Abstract:
New azabiphenylaminobenzoic acid derivatives having the chemcial structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
Abstract:
The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
Abstract:
New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine A 2a receptor of formula (I). The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine A 2a receptor.
Abstract:
New compounds having the chemical structure of formula (I) or pharmaceutically acceptable salts or N-oxides thereof wherein A is selected from the group consisting of -N-, -O- and -S-; B and C independently are selected from the group consisting of -N- and -O-, with the proviso that at least two of A, B and C are nitrogen atoms; G 1 is selected from the group consisting of nitrogen atoms and -CR c - groups, wherein R c represents a hydrogen atom, a halogen atom, a C 1-4 alkyl group or a C 1-4 alkoxy group.
Abstract:
New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine A2a receptor formula (I): (I) The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine A2a receptor.
Abstract:
The present invention relates to 5-bromo-2,6-di-(1 H-pyrazol-1-yl)pyrimidin-4-amine, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compounds for use in the treatment of cancer.
Abstract:
The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
Abstract:
A compound of formula (I) wherein : - one of the groups G 1 represents a nitrogen atom or a group CR c and the other represents a group CR c ; - G 2 represents a nitrogen atom or a group CR d ; - R 1 represents a group selected from hydrogen atoms, halogen atoms, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R 2 represents a group selected from hydrogen atoms, halogen atoms, hydroxyl groups, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R a , R b and R c independently represent groups selected from hydrogen atoms, halogen atoms, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R d represents a group selected from hydrogen atoms, halogen atoms, hydroxyl groups, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - one of the groups G 3 and G 4 is a nitrogen atom and the other is a CH group; - M is a hydrogen atom or an pharmaceutically acceptable cation with the proviso that, when at least one of the groups R a and R b represent a hydrogen atom and G 2 is a group CR d , then Rd represents a groups selected from C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, C 3-8 cycloalkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; and the pharmaceutically acceptable salts and N-oxides thereof.
Abstract translation:式(I)的化合物,其中:基团G 1中的一个表示氮原子或基团CR c,另一个表示基团CR SUP>; G 2表示氮原子或基团CR 11; R 1表示选自氢原子,卤素原子,C 1-4烷基的基团,其可任选被1,2或3个选自卤素原子的取代基取代 和羟基,以及可以被1,2或3个选自卤素原子和羟基的取代基任选取代的C 3-8环烷基; R 2表示选自氢原子,卤素原子,羟基,C 1-4烷基的基团,其可任选被1,2或3个选自以下的取代基取代 可以任选被1,2或3个选自卤素原子和羟基的取代基取代的C 1-4烷氧基和C 3-8烷基, 可以任选地被1,2或3个选自卤素原子和羟基的取代基取代的环烷基; R a,R b和R c独立地表示选自氢原子,卤素原子,C 1-4烷基的基团, 可以任选被1,2或3个选自卤素原子和羟基的取代基取代的亚烷基,和可以被1,2或3个取代基任意取代的C 1-4烷氧基 选自卤素原子和羟基; -R d表示选自氢原子,卤素原子,羟基,C 1-4烷基的基团,其可任选被1,2或3个选自下列的取代基取代: 可以任选地被1,2或3个选自卤素原子和羟基的取代基取代的C 1-4烷氧基和C 3-8烷氧基, 其可任选被1,2或3个选自卤素原子和羟基的取代基取代; G 3和G 4之一是氮原子,另一个是CH基团; - M是氢原子或药学上可接受的阳离子,条件是当基团R a和R b中的至少一个表示氢原子时,G 2 SUP>是基团CR d,则Rd表示选自C 1-4烷氧基的基团,其可任选被1,2或3个取代基 选自卤素原子和羟基的取代基,可以任选被1,2或3个选自卤素原子和羟基的取代基取代的C 3-8环烷氧基; 及其药学上可接受的盐和N-氧化物。
Abstract:
Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, m and n are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
Abstract translation:式(I)的化合物,包括其药学上可接受的盐,酯,溶剂合物,立体异构体和前药,其中R 1,R 2, R 3,R 4,R 5,X,m和n如本文所定义。 还公开了含有结构式(I)化合物的药物组合物,以及与其使用有关的方法。 p>
Abstract:
Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, R l , R 2 and R 3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof as antagonists of adenosine receptors, in particular antagonists of the A2A adenosine receptor subtype.