专利号:US-9353112-B2 优先权日:2012-03-07 标 题 :Synthesis of polycyclic alkaloids 发明人:GOFF DANE; PAYAN DONALD G; BRASELMANN SYLVIA 权利人:RIGEL PHARMACEUTICALS INC 摘要:Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
专利号:US-8524740-B2 优先权日:2010-07-15 标 题 :Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives 发明人:KUO SHENG-CHU; LEE KUO-HSIUNG; HUANG LI-JIAU; CHOU LI-CHEN; WU TIAN-SHUNG; WAY TZONG-DER; CHUNG JING-GUNG; YANG JAI-SING; HUANG CHI-HUNG; TSAI MENG-TUNG 权利人:KUO SHENG-CHU; LEE KUO-HSIUNG; HUANG LI-JIAU; CHOU LI-CHEN; WU TIAN-SHUNG; WAY TZONG-DER; CHUNG JING-GUNG; YANG JAI-SING; HUANG CHI-HUNG; TSAI MENG-TUNG; TAIRX INC 摘要:A compound of Formula I is disclosed as follows: n n n n n n n n n n n n or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein n R is hydrogen, P(â•?O)(OH) 2 , P(â•?O)(O(C 1 -C 18 )alkylene(C 6 -C 20 )aryl) 2 , P(â•?O)(OH)(OM), P(â•?O)(OM) 2 , Pâ•?O(O 2 M), S(â•?O)(OH) 2 , S(â•?O)(O(C 1 -C 18 )alkylene(C 6 -C 20 )aryl) 2 , S(â•?O)(OH)(OM), S(â•?O)(OM) 2 ; n M is a monovalent or divalent metal ion, or alkylammonium ion; n W is (C 6 -C 20 )aryl, (C 6 -C 20 )heteroaryl, (C 1 -C 18 )alkyl(C 6 -C 20 )aryl, (C 1 -C 18 )alkyl(C 6 -C 20 )heteroaryl, hydroxy(C 6 -C 20 )aryl, hydroxy(C 6 -C 20 )heteroaryl, (C 1 -C 18 )alkoxy(C 6 -C 20 )aryl, (C 1 -C 18 )alkoxy(C 6 -C 20 )heteroaryl, (C 1 -C 18 )alkylenedioxy(C 6 -C 20 )aryl, (C 1 -C 18 )alkylenedioxy(C 6 -C 20 )heteroaryl, halo(C 6 -C 20 )aryl, halo(C 6 -C 20 )heteroaryl, (C 1 -C 18 )alkylamino(C 6 -C 20 )aryl, (C 1 -C 18 )alkylamino(C 6 -C 20 )heteroaryl, (C 1 -C 18 )cycloalkylamino(C 6 -C 20 )aryl, or (C 1 -C 18 )cycloalkylamino(C 6 -C 20 )heteroaryl, and their OR 8 substutes; n R 5 is (C 1 -C 18 alkoxy, hydrogen, hydroxyl, O—(C 1 -C 18 )alkyl(C 6 -C 20 )aryl, halo or OR 8 , or R 5 and R 6 are (C 1 -C 18 )dioxy provided that R 7 is hydrogen; n R 6 is hydroxyl, O—(C 1 -C 18 )alkyl(C 6 -C 20 )aryl, halo or OR 8 , (C 1 -C 18 )alkoxy, (C 1 -C 18 )alkylamino, or (C 1 -C 18 )cycloalkylamino, or R 6 and R 7 are (C 1 -C 18 )dioxy provided that R 5 is hydrogen; n R 7 is hydrogen, halo or OR 8 , hydroxyl, or O—(C 1 -C 18 )alkyl(C 6 -C 20 )aryl; and n R 8 is P(â•?O)(OH) 2 , P(â•?O)(O(C 1 -C 18 )alkyl(C 6 -C 20 )aryl) 2 , Pâ•?O)(OH)(OM), or P(â•?O)(OM) 2 , Pâ•?O(O 2 M).
专利号:EP-0674008-A1 优先权日:1989-08-30 标 题:Preparation of optically active cyclohexenol and cyclohexenyl acetic acid via an enzymatic process followed by a rearrangement reaction and their use as intermediates in the synthesis of indolobenzoquinoline derivatives
专利号:US-8927564-B2 优先权日:2012-03-07 标题:Synthesis of polycyclic alkaloids
专利号:US-2015087633-A1 优先权日:2012-03-07 标题 :Synthesis of polycyclic alkaloids
专利号:ES-2773838-T3 优先权日:2012-03-07 标 题:Synthesis of polycyclic alkaloids and their use as TGR5 agonists
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