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1. US20090076091 - Indazole-heteroaryl derivatives

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Claims

1. Compounds selected from the group
[TABLE-US-00004]
 
  Chemical structure
No. Name
 
“A1”  
 
  Methyl 5-(3-amino-1H-indazol-5-yl)furan-2-carboxylate
 
“A2”  
 
  Methyl 5-(3-amino-1H-indazol-5-yl)furan-2-carboxylate
 
“A2a”  
 
  tert-Butyl 5-(3-amino-1H-indazol-5-yl)furan-2-
  carboxylate
 
“A3”  
 
  5-(3-Acetylamino-1H-indazol-5-yl)furan-2-carboxylic
  acid
 
“A4”  
 
  5-[3-(Cyclopropanecarbonylamino)-1H-indazol-5-
  yl]furan-2-carboxylic acid
 
“A5”  
 
  5-(3-Benzoylamino-1H-indazol-5-yl)furan-2-carboxylic
  acid
 
“A6”  
 
  5-[3-(4-Pentylbenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A7”  
 
  Isopropyl 5-(3-amino-1H-indazol-5-yl)furan-2-
  carboxylate
 
“A8”  
 
  5-[3-(Cyclohexanecarbonylamino)-1H-indazol-5-yl]furan-
  2-carboxylic acid
 
“A9”  
 
  5-(3-Phenylacetylamino-1H-indazol-5-yl)furan-2-
  carboxylic acid
 
“A10”  
 
  5-(3-Phenylacetylamino-1H-indazol-5-yl)furan-2-
  carboxylic acid
 
“A11”  
 
  5-{3-[(Furan-2-carbonyl)amino]-1H-indazol-5-yl}furan-
  2-carboxylic acid
 
“A12”  
 
  5-{3-[(Thiophene-2-carbonyl)amino]-1H-indazol-5-yl}-
  furan-2-carboxylic acid
 
“A13”  
 
  5-{3-[(Pyridine-2-carbonyl)amino]-1H-indazol-5-yl}-
  furan-2-carboxylic acid
 
“A14”  
 
  5-{3-[(Pyridine-3-carbonyl)amino]-1H-indazol-5-yl}-
  furan-2-carboxylic acid
 
“A15”  
 
  5-[3-(4-Methoxybenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A16”  
 
  5-[3-(4-Chlorobenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A17”  
 
  5-[3-(3-Chlorobenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A18”  
 
  5-[3-(2-Chlorobenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A19”  
 
  5-[3-(4-Hydroxybenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A20”  
 
  5-{3-[(5-Chlorothiophene-2-carbonyl)amino]-1H-indazol-
  5-yl}furan-2-carboxylic acid
 
“A21”  
 
  5-[3-(3-Bromobenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A22”  
 
  5-[3-(3-Fluorobenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A23”  
 
  5-[3-(3-Ethylbenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A24”  
 
  5-[3-(3-Trifluoromethylbenzoylamino)-1H-indazol-5-yl]-
  furan-2-carboxylic acid
 
“A25”  
 
  5-[3-(3-Methylbenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A26”  
 
  5-[3-(3-Methoxybenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A27”  
 
  5-[3-(3-Hydroxybenzoylamino)-1H-indazol-5-yl]furan-2-
  carboxylic acid
 
“A28”  
 
  5-{3-[3-(2-Dimethylaminoethoxy)benzoylamino]-1H-
  indazol-5-yl}furan-2-carboxylic acid
 
and pharmaceutically usable derivatives, salts, solvates, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios.
2. Medicament comprising at least one compound according to claim 1 and/or pharmaceutically usable derivatives, salts, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, and optionally excipients and/or adjuvants.
3. A method for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role, comprising administering to a patient an effective amount of a compound according to claim 1.
4. Use A method according to claim 3, where the kinases are selected from the group of the serine/threonine kinases.
5. A method according to claim 4, where the serine/threonine kinases are CHK1 and CHK2.
6. A method according to claim 5,
wherein said disease is influenced by inhibition of the CHK1 and/or CHK2 kinase.
7. A method according to claim 6, where the disease to be treated is a proliferative disorder.
8. A method according to claim 7, where the proliferative disorder is a cancer.
9. A method according to claim 8, where a checkpoint pathway in the cancer has been mutated or upregulated.
10. A method according to claim 9, where the compound is administered in combination with another therapeutic agent.
11. A method according to claim 10, where the compound and the other therapeutic agent are administered as part of the same pharmaceutical composition.
12. A method according to claim 11, where the compound and the other therapeutic agent are administered as separate pharmaceutical compositions and the compound is administered before, at the same time as, or after the administration of the other therapeutic agent.
13. A method according to claim 12, where the other therapeutic agent is an anticancer agent.
14. A method according to claim 3, where the kinase is SGK.
15. A method according to claim 14, wherein said diseases are influenced by inhibition of SGKs.
16. A method according to claim 15, wherein said method is for the treatment or prevention of diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic or pulmonary hypertonia, cardiovascular diseases or renal diseases, generally in fibroses and inflammatory processes of any type, cancer, tumour cells, tumour metastases, coagulopathies, neuronal excitability, glaucoma, cataract, bacterial infections and in antiinfection therapy, for increasing learning ability and attention, or for the treatment and prophylaxis of cell ageing and stress, or for the treatment of tinnitus.
17. A method according to claim 16, where diabetes is diabetes mellitus, diabetic nephropathy, diabetic neuropathy, diabetic angiopathy and microangiopathy.
18. A method according to claim 16, where cardiovascular diseases are cardiac fibroses after myocardial infarction, cardiac hypertrophy, cardiac insufficiency and arteriosclerosis.
19. A method according to claim 16, where renal diseases are glomerulosclerosis, nephrosclerosis, nephritis, nephropathy and electrolyte excretion disorder.
20. A method according to claim 16, where fibroses and inflammatory processes are liver cirrhosis, pulmonary fibrosis, fibrosing pancreatitis, rheumatism and arthroses, Crohn's disease, chronic bronchitis, radiation fibrosis, sclerodermatitis, cystic fibrosis, scarring and Alzheimer's disease.
21. Set (kit) consisting of separate packs of
(a) an effective amount of a compound according to claim 1 and/or pharmaceutically usable derivatives, solvates and stereoisomers thereof, including mixtures thereof in all ratios,
and
(b) an effective amount of a further medicament active ingredient.