发明授权
- 专利标题: Retinoid antagonists and use thereof
- 专利标题(中): 类视黄醇拮抗剂及其用途
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申请号: US09307009申请日: 1999-05-07
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公开(公告)号: US06326397B1公开(公告)日: 2001-12-04
- 发明人: Werner Bollag , Michael Klaus , Peter Mohr , Paola Panina-Bordignon , Michael Rosenberger , Francesco Sinigaglia
- 申请人: Werner Bollag , Michael Klaus , Peter Mohr , Paola Panina-Bordignon , Michael Rosenberger , Francesco Sinigaglia
- 主分类号: A01N5300
- IPC分类号: A01N5300
摘要:
The present invention relates to novel retinoid antagonists of the formula I wherein the dotted bond can be either hydrogenated or form a double bond; and, when the dotted bond forms a double bond, R1 is lower alkyl and R2 is hydrogen; and, when the dotted bond is hydrogenated, R1 and R2 taken together are methylene to form a cis-substituted cyclopropyl ring; R3 is hydroxy or lower alkoxy; R4 is alkyl or alkoxy; and R5 and R6 are, independently, a C4-12 alkyl or a 5-12 cycloalkyl substituent containing from 1-3 rings which are either unsubstituted or substituted with from 1-3 lower alkyl groups, with the carbon atom of R5 and R6 being linked to the remainder of the molecule to form a quaternary carbon atom pharmaceutically acceptable salts of carbocylic acids of the formula I; as well as method for the treatment of osteoporosis and preneoplastic and neoplastic diseases, and a method for reducing or abolishing adverse events in subjects receiving retinoid agonist treatment by administering a retinoid antagonist.
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