AZACARBOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC USE OF SAME
申请人:Arendt Christopher
公开号:US20110178053A1
公开(公告)日:2011-07-21
The invention relates to novel azacarbonlines having formula (I), wherein: R3, R4 represent independently H; hal; CF
3
; substituted oxy, optionally substituted alkoxy; optionally substituted amino; substituted carbonyl; optionally substituted carboxyl; optionally substituted amide; sulphur, such as optionally substituted sulphones, sulphoxides or sulphides; linear, branched or cyclic C
1
-C
10
alkyl optionally comprising an optionally substituted heteroatom; optionally substituted linear, branched or cyclic C
2
-C
7
alkenyl; optionally substituted linear or branched C
2
-C
6
alkynyl; optionally substituted aryl or heteroaryl; of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the use of same in therapeutics for the treatment of cancer and to synthesis methods.
Compounds of the formula (I), in which R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
9
, R
10
, R
11
, Q and W have the meanings indicated in Claim
1
, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumours.
Sauerstoff‐alkylierte Oxime gewinnen in der Arzneimittelsynthese zunehmend an Interesse. Als Beispiele seien die Antibiotika Cefuroxim (Zinacef®) und Cefotaxim (Claforan®), das Thymoleptikum Noxiptilin (Agedal®) und das Cardiotonikum Diclofurim2) aufgeführt, von denen die letzten beiden am Oximsauerstoff aminoethyliert sind.
Zur Umsetzung von Trialkylsulfonyldiamiden mit 2-Chlor-1-dimethylaminopropan und 3-Chlor-1-ethylpiperidin
作者:Bernard Unterhalt、Edmar Seebach
DOI:10.1002/ardp.19843171008
日期:——
Trimethylsulfonyldiamid‐Natrium (1) wurde mit 2‐Chlor‐1‐dimethylaminopropan zu den Isomeren 2 und 3 umgesetzt, die durch Säulenchromatographie getrennt werden konnten. Bei der Reaktion von 3‐Chlor‐1‐ethylpiperidin mit 1 sowie mit 4 entstand jeweils nur 1 Isomer, nämlich 6a bzw 6b.
3-Arylcarbonyl-1H-indoles useful as therapeutic agents
申请人:STERLING WINTHROP INC.
公开号:EP0444451A2
公开(公告)日:1991-09-04
2-R₂-R₄-substituted-3-R₃-CO-1-[(C-attached-N-heteryl)-(Alk)n]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.