IP Library Granted Patent US 7,132,428
Granted Patent B2
US 7,132,428 · App. 10/613,588 · Granted Nov 7, 2006

Pyrazoloisoquinoline derivative as kinase inhibitors for the treatment of various disorders

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Quick Facts
Patent No.
US 7,132,428
App. No.
10/613,588
Granted
Nov 7, 2006
Kind
B2
Abstract

Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.

Claims (27)

1. A compound selected from the group consisting of:

5-pyridin-2-yl-3-trifluoromethyl-1H-pyrazolo[4,3-c]isoquionoline,

3-methyl-5-(2-trifluoromethyl-phenyl-1H-pyrazolo[4,3-c]isoquinoline,

3-methyl-5-(3-trifluoromethyl-phenyl)-1H-pyrazolo[4,3-c]isoquinoline,

3-methyl-5-(4-trifluoromethyl-phenyl)-1H-pyrazolo[4,3-c]isoquinoline,

1,3-dimethyl-5-(3-trifluoromethylphenyl)-1H-pyrazolo[4,3-c]-isoquinoline,

5-phenyl-3-trifluoromethyl-1H-pyrazolo[4,3-c]isoquinoline,

1,3-dimethyl-5-(3-trifluoromethylphenyl-1H-pyrazolo[4,3-c]-isoquinoline,

1,3-dimethyl-5-(2,6-difluorophenyl)-1H-pyrazolo[4,3-c]-isoquinoline,

1-benzyl-5-cyclohexyl-3-methyl-1H-pyrazolo[4,3-c]-isoquinoline,

1-benzyl-5-naphthyl-3-methyl-1H-pyrazolo[4,3-c]-isoquinoline,

7methoxycarbonyl-3-methyl-5-phenyl-1H-pyrazolo[4,3-c]-isoquinoline,

7-methoxycarbonyl-3-methyl-5-pyridin-2-yl-1H -pyrazolo[4,3-c]-isoquinoline,

7-dimethylamino-3-methyl-5-phenyl-1H-pyrazolo[4,3-c]isoquinoline,

7-dimethylamino-3-methyl-5pyridin-2-yl-1H-pyrazolo]4,3-c]-isoquinoline,

6-dimethylamino-3-methyl-5-phenyl-1H-pyrazolo[4,3-c]-isoquinoline,

6-dimethylamino-3-methyl-5-pyridin-2-yl-1H-pyrazolo[4,3-c]-isoquinoline,

8-dimethylamino-3-methyl-5-phenyl-1H-pyrazolo[4,3-c]isoquinoline,

8-dimethylamino-3-methyl-5-pyridin-2-yl-1H-pyrazolo[4,3-c]-isoquinoline,

1,3-dimethyl-5-(3-methyl-thiophen-2-yl)-1H-pyrazolo[4,3-c]-isoquinoline,

3-methyl-5-phenyl-9-trifluoromethyl-1H-pyrazolo[4,3-c]isoquinoline,

3-methyl-5-pyridin-2-yl-9-trifluoromethyl-1H-pyrazolo[4,3-c]-isoquinoline, and

3-methyl-5-(2,3,4,5,6-pentafluoro-phenyl)-1H-pyrazolo[4,3-c]-isoquinoline.

2. A pharmaceutical composition comprising a therapeutically effective content of at least one compound as claimed in claim 1 together with a pharmaceutically suitable carrier.

3. A method of treating a disease condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, asthma, comprising administering to a patient suffering from said disease condition a therapeutically effective amount of a compound according to claim 1 .

4. The method as claimed in claim 3 , wherein the disease condition is osteoarthritis.

5. The method as claimed in claim 3 , wherein the disease condition is rheumatoid arthritis.

Assignments (3)
MERGER Recorded Jan 19, 2015
From: AVENTIS PHARMACEUTICALS INC.
To: AVENTISUB LLC
Reel/Frame 034781/0334 →
CERTIFICATE OF CONVERSION Recorded Dec 9, 2014
From: AVENTISUB INC.
To: AVENTISUB LLC
Reel/Frame 034566/0976 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 16, 2005
From: MAJID, TAHIR NADEEM; HOPKINS, COREY; PEDGRIFT, BRIAN LESLIE; COLLAR, NICOLA; WIRTZ-BRUGGER, FRIEDERIKE; MERRILL, JEAN
To: AVENTIS PHARMACEUTICALS INC.
Reel/Frame 016020/0559 →