Patent classifications
C07C235/28
KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF
Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.
Ketamine derivatives and compositions thereof
Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.
ANTIMICROBIAL AGENTS
The invention provides novel analogues of enacyloxin Ha and their pharmaceutically acceptable salts, metabolites, isomers (e.g. stereoisomers) and prodrugs. Such compounds are effective in the treatment of infections caused by Gram-negative bacteria such as Acinetobacter baumannii. Compounds in accordance with the invention include those of formula (A), and their pharmaceutically acceptable salts, metabolites, isomers (e.g. stereoisomers) and prodrugs: In formula (A): X is 0 or NR.sup.x (where R* is either H or C.sub.1-3 alkyl, e.g. CH.sub.3); R.sup.1 is a 5- or 6-membered, saturated or unsaturated, carbocyclic ring optionally substituted by one or more substituents, or R.sup.1 is an optionally substituted straight-chained or branched C.sub.1-6 alkyl group (e.g. C.sub.1-3 alkyl group); R.sup.2 is H, F, Cl, Br, I or CH.sub.3; R.sup.3 is H or OH; R.sup.8 is a straight-chained or branched C.sub.1-8 alkyl group (e.g. a C.sub.1-6 alkyl group); Y is one of the following groups: (wherein each * denotes the point of attachment of the group to the remainder of the molecule; R.sup.9 is H, F, Cl, Br or I; R.sup.4 and R.sup.5 are independently selected from H and OH, or R.sup.4 and R.sup.5 together are =0, preferably R.sup.4 is H and R.sup.5 is OH; R.sup.6 is H, F, Cl, Br, I or CH.sub.3; R.sup.7 is H and R.sup.7 is OH, or R.sup.7 and R.sup.7 together are =0, preferably R7 is H and R7 is OH); and each independently represents an optional bond (i.e. each of C.sub.2-C.sub.3, C.sub.4-C.sub.5, C.sub.6-C.sub.7, C.sub.8-C.sub.9 and C.sub.10-C.sub.11 are independently either CC (single) or CC (double) bonds).
20-HETE RECEPTOR (GPR75) ANTAGONISTS AND METHODS OF USE
The present invention concerns compounds and their use to treat cardiovascular disease, renal disease, thrombic disease, stroke, metabolic syndrome, cell proliferation, and ischemic cardiovascular disorders. Compounds of the present invention display significant potency as antagonists of 20-hydroxyeicosatetraenoic acid (20-HETE), and function as anti-hypertensive, anti-inflammatory, or anti-growth agents.
Maleamic acid monomer and preparation method and use thereof
A maleamic acid monomer, and a preparation method and a use of the maleamic acid monomer. The structural formula of the monomer is as follows: ##STR00001##
formula (1), wherein, R is selected from ##STR00002##
The maleamic acid monomer provided in the present invention may be used as a comonomer to prepare temperature-tolerant and calcium salt-tolerant polymers.
Maleamic acid monomer and preparation method and use thereof
A maleamic acid monomer, and a preparation method and a use of the maleamic acid monomer. The structural formula of the monomer is as follows: ##STR00001##
formula (1), wherein, R is selected from ##STR00002##
The maleamic acid monomer provided in the present invention may be used as a comonomer to prepare temperature-tolerant and calcium salt-tolerant polymers.
20-HETE RECEPTOR (GPR75) ANTAGONISTS AND METHODS OF USE
The present invention concerns compounds and their use to treat cardiovascular disease, renal disease, thrombic disease, stroke, metabolic syndrome, cell proliferation, and ischemic cardiovascular disorders. Compounds of the present invention display significant potency as antagonists of 20-hydroxyeicosatetraenoic acid (20-HETE), and function as anti-hypertensive, anti-inflammatory, or anti-growth agents.
KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF
Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.
NOVEL EICOSANOID DERIVATIVES
The present invention provides compounds (n-3 PUFA derivatives) of formula (I):
##STR00001##
that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.
NOVEL EICOSANOID DERIVATIVES
The present invention provides compounds (n-3 PUFA derivatives) of formula (I):
##STR00001##
that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.