Title:
SPIRO COMPOUNDS, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES OF THE COMPOUNDS
Document Type and Number:
WIPO Patent Application WO/2004/031125
Kind Code:
A1
Abstract:
Spiro compounds represented by the following general formula (I) or pharmaceutically acceptable acid-addition salts thereof: (I) wherein R1 and R2 are the same or different and each represents hydrogen, chlorine, etc.; n is 1, 2 or 3; a bond having a broken line represents a single or double bond; and A represents -X-(CH2)q-N(R3)(R4), a group represented by the following general formula (a), etc. (a) (wherein X represents oxygen or sulfur; q is 2 or 3; R3 and R4 are the same or different and each represents C1-6 alkyl, etc., or R3 and R4 may form together with the adjacent nitrogen atom a piperidine ring, etc. optionally having one or two C1-6 alkyl substituents, etc.; R5 represents C1-6 alkyl, etc.; R6 represents hydrogen, etc.; and r and t independently represent each 1 or 2. These compounds are useful as selective estrogen receptor modulators having an effect of ameliorating symptoms of menopause. They are also expected as being usable as preventives and/or remedies for osteoporosis, symptoms of menopause and breast cancer.
Inventors:
WATANABE NOBUHIDE (JP)
NAKAGAWA HIROSHI (JP)
TSUJI JUN-ICHI (JP)
MINATO HISAO (JP)
IKENO AKIHISA (JP)
KOHAYAKAWA CHIE (JP)
NAKAGAWA HIROSHI (JP)
TSUJI JUN-ICHI (JP)
MINATO HISAO (JP)
IKENO AKIHISA (JP)
KOHAYAKAWA CHIE (JP)
Application Number:
PCT/JP2003/004889
Publication Date:
April 15, 2004
Filing Date:
April 17, 2003
Export Citation:
Assignee:
DAINIPPON PHARMACEUTICAL CO (JP)
WATANABE NOBUHIDE (JP)
NAKAGAWA HIROSHI (JP)
TSUJI JUN-ICHI (JP)
MINATO HISAO (JP)
IKENO AKIHISA (JP)
KOHAYAKAWA CHIE (JP)
WATANABE NOBUHIDE (JP)
NAKAGAWA HIROSHI (JP)
TSUJI JUN-ICHI (JP)
MINATO HISAO (JP)
IKENO AKIHISA (JP)
KOHAYAKAWA CHIE (JP)
International Classes:
A61K31/40; A61K31/445; A61K31/4453; A61K31/451; A61K31/495; A61K31/55; A61P15/12; A61P19/10; A61P35/00; A61P43/00; C07C217/20; C07C217/24; C07D211/14; C07D295/092; (IPC1-7): C07C217/18; A61K31/138; A61K31/40; A61K31/4453; A61K31/495; A61P15/12; A61P19/10; A61P35/00; A61P43/00; C07D211/22; C07D295/088; A61K31/55; A61K31/445; A61K31/451; C07D295/096; C07D211/14
Other References:
COLLINS DAVID J. ET AL.: "The structure and function of estrogens. I. Synthesis of 4b-methyl-trans-4b,5,6,10b,11,12-hexahydrochrysene-2,8-diol", AUSTRALIAN JOURNAL OF CHEMISTRY, vol. 32, no. 5, 1979, pages 1093 - 1106, XP002971304
CARLSON HEATHER A. ET AL.: "Developing a dynamic pharmacophore model for HIV-1 integrase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, no. 11, 2000, pages 2100 - 2114, XP000999138
See also references of EP 1559707A4
CARLSON HEATHER A. ET AL.: "Developing a dynamic pharmacophore model for HIV-1 integrase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, no. 11, 2000, pages 2100 - 2114, XP000999138
See also references of EP 1559707A4
Attorney, Agent or Firm:
Takashima, Hajime (1-1 Fushimimachi 4-chome, Chuo-ku, Osaka-sh, Osaka ., JP)
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