RU2002117440A

RU2002117440A - NEW ANDROGENS

Info

Publication number: RU2002117440A
Application number: RU2002117440/04A
Authority: RU
Inventors: Дирк Лейсен; ДЕР ЛАУ Яп ВАН; БУРСИ Роберта БУМА; ГОЙЕР Марсель Эверт ДЕ
Original assignee: Акцо Нобель Н.В.
Priority date: 1999-12-02
Filing date: 2000-11-29
Publication date: 2003-12-20

Claims

1. The compound corresponding to the structural formula

where R ₁ represents O, (H, H), (H, OR), NOR, wherein R represents hydrogen, (C _1-6 ) alkyl, (C _1-6 ) acyl;

R ₂ represents hydrogen or (C _1-6 ) alkyl;

R ₃ is hydrogen or R ₃ is (C _1-6 ) alkyl, (C _2-6 ) alkenyl or (C _2-6 ) alkynyl, each of which is optionally substituted with halogen;

R ₄ represents hydrogen, (C _1-6 ) alkyl or (C _2-6 ) alkenyl;

R ₅ represents (C _1-6 ) alkyl;

R ₆ represents hydrogen, halogen or (C _1-4 ) alkyl;

R ₇ represents hydrogen or (C _1-6 ) alkyl;

R ₈ represents hydrogen, hydroxy, (C _1-6 ) alkoxy, halogen or (C _1-6 ) alkyl;

R ₉ and R ₁₀ independently represent hydrogen or R ₉ and R ₁₀ independently represent (C _1-6 ) alkyl, (C _2-6 ) alkenyl, (C _3-6 ) cycloalkyl, (C _5-6 ) cycloalkenyl or (C _2-6 ) alkynyl, each of which is optionally substituted with (C _1-4 ) alkoxy or halogen;

R ₁₁ represents hydrogen, SO ₃ H, (C _1-15 ) acyl;

dashed lines indicate optional bonds selected from Δ ⁴ -, Δ ^{5 (10) -} or Δ ¹¹ double bond, or Δ ^4.9 - or Δ ^4.11 diene system.

2. The compound according to claim 1, characterized in that the substituent R ₁ represents O.

3. The compound according to claim 1 or 2, characterized in that the dashed lines indicate a double bond Δ ⁴ .

4. The compound according to any one of the preceding paragraphs, characterized in that R ₄ represents 7α-methyl.

5. The compound (7α, 14β, 15β, 17α) -17 (hydroxymethyl) -7-methyl-14,15-methyleneestra-4-en-3-one.

6. The compound according to any one of the preceding paragraphs for use in therapy.

7. The use of a compound according to any one of claims 1 to 6 for the manufacture of a medicament having androgenic activity.

8. A kit that provides hormonal contraception in a male individual and includes a sterilizing agent and androgen, characterized in that the androgen is a compound according to any one of claims 1 to 6.

9. A method of treatment, comprising administering to a person having androgen deficiency an effective amount of a compound according to any one of claims 1 to 6.

10. The method according to claim 9, characterized in that the person is male and androgen deficiency is the result of the introduction of a sterilizing agent to the indicated male person during the method of male contraception.