摘要:
A pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt or N-oxide thereof are disclosed, as well as pharmaceutical compositions comprising said compounds and methods of treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4 using said compounds are disclosed.
摘要:
The present disclosure relates to a pyridofuropyrimidine derivative of formula (I): whereinG1 is a group chosen from —CR6R7— and —O— wherein R6 and R7 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R1 and R2 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R3 is chosen from C1-4 alkyl, C1-4 alkoxy, amino, hydroxy, mono-C1-4alkylamino, di-C1-4alkylamino, C3-8cycloalkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups which are bound to the pyridine ring through their nitrogen atom, all of them being optionally substituted by one or more substituents chosen from halogen atoms and hydroxy, C1-4 alkyl, C1-4alkoxy-C1-4alkyl, aryl-C1-4alkyl, —O(CO)OR8, C1-4 alkoxy, —(CO)NR8R9, —CN, —CF3, —NR8R9, —SR8 and —SO2NH2 groups wherein R8 and R9 are each independently chosen from a hydrogen atom or a C1-4 alkyl group; R4 and R5 are independently chosen from hydrogen atoms, C1-4alkyl groups, hydroxyl-C1-4alkyl groups and groups of formula (II): wherein p and q are integers chosen from 0, 1, 2 and 3; A is either a direct bond or a group chosen from —CONR14—, —NR14CO—, —O—, —COO—, —OCO—, —S—, —SO— and —SO2—, wherein each R10, R11, R12, R13 and R14 are independently chosen from a hydrogen atom and a C1-4alkyl group and G2 is chosen from aryl, heteroaryl and heterocyclyl groups; wherein the group G2 is optionally substituted by one or more substituents chosen from halogen atoms and C1-4alkyl, hydroxy, oxo, C1-4alkoxy-C1-4alkyl, aryl-C1-4alkyl, —(CO)OR16, C1-4alkoxy, —(CO)NR16R17, —CN, —CF3, —NR16R17—SR16 and —SO2NH2 groups; wherein R16 and R17 each independently chosen from hydrogen atom and a C1-4alkyl group and the pharmaceutically acceptable salts and N-oxides thereof.
摘要:
New pyrrolotriazinone derivatives having the chemical 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 Phosphoinositide 3-Kinases (PI3Ks).
摘要:
The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis or irritable bowel disease.
摘要:
New pyrazole derivatives having the chemical 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 Janus Kinases (JAK).
摘要:
New pyrazole derivatives having the chemical 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 Janus Kinases (JAK).
摘要:
New pyrazole derivatives having the chemical 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 Janus Kinases (JAK).
摘要:
New imidazopyridine derivatives having the chemical 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 Janus Kinases (JAK).
摘要:
The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatilis, psoriasis or irritable bowel disease.
摘要:
A pyridothienopyrimidine derivative of formula (I), or the pharmaceutically acceptable salts or N-oxides thereof are disclosed, as well as pharmaceutical compositions comprising said compounds and methods of treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4 using said compounds are disclosed.