153813-69-5Relevant academic research and scientific papers
N-HYDROXYCARBOXAMIDE DERIVATIVES USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY
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, (2022/03/09)
A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful for the treatment of a disorder selected from autoimmune disorders, mental disorders, neurodegenerative disorders, pain, respiratory diseases, and hyperproliferative disorders, in particular cancers.
COMBINATION OF HEPATITIS B VIRUS (HBV) VACCINES AND PYRIDOPYRIMIDINE DERIVATIVES
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, (2021/01/22)
Therapeutic combinations of hepatitis B virus (HBV) vaccines and a pyridopyrimidine derivative are described. Methods of inducing an immune response against HBV or treating an HBV-induced disease, particularly in individuals having chronic HBV infection, using the disclosed therapeutic combinations are also described. The invention provides therapeutic combinations or compositions and methods for inducing an immune response against hepatitis B viruses (HBV) infection.
BENZAZEPINE DICARBOXAMIDE COMPOUNDS WITH SECONDARY AMIDE FUNCTION
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, (2017/12/29)
This invention relates to new benzazepine dicarboxamide compounds of the formula (I) wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
DIHYDROPYRIMIDINYL BENZAZEPINE CARBOXAMIDE COMPOUNDS
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, (2018/02/03)
This invention relates to new benzazepine carboxamide compounds of the formula (i) wherein X and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR8 agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
BENZAZEPINE DICARBOXAMIDE COMPOUNDS WITH TERTIARY AMIDE FUNCTION
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, (2017/12/29)
This invention relates to new benzazepine dicarboxamide compounds of the formula (I) wherein R1 to R 3 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
NEW SPIRO[3H-INDOLE-3,2′-PYRROLIDIN]-2(1H)-ONE COMPOUNDS AND DERIVATIVES AS MDM2-P53 INHIBITORS
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Page/Page column 93, (2016/03/13)
The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, A, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.
Benzazepine Dicarboxamide Compounds
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Paragraph 0253; 0255, (2016/09/26)
This invention relates to novel benzazepine dicarboxamide compounds of the formula wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
ISOXAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS
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Page/Page column 87; 89-90, (2013/03/26)
The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group P, L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is -C(R4)R4-; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1, Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is chloro, bromo, fluoro; X2 is C-X6 or nitrogen; Χ1, Χ3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also relates to methods of using the compounds to control insects, acarines, nematodes or molluscs, as well as intermediates usefor the the sysnthesis of the compounds.
ISOXAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS
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Page/Page column 153-154; 156, (2013/03/26)
The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is -C(R4)R4-R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C-R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a -CH=CH-CH=CH- bridge; X2 is C-X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
HYDROXAMIC ACID DERVICATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY
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, (2008/06/13)
Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: formula (I) wherein Y1 is a bond, -(C=O)-, -S(O2)-, -C(=O)O-, -OC(=O)-, -(C=O)NR3, -NR3(C=O)-, -S(O2)NR3-, -NR3S(O2)-, or -NR3(C=O)NR5-, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, AIk1, AIk2 and Q are as defined in the claims; z is O or 1 ; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y); wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, -(C=O)R3, -(C=O)OR3, or -(C=O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroary(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.

