AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX
申请人:THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
公开号:US20160215012A1
公开(公告)日:2016-07-28
Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.
[EN] UREA DERIVATIVES OF AMPHOTERICIN B DERIVED FROM SECONDARY AMINES<br/>[FR] DÉRIVÉS D'URÉE DE L'AMPHOTÉRICINE B DÉRIVÉE D'AMINES SECONDAIRES
申请人:UNIV ILLINOIS
公开号:WO2016112243A1
公开(公告)日:2016-07-14
Provided are certain urea derivatives of amphotericin B (AmB) having improved therapeutic index compared to AmB. The compounds of the invention are less toxic than AmB and are useful to treat fungal infections. In certain embodiments the urea derivative of AmB is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof: wherein, independently for each occurrence: R represents methyl, ethyl, propyl, or isopropyl; R' represents methyl, ethyl, propyl, or isopropyl; or R and R', taken together with the nitrogen atom to which they are attached, represent a radical of a cyclic secondary amine. Also provided are methods for making the urea derivatives of AmB.
Methods for treating an inflammatory condition or inhibiting JNK
申请人:——
公开号:US20040127536A1
公开(公告)日:2004-07-01
This invention is generally directed to Indazole Derivatives having the following structure:
1
or pharmaceutically acceptable salt thereof, wherein R
1
, R
2
and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
Indazole compounds, compositions thereof and methods of treatment therewith
申请人:Bhagwat S. Shripad
公开号:US20050009876A1
公开(公告)日:2005-01-13
This invention is generally directed to the use of Indazole Compounds for treating or preventing diseases associated with protein kinases, including tyrosine kinases, such as proliferative diseases, inflammatory diseases, abnormal angiogenesis and diseases related thereto, atherosclerosis, macular degeneration, diabetes, obesity, pain and others. The methods comprise the administration to a patient in need thereof of an effective amount of an indazole compound that inhibits, modulates or regulates tyrosine kinase signal transduction. Novel indazole compounds or pharmaceutically acceptable salt thereof are presented herein.
Novel aminotriazolone compounds, method for preparing same and pharmaceutical compositions containing same
申请人:——
公开号:US20040029875A1
公开(公告)日:2004-02-12
A compound of formula (I):
1
wherein:
R
1
and R
2
represent hydrogen or a group as defined in the description,
R
3
represents hydrogen or alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl,
R
4
represents a group of formula (II):
2
wherein W and B are as defined in the description,
R
5
represents hydrogen or alkyl,
A represents a group selected from -A
2
-, -A
1
-A
2
-, -A
2
-A
1
- and -A
1
-A
2
-A
1
-,
V is as defined in the description.