Antiinflammation agents

• US 7,199,119 B2
• Filed: 09/19/2003
• Issued: 04/03/2007
• Est. Priority Date: 10/31/2002
• Status: Expired due to Fees

• Current Assignee: Amgen Inc.
• Original Assignee: Amgen Inc.
• Inventors: Farthing, Christopher N., Smith, Andrew, Lively, Sarah E., Jaen, Juan C., Shin, Youngsook, Hao, Xiaolin, Cushing, Timothy D., Labelle, Marc, Jiao, XianYun, McMinn, Dustin L., Kopecky, David J., Burkitt, Simon A., Cardozo, Mario G., Rasmussen, Sven P., DeGraffenreid, Michael R., Smith, Marie-Louise
• Primary Examiner(s): ANDERSON, REBECCA L
• Application Number:
  US10/666,857
• Publication Number:
  US 20040097485A1
• Time in Patent Office: 1,292 Days
• Field of Search: 546/114, 514/301, 514/233.8, 544/127
• US Class Current: 514/233.8
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: C07D 231/56 Benzopyrazoles; Hydrogenated benzopyrazoles
• CPC Class Codes: C07D 239/74 with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
• CPC Class Codes: C07D 471/04 Ortho-condensed systems
• CPC Class Codes: C07D 491/04 Ortho-condensed systems
• CPC Class Codes: C07D 495/04 Ortho-condensed systems
• CPC Class Codes: C07D 495/14 Ortho-condensed systems
• CPC Class Codes: C07D 513/04 Ortho-condensed systems

Abstract

Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism, infection and cell proliferation. The subject compounds contain a fused heterobicyclic ring.

Claims

1. A compound having the formula (Ia.1):

2. The compound of claim 1, wherein R¹ is selected from the group consisting Of —

C(O)NR^1aR^1b, —

SO₂NR^1aR^1b, —

SO₂R^1a, and —

C(O)R^1a.

3. The compound of claim 1, having the formula (III):

4. The compound of claim 1, having the formula (V):

5. The compound of claim 1, having the formula (VI):

6. The compound of claim 5, wherein R² is —

NHR^2b.

7. The compound of claim 5, wherein R¹ is selected from the group consisting of —

C(O)NHR^1a, —

SO₂NHR^1a, and —

C(O)CH₃ and R² is —

NHR^2b.

8. The compound of claim 5, wherein R¹ is selected from the group consisting Of —

C(O)NHR^1a, —

SO₂NHR^1a, —

SO₂R^1a and —

C(O)CH₃, R² is —

NHR^2b and each R^5a is hydrogen.

9. The compound of claim 8, wherein the compound is:

10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, excipient or diluent and a compound of claim 1.

11. A compound of claim 1, wherein the compound is selected from: