发明授权
US06875775B2 Triphenylalkene derivatives and their use as selective estrogen receptor modulators
有权
三苯基烯烃衍生物及其作为选择性雌激素受体调节剂的用途
- 专利标题: Triphenylalkene derivatives and their use as selective estrogen receptor modulators
- 专利标题(中): 三苯基烯烃衍生物及其作为选择性雌激素受体调节剂的用途
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申请号: US10408303申请日: 2003-04-08
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公开(公告)号: US06875775B2公开(公告)日: 2005-04-05
- 发明人: Marja-Liisa Södervall , Arja Kalapudas , Lauri Kangas , Risto Lammintausta , Pirkko Härkönen , Kalervo Väänänen , Arto Karjalainen
- 申请人: Marja-Liisa Södervall , Arja Kalapudas , Lauri Kangas , Risto Lammintausta , Pirkko Härkönen , Kalervo Väänänen , Arto Karjalainen
- 申请人地址: FI Turku
- 专利权人: Hormos Medical Oy LTD
- 当前专利权人: Hormos Medical Oy LTD
- 当前专利权人地址: FI Turku
- 代理机构: Sterne, Kessler, Goldstein & Fox P.L.L.C.
- 主分类号: A61K31/4164
- IPC分类号: A61K31/4164 ; A61K31/085 ; A61K31/09 ; A61K31/10 ; A61K31/136 ; A61K31/138 ; A61K31/145 ; A61K31/192 ; A61K31/4453 ; A61P5/30 ; A61P5/32 ; A61P9/02 ; A61P13/02 ; A61P15/02 ; A61P15/12 ; A61P19/10 ; A61P25/04 ; A61P25/20 ; A61P25/24 ; A61P25/28 ; A61P43/00 ; C07C43/225 ; C07C43/23 ; C07C59/68 ; C07C211/10 ; C07C211/53 ; C07C215/16 ; C07C217/18 ; C07C217/20 ; C07C323/12 ; C07C323/25 ; C07D211/14 ; C07D233/61 ; C07D295/092 ; C07D521/00 ; A61K31/445 ; A61K31/415 ; C07D211/32 ; C07D233/00 ; C07D211/21
摘要:
The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.
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