Patent classifications
C07D243/24
BICYCLIC 1,4-DIAZEPANONES AND THERAPEUTIC USES THEREOF
Provided herein are compounds of formula (I):
##STR00001##
or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X.sup.1, X.sup.2, R.sup.y, R.sup.z, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein.
Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing.
Also provided herein are methods of using a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to treat various diseases, disorders, and conditions responsive to the modulation of the contractility of the skeletal sarcomere.
COMBINATION PHARMACEUTICAL AGENTS AS RSV INHIBITORS
The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound effective to inhibit the function of the RSV and an additional compound or combinations of compounds having anti-RSV activity.
COMBINATION PHARMACEUTICAL AGENTS AS RSV INHIBITORS
The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound effective to inhibit the function of the RSV and an additional compound or combinations of compounds having anti-RSV activity.
METHODS OF PREPARING CHIRAL BENZODIAZEPINONE DERIVATIVES
The present invention provides methods of preparing compound of Formula (I), wherein the compounds are represented by the structure of Formula (I) wherein: R.sup.1 each is independently F, Cl, Br, I, OCH.sub.3, CN or NO.sub.2; R.sup.2 each is independently identical or different C.sub.1-C.sub.5 alkyl; n.sup.1 is an integer between 1 and 5; and n.sup.2 is an integer between 1 and 4. In addition, the present invention provides a compound represented by the following structures: Compound (1a) and Compound (2), wherein X comprises: chloride, acetate, adipate, alginate, ascorbate, aspartate, benzoate, benzenesulfonate, bisulfate, borate, butyrate, citrate, camphorate, camphorsulfonate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, fumarate, glucoheptanoate, glycerophosphate, hemisulfate, heptanoate, hexanoate, hydroiodide, maleate, 2-hydroxyethanesulfonate, lactate, methanesulfonate, 2-naphthalenesulfonate, nicotinate, nitrate, oxalate, pectinate, persulfate, 3-phenylpropionate, phosphate, picrate, pivalate, propionate, salicylate, succinate, sulfate, sulfonate, tartrate, thiocyanate, toluene sulfonate, or undecanoate salt, or any combination thereof.
METHODS OF PREPARING CHIRAL BENZODIAZEPINONE DERIVATIVES
The present invention provides methods of preparing compound of Formula (I), wherein the compounds are represented by the structure of Formula (I) wherein: R.sup.1 each is independently F, Cl, Br, I, OCH.sub.3, CN or NO.sub.2; R.sup.2 each is independently identical or different C.sub.1-C.sub.5 alkyl; n.sup.1 is an integer between 1 and 5; and n.sup.2 is an integer between 1 and 4. In addition, the present invention provides a compound represented by the following structures: Compound (1a) and Compound (2), wherein X comprises: chloride, acetate, adipate, alginate, ascorbate, aspartate, benzoate, benzenesulfonate, bisulfate, borate, butyrate, citrate, camphorate, camphorsulfonate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, fumarate, glucoheptanoate, glycerophosphate, hemisulfate, heptanoate, hexanoate, hydroiodide, maleate, 2-hydroxyethanesulfonate, lactate, methanesulfonate, 2-naphthalenesulfonate, nicotinate, nitrate, oxalate, pectinate, persulfate, 3-phenylpropionate, phosphate, picrate, pivalate, propionate, salicylate, succinate, sulfate, sulfonate, tartrate, thiocyanate, toluene sulfonate, or undecanoate salt, or any combination thereof.
NEW BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
The invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein.
##STR00001##
Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.
NEW BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
The invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein.
##STR00001##
Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.
THERAPEUTIC COMPOUNDS AND USES THEREOF
The present invention relates to compounds of formula (I):
##STR00001##
and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
THERAPEUTIC COMPOUNDS AND USES THEREOF
The present invention relates to compounds of formula (I):
##STR00001##
and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action
The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.