Treating agent for Paget's disease of bone

• US 7,163,933 B2
• Filed: 02/21/2003
• Issued: 01/16/2007
• Est. Priority Date: 02/22/2002
• Status: Expired due to Fees

• Current Assignee: Board of Regents of the University of Texas System (University of Texas System)
• Original Assignee: Teijin Limited
• Inventors: Oue, Yasuhiro, Takenouchi, Kazuya, Ishizuka, Seiichi, Kurihara, Noriyoshi, Roodman, G. David, Imaizumi, Atsushi, Reddy, Sakamuri V.
• Primary Examiner(s): HUI, SAN MING R
• Application Number:
  US10/369,752
• Publication Number:
  US 20030191094A1
• Time in Patent Office: 1,425 Days
• Field of Search: 514/167
• US Class Current: 514/167
• CPC Class Codes: A61K 31/592 9,10-Secoergostane derivatives, e.g. ergocalciferol, i.e. vitamin D2
• CPC Class Codes: A61K 31/593 9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
• CPC Class Codes: A61K 38/06 Tripeptides
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease

Abstract

To obtain a treating agent for Paget'"'"'s disease of bone, there is provided a method of inhibiting expression of general transcription factor of steroid hormone receptor.

Claims

1. A method for treating Paget'"'"'s disease of bone, comprising administering to a patient a compound which inhibits expression of general transcription factor with an interactive relation to Vitamin D receptor, wherein said compound has the formula (2):

2. The method of claim 1, wherein R⁴ is n-butylcarbonyl, n-pentylcarbonyl, n-hexylcarbonyl, n-heptylcarbonyl, 1-pentenylcarbonyl, methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, iso-propoxycarbonyl, 2-methylpropoxycarbonyl, n-butoxycarbonyl, t-butoxycarbonyl, n-pentyloxycarbonyl, n-hexyloxycarbonyl, n-heptyloxycarbonyl, n-butylaminocarbonyl, n-pentylaminocarbonyl, n-heptylaminocarbonyl, n-pentenylaminocarbonyl, 2-(5-butyl)oxazolyl, 2-(5-butyl)thiazolyl, 2-(4-methyl)thiazolyl or 2-(4-propyl)thiazolyl.

3. The method of claim 1, wherein R¹ and R² together form an exocyclic methylene;

R³ is a single bond;

R⁴ is n-butoxycarbonyl or 2-methylpropoxycarbonyl;

R⁵ is hydrogen.

4. The method of claim 1, wherein R¹ and R² together form an exocyclic methylene;

R³ is a single bond;

R⁴ is n-butylcarbonyl, n-pentylcarbonyl, n-heptylcarbonyl or 1-pentenylcarbonyl;

R⁵ is hydrogen.

5. The method of claim 1, wherein R¹ and R² together form an exocyclic methylene;

R³ is a single bond;

R⁴ is n-butylaminocarbonyl, n-pentylaminocarbonyl, n-heptylaminocarbonyl or 1-pentenylaminocarbonyl;

R⁵ is hydrogen.

6. The method of claim 1, wherein R¹ and R² together form an exocyclic methylene;

R³ is a single bond;

R⁴ is 2-(5-butyl)oxazolyl, 2-(5-butyl)thiazolyl, 2-(4-methyl)thiazolyl or 2-(4-propyl)thiazolyl;

R⁵ is hydrogen.

7. The method of claim 1, wherein R¹ and R² together form an exocyclic methylene;

R³ is vinylene;

R⁴ is ethoxycarbonyl or t-butoxycarbonyl;

R⁵ is hydrogen.

8. The method of claim 1, wherein R¹ and R² are each hydrogen;

R³ is a single bond;

R⁴ is n-butoxycarbonyl;

R⁵ is hydrogen.

9. The method of claim 1, wherein R¹ and R² are each hydrogen;

R³ is vinylene;

R⁴ is ethoxycarbonyl;

R⁵ hydrogen.

10. The method of claim 1, wherein R¹ and R² are each hydrogen;

R³ is a single bond;

R⁴ is 2-(4-methyl)thiazolyl;

R⁵ is hydrogen.