Patent classifications
C07D295/04
DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
This invention is directed to compounds of formula (I):
##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Amyloid targeting agents and methods of using the same
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the methods for treating of diseases associated with an amyloid or amyloid like proteins.
Amyloid targeting agents and methods of using the same
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the methods for treating of diseases associated with an amyloid or amyloid like proteins.
Diarylalkylamine REV-ERB antagonists and their use as medicaments
The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: ##STR00001## It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and proapoptotic agents for cancer therapy.
Diamine derivatives as inhibitors of leukotriene A.SUB.4 .hydrolase
This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Diamine derivatives as inhibitors of leukotriene A.SUB.4 .hydrolase
This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
SYNTHESIS AND USE OF AMINO LIPIDS
The present invention provides novel amino lipids and a method for synthesizing these compounds. According to the invention, the amino lipids have a structure of the following formula:
##STR00001##
wherein Z is hydrogen or X.sup.1R.sup.1,
R.sup.1 and R.sup.2 are the same or different and independently C.sub.6-C.sub.24 alkyl, C.sub.6-C.sub.24 alkenyl, C.sub.6-C.sub.24 alkynyl, or C.sub.6-C.sub.24 acyl,
X.sup.1 and X.sup.2 are the same or different, S, SO or S(O).sub.2,
Y is
##STR00002##
or heterocycles of the formula
##STR00003##
wherein k and l are integers from 0 to 2,
R.sup.3 and R.sup.4 are either the same or different and independently C.sub.1-C.sub.12 alkyl, C.sub.1-C.sub.12 alkenyl, or C.sub.1-C.sub.12 alkynyl, wherein alkyl, alkenyl or alkynyl may be optionally substituted with a C.sub.1-C.sub.6 hydrocarbyl group, or R.sup.3 and R.sup.4 optionally join to form, together with the nitrogen atom to which they are bound, an optionally substituted N-heterocyclic ring of 3 to 10 atoms comprising 1 to 7 nitrogen atoms, or R.sup.3 and R.sup.4 are the same or different alkyl amines;
R.sup.5 and R.sup.6 are absent or are hydrogen or C.sub.1-C.sub.12 alkyl,
R.sup.7 is hydrogen or C.sub.1-C.sub.12 alkyl,
m is an integer from 1 to 12, n is an integer from 1 to 12, and p is an integer from 1 to 3, wherein YN for p=2 or 3.
DIARYLALKYLAMINE REV-ERB ANTAGONISTS AND THEIR USE AS MEDICAMENTS
The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof:
##STR00001##
It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and proapoptotic agents for cancer therapy.
Liquid Crystal composition
Provided is a composition that can form a polarizing film with high dichroic ratio, which contains a compound having a function as a dichroic dye and having a local maximum absorption in a wavelength range of 350 to 550 nm. The composition contains a compound represented by the formula (1) and a polymerizable liquid crystal compound: ##STR00001## wherein Y represents a group represented by the formula (Y1) or the formula (Y2) ##STR00002##
Liquid Crystal composition
Provided is a composition that can form a polarizing film with high dichroic ratio, which contains a compound having a function as a dichroic dye and having a local maximum absorption in a wavelength range of 350 to 550 nm. The composition contains a compound represented by the formula (1) and a polymerizable liquid crystal compound: ##STR00001## wherein Y represents a group represented by the formula (Y1) or the formula (Y2) ##STR00002##