(4,2-Disubstituted-thiazol-5-yl)amine compounds as PDE7 inhibitors
AssigneeWarner-Lambert Company
InventorsFabrice Vergne, Patrick Bernardelli, Edwige Lorthiois, Pierre Ducrot
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AssigneeWarner-Lambert Company
InventorsFabrice Vergne, Patrick Bernardelli, Edwige Lorthiois, Pierre Ducrot
Estimating the term…
A compound selected from those of formula (I): 1 wherein R1a, R1b, R2, R3, are as defined in the description,and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of phosphosdiesterase-7 (PDE-7).
A compound of formula (I):
Dependencies are inferred from the claim text.
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Containing two hetero rings: directly linked by a ring-member-to-ring-member bond
Drugs for disorders of the alimentary tract or the digestive system
Drugs for disorders of the alimentary tract or the digestive system: for pancreatic disorders, e.g. pancreatic enzymes
Drugs for disorders of the respiratory system
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The present invention relates to (4,2-disubstituted-thiazol-5-yl)amine derivatives, a process for their preparation, and pharmaceutical compositions containing them. These new compounds are useful as phosphodiesterase 7 (PDE7) inhibitors. Further contained in this invention are pharmaceutical compositions containing these phosphodiesterase 7 inhibitors as active principle for the treatment of disease for which treatment by PDE7 inhibitor is relevant. These medicinal products are useful in particular for treating T-cell-related diseases, autoimmune diseases, visceral pain, osteoarthritis, multiple sclerosis, osteoporosis, chronic obstructive pulmonary disease, allergic rhinitis, asthma, cancer, acquired immune deficiency syndrome, allergy, fertility diseases or inflammatory bowel disease.
Phosphodiesterases (PDE) play an important role in various biological processes by hydrolysing the key second messengers adenosine and guanosine 3′,5′-cyclic monophosphates (cAMP and cGMP respectively) into their corresponding 5′-monophosphate nucleotides. Therefore, inhibition of PDE activity produces an increase of cAMP and cGMP intracellular levels that activate specific protein phosphorylation pathways involved in a variety of functional responses.
At least eleven isoenzymes of mammalian cyclic nucleotide phosphodiesterases, numbered PDE 1 through PDE 11, have been identified on the basis of primary structure, substrate specificity or sensitivity to cofactors or inhibitory drugs.
N-{4-[5-(cyclohexylamino)-4-methyl-1,3-thiazol-2-yl]phenyl}acetamide 12
Step 1:
tert-Butyl(2S)-2-[(4-nitrobenzoyl)amino]-propanoate