16-ENE-vitamin D derivatives

• US 6,555,699 B2
• Filed: 06/24/2002
• Issued: 04/29/2003
• Est. Priority Date: 12/20/1996
• Status: Expired due to Fees

• Current Assignee: Chugai Seiyaku Kabushiki Kaisha (Roche Holding AG)
• Original Assignee: Chugai Seiyaku Kabushiki Kaisha (Roche Holding AG)
• Inventors: Kawase, Akira
• Primary Examiner(s): QAZI, SABIHA NAIM
• Application Number:
  US10/177,603
• Publication Number:
  US 20020193616A1
• Time in Patent Office: 309 Days
• Field of Search: 552/653, 514/167
• US Class Current: 552/653
• CPC Class Codes: C07C 401/00 Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
• CPC Class Codes: C07J 31/006 not covered by C07J31/003
• CPC Class Codes: C07J 7/007 not substituted in position 17 alfa
• CPC Class Codes: Y02P 20/55 Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

The compound of the formula (24):

wherein R₉ and R₁₀ may be the same or different and each represent a hydrogen atom or a protecting group.

Claims

1. A compound of the formula (24):

wherein R₉ and R₁₀ may be the same or different and each represent a hydrogen atom or a protecting group.

2. A method for treating a tumor, comprising administering to a patient in need thereof a therapeutically effective amount for said treatment of a vitamin D derivative of formula (1):

wherein X represents an oxygen or sulfur atom, R₁₁ represents

(i) a saturated or unsaturated aliphatic hydrocarbon group which may be substituted by a hydroxyl group or a protected hydroxyl group,

(ii) a —

COR₁₂ group where R₁₂ represents an alkyl, aryl or alkoxy group, or

(iii)

wherein R₅ and R₆ represent a hydrogen atom or a hydroxyl group, m represents an integer of 1 to 4 and n represents an integer of 0 to 2, or R₂ represents —

OR₉ or a hydrogen atom, and R₁₀ and R₁₀ may be the same or different and each represent a hydrogen atom or a protecting group.

3. The method of claim 2, wherein said vitamin D derivative of formula (1) is administered in a pharmaceutical composition thereof.

4. A method for treating rheumatism, comprising administering to a patient in need thereof a therapeutically effective amount for said treatment for a vitamin D derivative of formula (1)

wherein X represents an oxygen or sulfur atom, R₁₁ represents

(i) a saturated or unsaturated aliphatic hydrocarbon group which may be substituted by a hydroxyl group or a protected hydroxyl group,

(ii) a —

COR₁₂ group where R₁₂ represents an alkyl, aryl or alkoxy group, or

(iii)

wherein R₅ and R₆ each represent a hydrogen atom or a hydroxyl group, m represents an integer of 1 to 4 and n represents an integer of 0 to 2, or R₂ represents —

OR₉ or a hydrogen atom, and R₉ and R₁₀ may be the same or different and each represent a hydrogen atom or a protecting group.

5. The method of claim 4 wherein R₉ and R₁₀ may be the same or different and each represent a hydrogen atom or a protecting group.