公开(公告)号：US20060281760A1

公开(公告)日：2006-12-14

申请号：US11451078

申请日：2006-06-12

申请人： David Blum ,  Yanzhong Wu ,  Jean Schmid ,  Timothy Doyle ,  Jay Afragola

发明人： David Blum ,  Yanzhong Wu ,  Jean Schmid ,  Timothy Doyle ,  Jay Afragola

IPC分类号： C07D403/04 ,  A61K31/506

CPC分类号： C07D403/04

摘要： The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2-pyrazin-2-yl-N-[(1S)-2,2,2-trifluoro-1-methylethyl]pyrimidin-4-amine hemifumarate which is a tubulin inhibitor useful in the treatment of cancer and processes of making said hemifumarate.

公开(公告)号：US20050124635A1

公开(公告)日：2005-06-09

申请号：US11007839

申请日：2004-12-08

申请人： Yanzhong Wu ,  Jean Schmid ,  Jay Afragola ,  David Blum ,  Semiramis Ayral-Kaloustian

发明人： Yanzhong Wu ,  Jean Schmid ,  Jay Afragola ,  David Blum ,  Semiramis Ayral-Kaloustian

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： C07D487/04

摘要： The present invention provides a process for the preparation of 6-[(substituted)phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R1 is CF3 or C2F5; R2 is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R3 and R4 are each independently H or C1-C3 alkyl; or R3 and R4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R5; R5 is C1-C3 alkyl; wherein the dotted line is an optional bond.

摘要翻译： 本发明提供了制备6 - [（取代的）苯基] - 三唑并嘧啶二羧酸盐和具有结构式（I）的水合盐的方法，其中：R 1是CF _{3 或C 2 F 5; R 2是H或C 1 -C 3烷基; n是2,3或4的整数; X是Cl或Br; R 3和R 4各自独立地为H或C 1 -C 3烷基; 或R 3和R 4当任选地与各自连接的氮原子一起形成具有1-2个氮原子的4至6元饱和杂环和0 -1个氧原子或0-1个硫原子，并且任选被R 5取代; R 5是C 1 -C 3烷基; R 5是C 1 -C 3烷基; 其中虚线是任选的键。}

公开(公告)号：US5570907A

公开(公告)日：1996-11-05

申请号：US338849

申请日：1994-11-14

申请人： Aviva Dromi ,  David Blum ,  Abraham Pick

发明人： Aviva Dromi ,  David Blum ,  Abraham Pick

IPC分类号： B42F9/00 ,  B42F13/42

CPC分类号： B42F9/00

摘要： A device for clamping together a plurality of loose leafs including first and second clamp members arranged in a jaw-like arrangement; force responsive closure apparatus for closing the first and second clamp members together in response to an externally applied closure force so as cause the first and second clamp members to enclose therebetween a selected plurality of loose leafs and so as to apply a clamping force thereto; and releasable locking apparatus for selectably locking the first and second clamp members together in clamping engagement with the plurality of loose leafs.

摘要翻译： 一种用于将多个松散叶片夹紧在一起的装置，包括以颚状布置布置的第一和第二夹紧构件; 力响应闭合装置，用于响应于外部施加的闭合力将第一和第二夹紧构件关闭在一起，从而使第一和第二夹紧构件在其间包围所选择的多个松散叶片并且向其施加夹紧力; 以及用于将第一和第二夹紧构件可选择地锁定在一起以与多个松散叶片夹紧接合的可释放锁定装置。