专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-9422321-B2 优先权日:2010-09-07 标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments 发明人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE 权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU 摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
专利号:US-7250435-B2 优先权日:1999-10-20 标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-7179918-B2 优先权日:2001-06-11 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-7468375-B2 优先权日:2004-04-26 标题:Inhibitors of the HIV integrase enzyme 发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.
专利号:US-6407103-B2 优先权日:1998-04-21 标 题:Indeno [1,2-c] pyrazol-4-ones and their uses 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
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合成参考文献
参考文献:10.1007/128_2011_200 摘要:Miller BL. DCC in the development of nucleic acid targeted and nucleic acid inspired structures. Top Curr Chem. 2012;322():107–37. doi: 10.1007/128_2011_200.