发明公开
EP1042313A1 BENZOPYRAN AND BENZOTHIOPYRAN DERIVATIVES HAVING RETINOID ANTAGONIST LIKE ACTIVITY
有权
苯并吡喃和以维A拮抗剂样活性苯并噻衍生物
- 专利标题: BENZOPYRAN AND BENZOTHIOPYRAN DERIVATIVES HAVING RETINOID ANTAGONIST LIKE ACTIVITY
- 专利标题(中): 苯并吡喃和以维A拮抗剂样活性苯并噻衍生物
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申请号: EP98964231.9申请日: 1998-12-21
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公开(公告)号: EP1042313A1公开(公告)日: 2000-10-11
- 发明人: KLEIN, Elliott, S. , JOHNSON, Alan, T. , STANDEVEN, Andrew, M. , BEARD, Richard, L. , GILLETT, Samuel, J. , DUONG, Tien, T. , NAGPAL, Sunil , VULIGONDA, Vidyasagar , TENG, Min , CHANDRARATNA, Roshantha, A.
- 申请人: Allergan Sales, Inc.
- 申请人地址: 2525 Dupont Drive Irvine, CA 92612 US
- 专利权人: Allergan Sales, Inc.
- 当前专利权人: Allergan Sales, Inc.
- 当前专利权人地址: 2525 Dupont Drive Irvine, CA 92612 US
- 代理机构: HOFFMANN - EITLE
- 优先权: US998319 19971224
- 国际公布: WO9933821 19990708
- 主分类号: C07D335/06
- IPC分类号: C07D335/06 ; C07D311/58 ; C07D213/55 ; C07D277/30 ; C07D333/24 ; C07D307/54 ; C07D409/04 ; C07D409/06 ; C07C69/78 ; C07C233/65 ; C07C327/48 ; A61K31/44 ; A61K31/335 ; A61K31/38 ; A61K31/425
摘要:
2,2-Dialkyl- 4-aryl-substituted benzopyran and benzothiopyran derivatives of formula (I) where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action or RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.
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