C07C65/40

Compound having higher inhibitory activity on protein kinase G and preparation method thereof

Disclosed are a compound of Formula I, ##STR00001##
having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, R.sub.1 and R.sub.2 are the same or different, each being independently chosen from the halogens, the C.sub.1-C.sub.6 alkoxyl group, the C.sub.1-C.sub.6 alkyl group, the C.sub.2-C.sub.6 alkenyl group, and the C.sub.2-C.sub.6 alkynyl group; R.sub.3 is chosen from H, the halogens, the substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, C.sub.3-C.sub.6 cycloalkyl group, C.sub.2-C.sub.6 alkenyl group, and C.sub.2-C.sub.6 alkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.

Compound having higher inhibitory activity on protein kinase G and preparation method thereof

Disclosed are a compound of Formula I, ##STR00001##
having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, R.sub.1 and R.sub.2 are the same or different, each being independently chosen from the halogens, the C.sub.1-C.sub.6 alkoxyl group, the C.sub.1-C.sub.6 alkyl group, the C.sub.2-C.sub.6 alkenyl group, and the C.sub.2-C.sub.6 alkynyl group; R.sub.3 is chosen from H, the halogens, the substituted or unsubstituted C.sub.1-C.sub.6 alkyl group, C.sub.3-C.sub.6 cycloalkyl group, C.sub.2-C.sub.6 alkenyl group, and C.sub.2-C.sub.6 alkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.

LANTHIONINE SYNTHETASE C-LIKE 2-BASED THERAPEUTICS

Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

INHIBITORS OF THE ONCOGENIC SHP2 PHOSPHATASE AND USES THEREOF

Described herein are compounds which are inhibitors of oncogenic and wild-type SHP2 and methods of treatment using SHP2 inhibitors.

INHIBITORS OF THE ONCOGENIC SHP2 PHOSPHATASE AND USES THEREOF

Described herein are compounds which are inhibitors of oncogenic and wild-type SHP2 and methods of treatment using SHP2 inhibitors.

Lanthionine synthetase C-like 2-based therapeutics

Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

Method for production of 3-hydroxypropan-1-one compound, method for production of 2-propen-1-one compound and method for production of isoxazoline compound

There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C.sub.1-C.sub.6 alcohol and an aprotic polar solvent in the presence of a base and water.

Method for production of 3-hydroxypropan-1-one compound, method for production of 2-propen-1-one compound and method for production of isoxazoline compound

There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C.sub.1-C.sub.6 alcohol and an aprotic polar solvent in the presence of a base and water.

METHOD FOR PRODUCTION OF 3-HYDROXYPROPAN-1-ONE COMPOUND, METHOD FOR PRODUCTION OF 2-PROPEN-1-ONE COMPOUND AND METHOD FOR PRODUCTION OF ISOXAZOLINE COMPOUND

There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C.sub.1-C.sub.6 alcohol and an aprotic polar solvent in the presence of a base and water.

METHOD FOR PRODUCTION OF 3-HYDROXYPROPAN-1-ONE COMPOUND, METHOD FOR PRODUCTION OF 2-PROPEN-1-ONE COMPOUND AND METHOD FOR PRODUCTION OF ISOXAZOLINE COMPOUND

There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C.sub.1-C.sub.6 alcohol and an aprotic polar solvent in the presence of a base and water.