Patent classifications
C07D239/42
COMPOUNDS AS AUTOTAXIN INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same.
The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.
ARYLAMINE COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE
The present disclosure relates to an arylamine compound and an organic electroluminescent device. The arylamine compound has a structure represented by Formula (1), and contains N atoms rich in electrons and a number of large conjugated systems, so that the electron mobility and the transition rate can be improved. The device prepared from the arylamine compound has high electrical stability, and device efficiency and long device lifetime.
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ARYLAMINE COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE
The present disclosure relates to an arylamine compound and an organic electroluminescent device. The arylamine compound has a structure represented by Formula (1), and contains N atoms rich in electrons and a number of large conjugated systems, so that the electron mobility and the transition rate can be improved. The device prepared from the arylamine compound has high electrical stability, and device efficiency and long device lifetime.
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AROMATIC SULFONAMIDE DERIVATIVES
Substituted aromatic sulfonamides of formula (I)
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pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
AROMATIC SULFONAMIDE DERIVATIVES
Substituted aromatic sulfonamides of formula (I)
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pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
AMINE-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS, SALTS THEREOF, AND METHODS OF SYNTHESIS THEREOF
The present disclosure relates to amine-substituted heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) by administering an amine-substituted heterocyclic heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)-4-(2-(methylsulfonamido)pyrimidin-4-yl) tetrahydro-2H-pyran-4-carboxamide derivatives and related compounds as human CTPS1 inhibitors for the treatment of proliferative diseases
Compounds of formula (I) as human cytidine triphosphate synthase 1 (CTPS1) inhibitors for the treatment of prolifera-tive diseases, such as e.g. cancer, such as e.g. leukemia and lymphoma, e.g. inflammatory skin diseases such as psoriasis, or e.g. multiple sclerosis. The present description discloses the synthesis and characterisa-tion of exemplary compounds as well as pharmacological data thereof (e.g. pages 64 to 80; examples; biological examples 1 and 2; e.g. compounds P140, P231 to P263; tables 1 to 10). Specific examples are e.g.: N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)-4-(2-(methylsulfonami-N do) pyrimidin-4-yl)tetrahydro-2H-pyran-4-carboxamide (Formula (II)), or 1-(2-(cyclopropanesulfonamido)pyrimidin-4-yl)-N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)cyclohexane-1-carboxamide (Formula (III)).
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N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)-4-(2-(methylsulfonamido)pyrimidin-4-yl) tetrahydro-2H-pyran-4-carboxamide derivatives and related compounds as human CTPS1 inhibitors for the treatment of proliferative diseases
Compounds of formula (I) as human cytidine triphosphate synthase 1 (CTPS1) inhibitors for the treatment of prolifera-tive diseases, such as e.g. cancer, such as e.g. leukemia and lymphoma, e.g. inflammatory skin diseases such as psoriasis, or e.g. multiple sclerosis. The present description discloses the synthesis and characterisa-tion of exemplary compounds as well as pharmacological data thereof (e.g. pages 64 to 80; examples; biological examples 1 and 2; e.g. compounds P140, P231 to P263; tables 1 to 10). Specific examples are e.g.: N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)-4-(2-(methylsulfonami-N do) pyrimidin-4-yl)tetrahydro-2H-pyran-4-carboxamide (Formula (II)), or 1-(2-(cyclopropanesulfonamido)pyrimidin-4-yl)-N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)cyclohexane-1-carboxamide (Formula (III)).
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PESTICIDAL COMPOUNDS
The present application relates to the compounds of formula (I), and the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof wherein the variables are defined in the claims. The compounds of formula (I), as well as the N-oxides, stereoisomers tautomers and agriculturally or veterinarily acceptable salts thereof are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The application also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
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INHIBITORS OF NICOTINAMIDE N-METHYLTRANSFERASE, COMPOSITIONS AND USES THEREOF
Disclosed are compounds and pharmaceutically acceptable salts thereof, which are useful as inhibitors nicotinamide N-methyltransferase (NNIMT). Also disclosed are pharmaceutical compositions comprising a compound disclosed herein. Related methods of treating cancer in a subject and methods of inhibiting tumor growth in subject are also disclosed.