Patent classifications
C07D233/60
1,3-Disubstituted cyclopentane derivatives
Compounds of the formula I ##STR00001##
in which R, Y, R.sup.1, X.sup.1, X.sup.2, X.sup.3 and q have the meanings indicated in claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
METHODS FOR THE SAFE ADMINISTRATION OF IMIDAZOLE OR IMIDAZOLIUM COMPOUNDS
Methods for the safe administration of imidazole or imidazolium compounds such as zoledronic acid, and conditions that may be treated by these methods, are described herein.
METHODS FOR THE SAFE ADMINISTRATION OF IMIDAZOLE OR IMIDAZOLIUM COMPOUNDS
Methods for the safe administration of imidazole or imidazolium compounds such as zoledronic acid, and conditions that may be treated by these methods, are described herein.
SHIP1 MODULATORS AND METHODS RELATED THERETO
Compounds of formula (I):
##STR00001##
where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
SHIP1 MODULATORS AND METHODS RELATED THERETO
Compounds of formula (I):
##STR00001##
where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
SAFE AND EFFICIENT PROCESS FOR THE PREPARATION OF CARMUSTINE
Carmustine may be safely and efficiently produced by reacting 2-chloroethylamine hydrochloride and 1,1′-carbonyldiimidazole to afford 1,3-bis(2-chloroethyl)-1-urea, followed by nitrosation to give the final product.
GRAFTED POLYMER CARRYING PENDENT IMIDAZOLE FUNCTIONAL GROUPS
A modified polymer is obtained by grafting of at least one compound of formula (I) onto at least one unsaturation of the initial polymer chain
##STR00001##
in which Q represents a dipole comprising at least one nitrogen atom; A represents a divalent heteroaromatic ring optionally substituted with one or more identical or different linear or branched aliphatic hydrocarbon-based chains, optionally substituted or interrupted with one or more heteroatoms; E represents a divalent hydrocarbon-based group which may optionally contain one or more heteroatoms; R.sub.1 represents a hydrogen atom or a C.sub.1-C.sub.20 alkyl group; and Y and Z, which may be identical or different, each represent a hydrogen atom or a hydrocarbon-based chain, Y and Z together also possibly forming a ring, notably an aromatic ring, with the carbon atoms of the imidazole ring to which they are attached.
CYCLIC FORMYL AND CYCLIC KETONE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL USE
The present invention provides a cycloyl formyl and cycloyl ketone compounds, a preparation method therefor, and a pharmaceutical use. The present invention finds that the compounds shown in formula (I) better inhibits Zika virus and dengue virus infection and replication, may be used as a drug for treating and preventing diseases caused by Zika virus and dengue virus, and may also become a drug for treating and preventing diseases caused by other flaviviruses, such as yellow fever, West Nile virus infection, Japanese encephalitis, AIDS caused by HIV etc., and diseases caused by hand, foot and mouth virus infection etc. The compounds may treat disease caused by bacterial infections, including inflammatory bowel disease ulcerative colitis and Crohn's disease, diseases caused by Escherichia coli, diseases caused by Staphylococcus aureus etc., and diseases caused by Acinetobacter baumannii.
CYCLIC FORMYL AND CYCLIC KETONE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL USE
The present invention provides a cycloyl formyl and cycloyl ketone compounds, a preparation method therefor, and a pharmaceutical use. The present invention finds that the compounds shown in formula (I) better inhibits Zika virus and dengue virus infection and replication, may be used as a drug for treating and preventing diseases caused by Zika virus and dengue virus, and may also become a drug for treating and preventing diseases caused by other flaviviruses, such as yellow fever, West Nile virus infection, Japanese encephalitis, AIDS caused by HIV etc., and diseases caused by hand, foot and mouth virus infection etc. The compounds may treat disease caused by bacterial infections, including inflammatory bowel disease ulcerative colitis and Crohn's disease, diseases caused by Escherichia coli, diseases caused by Staphylococcus aureus etc., and diseases caused by Acinetobacter baumannii.
BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS
Compounds having a structure of Formula I:
##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.