RU2007131105A - Pyrazole derivatives for the inhibition of cyclin-dependent kinases (CDK) and glycogen synthase kinases (GSK) - Google Patents

Claims (30)

1. The compound of formula (I)

or its salts, tautomers, solvates and N-oxides; where R ¹ represents 2,6-dichlorophenyl; R ^2a and R ^{2b are} both hydrogen; and R ³ represents a group:

in which R ⁴ represents C _1-4 alkyl. 2. The compound according to claim 1, where R ⁴ represents a C _1-3 alkyl. 3. The compound according to claim 2, where R ⁴ represents methyl. 4. The compound according to claim 2, where R ⁴ represents ethyl. 5. The compound according to claim 2, where R ⁴ represents n-propyl. 6. The compound according to claim 2, where R ⁴ represents isopropyl. 7. The compound according to any one of the preceding paragraphs, which is not a salt or N-oxide. 8. The compound according to any one of claims 1 to 6 in the form of a salt, solvate or N-oxide. 9. The compound according to any one of claims 1 to 8 for use in the prophylaxis or treatment of a disease or disease condition mediated by a cyclin-dependent kinase or glycogen synthase kinase-3. 10. A method for the prevention or treatment of a disease or disease state mediated by a cyclin-dependent kinase or glycogen synthase-3 kinase, comprising administering to a patient in need thereof a compound according to any one of claims 1 to 8. 11. A method of alleviating or reducing the manifestations of a disease or disease state mediated by a cyclin-dependent kinase or glycogen synthase kinase-3, comprising administering to a patient in need thereof a compound according to any one of claims 1 to 8. 12. A method of treating a disease or condition including abnormal cell growth or resulting in abnormal cell growth in a mammal, comprising administering to the mammal a compound according to any one of claims 1 to 8 in an amount effective to inhibit abnormal cell growth. 13. A method of alleviating or reducing the manifestations of a disease or condition involving abnormal cell growth or resulting from abnormal cell growth in a mammal, comprising administering to the mammal a compound according to any one of claims 1 to 8 in an amount effective to inhibit abnormal cell growth. 14. A method of treating a disease or condition involving abnormal cell growth or resulting in abnormal cell growth in a mammal, comprising administering to the mammal a compound according to any one of claims 1 to 8 in an amount effective to inhibit cdk activity (such as cdk1 or cdk2) or activity glycogen synthase-3 kinases. 15. A method of alleviating or reducing the manifestations of a disease or condition involving abnormal cell growth or resulting in abnormal cell growth in a mammal, comprising administering to the mammal a compound according to any one of claims 1 to 8 in an amount effective to inhibit cyclin-dependent kinase activity (cdk, such like cdk1 or cdk2) or glycogen synthase-3 kinase activity. 16. A method of inhibiting a cyclin-dependent kinase or glycogen synthase-3 kinase, comprising contacting said kinase with a kinase-inhibiting compound according to any one of claims 1 to 8. 17. A method of modulating cellular processes (eg, cell division) by inhibiting the activity of a cyclin-dependent kinase or glycogen synthase-3 kinase using the compound according to any one of claims 1 to 8. 18. The compound according to any one of claims 1 to 8 for use in the prevention or treatment of a disease state as described above. 19. The use of a compound according to any one of claims 1 to 8 for the manufacture of a medicament, wherein the medicament is intended for any one or more of the uses indicated above. 20. A pharmaceutical composition comprising a compound according to any one of claims 1 to 8 and a pharmaceutically acceptable carrier. 21. A pharmaceutical composition comprising a compound according to any one of claims 1 to 8 and a pharmaceutically acceptable carrier in a form suitable for oral administration. 22. The compound according to any one of claims 1 to 8 for use in medicine. 23. The compound according to any one of claims 1 to 8 for any application and method specified above, thus, as described in the text of this application. 24. A method of producing a compound according to any one of claims 1 to 8, comprising reacting a compound of formula (XVII)

with a sulfonylating agent (for example, sulfonyl chloride, such as methanesulfonyl chloride), suitable for introducing the group SO ₂ R ⁴ . 25. A method for diagnosing and treating a disease or disease condition mediated by a cyclin-dependent kinase, comprising (i) screening a patient to determine whether the condition or disease to which the patient is or may be susceptible is one that is treatable using a compound having activity against cyclin-dependent kinases; and (ii) when it is shown that the disease or condition of the patient is susceptible to the specified treatment, administering to the patient a compound according to any one of claims 1 to 8. 26. The use of a compound according to any one of claims 1 to 8 for the manufacture of a medicament for the treatment or prophylaxis of diseases and painful conditions in a patient in which, as a result of a patient’s screening, the patient is found to be or is at risk of a disease or condition, which is treatable using a compound having cyclin-dependent kinase activity. 27. The compound according to any one of claims 1 to 8 for use in inhibiting tumor growth in a mammal. 28. The compound according to any one of claims 1 to 8 for use in inhibiting the growth of tumor cells (for example, in a mammal). 29. A method of inhibiting tumor growth in a mammal (eg, human), comprising administering to the mammal (eg, human) an effective tumor growth inhibiting amount of a compound according to any one of claims 1 to 8. 30. A method of inhibiting the growth of tumor cells (for example, tumor cells present in a mammal, such as a human), comprising contacting the tumor cells with an effective tumor growth inhibitory amount of a compound according to any one of claims 1 to 8.