Patent classifications
C07D417/10
Fungicidal oxadiazoles
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R.sup.1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. ##STR00001##
Flavone derivatives for the treatment and prophylaxis of hepatitis B virus disease
The present invention provides novel compounds having the general formula (Formula I): wherein R.sup.1 to R.sup.6, G.sub.1, G.sub.2, A.sub.1 to A.sub.4 and m are as described herein, compositions including the compounds and methods of using the compounds. ##STR00001##
Flavone derivatives for the treatment and prophylaxis of hepatitis B virus disease
The present invention provides novel compounds having the general formula (Formula I): wherein R.sup.1 to R.sup.6, G.sub.1, G.sub.2, A.sub.1 to A.sub.4 and m are as described herein, compositions including the compounds and methods of using the compounds. ##STR00001##
ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR.sub.12R.sub.13; or one of P and Q is NR.sub.14 and the other is CR.sub.12R.sub.13; the group X—Y is —NHSO.sub.2— or —SO2NH—; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, heteroaryl, SO.sub.2NR.sub.16R.sub.17, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H or halo; and R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.16 and R.sub.17 are each independently H or alkyl; R.sub.15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.
##STR00001##
ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR.sub.12R.sub.13; or one of P and Q is NR.sub.14 and the other is CR.sub.12R.sub.13; the group X—Y is —NHSO.sub.2— or —SO2NH—; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, heteroaryl, SO.sub.2NR.sub.16R.sub.17, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H or halo; and R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.16 and R.sub.17 are each independently H or alkyl; R.sub.15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.
##STR00001##
CD38 INHIBITORS
The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD.sup.+ or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).
##STR00001##
CD38 INHIBITORS
The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD.sup.+ or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).
##STR00001##
PHENOTHIAZINE FERROPTOSIS INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A phenothiazine ferroptosis inhibitor, a preparation method therefor and an application thereof. Specifically provided is a compound represented by formula I, or a salt thereof, or a stereoisomer thereof. The synthesized phenothiazine compound has a good inhibitory effect on ferroptosis and has good drug safety. Moreover, the compound can be used to prepare a ferroptosis inhibitor, and can also be used to prepare a drug for treating diseases related to ferroptosis, such as neurodegenerative diseases, tumors, tissue ischemia reperfusion injury, stroke, cardiovascular diseases, renal failure, and diabetic complications.
PHENOTHIAZINE FERROPTOSIS INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A phenothiazine ferroptosis inhibitor, a preparation method therefor and an application thereof. Specifically provided is a compound represented by formula I, or a salt thereof, or a stereoisomer thereof. The synthesized phenothiazine compound has a good inhibitory effect on ferroptosis and has good drug safety. Moreover, the compound can be used to prepare a ferroptosis inhibitor, and can also be used to prepare a drug for treating diseases related to ferroptosis, such as neurodegenerative diseases, tumors, tissue ischemia reperfusion injury, stroke, cardiovascular diseases, renal failure, and diabetic complications.
PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
The present disclosure provides selective phosphoinositide 3-kinase gamma inhibitors of Formula (I) including (I-a), (I-b), (I-c), and (I-d), or pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of conditions mediated by one or more PI3K isoforms, such as PI3K gamma (PI3Kγ). The present disclosure further provides methods of inhibiting phosphoinositide 3-kinase gamma using these compounds for treatment of disorders related to phosphatidylinositol 3-kinase gamma activity.