New pyrazole derivatives are tyrosine kinase inhibitors useful to treat e.g. solid tumors, diabetic retinopathy, age-related macular degeneration or inflammatory disease, osteoarthritis and rickets

摘要

Pyrazole derivatives (I) and their solvates, salts, tautomers and/or stereoisomers are new. Pyrazole derivatives of formula (I) and their solvates, salts, tautomers and/or stereoisomers are new. R 1>phenyl (optionally substituted with 1-3 of A and/or hal); R 2>A, R 1> or Het; A : 1-6C alkyl, where 1-5 of H atoms are replaced by F and/or Cl; Het : aromatic heterocycle with 1-4 of N-, O- and/or S atoms that are replaced by 1-2 of hal and/or A; and hal : F, Cl, Br or I. Independent claims are included for: (1) the preparation of (I); (2) a medicament comprising (I) and optionally carrier and/or additives; and (3) use of (I) for the manufacture of a medicament to treat disease associated with the inhibition, regulation or modulation by signal transduction kinase. [Image] ACTIVITY : Cytostatic; Antiinflammatory; Antiangiogenic; Antidiabetic; Ophthalmological; Antiarthritic; Antirheumatic; Antipsoriatic; Dermatological; Antiallergic; Immunosuppressive; Osteopathic; Antibacterial; Gynecological; Vulnerary. MECHANISM OF ACTION : Tyrosine kinase inhibitor; Tyrosine protein kinase (TIE-2) inhibitor; Raf-Kinase inhibitor.