Patent classifications
C07D237/32
COMPOUNDS
The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasone production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R.sup.1, R.sup.2 and R.sup.3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.
##STR00001##
OLAPARIB HYDROXYBENZOIC ACID COCRYSTALS AND THEIR PHARMACEUTICAL USE
The invention relates to new 1:1 olaparib:hydroxybenzoic acid cocrystals. The invention also relates to new 2:1 olaparib:hydroxybenzoic acid cocrystals which may contain no water (anhydrous) or may optionally be hydrated. The invention also relates to pharmaceutical compositions containing an olaparib hydroxybenzoic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib hydroxybenzoic acid cocrystals of the invention may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP).
OLAPARIB HYDROXYBENZOIC ACID COCRYSTALS AND THEIR PHARMACEUTICAL USE
The invention relates to new 1:1 olaparib:hydroxybenzoic acid cocrystals. The invention also relates to new 2:1 olaparib:hydroxybenzoic acid cocrystals which may contain no water (anhydrous) or may optionally be hydrated. The invention also relates to pharmaceutical compositions containing an olaparib hydroxybenzoic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib hydroxybenzoic acid cocrystals of the invention may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP).
MTA-cooperative PRMT5 inhibitors
The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds of Formula (I) ##STR00001##
to pharmaceutical compositions comprising compounds of Formula (I) and to methods of use thereof, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions comprising those compounds.
MTA-cooperative PRMT5 inhibitors
The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds of Formula (I) ##STR00001##
to pharmaceutical compositions comprising compounds of Formula (I) and to methods of use thereof, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions comprising those compounds.
CARDIAC TROPONIN I ULTRA-SENSITIVE DETECTION REAGENT KIT, AND ULTRA-SENSITIVE DETECTION METHOD THEREFOR
A cardiac troponin I ultra-sensitive detection reagent kit, a preparation method, and a detection method. The reagent kit comprises at least one first anti-cardiac troponin I antibody marked with a trace marker and at least one second anti-cardiac troponin I antibody coated on magnetic microspheres, the first anti-cardiac troponin I antibody and cardiac troponin I binding site being different from the second anti-cardiac troponin I antibody and cardiac troponin I binding site. The reagent kit may further comprise a diluent capable of significantly reducing non-specific binding in a detection process, so as to further increase the detection accuracy and sensitivity. The method using the reagent kit to detect cardiac troponin I sensitively and accurately detects the amount of cardiac troponin I in a sample, and provides more timely and reliable information for the early diagnosis and treatment of AMI.
Small molecule CD4 mimetics and uses thereof
The invention provides for compounds of formula I: wherein Z is absent or (CR.sub.AR.sub.B).sub.nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHR.sub.c, NR.sub.cR.sub.c, SH, S(O).sub.mR.sub.c; or (iii) R.sub.A and R.sub.B together form C(O); W is absent, C(O), C(O)O, C(O)NR.sub.cR.sub.c, O, S(O).sub.m, or NR.sub.cR.sub.c; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NR.sub.XR.sub.Y; wherein R.sub.x and R.sub.y are each independently H, alkyl or aryl; X.sup.1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each R.sub.c is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof. ##STR00001##
Small molecule CD4 mimetics and uses thereof
The invention provides for compounds of formula I: wherein Z is absent or (CR.sub.AR.sub.B).sub.nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHR.sub.c, NR.sub.cR.sub.c, SH, S(O).sub.mR.sub.c; or (iii) R.sub.A and R.sub.B together form C(O); W is absent, C(O), C(O)O, C(O)NR.sub.cR.sub.c, O, S(O).sub.m, or NR.sub.cR.sub.c; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NR.sub.XR.sub.Y; wherein R.sub.x and R.sub.y are each independently H, alkyl or aryl; X.sup.1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each R.sub.c is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof. ##STR00001##
THERAPEUTIC COMPOUNDS AND USES THEREOF
The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof:
##STR00001##
wherein ring A, R.sup.1, R.sup.3, R.sup.4, R.sup.5, and each R.sup.e have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
THERAPEUTIC COMPOUNDS AND USES THEREOF
The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof:
##STR00001##
wherein ring A, R.sup.1, R.sup.3, R.sup.4, R.sup.5, and each R.sup.e have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.