level (invention and additional information)

A61K 31/58 (2006.01); A61K 31/00 (2006.01); A61K 31/435 (2006.01); A61P 5/24 (2006.01); C07J 43/00 (2006.01); C07J 73/00 (2006.01)

CPC (invention and additional information)

C07J 73/005 (2013.01); A61K 31/435 (2013.01)

Citation (search report)

  • [Y] WO 9407861 A1 19940414 - MERCK & CO INC [US], et al
  • [Y] BAKSHI R K ET AL: "4-Aza-3-oxo-5.alpha.-androst-1-ene-17.beta.-N-arylcarboxamides as Dual Inhibitors of Human Type 1 and Type 2 Steroid 5.alpha.-Reductases. Dramatic Effect of N-Aryl Substituents on Type 1 and Type 2 5.alpha.-Reductase Inhibitory Potency", JOURNAL OF MEDICINAL CHEMISTRY., vol. 38, no. 17, 18 August 1995 (1995-08-18), WASHINGTON US, XP002087243
  • [L] BAKSHI ET AL: "Erratum to J. Med. Chem. Vol 38, Nr 17, pages 3189-3192, 18 August 1995", JOURNAL OF MEDICINAL CHEMISTRY., vol. 39, no. 5, 1 March 1996 (1996-03-01), WASHINGTON US, pages 1192, XP002089558
  • [Y] MELLIN T N ET AL: "AZASTEROIDS AS INHIBITORS OF TESTOSTERONE 5ALPHA-REDUCTASE IN MAMMALIAN SKIN", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 44, no. 2, February 1993 (1993-02-01), pages 121 - 131, XP002028037
  • [Y] RASMUSSON G H ET AL: "AZASTEROIDS AS INHIBITORS OF RAT PROSTATIC 5ALPHA-REDUCTASE", JOURNAL OF MEDICINAL CHEMISTRY, vol. 27, no. 12, December 1984 (1984-12-01), pages 1690 - 1701, XP002043194
  • [Y] CHEMICAL ABSTRACTS, vol. 122, no. 25, 19 June 1995, Columbus, Ohio, US; abstract no. 314919, ZHENG, JINHONG ET AL: "Synthesis of N-substituted-4-methyl-3-oxo-4-aza-5.alpha.-androstane- 17.beta.-carboxamide compounds" XP002121894 & ZHONGGUO YAOKE DAXUE XUEBAO (1995), 26(1), 1-4ZHONGGUO YAOKE DAXUE XUEBAO (1995), 26(1), 1-4
  • [PY] KURATA H ET AL: "SYNTHESIS AND TESTOSTERONE 5ALPHA-REDUCTASE-INHIBITORY ACTIVITY OF 4-AZA-5ALPHA-ANDROSTANE-17-CARBOXAMIDE COMPOUND WITH AN AROMATIC MOIETY IN THE C-17 CARBAMOYL GROUP", CHEMICAL AND PHARMACEUTICAL BULLETIN,JP,PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, vol. 44, no. 1, pages 115-121, XP000569266, ISSN: 0009-2363
  • See also references of WO 9710217A1

Designated contracting state (EPC)

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

EPO simple patent family

WO 9710217 A1 19970320; AU 6973796 A 19970401; AU 707324 B2 19990708; CA 2231041 A1 19970320; EP 0859761 A1 19980826; EP 0859761 A4 20000126; JP H11512434 A 19991026

INPADOC legal status


2005-04-27 [18R] REFUSED

- Effective date: 20041119

2003-03-05 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20030117

2000-01-26 [A4] SUPPLEMENTARY SEARCH REPORT

- Effective date: 19991209

2000-01-26 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A4

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

1998-08-26 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 19980415

1998-08-26 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

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