Novel compound useful for the treatement of degenerative and inflammatory diseases

Abstract

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

What is claimed is: 
     
         1 . The compound according to Formula I: 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt, or a solvate, or a solvate of the pharmaceutically acceptable salt, or a biologically active metabolite thereof. 
     
     
         2 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound or pharmaceutically acceptable salt thereof, according to  claim 1 . 
     
     
         3 . The pharmaceutical composition of  claim 2 , wherein the carrier is selected from a parenteral carrier, an oral carrier and a topical carrier. 
     
     
         4 . The pharmaceutical composition according to  claim 2  comprising a further therapeutic agent. 
     
     
         5 . A method for the treatment, or prophylaxis of allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons, comprising administering an amount of a compound or pharmaceutically acceptable salt thereof according to  claim 1 , sufficient to effect said treatment, or prophylaxis. 
     
     
         6 . The method according to  claim 5 , wherein the compound or pharmaceutically acceptable salt thereof, is administered in combination with a further therapeutic agent. 
     
     
         7 . A method for the treatment, or prophylaxis of allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons, comprising administering an amount of the pharmaceutical composition of  claim 2 , sufficient to effect said treatment, or prophylaxis. 
     
     
         8 . The method according to  claim 7 , wherein the pharmaceutical composition is administered in combination with a further therapeutic agent. 
     
     
         9 . The method according to  claim 8 , wherein the further therapeutic agent is an agent for the treatment, or prophylaxis of allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. 
     
     
         10 . The pharmaceutical composition according to  claim 2  comprising a further therapeutic agent selected from arthritis treatment agents. 
     
     
         11 . The pharmaceutical composition according to  claim 10 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs). 
     
     
         12 . A method for the treatment of rheumatoid arthritis, comprising administering an amount of a compound of  claim 1 , sufficient to effect said treatment. 
     
     
         13 . The method according to  claim 12 , wherein said compound is administered in combination with one or more further therapeutic agents selected from arthritis treatment agents. 
     
     
         14 . The method according to  claim 12 , wherein said compound is administered in combination with one further therapeutic agent selected from arthritis treatment agents. 
     
     
         15 . A method for the treatment of rheumatoid arthritis, comprising administering an amount of a pharmaceutical composition of  claim 2 , sufficient to effect said treatment. 
     
     
         16 . A method for the treatment of rheumatoid arthritis, comprising administering an amount of a pharmaceutical composition of  claim 4 , sufficient to effect said treatment. 
     
     
         17 . The method according to  claim 15 , wherein said pharmaceutical composition is administered in combination with one or more further therapeutic agents selected from arthritis treatment agents. 
     
     
         18 . The method according to  claim 15 , wherein said pharmaceutical composition is administered in combination with one further therapeutic agent selected from arthritis treatment agents. 
     
     
         19 . The method according to  claim 16 , wherein the further therapeutic agent is selected from arthritis treatment agents. 
     
     
         20 . The method according to  claim 13 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs). 
     
     
         21 . The method according to  claim 14 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs). 
     
     
         22 . The method according to  claim 17 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs). 
     
     
         23 . The method according to  claim 18 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs). 
     
     
         24 . The method according to  claim 19 , wherein the further therapeutic agent is an agent selected from analgesics, NSAIDS (non-steroidal anti-inflammatory drugs), and DMARDS (disease-modifying anti-rheumatic drugs).