Patent classifications
C07D253/06
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land 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, SO.sub.2NR.sub.12R.sub.13, heteroaryl, 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; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
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Protein tyrosine phosphatase inhibitors
Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. ##STR00001##
GLP-1 receptor modulators
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): ##STR00001##
where A, B, C, Y.sub.1, Y.sub.2, Z, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W.sub.1, n, p and q are as defined herein.
GLP-1 receptor modulators
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): ##STR00001##
where A, B, C, Y.sub.1, Y.sub.2, Z, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W.sub.1, n, p and q are as defined herein.
Compositions and methods for reducing cell viability
This invention is directed to compositions, methods and kits that can be used for reducing cell viability, inducing cell apoptosis, and inhibiting cell proliferation, such as for the treatment of cancer. The invention is also directed to compositions, methods and kits that can be used for treating inflammatory conditions, such as by modulating inflammatory cytokines.
Compositions and methods for reducing cell viability
This invention is directed to compositions, methods and kits that can be used for reducing cell viability, inducing cell apoptosis, and inhibiting cell proliferation, such as for the treatment of cancer. The invention is also directed to compositions, methods and kits that can be used for treating inflammatory conditions, such as by modulating inflammatory cytokines.
Sulfonyl-structure-containing triazinone derivatives, their preparation methods and their uses in insect killing and/or bacterium killing
The present invention belongs to the technical field of pesticides, particularly relates to sulfonyl-structure-containing triazinone derivatives, their preparation methods, and their uses in insect killing and/or bacterium killing. The sulfonyl-structure-containing triazinone derivatives are compounds represented by formula (I.sub.a) or (I.sub.b). The sulfonyl-structure-containing triazinone derivatives provided in the present invention exhibit outstanding insecticidal activity as well as bactericidal activity.
Sulfonyl-structure-containing triazinone derivatives, their preparation methods and their uses in insect killing and/or bacterium killing
The present invention belongs to the technical field of pesticides, particularly relates to sulfonyl-structure-containing triazinone derivatives, their preparation methods, and their uses in insect killing and/or bacterium killing. The sulfonyl-structure-containing triazinone derivatives are compounds represented by formula (I.sub.a) or (I.sub.b). The sulfonyl-structure-containing triazinone derivatives provided in the present invention exhibit outstanding insecticidal activity as well as bactericidal activity.
Method for producing triazine compound
The present invention provides an industrially advantageous method for producing a 3,5-disubstituted triazine compound that is useful as an active pharmaceutical ingredient. More specifically, the present invention provides a production method, whereby it becomes possible to efficiently produce a 3-oxo-5-substituted triazine in water without the need to isolate an intermediate that may have mutagenicity, and it also becomes possible to perform the production without the need to isolate a product in each of multiple steps. Namely, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of reacting a compound represented by the following formula IV or a salt thereof with a base in water, and optionally including a step of forming a salt thereof. Specifically, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of derivatizing a compound represented by formula II or a salt thereof into a corresponding compound represented by formula III, a salt thereof, or a derivative thereof, then a step of reacting the resulting compound, a salt thereof, or a derivative thereof with aminourea or a salt thereof in water to produce a compound represented by formula IV or a salt thereof, and then a step of reacting the resulting compound or a salt thereof in the presence of a base. ##STR00001##
(wherein ring A represents an optionally substituted aryl group or an optionally substituted heteroaryl group)
1,2,4-TRIAZIN-3(2H)-ONE COMPOUNDS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
The present invention includes name compounds of general formula (I): (I) in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, methods for their preparation, pharmaceutical compositions and combinations comprising said compounds, and their use for the treatment of hyperproliferative diseases.
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