Patent classifications
C07D261/02
Hepatitis B antiviral agents
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Hepatitis B antiviral agents
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
ISOXAZOLIDINE DERIVED INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE 1 (RIPK1)
The present disclosure relates generally to methods and compositions for preventing or arresting cell death and/or inflammation.
Necrosis inhibitors
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
ISOXAZOLINE-SUBSTITUTED BENZAMIDES AND ANALOGUES AS INSECTICIDES
The present invention relates to compounds of formula (I) wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are as defined in claim 1; or a tautomer, isomer, enantiomer, salt or N-oxide thereof; to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
##STR00001##
ISOXAZOLINE-SUBSTITUTED BENZAMIDES AND ANALOGUES AS INSECTICIDES
The present invention relates to compounds of formula (I) wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are as defined in claim 1; or a tautomer, isomer, enantiomer, salt or N-oxide thereof; to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
##STR00001##
NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula:
##STR00001##
where R.sup.1-R.sup.5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula:
##STR00001##
where R.sup.1-R.sup.5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
INSECTICIDAL COMPOUNDS
The present invention provides compounds of formula (I):
##STR00001##
wherein
A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are independently of one another CH, CR.sup.5, or nitrogen;
B.sup.1-B.sup.2-B.sup.3-B.sup.4 is CH.sub.2CNCH.sub.2, CH.sub.2NCH.sub.2CH.sub.2, CH.sub.2CCHO or CHCCH.sub.2O;
G.sup.1 is oxygen or sulfur;
L is a single bond or C.sub.1-C.sub.8alkylene;
R.sup.1 is hydrogen, C.sub.1-C.sub.8alkyl, C.sub.1-C.sub.8alkylcarbonyl-, C.sub.1-C.sub.8alkoxy, C.sub.2-C.sub.8alkenyl, C.sub.2-C.sub.8alkynyl, C.sub.1-C.sub.8alkoxy-C.sub.1-C.sub.8alkyl, aryl or aryl substituted by one to three R.sup.6, or R.sup.1 is heterocyclyl or heterocyclyl substituted by one to three R.sup.6 or C.sub.1-C.sub.8alkoxycarbonyl-;
R.sup.2 is hydrogen, C.sub.1-C.sub.8haloalkyl or C.sub.1-C.sub.8alkyl;
R.sup.3 is C.sub.1-C.sub.8haloalkyl;
R.sup.4 is aryl or aryl substituted by one to three R.sup.6, or R.sup.4 is heterocyclyl or heterocyclyl substituted by one to three R.sup.6;
Y.sup.1 is CR.sup.7R.sup.8, CO or CS;
Y.sup.2, Y.sup.3 and Y.sup.4 are independently CR.sup.7R.sup.8, CO, CS, NR.sup.9, O, S, SO or SO.sub.2;
wherein at least two adjacent ring atoms in the ring formed by Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are heteroatoms;
each R.sup.7 and R.sup.8 is independently hydrogen, halogen, C.sub.1-C.sub.8alkyl, or C.sub.1-C.sub.8haloalkyl;
and R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are as defined in the claims.
The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
INSECTICIDAL COMPOUNDS
The present invention provides compounds of formula (I):
##STR00001##
wherein
A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are independently of one another CH, CR.sup.5, or nitrogen;
B.sup.1-B.sup.2-B.sup.3-B.sup.4 is CH.sub.2CNCH.sub.2, CH.sub.2NCH.sub.2CH.sub.2, CH.sub.2CCHO or CHCCH.sub.2O;
G.sup.1 is oxygen or sulfur;
L is a single bond or C.sub.1-C.sub.8alkylene;
R.sup.1 is hydrogen, C.sub.1-C.sub.8alkyl, C.sub.1-C.sub.8alkylcarbonyl-, C.sub.1-C.sub.8alkoxy, C.sub.2-C.sub.8alkenyl, C.sub.2-C.sub.8alkynyl, C.sub.1-C.sub.8alkoxy-C.sub.1-C.sub.8alkyl, aryl or aryl substituted by one to three R.sup.6, or R.sup.1 is heterocyclyl or heterocyclyl substituted by one to three R.sup.6 or C.sub.1-C.sub.8alkoxycarbonyl-;
R.sup.2 is hydrogen, C.sub.1-C.sub.8haloalkyl or C.sub.1-C.sub.8alkyl;
R.sup.3 is C.sub.1-C.sub.8haloalkyl;
R.sup.4 is aryl or aryl substituted by one to three R.sup.6, or R.sup.4 is heterocyclyl or heterocyclyl substituted by one to three R.sup.6;
Y.sup.1 is CR.sup.7R.sup.8, CO or CS;
Y.sup.2, Y.sup.3 and Y.sup.4 are independently CR.sup.7R.sup.8, CO, CS, NR.sup.9, O, S, SO or SO.sub.2;
wherein at least two adjacent ring atoms in the ring formed by Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are heteroatoms;
each R.sup.7 and R.sup.8 is independently hydrogen, halogen, C.sub.1-C.sub.8alkyl, or C.sub.1-C.sub.8haloalkyl;
and R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are as defined in the claims.
The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.