Remedial agent for osteoporosis

• US 20030220307A1
• Filed: 02/19/2003
• Published: 11/27/2003
• Est. Priority Date: 08/17/2000
• Status: Abandoned Application

• Current Assignee: Chugai Seiyaku Kabushiki Kaisha (Roche Holding AG)
• Original Assignee: Chugai Seiyaku Kabushiki Kaisha (Roche Holding AG)
• Inventors: Takeda, Satoshi, Uchiyama, Yasushi, Kawase, Akira
• Application Number:
  US10/344,859
• Publication Number:
  US 20030220307A1
• Time in Patent Office: Days
• US Class Current: 514/167
• CPC Class Codes: A61K 31/593 9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: A61P 3/02 Nutrients, e.g. vitamins, minerals

Abstract

The object of the present invention is to provide a therapeutic agent for osteoporosis with a good bone mass-increasing effect, but almost no blood calcium-increasing effect.

The present invention provides a therapeutic agent for osteoporosis which comprises, as an active ingredient, a compound of Formula (1):

wherein

R₁ and R₂ each represent a hydrogen atom or a methyl group,

R₃ represents a C₁-C₄ alkyl group which may be substituted with a fluorine atom,

m represents an integer of 0 to 3, and

A represents —CH₂—CH₂—, —CH═CH— or —C≡C—.

Claims

1. A therapeutic agent for osteoporosis which comprises, as an active ingredient, a compound of Formula (1):

2. The therapeutic agent for osteoporosis according to claim 1, which comprises, as an active ingredient, a compound of Formula (1) wherein R₁ is a hydrogen atom and R₂ is a methyl group.

3. The therapeutic agent for osteoporosis according to claim 1, which comprises, as an active ingredient, a compound of Formula (1) wherein R₁ is a hydrogen atom, R₂ is a methyl group, R₃ represents a C₁-C₃ alkyl group which may be substituted with a fluorine atom, m represents an integer of 0 to 3, and A is —

CH═

CH—

or —

C≡

C—

.

4. The therapeutic agent for osteoporosis according to claim 1, which comprises, as an active ingredient, a compound of Formula (1) wherein R₁ is a hydrogen atom, R₂ is a methyl group, R₃ represents a C₁-C₃ alkyl group, m represents an integer of 2 or 3, and A is —

CH═

CH—

or —

C≡

C—

.

5. The therapeutic agent for osteoporosis according to claim 1, wherein the compound of Formula (1) is 1α

,3β

-dihydroxy-20(S)-(5-ethyl-5-hydroxy-3-heptynyl)-9,10-secopregna-5,7,10(19),16-tetraene.

6. The therapeutic agent for osteoporosis according to claim 1, which comprises, as an active ingredient, a compound of Formula (1) wherein R₁ is a hydrogen atom, R₂ is a methyl group, R₃ represents a C₁-C₃ alkyl group which may be substituted with a fluorine atom, m represents an integer of 0 to 3, and A is —

CH₂—

CH₂—

.

7. The therapeutic agent for osteoporosis according to claim 1, which comprises, as an active ingredient, a compound of Formula (1) wherein R₁ is a hydrogen atom, R₂ is a methyl group, R₃ represents a C₁-C₃ alkyl group, m represents 0, and A is —

CH₂—

CH₂—

.

8. The therapeutic agent for osteoporosis according to claim 1, wherein the compound of Formula (1) is 1α

,3β

-dihydroxy-20(S)-(3-ethyl-3-hydroxypentyl)-9,10-secopregna-5,7,10(19),16-tetraene.

9. A vitamin D derivative of the following Formula (2):

10. The vitamin D derivative according to claim 9, wherein in Formula (2), R₁ is a hydrogen atom and R₂ is a methyl group.

11. The vitamin D derivative according to claim 9, wherein the compound of Formula (2) is 1α

,3β

-dihydroxy-20(S)-(5-ethyl-5-hydroxy-3-heptynyl)-9,10-secopregna-5,7,10(19),16-tetraene.

12. A pharmaceutical composition comprising the vitamin D derivative according to any one of claims 9 to 11 as an active ingredient.

13. A method for treating osteoporosis, which comprises the step of administering to a patient in need of such treatment a therapeutically effective amount of a compound of Formula (1):