Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, diastereoisomer, enantiomer, polymorph, racemic mixture, solvate or isomers and mixtures thereof. The invention further relates to a process for the stereoselective preparation of such compounds. The compound of formula (I) can be used as a medicament, in particular for inhibiting coronin 1 expression in the induction of immunosuppression or in the treatment and/or prevention of a disease or disorder selected from the group consisting of transplant rejection, autoimmune diseases, inflammatory diseases, infectious diseases, and lymphoproliferative disorders. The present invention further relates to a vector comprising a coronin 1 promoter element, wherein in a vertebrate genome, said coronin 1 promoter element starts directly upstream from a transcription starting site (TSS) of a coronin 1 gene and spans a sequence stretch of at least about 700 bp in said genome.

Abstract: Compounds of formula (I) as human cytidine triphosphate synthase 1 (CTPS1) inhibitors for the treatment of proliferative 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 characterisation 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-(methylsulfonamido) 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)).

Abstract: The present invention relates to a compound of formula (I) wherein R1 represents a (C3-C8)cycloalkyl group, a bridged (C6-C10)cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R?-L- group, wherein L is either a single bond or a (C1-C3)alkanediyl group, and R? represents, a (C3-C8)heterocycloalkyl group, or a (C3-C8)heteroaryl u group, or a R?-L- group wherein L is a (C1-C3)alkanediyl group, and R? is an optionally substituted phenyl group; R2 is selected from the group consisting of a hydrogen atom and a (C1-C3)alkyl group; R5 represents a hydrogen atom, a (C1-C4)alkyl group or a (C3-C6)cycloalkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates.

Abstract: The present invention relates to a compound of formula (I) wherein R1 represents a (C1-C6)alkyl group, a spiro(C5-C11)bicyclic ring, a fused phenyl group, a substituted phenyl group, a R?-L- group, wherein L is either a single bond or a (C1-C3)alkanediyl group, and R? represents a (C3-C8)cycloalkyl group, abridged (C6-C10)cycloalkyl group, a (C3-C8)heterocycloalkyl group, or a (C3-C8)heteroaryl group, or a R?-L- group wherein L is a (C1-C3)alkanediyl group, and R? is an optionally substituted phenyl group, and wherein R2 represents a hydrogen atom or a (C1-C3)alkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates.

Abstract: Compounds of formula (I): and related aspects.

Abstract: Compounds of formula (I): (I) and related aspects.

Abstract: Compounds of formula (I): and related aspects.

Abstract: Compounds of formula (I) and related aspects.

Abstract: The present invention relates to a compound of formula (I) wherein R1 represents a (C1-C6)alkyl group, a spiro(C5-C11)bicyclic ring, a fused phenyl group, a substituted phenyl group, a R?-L- group, wherein L is either a single bond or a (C1-C3)alkanediyl group, and R? represents a (C3-C8)cycloalkyl group, abridged (C6-C10)cycloalkyl group, a (C3-C8)heterocycloalkyl group, or a (C3-C8)heteroaryl group, or a R?-L- group wherein L is a (C1-C3)alkanediyl group, and R? is an optionally substituted phenyl group, and wherein R2 represents a hydrogen atom or a (C1-C3)alkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates.

Abstract: Compounds of formula (I): (I) and related aspects.

Abstract: Compounds of formula (I) wherein ring B is selected from the group consisting of Formula (B-a) and Formula (B-bc) as human cytidine triphosphate synthase 1 (CTPS 1) inhibitors for the treatment of proliferative 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 characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 129 to page 302; examples; biological examples 1 and 2; tables 1-17). Specific examples are e.g.: N-(4-(5-Chloropyridin-3-yl)phenyl)-2-(2-(cyclopropane-sulfonamido) pyrimidin-4-yl)butanamide (Formula P1) or 1-(2-(Cyclopropanesulfonamido)pyrimidin-4-yl)-N-(4-(6-ethoxypyrazin-2-yl)phenyl)cyclopentanecarboxamide (Formula P2).

Abstract: The invention provides a compound of formula (I) and processes for the manufacture of such compounds, related intermediates, compositions comprising such compounds and the use of such compounds as cytidine triphosphate synthase 1 inhibitors, particularly in the treatment or prophylaxis of disorders associated with cell proliferation.

Abstract: The invention provides a compound of formula (I): formula (I) and the use of such compounds as cytidine triphosphate synthase 1 inhibitors, particularly in the treatment or prophylaxis of disorders associated with cell proliferation.

Abstract: Compounds of formula (I) and related aspects.

Abstract: 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)).

Abstract: Compounds of formula (I), and related aspects.

Abstract: Compounds of formula (I) and related aspects.

Abstract: Compounds of formula (I): and related aspects.

Abstract: Compounds of formula (I): (I) and related aspects.

Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.