- IDENTIFICATION AND USE OF ERK5 INHIBITORS
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The present invention covers heterocyclic compounds of general formula (I) in which T, U, Y, Z, R1 and R3 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer disorders, as a sole agent or in combination with other active ingredients.
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Page/Page column 51; 71
(2019/10/01)
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- BICYCLIC PYRIMIDINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
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- CHEMICAL COMPOUNDS
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The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 45
(2008/06/13)
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- PHARMACEUTICAL COMPOUNDS
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The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J2-J1 is N=CR7 or R1aN-CO; G is OH or NR5R6; E is CONR7, NR7CO, C(R8)=C(R8) or (X)m(CR8R8a)n where X is O, S or NR7; provided that when J2-J1 is R1aN-CO, E is other than NR7CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R4 and R4a are absent, or A is a saturated optionally substituted C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R1,Rla, R2, and R3 are each H; halogen; C1-6 hydrocarbyl optionally substituted by halogen, OH or C1-2 alkoxy; CN; CONHR8; NH2; NHCOR10 or NHCONHR10; R4 is H or C1-4 alkyl; R4a is H, C1-4 alkyl or a group R9; R5 and R6 are each selected from H, R9 and C1-4 hydrocarbyl optionally substituted by halogen, C1-2 alkoxy or R9;or NR5R6 forms a saturated 4-7 membered monocyclic heterocyclic group; R7 is H or C1-4 alkyl; R8 and R8a each H or saturated C1-4 hydrocarbyl optionally substituted by fluorine; R9is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R4, R4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR5R6, R4 and A form a saturated 4-7 membered monocyclic heterocycle; or R4,together with R7 or R8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR5R6 and R7 or R8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R10 is optionally substituted phenyl or benzyl.
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Page/Page column 98-99
(2010/11/30)
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- NOVEL BICYCLIC AROMATIC COMPOUNDS, THE PRODUCTION AND USE THEREOF IN THE FORM OF DRUGS
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The invention relates to novel aromatic bicycle compounds of formula (I), wherein Ar, X, Y and R1-R3 are such as specified in a claim 1. Said invention also relates to the tautomers, enantiomers, diasteriomers, mixtures, pro-drugs an
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- Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: Design, synthesis and structure-activity relationship studies
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The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4.
- Vergne, Fabrice,Bernardelli, Patrick,Lorthiois, Edwige,Pham, Nga,Proust, Emmanuelle,Oliveira, Chrystelle,Mafroud, Abdel-Kader,Royer, Frederique,Wrigglesworth, Roger,Schellhaas, Jennifer,Barvian, Mark,Moreau, Fran?ois,Idrissi, Moulay,Tertre, Anita,Bertin, Bernadette,Coupe, Magali,Berna, Patrick,Soulard, Patricia
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p. 4607 - 4613
(2007/10/03)
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