Patent classifications
C07D243/10
COMPOSITIONS AND METHODS FOR TREATING PROLIFERATIVE DISEASES
The present invention features compositions and methods for treating proliferative diseases such as cancer (e.g., sarcoma, pancreas, prostate, head and neck, liver, and breast cancer) that inhibit the growth of NF-κB and/or Hippo associated neoplasias.
PEPTIDOMIMETIC N5-METHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE DERIVATIVES, TRIAZASPIRO[4.14]NONADECANE DERIVATIVES AND SIMILAR COMPOUNDS AS INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and B1 to B66; tables A to E).
##STR00001##
Substituted benzo[5,6][1,4]diazepino[1,2-a]indoles for the treatment of proliferative disorders
The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I), (II) and (III). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. ##STR00001##
Antiviral Pyrazolopiridinone Compounds
The invention provides compounds of Formula (I)
##STR00001##
as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
Antiviral Pyrazolopiridinone Compounds
The invention provides compounds of Formula (I)
##STR00001##
as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
P2X4 receptor antagonist
The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R.sup.1 and R.sup.2 represent hydrogen atom and the like, or R.sup.1 and R.sup.2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R.sup.3 and R.sup.4 represent hydrogen atom and the like, R.sup.5 represents hydrogen atom and the like, R.sup.6 and R.sup.7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(═O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(═O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(═O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist. ##STR00001##
P2X4 receptor antagonist
The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R.sup.1 and R.sup.2 represent hydrogen atom and the like, or R.sup.1 and R.sup.2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R.sup.3 and R.sup.4 represent hydrogen atom and the like, R.sup.5 represents hydrogen atom and the like, R.sup.6 and R.sup.7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(═O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(═O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(═O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist. ##STR00001##
Methods of treating anxiety by administering a substituted quinolone
A heterocyclic compound represented by the general formula (1) or a salt thereof: ##STR00001## wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH.sub.2—; R.sup.1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R.sup.2 and R.sup.3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R.sub.2 and R.sub.3 are bonded to form a cyclo-C3-C8 alkyl group; and R.sup.4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
Methods of treating anxiety by administering a substituted quinolone
A heterocyclic compound represented by the general formula (1) or a salt thereof: ##STR00001## wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH.sub.2—; R.sup.1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R.sup.2 and R.sup.3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R.sub.2 and R.sub.3 are bonded to form a cyclo-C3-C8 alkyl group; and R.sup.4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
SUBSTITUTED PHENYL SULFONYL PHENYL TRIAZOLE THIONES AND USES THEREOF
The present disclosure relates to substituted phenyl sulfonyl phenyl triazole thiones, pharmaceutical compositions containing them, and methods of using them.