Abstract: The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formula (I), to their medical use and to their process of preparation.

Abstract: The present application relates to compounds of formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present invention relates to imidazole derivatives, wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present invention relates to imidazole derivatives, wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present application relates to compounds of formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present invention relates to imidazole derivatives of Formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present invention relates to imidazole derivatives of Formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present application relates to thienopyrrole derivatives, compounds of Formulas (I) and (Ia), wherein R, R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. The compounds of the application can be useful for inhibiting KDM1 and the prevention and/or treatment of cancer, infectious disease, or a disease characterized by aberration of cellular energy metabolism, e.g., obesity.

Abstract: The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present application relates to thienopyrrole derivatives, compounds of Formulas (I) and (Ia), wherein R, R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. The compounds of the application can be useful for inhibiting KDM1 and the prevention and/or treatment of cancer, infectious disease, or a disease characterized by aberration of cellular energy metabolism, e.g., obesity.

Abstract: The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen or C1-C6 alkyl, R3, R4 are, independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1-C6 haloalkoxy, and R5 and R6 are as further defined in the specification, and pharmaceutical acceptable salts thereof.

Abstract: The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.