Patent classifications
C07D231/20
SYNTHESIS OF NOVEL EP4 ANTAGONIST AND USE IN CANCER AND INFLAMMATION
The present disclosure provides a novel compound effective in antagonizing EP4, which is a compound represented by Formula I, or a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the compound represented by Formula I:
##STR00001## wherein: R.sup.1 is selected from —CH.sub.3, —CHF.sub.2, and —CF.sub.3; R.sup.2 is selected from C.sub.2-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl, C.sub.2-C.sub.6 halogen-substituted alkyl, C.sub.3-C.sub.6 halogen-substituted cycloalkyl; R.sup.3 is selected from hydrogen, halogen, C.sub.1-C.sub.2 alkyl, C.sub.1-C.sub.2 fluorine- or chlorine-substituted alkyl; R.sup.4 is selected from hydrogen, halogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, C.sub.1-C.sub.6 halogen-substituted alkyl, C.sub.1-C.sub.6 halogen-substituted alkoxyl.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where X, R.sup.a, R.sup.b, R.sup.2, and R.sup.7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where X, R.sup.a, R.sup.b, R.sup.2, and R.sup.7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
Compounds which are inhibitors of Notum
A compound for use in the treatment of a disease ameliorated by the inhibition of Notum of formula (I): (I) ##STR00001##
Compounds which are inhibitors of Notum
A compound for use in the treatment of a disease ameliorated by the inhibition of Notum of formula (I): (I) ##STR00001##
Pyrazole compounds or salts thereof, preparation method therefor, herbicidal composition and use thereof
Disclosed are a pyrazole compound or a salt thereof, a preparation method therefor, a herbicidal composition and use thereof. The pyrazole compound or a salt thereof has a structure as shown in formula (I): ##STR00001##
wherein, R represents ##STR00002##
wherein, R′, R″, and R′″ represent hydrogen, C1-C4 alkyl, C1-C4 halogenated alkyl, C1-C4 alkoxy or halogen, R′, R″, and R′″ may be the same or different; R.sub.1 represents C1-C3 alkyl; R.sub.2 represents hydrogen or C1-C4 alkyl; R.sub.3 represents hydrogen or C1-C6 alkyl, optionally substituted phenyl, optionally substituted pyridyl, optionally substituted alkenyl, optionally substituted alkynyl, C1-C6 alkyl carbonyl, C1-C6 alkoxyl carbonyl, C1-C6 alkyl carbonyl methyl, etc. A compound having a pyrazole structure not only has excellent herbicidal effect on barnyard grass, but also is safe to rice in post-emergence application. More surprisingly, it also has good control efficacy on barnyard grass resistant to major herbicides, such as penoxsulam, quinclorac, cyhalofop-butyl, propanil, etc.
Pyrazole compounds or salts thereof, preparation method therefor, herbicidal composition and use thereof
Disclosed are a pyrazole compound or a salt thereof, a preparation method therefor, a herbicidal composition and use thereof. The pyrazole compound or a salt thereof has a structure as shown in formula (I): ##STR00001##
wherein, R represents ##STR00002##
wherein, R′, R″, and R′″ represent hydrogen, C1-C4 alkyl, C1-C4 halogenated alkyl, C1-C4 alkoxy or halogen, R′, R″, and R′″ may be the same or different; R.sub.1 represents C1-C3 alkyl; R.sub.2 represents hydrogen or C1-C4 alkyl; R.sub.3 represents hydrogen or C1-C6 alkyl, optionally substituted phenyl, optionally substituted pyridyl, optionally substituted alkenyl, optionally substituted alkynyl, C1-C6 alkyl carbonyl, C1-C6 alkoxyl carbonyl, C1-C6 alkyl carbonyl methyl, etc. A compound having a pyrazole structure not only has excellent herbicidal effect on barnyard grass, but also is safe to rice in post-emergence application. More surprisingly, it also has good control efficacy on barnyard grass resistant to major herbicides, such as penoxsulam, quinclorac, cyhalofop-butyl, propanil, etc.
ALKENE-CONTAINING CARBOXYLATE COMPOUND AND USE THEREOF
An alkene-containing carboxylic ester compound of formula (I) and its agriculturally acceptable salt can be used as a herbicide.
##STR00001##
ALKENE-CONTAINING CARBOXYLATE COMPOUND AND USE THEREOF
An alkene-containing carboxylic ester compound of formula (I) and its agriculturally acceptable salt can be used as a herbicide.
##STR00001##
COMPOUNDS AND METHODS FOR TREATING OXALATE-RELATED DISEASES
Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject are also provided.