-
公开(公告)号:US20050240047A1
公开(公告)日:2005-10-27
申请号:US11088667
申请日:2005-03-24
申请人: I. Pickersgill , John Bishop , Christoph Koellner , Jean-Marc Gomez , Achim Geiser , Robert Hett , Vince Ammoscato , Stephen Munk , Young Lo , Fang-Ting Chiu , Vithalanand Kulkarni
发明人: I. Pickersgill , John Bishop , Christoph Koellner , Jean-Marc Gomez , Achim Geiser , Robert Hett , Vince Ammoscato , Stephen Munk , Young Lo , Fang-Ting Chiu , Vithalanand Kulkarni
CPC分类号: C07K5/06191 , C07F5/025 , C07F5/04 , Y02P20/55
摘要: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
摘要翻译: 本发明涉及硼酸酯和酸化合物的合成。 更具体地,本发明提供了用于大规模生产硼酸酯和酸化合物的改进的合成方法,包括肽硼酸蛋白酶体抑制剂硼替佐米。
-
公开(公告)号:US20100174072A1
公开(公告)日:2010-07-08
申请号:US12706063
申请日:2010-02-16
申请人: I. Fraser Pickersgill , John E. Bishop , Christoph Koellner , Jean-Marc Gomez , Achim Geiser , Robert Hett , Vince Ammoscato , Stephen Munk , Young Lo , Fang-Ting Chiu , Vithalanand R. Kulkarni
发明人: I. Fraser Pickersgill , John E. Bishop , Christoph Koellner , Jean-Marc Gomez , Achim Geiser , Robert Hett , Vince Ammoscato , Stephen Munk , Young Lo , Fang-Ting Chiu , Vithalanand R. Kulkarni
IPC分类号: C07F5/04
CPC分类号: C07K5/06191 , C07F5/025 , C07F5/04 , Y02P20/55
摘要: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
摘要翻译: 本发明涉及硼酸酯和酸化合物的合成。 更具体地,本发明提供了用于大规模生产硼酸酯和酸化合物的改进的合成方法,包括肽硼酸蛋白酶体抑制剂硼替佐米。
-
公开(公告)号:US20130005968A1
公开(公告)日:2013-01-03
申请号:US13615894
申请日:2012-09-14
申请人: I. Fraser Pickersgill , John E. Bishop , Christoph Koellner , Jean-Marc Gomez , Achim Geiser , Robert Hett , Vince Ammoscato , Stephen Munk , Young Lo , Fang-Ting Chiu , Vithalanand R. Kulkarni
发明人: I. Fraser Pickersgill , John E. Bishop , Christoph Koellner , Jean-Marc Gomez , Achim Geiser , Robert Hett , Vince Ammoscato , Stephen Munk , Young Lo , Fang-Ting Chiu , Vithalanand R. Kulkarni
IPC分类号: C07F5/04
CPC分类号: C07K5/06191 , C07F5/025 , C07F5/04 , Y02P20/55
摘要: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
-
公开(公告)号:US08283467B2
公开(公告)日:2012-10-09
申请号:US12706063
申请日:2010-02-16
申请人: Vince Ammoscato , John E. Bishop , Fang-Ting Chiu , Achim Geiser , Jean-Marc Gomez , Robert Hett , Christoph Koellner , Vithalanand R. Kulkarni , Young Lo , Stephen Munk , I. Fraser Pickersgill
发明人: Vince Ammoscato , John E. Bishop , Fang-Ting Chiu , Achim Geiser , Jean-Marc Gomez , Robert Hett , Christoph Koellner , Vithalanand R. Kulkarni , Young Lo , Stephen Munk , I. Fraser Pickersgill
IPC分类号: C07F5/02
CPC分类号: C07K5/06191 , C07F5/025 , C07F5/04 , Y02P20/55
摘要: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
摘要翻译: 本发明涉及硼酸酯和酸化合物的合成。 更具体地,本发明提供了用于大规模生产硼酸酯和酸化合物的改进的合成方法,包括肽硼酸蛋白酶体抑制剂硼替佐米。
-
公开(公告)号:US06403798B2
公开(公告)日:2002-06-11
申请号:US09793024
申请日:2001-02-26
申请人: Fang-Ting Chiu , Young S. Lo
发明人: Fang-Ting Chiu , Young S. Lo
IPC分类号: C07D48900
CPC分类号: C07D489/06
摘要: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.
摘要翻译: 制备可待因的可待因的方法及其盐,所述可待因包括可待因氧化可卡因酮,在强胺碱中形成二烯醇基醚同系物,使用过乙酸的二烯醇醚同族物的氧化,以及所得的14 - 羟可待因酮产品。
-
公开(公告)号:US20100317873A1
公开(公告)日:2010-12-16
申请号:US12483918
申请日:2009-06-12
申请人: Fang-Ting Chiu
发明人: Fang-Ting Chiu
IPC分类号: C07D339/08 , C07D339/04
CPC分类号: C07D339/04 , C07D339/08
摘要: R-α-Lipoic acid and its homologs are converted to their magnesium salts in the presence of a reduced form of the acid, dihydro-(+)-lipoic acid in the case of R-α-lipoic acid itself. The reduced form serves as a polymerization inhibitor, resulting in a Mg di-R-α-lipoate product of higher purity. The reduced acid retained in the product tends to convert to the starting acid, thereby avoiding the inclusion of an extraneous polymerization inhibitor in the product.
摘要翻译: 在R-α-硫辛酸本身的情况下,在还原形式的二氢 - (+) - 硫辛酸存在下,将R-α-硫辛酸及其同系物转化为其镁盐。 还原形式用作阻聚剂,得到更高纯度的Mg二-R-α-脂肪酸酯产物。 产物中残留的还原酸倾向于转化为起始酸,从而避免在产物中包含外来阻聚剂。
-
公开(公告)号:US06177567B1
公开(公告)日:2001-01-23
申请号:US09419409
申请日:1999-10-15
申请人: Fang-Ting Chiu , Young S. Lo
发明人: Fang-Ting Chiu , Young S. Lo
IPC分类号: C07D47100
CPC分类号: C07D489/06
摘要: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.
-
公开(公告)号:US4667038A
公开(公告)日:1987-05-19
申请号:US909659
申请日:1986-09-22
IPC分类号: C07D319/18 , A61K31/47 , A61K31/472 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07C67/00 , C07C253/00 , C07C255/42 , C07C255/43 , C07D217/04 , C07D217/18 , C07D217/20 , C07D405/06 , C07D405/12
CPC分类号: C07D405/06 , C07D217/20
摘要: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 and each independently --H or lower alkoxy; R.sub.3 and R.sub.4 are each independently lower alkyl; and R.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--, and pharmaceutically acceptable acid addition salts thereof are prepared by cyclizing, deoxygenating, coupling, or hydrogenating the intermediates disclosed herein.
摘要翻译: 式(1)的化合物其中R1和R2各自独立地是-H或低级烷氧基; R3和R4各自独立地为低级烷基; 并且R 5和R 6各自为-OCH 3,或一起形成-OCH 2 O-或-OCH 2 CH 2 O-,并且其药学上可接受的酸加成盐通过使本文公开的中间体环化,脱氧,偶联或氢化来制备。
-
公开(公告)号:US4613606A
公开(公告)日:1986-09-23
申请号:US803464
申请日:1985-12-02
IPC分类号: C07D319/18 , A61K31/47 , A61K31/472 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07C67/00 , C07C253/00 , C07C255/42 , C07C255/43 , C07D217/04 , C07D217/18 , C07D217/20 , C07D405/06
CPC分类号: C07D405/06 , C07D217/20
摘要: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.
摘要翻译: 式(1)的化合物其中R 1和R 2各自独立地为-H或低级烷氧基; R3和R4各自独立地为低级烷基; 并且R 5和R 6各自为-OCH 3,或一起形成-OCH 2 O-或-OCH 2 CH 2 O-,及其药学上可接受的酸加成盐是可用于治疗包括心绞痛,高血压和充血性心力衰竭的心血管疾病的钙通道阻滞剂。
-
公开(公告)号:US06262266B1
公开(公告)日:2001-07-17
申请号:US09667997
申请日:2000-09-22
申请人: Fang-Ting Chiu , Young S. Lo
发明人: Fang-Ting Chiu , Young S. Lo
IPC分类号: C07D47100
CPC分类号: C07D489/06
摘要: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.
-
-
-
-
-
-
-
-
-