Ranbaxy Laboratories, Inc.

Manoj Kumar Khera

Venkata Poornapragnacharyulu Palle

Sunanda Ghosh Dastidar

Viswajanani Jitendra Sattigeri

Arpita Musib

Manoj Kumar Tiwari

Ajay Soni

Abdul Rehman Abdul Rauf

Ranadheer Reddy

Sony Joseph

Punit Kumar Srivastava

Abhijit Ray

Punit Kumar Sricastava

Sreedhara Rao Voleti

Viswajanani J Sattigeri

The present invention relates to &#x3b2;-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure &#x3b2;-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.

Matrix metalloproteinase inhibitors

The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; Ris optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; Ris alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NRR, &#x2014;NHC(&#x2550;Y)R, &#x2014;NHC(&#x2550;Y)NRR, &#x2014;NHC(&#x2550;O)OR, &#x2014;NHSOR, C(&#x2550;Y)NRR, C(&#x2550;O)OR[wherein Y is oxygen or sulphur], OR, &#x2014;O(C&#x2550;O)NRR, O-acyl, S(O)R, &#x2014;SON(R), cyano, amidino or guanidino [wherein Ris alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; Ris hydrogen or R; Ris Ror &#x2014;SON(R)and Ris hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; Ris hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR, &#x2014;OC(&#x2550;O)NRR, O-acyl, NH, NRR, &#x2014;NHC(&#x2550;Y)R, &#x2014;NHC(&#x2550;Y)NRR, &#x2014;NHC(&#x2550;O)OR, &#x2014;NHSOR, and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by over-expression and over-activation of an matrix metalloproteinase, using the compounds. 

5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases

The present invention relates to &#x3b2;-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure &#x3b2;-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, periodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.

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Gurgaon, India

Manoj Kumar Khera