IP Library Granted Patent US 9,284,288
Granted Patent B2
US 9,284,288 · App. 14/401,774 · Granted Mar 15, 2016

1-(p-tolyl) cyclopropyl substituted bridged spiro[2.4]heptane derivatives as ALX receptor agonists

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,284,288
App. No.
14/401,774
Granted
Mar 15, 2016
Kind
B2
Abstract

The present invention relates to 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives of formula (I), wherein R 1 is as defined in the description, their preparation and their use as pharmaceutically active compounds.

Claims (21)

1. A compound of formula (I)

wherein

R 1 represents hydrogen or fluoro;

or a salt thereof.

2. The compound according to claim 1 , wherein

R 1 represents hydrogen; or a salt thereof.

3. The compound according to claim 1 , wherein

R 1 represents fluoro; or a salt thereof.

4. The compound according to claim 1 , wherein the compound is: (5R)—N5-(1-(p-tolyl)cyclopropyl)-(6R)—N6-(4-(pyrrolidino)butyl)-(4S,7R)-[4,7-ethylene-spiro[2.4]heptane]-5,6-dicarboxamide; or a salt thereof.

5. A medicament comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition comprising, as active principle, a compound according to claim 1 or a pharmaceutically acceptable salt thereof, and at least one therapeutically inert excipient.

7. A method of treating a disease comprising administering to a subject in need thereof a compound according to claim 1 , wherein the disease is inflammatory diseases, obstructive airway diseases, allergic conditions, HIV-mediated retroviral infections, cardiovascular disorders, neurological disorders, pain, or amyloid-mediated disorders.

8. A method of treating a disease comprising administering to a subject in need thereof a pharmaceutical composition according to claim 6 , wherein the disease is inflammatory diseases, obstructive airway diseases, allergic conditions, HIV-mediated retroviral infections, cardiovascular disorders, neurological disorders, pain, or amyloid-mediated disorders.

9. A method of modulating an immune response in a subject comprising administering to the subject in need thereof a compound according to claim 1 .

10. A method of modulating an immune response in a subject comprising administering to the subject in need thereof the pharmaceutical composition according to claim 6 .

11. A method of treating a disease comprising administering to a subject in need thereof the compound according to claim 1 , wherein the disease is neuroinflammation.

12. A method of treating a disease comprising administering to a subject in need thereof the pharmaceutical composition according to claim 6 , wherein the disease is neuroinflammation.

13. A method of treating a disease comprising administering to a subject in need thereof the compound according to claim 1 , wherein the disease is a prion-mediated disease.

14. A method of treating a disease comprising administering to a subject in need thereof the pharmaceutical composition according to claim 6 , wherein the disease is a prion-mediated disease.

15. A method of treating a disease comprising administering to a subject in need thereof the compound according to claim 1 , wherein the disease is rheumatoid arthritis, acute lung injury, asthma, cystic fibrosis, inflammatory bowel disease, keratoconjunctivitis sicca, HIV-mediated retroviral infections, cardiovascular disorders, atopic dermatitis, pulmonary fibrosis or Alzheimer's disease.

16. A method of treating a disease comprising administering to a subject in need thereof the pharmaceutical composition according to claim 6 , wherein the disease is rheumatoid arthritis, acute lung injury, asthma, cystic fibrosis, inflammatory bowel disease, keratoconjunctivitis sicca, HIV-mediated retroviral infections, cardiovascular disorders, atopic dermatitis, pulmonary fibrosis or Alzheimer's disease.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE ADDRESS PREVIOUSLY RECORDED AT REEL: 042464 FRAME: 0407. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jun 28, 2017
From: ACTELION PHARMACEUTICALS LTD
To: IDORSIA PHARMACEUTICALS LTD
Reel/Frame 043017/0022 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 13, 2017
From: ACTELION PHARMACEUTICALS LTD
To: IDORSIA PHARMACEUTICALS LTD
Reel/Frame 042464/0407 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 18, 2014
From: CREN, SYLVAINE; CORMINBOEUF, OLIVIER
To: ACTELION PHARMACEUTICALS LTD.
Reel/Frame 034194/0767 →